TTD - Therapeutic Targets Database Full Data Download File Title - TTD targets information in raw format Version 8.1.01 (2021.11.08) Provided by IDRB Lab of Innovative Drug Reasearch and Bioinformatics College of Pharmaceutical Sciences Zhejiang University https://idrblab.org/ Provided by BIDD BioInformatic and Drug Design Group Department of Pharmacy National Unviersity of Singapore http://bidd.nus.edu.sg/ Any question about data provided here, please contact with: Dr. Zhou (zhou_ying@zju.edu.cn) and Dr. Zhang (zhangyintao@zju.edu.cn) -------------------------------------------------------------------------------------------------------- Abbreviations: TARGETID TTD Target ID FORMERID TTD Former Target ID UNIPROID Uniprot ID TARGNAME Target Name GENENAME Target Gene Name TARGTYPE Target Type SYNONYMS Synonyms FUNCTION Function PDBSTRUC PDB Structure BIOCLASS BioChemical Class ECNUMBER EC Number SEQUENCE Sequence DRUGINFO TTD Drug ID Drug Name Highest Clinical Status KEGGPATH KEGG Pathway WIKIPATH WiKipathway WHIZPATH PathWhiz Pathway REACPATH Reactome Pathway NET_PATH NetPathway INTEPATH Pathway Interact PANTPATH PANTHER Pathway BIOCPATH BioCyc -------------------------------------------------------------------------------------------------------- T47101 TARGETID T47101 T47101 FORMERID TTDC00024 T47101 UNIPROID FGFR1_HUMAN T47101 TARGNAME Fibroblast growth factor receptor 1 (FGFR1) T47101 GENENAME FGFR1 T47101 TARGTYPE Successful target T47101 SYNONYMS c-fgr; bFGF-R-1; bFGF-R; N-sam; HBGFR; Fms-like tyrosine kinase 2; FLT2; FLT-2; FLG; FGFR-1; FGFBR; CEK; CD331 antigen; CD331; Basic fibroblast growth factor receptor 1; BFGFR T47101 FUNCTION Required for normal mesoderm patterning and correct axial organization during embryonic development, normal skeletogenesis and normal development of the gonadotropin-releasing hormone (GnRH) neuronal system. Phosphorylates PLCG1, FRS2, GAB1 and SHB. Ligand binding leads to the activation of several signaling cascades. Activation of PLCG1 leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate. Phosphorylation of FRS2 triggers recruitment of GRB2, GAB1, PIK3R1 and SOS1, and mediates activation of RAS, MAPK1/ERK2, MAPK3/ERK1 and the MAP kinase signaling pathway, as well as of the AKT1 signaling pathway. Promotes phosphorylation of SHC1, STAT1 and PTPN11/SHP2. In the nucleus, enhances RPS6KA1 and CREB1 activity and contributes to the regulation of transcription. FGFR1 signaling is down-regulated by IL17RD/SEF, and by FGFR1 ubiquitination, internalization and degradation. Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of embryonic development, cell proliferation, differentiation and migration. T47101 PDBSTRUC 6MZW; 6MZQ; 6C1O; 6C1C; 6C1B T47101 BIOCLASS Kinase T47101 ECNUMBER EC 2.7.10.1 T47101 SEQUENCE MWSWKCLLFWAVLVTATLCTARPSPTLPEQAQPWGAPVEVESFLVHPGDLLQLRCRLRDDVQSINWLRDGVQLAESNRTRITGEEVEVQDSVPADSGLYACVTSSPSGSDTTYFSVNVSDALPSSEDDDDDDDSSSEEKETDNTKPNRMPVAPYWTSPEKMEKKLHAVPAAKTVKFKCPSSGTPNPTLRWLKNGKEFKPDHRIGGYKVRYATWSIIMDSVVPSDKGNYTCIVENEYGSINHTYQLDVVERSPHRPILQAGLPANKTVALGSNVEFMCKVYSDPQPHIQWLKHIEVNGSKIGPDNLPYVQILKTAGVNTTDKEMEVLHLRNVSFEDAGEYTCLAGNSIGLSHHSAWLTVLEALEERPAVMTSPLYLEIIIYCTGAFLISCMVGSVIVYKMKSGTKKSDFHSQMAVHKLAKSIPLRRQVTVSADSSASMNSGVLLVRPSRLSSSGTPMLAGVSEYELPEDPRWELPRDRLVLGKPLGEGCFGQVVLAEAIGLDKDKPNRVTKVAVKMLKSDATEKDLSDLISEMEMMKMIGKHKNIINLLGACTQDGPLYVIVEYASKGNLREYLQARRPPGLEYCYNPSHNPEEQLSSKDLVSCAYQVARGMEYLASKKCIHRDLAARNVLVTEDNVMKIADFGLARDIHHIDYYKKTTNGRLPVKWMAPEALFDRIYTHQSDVWSFGVLLWEIFTLGGSPYPGVPVEELFKLLKEGHRMDKPSNCTNELYMMMRDCWHAVPSQRPTFKQLVEDLDRIVALTSNQEYLDLSMPLDQYSPSFPDTRSSTCSSGEDSVFSHEPLPEEPCLPRHPAQLANGGLKRR T47101 DRUGINFO D09HNV Intedanib Approved T47101 DRUGINFO D0O6UY Pemigatinib Approved T47101 DRUGINFO D01PZD Romiplostim Approved T47101 DRUGINFO D07PQJ ARQ-087 Phase 3 T47101 DRUGINFO D03LWG BGJ398 Phase 3 T47101 DRUGINFO D02WVT E-3810 Phase 3 T47101 DRUGINFO D0A1AQ Rosiglitazone + metformin Phase 3 T47101 DRUGINFO D05PWX Sulfatinib Phase 3 T47101 DRUGINFO D0NU0U AZD4547 Phase 2/3 T47101 DRUGINFO D08DFF AM-001 Phase 2 T47101 DRUGINFO D0XT0W Debio 1347 Phase 2 T47101 DRUGINFO D08ZHL FGF-1 Phase 2 T47101 DRUGINFO D0U2DO FP-1039 Phase 2 T47101 DRUGINFO D00DRL MK-2461 Phase 1/2 T47101 DRUGINFO D00ABO KW-2449 Phase 1 T47101 DRUGINFO D0DJ0S NGM313 Phase 1 T47101 DRUGINFO D0LF0O BMS-695735 Preclinical T47101 DRUGINFO D0Z0KD PD-0183812 Terminated T47101 DRUGINFO D0XC6G 2-(1H-indazol-3-yl)-1H-benzo[d]imidazole Investigative T47101 DRUGINFO D06QUJ 3-(3-methoxybenzyl)-1H-pyrrolo[2,3-b]pyridine Investigative T47101 DRUGINFO D07QMC 3-Benzimidazol-2-ylhydroquinolin-2-one Investigative T47101 DRUGINFO D0EE6A AAL-993 Investigative T47101 DRUGINFO D0R6OM ACTB-1003 Investigative T47101 DRUGINFO D00JZS Anti-FGFR1 mab program Investigative T47101 DRUGINFO D0D5EW HKI-9924129 Investigative T47101 DRUGINFO D04FNY NP-506 Investigative T47101 DRUGINFO D0P3JW PD-0166326 Investigative T47101 DRUGINFO D0S1KJ PD-0173952 Investigative T47101 DRUGINFO D03NPX PD-0173955 Investigative T47101 DRUGINFO D0GW4Q PD-0173956 Investigative T47101 DRUGINFO D0Z7GH PD-0173958 Investigative T47101 DRUGINFO D0OH3J PD-0179483 Investigative T47101 DRUGINFO D0C2GE PMID22765894C8h Investigative T47101 DRUGINFO D0E7VO PMID24900538C2c Investigative T47101 DRUGINFO D06FFZ PMID26080733C7r Investigative T47101 DRUGINFO D09XIL Ro-4396686 Investigative T47101 DRUGINFO D01AVF SAR-106881 Investigative T47101 KEGGPATH hsa04010:MAPK signaling pathway T47101 KEGGPATH hsa04014:Ras signaling pathway T47101 KEGGPATH hsa04015:Rap1 signaling pathway T47101 KEGGPATH hsa04151:PI3K-Akt signaling pathway T47101 KEGGPATH hsa04520:Adherens junction T47101 KEGGPATH hsa04550:Signaling pathways regulating pluripotency of stem cells T47101 KEGGPATH hsa04810:Regulation of actin cytoskeleton T47101 KEGGPATH hsa05200:Pathways in cancer T47101 KEGGPATH hsa05205:Proteoglycans in cancer T47101 KEGGPATH hsa05215:Prostate cancer T47101 KEGGPATH hsa05218:Melanoma T47101 KEGGPATH hsa05230:Central carbon metabolism in cancer T47101 WIKIPATH WP1911:Signaling by FGFR T47101 WIKIPATH WP2064:Neural Crest Differentiation T47101 WIKIPATH WP2261:Signaling Pathways in Glioblastoma T47101 WIKIPATH WP2377:Integrated Pancreatic Cancer Pathway T47101 WIKIPATH WP2804:Hair Follicle Development: Induction (Part 1 of 3) T47101 WIKIPATH WP2857:Mesodermal Commitment Pathway T47101 WIKIPATH WP382:MAPK Signaling Pathway T47101 WIKIPATH WP474:Endochondral Ossification T47101 WIKIPATH WP51:Regulation of Actin Cytoskeleton T47101 NET_PATH NetPath_11:TCR Signaling Pathway T47101 INTEPATH fgf_pathway:FGF signaling pathway T47101 INTEPATH glypican_1pathway:Glypican 1 network T47101 INTEPATH ncadherinpathway:N-cadherin signaling events T47101 INTEPATH syndecan_4_pathway:Syndecan-4-mediated signaling events T47101 PANTPATH P00005:Angiogenesis T47101 PANTPATH P00021:FGF signaling pathway T59328 TARGETID T59328 T59328 FORMERID TTDS00355 T59328 UNIPROID EGFR_HUMAN T59328 TARGNAME Epidermal growth factor receptor (EGFR) T59328 GENENAME EGFR T59328 TARGTYPE Successful target T59328 SYNONYMS Receptor tyrosine-protein kinase erbB-1; Proto-oncogene c-ErbB-1; HER1; ERBB1; ERBB T59328 FUNCTION Receptor tyrosine kinase binding ligands of the EGF family and activating several signaling cascades to convert extracellular cues into appropriate cellular responses. Known ligands include EGF, TGFA/TGF-alpha, AREG, epigen/EPGN, BTC/betacellulin, epiregulin/EREG and HBEGF/heparin-binding EGF. Ligand binding triggers receptor homo- and/or heterodimerization and autophosphorylation on key cytoplasmic residues. The phosphorylated receptor recruits adapter proteins like GRB2 which in turn activates complex downstream signaling cascades. Activates at least 4 major downstream signaling cascades including the RAS-RAF-MEK-ERK, PI3 kinase-AKT, PLCgamma-PKC and STATs modules. May also activate the NF-kappa-B signaling cascade. Also directly phosphorylates other proteins like RGS16, activating its GTPase activity and probably coupling the EGF receptor signaling to the G protein-coupled receptor signaling. Also phosphorylates MUC1 and increases its interaction with SRC and CTNNB1/beta-catenin. Plays a role in enhancing learning and memory performance (By similarity). T59328 PDBSTRUC 6D8E; 6B3S; 6ARU; 5ZWJ; 5YU9 T59328 BIOCLASS Kinase T59328 ECNUMBER EC 2.7.10.1 T59328 SEQUENCE MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEEDGVRKCKKCEGPCRKVCNGIGIGEFKDSLSINATNIKHFKNCTSISGDLHILPVAFRGDSFTHTPPLDPQELDILKTVKEITGFLLIQAWPENRTDLHAFENLEIIRGRTKQHGQFSLAVVSLNITSLGLRSLKEISDGDVIISGNKNLCYANTINWKKLFGTSGQKTKIISNRGENSCKATGQVCHALCSPEGCWGPEPRDCVSCRNVSRGRECVDKCNLLEGEPREFVENSECIQCHPECLPQAMNITCTGRGPDNCIQCAHYIDGPHCVKTCPAGVMGENNTLVWKYADAGHVCHLCHPNCTYGCTGPGLEGCPTNGPKIPSIATGMVGALLLLLVVALGIGLFMRRRHIVRKRTLRRLLQERELVEPLTPSGEAPNQALLRILKETEFKKIKVLGSGAFGTVYKGLWIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDNPHVCRLLGICLTSTVQLITQLMPFGCLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAARNVLVKTPQHVKITDFGLAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSYGVTVWELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPKFRELIIEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQQGFFSSPSTSRTPLLSSLSATSNNSTVACIDRNGLQSCPIKEDSFLQRYSSDPTGALTEDSIDDTFLPVPEYINQSVPKRPAGSVQNPVYHNQPLNPAPSRDPHYQDPHSTAVGNPEYLNTVQPTCVNSTFDSPAHWAQKGSHQISLDNPDYQQDFFPKEAKPNGIFKGSTAENAEYLRVAPQSSEFIGA T59328 DRUGINFO D05UFG BIBW 2992 Approved T59328 DRUGINFO D0N5OV Cetuximab Approved T59328 DRUGINFO D06XXH Dacomitinib Approved T59328 DRUGINFO D08TPS Epidermal growth factor Approved T59328 DRUGINFO D07POC Erlotinib Approved T59328 DRUGINFO D09XZB Gefitinib Approved T59328 DRUGINFO D05GGP HEGF Approved T59328 DRUGINFO D08CDI Lapatinib Approved T59328 DRUGINFO D0F0ZE Merimepodib Approved T59328 DRUGINFO D03WPP Necitumumab Approved T59328 DRUGINFO D0U1ZV NERATINIB MALEATE Approved T59328 DRUGINFO D07YDE Nitroglycerin Approved T59328 DRUGINFO D0O8GK Osimertinib Approved T59328 DRUGINFO D0HU9H Panitumumab Approved T59328 DRUGINFO D03MNN SKI-758 Approved T59328 DRUGINFO D0W5HK Sorafenib Approved T59328 DRUGINFO D0G6QF Vandetanib Approved T59328 DRUGINFO D06WRJ Icotinib hydrochloride Registered T59328 DRUGINFO DDH8L6 Almonertinib Phase 3 T59328 DRUGINFO DQ5X1Z Amivantamab Phase 3 T59328 DRUGINFO DWK96T ASP1929 Phase 3 T59328 DRUGINFO D09BKY Bevacizumab + Erlotinib Phase 3 T59328 DRUGINFO D0M4AV CO-1686 Phase 3 T59328 DRUGINFO D0FJ1W DE-766 Phase 3 T59328 DRUGINFO D0K7FY EGF816 Phase 3 T59328 DRUGINFO D0Q9CY HKI-272 Phase 3 T59328 DRUGINFO D05FRP Rindopepimut Phase 3 T59328 DRUGINFO D0CR8H SYM-004 Phase 3 T59328 DRUGINFO D0R4PW Zalutumumab Phase 3 T59328 DRUGINFO D0F3KC Indium-111 Phase 2/3 T59328 DRUGINFO D00NYJ Varlitinib Phase 2/3 T59328 DRUGINFO D06XIT ABT-414 Phase 2 T59328 DRUGINFO D0P9RG ABX-EGF Phase 2 T59328 DRUGINFO D02BYZ ASP8273 Phase 2 T59328 DRUGINFO D0U4FF BMS-599626 Phase 2 T59328 DRUGINFO D0R6UV BMS-690514 Phase 2 T59328 DRUGINFO D0K9MC CetuGEX Phase 2 T59328 DRUGINFO D0YB3W CI-1033 Phase 2 T59328 DRUGINFO D0A6CC Depatuxizumab Phase 2 T59328 DRUGINFO D0C3LL HER1-VSSP vaccine Phase 2 T59328 DRUGINFO D00YER HM-78136B Phase 2 T59328 DRUGINFO D0BZ7V Matuzumab Phase 2 T59328 DRUGINFO D09BZJ MEHD-7945A Phase 2 T59328 DRUGINFO D03UKJ Pazopanib + Tyverb/Tykerb Phase 2 T59328 DRUGINFO D0S3PO Pelitinib Phase 2 T59328 DRUGINFO D0FN4T RM-1929 Phase 2 T59328 DRUGINFO DUW81M Tarloxotinib Phase 2 T59328 DRUGINFO D0T5JS TT-100 Phase 2 T59328 DRUGINFO D0P6DJ VATALANIB Phase 2 T59328 DRUGINFO DK8QG3 AFM24 Phase 1/2 T59328 DRUGINFO D9FJ5V BDTX-189 Phase 1/2 T59328 DRUGINFO D04DHZ CART-EGFR Phase 1/2 T59328 DRUGINFO D0G1ZU EGFR CART Phase 1/2 T59328 DRUGINFO DWQ6J1 EMB-01 Phase 1/2 T59328 DRUGINFO D0S8BG EMD 55900 Phase 1/2 T59328 DRUGINFO D05ETC SN-32793 Phase 1/2 T59328 DRUGINFO D0FF2G Sym013 Phase 1/2 T59328 DRUGINFO D0B4OK Sym015 Phase 1/2 T59328 DRUGINFO DF0PR6 ZN-e4 Phase 1/2 T59328 DRUGINFO D0V4XY S-222611 Phase 1b T59328 DRUGINFO D05LMC AMG 595 Phase 1 T59328 DRUGINFO D0T0SE Anti-EGFR CAR T Phase 1 T59328 DRUGINFO D0JW2O Anti-HER3/EGFR DAF Phase 1 T59328 DRUGINFO D0X7BN AP32788 Phase 1 T59328 DRUGINFO D04OLK AST-1306 Phase 1 T59328 DRUGINFO D0U7XJ BCA101 Phase 1 T59328 DRUGINFO D00RMC BIBX-1382 Phase 1 T59328 DRUGINFO D08JAN Cipatinib Phase 1 T59328 DRUGINFO D68RMI CLN-081 Phase 1 T59328 DRUGINFO D0Z4RC CUDC-101 Phase 1 T59328 DRUGINFO DR4ND6 D2C7 Phase 1 T59328 DRUGINFO D0I7ZH EGFR806-specific CAR T cell Phase 1 T59328 DRUGINFO D0E7RC HER-2/HER-1 vaccine Phase 1 T59328 DRUGINFO D04HSH IMGN289 Phase 1 T59328 DRUGINFO D0U3XL JNJ-26483327 Phase 1 T59328 DRUGINFO D01IJM LY3164530 Phase 1 T59328 DRUGINFO DV8I4Q MCLA-158 Phase 1 T59328 DRUGINFO D01NAP MM-151 Phase 1 T59328 DRUGINFO D0N3PC MR1-1 Phase 1 T59328 DRUGINFO D0JS0W PF-05230907 Phase 1 T59328 DRUGINFO D6JM8Z SI-B001 Phase 1 T59328 DRUGINFO D00KML SYN004 Phase 1 T59328 DRUGINFO D0Z2PC Pyrrolo[2,3-d]pyrimidine derivative 24 Patented T59328 DRUGINFO D07GFF PKI166 Discontinued in Phase 2 T59328 DRUGINFO D0E2CQ RG7160 Discontinued in Phase 2 T59328 DRUGINFO D02RZL AZD4769 Discontinued in Phase 1 T59328 DRUGINFO D0Q7HO PD-153035 Discontinued in Phase 1 T59328 DRUGINFO D0A9OV TAK165 Discontinued in Phase 1 T59328 DRUGINFO D0V2FZ 111In-hEGF Preclinical T59328 DRUGINFO D0TI4U EGFR/IGFR tandem adnectin Preclinical T59328 DRUGINFO D0Y1YX AZD-9935 Terminated T59328 DRUGINFO D03QTP CGP-52411 Terminated T59328 DRUGINFO D0HO1S CGP-53353 Terminated T59328 DRUGINFO D02GFZ Heparin-EGF-like factor Terminated T59328 DRUGINFO D0Y2AM (3-Bromo-phenyl)-(5-nitro-quinazolin-4-yl)-amine Investigative T59328 DRUGINFO D02ZRO (3-Bromo-phenyl)-quinazolin-4-yl-amine Investigative T59328 DRUGINFO D06UEK (E)-5-(4-Hydroxybenzylidene)-1-phenethylhydantoin Investigative T59328 DRUGINFO D0KN1L (S)-benzyl 4-chloro-3-oxobutan-2-ylcarbamate Investigative T59328 DRUGINFO D0W6CE 10-hydroxy-18-methoxybetaenone Investigative T59328 DRUGINFO D02RIG 2-(4,5-Dihydroxy-indan-1-ylidene)-malononitrile Investigative T59328 DRUGINFO D07IHD 2-(5,6-Dihydroxy-indan-1-ylidene)-malononitrile Investigative T59328 DRUGINFO D00VZA 2-benzoyl-3-(3,4-dihydroxyphenyl)acrylonitrile Investigative T59328 DRUGINFO D01NTW 2-cyano-3-(3,4-dihydroxyphenyl)acrylamide Investigative T59328 DRUGINFO D0O9UR 2-methoxy-4-(2-nitrovinyl)phenol Investigative T59328 DRUGINFO D0C9KC 3-(3-Chloro-phenyl)-5,7-dihydroxy-chromen-4-one Investigative T59328 DRUGINFO D0EK0G 3-(4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione Investigative T59328 DRUGINFO D06AOY 3-(indole-3-yl)-4-phenyl-1H-pyrrole-2,5-dione Investigative T59328 DRUGINFO D00NYT 3,4-di-(4-methoxyphenyl)-1H-pyrrole-2,5-dione Investigative T59328 DRUGINFO D0C3WY 3,4-diphenyl-1H-pyrrole-2,5-dione Investigative T59328 DRUGINFO D0B8DE 3-Pyridin-4-yl-quinoline-6,7-diol Investigative T59328 DRUGINFO D0K2YY 4-(2-nitroprop-1-enyl)benzene-1,2-diol Investigative T59328 DRUGINFO D0L3SN 4-(2-nitrovinyl)benzene-1,2-diol Investigative T59328 DRUGINFO D0W1BE 4-(2-nitrovinyl)phenol Investigative T59328 DRUGINFO D03HLH 4-(3-Bromo-phenoxy)-6,7-dimethoxy-quinazoline Investigative T59328 DRUGINFO D05QMN 4-(3-Bromo-phenoxy)-6,7-dimethoxy-quinoline Investigative T59328 DRUGINFO D0J9WO 4-(3-Bromo-phenylamino)-quinazoline-6,7-diol Investigative T59328 DRUGINFO D0G4HR 4-(4-(2-nitrovinyl)phenoxysulfonyl)benzoic acid Investigative T59328 DRUGINFO D0I7RA 4-(5-Bromoindole-3-yl)-6,7-dimethoxyquinazoline Investigative T59328 DRUGINFO D0X4OU 4557W Investigative T59328 DRUGINFO D0W2PQ 4-acrylamido-N-(3-bromophenyl)-2-hydroxybenzamide Investigative T59328 DRUGINFO D0S9QP 4-biphenyl-2-ylethynyl-6,7-dimethoxy-quinazoline Investigative T59328 DRUGINFO D0EH6L 5,6-Bis-p-tolylamino-isoindole-1,3-dione Investigative T59328 DRUGINFO D03WEN 5-acrylamido-N-(3-bromophenyl)-2-hydroxybenzamide Investigative T59328 DRUGINFO D03CVQ 6,7-diethoxy-4-(4-phenylbut-1-enyl)quinazoline Investigative T59328 DRUGINFO D04LXG 6,7-diethoxy-4-(5-phenylpent-1-enyl)quinazoline Investigative T59328 DRUGINFO D01WXV 6,7-diethoxy-4-styrylquinazoline Investigative T59328 DRUGINFO D0P2GE 6,7-dimethoxy-4-(2-phenylethynyl)quinazoline Investigative T59328 DRUGINFO D00WZG 6,7-dimethoxy-4-(3-phenoxyprop-1-ynyl)quinazoline Investigative T59328 DRUGINFO D0K2VO 6,7-dimethoxy-4-(4-phenylbut-1-ynyl)quinazoline Investigative T59328 DRUGINFO D0DF3Z 6,7-dimethoxy-N-m-tolylquinazolin-4-amine Investigative T59328 DRUGINFO D0J5SK 6-chloro-N-(3-chlorophenyl)quinazolin-4-amine Investigative T59328 DRUGINFO D02FGG AFM-21 Investigative T59328 DRUGINFO D02KVB AG 112 Investigative T59328 DRUGINFO D0H3UI AG 9 Investigative T59328 DRUGINFO D0Q3GG AG-213 Investigative T59328 DRUGINFO D0NH7M AG-538 Investigative T59328 DRUGINFO D0C5WE AGT-2000 Investigative T59328 DRUGINFO D0T7OS AL-6802 Investigative T59328 DRUGINFO D0R2RV Anti-EGFR humanized mabs Investigative T59328 DRUGINFO D09RXX Anti-EGFR mab Investigative T59328 DRUGINFO D0GB7F ARX-AHD Investigative T59328 DRUGINFO D0G9KD Benzo[g]quinazolin-4-yl-(3-bromo-phenyl)-amine Investigative T59328 DRUGINFO D01WDI Benzyl-quinazolin-4-yl-amine Investigative T59328 DRUGINFO D04GCH Bmab-200 Investigative T59328 DRUGINFO D0U6WB BPIQ-I Investigative T59328 DRUGINFO D00TZD CL-387785 Investigative T59328 DRUGINFO D0ZT9D Cochliobolic acid Investigative T59328 DRUGINFO D0K3FG EDP-13 Investigative T59328 DRUGINFO D03BJB EGFR inhibitor Investigative T59328 DRUGINFO D05MEY Epitinib Investigative T59328 DRUGINFO D0D0GS FHT-2107 Investigative T59328 DRUGINFO D0D0YK GI-3000 Investigative T59328 DRUGINFO D05FFT HDS-029 Investigative T59328 DRUGINFO D0D5EW HKI-9924129 Investigative T59328 DRUGINFO D01SQP HM-61713B Investigative T59328 DRUGINFO D04HGN HTS-00213 Investigative T59328 DRUGINFO D07CZM HTS-02876 Investigative T59328 DRUGINFO D0EP1G HTS-05058 Investigative T59328 DRUGINFO D03ZIW ICR 62 Investigative T59328 DRUGINFO D0AC7C IPS-01003 Investigative T59328 DRUGINFO D03MTY LA22-radioimmunoconjugates Investigative T59328 DRUGINFO D0D9TU LAVENDUSTIN A Investigative T59328 DRUGINFO D0V0JV mabionHER2 Investigative T59328 DRUGINFO D0WD8R MDP-01 Investigative T59328 DRUGINFO D0P0JW MG-111 Investigative T59328 DRUGINFO D08RXW MT-062 Investigative T59328 DRUGINFO D0N8TQ N-(4-(phenylamino)quinazolin-6-yl)acrylamide Investigative T59328 DRUGINFO D01WYI N-(4-m-Tolylamino-quinazolin-6-yl)-acrylamide Investigative T59328 DRUGINFO D0F6FZ N-(4-m-Tolylamino-quinazolin-7-yl)-acrylamide Investigative T59328 DRUGINFO D0B4PH N*4*-(3-Bromo-phenyl)-quinazoline-4,6,7-triamine Investigative T59328 DRUGINFO D0HM5W N*4*-(3-Bromo-phenyl)-quinazoline-4,6-diamine Investigative T59328 DRUGINFO D0K7GD N*4*-(3-Bromo-phenyl)-quinazoline-4,7-diamine Investigative T59328 DRUGINFO D05ARF N*4*-Benzyl-pyrido[4,3-d]pyrimidine-4,7-diamine Investigative T59328 DRUGINFO D00TJF N4-(3-chlorophenyl)quinazoline-4,6-diamine Investigative T59328 DRUGINFO D0X4UE N4-(3-methylphenyl)-4,6-quinazolinediamine Investigative T59328 DRUGINFO D0Y6MD NRC-2694 Investigative T59328 DRUGINFO D0CY9O ON-128 Investigative T59328 DRUGINFO D06QEQ OSI-75 Investigative T59328 DRUGINFO D0P3JW PD-0166326 Investigative T59328 DRUGINFO D0GW4Q PD-0173956 Investigative T59328 DRUGINFO D03ATU PD-158780 Investigative T59328 DRUGINFO D01VFR PD-168393 Investigative T59328 DRUGINFO D02GCE PD182905 Investigative T59328 DRUGINFO D0J2CP PF 5208766 Investigative T59328 DRUGINFO D06BJG PMID24915291C38 Investigative T59328 DRUGINFO D07UYV PMID8568816C56 Investigative T59328 DRUGINFO D03EHM PP121 Investigative T59328 DRUGINFO D0A0JL RG-50810 Investigative T59328 DRUGINFO D0AH2V RM-6427 Investigative T59328 DRUGINFO D09XIL Ro-4396686 Investigative T59328 DRUGINFO D0Y1LD RX-1792 Investigative T59328 DRUGINFO D0Q8GX SYM-011 Investigative T59328 DRUGINFO D0H3FX TGF alpha Investigative T59328 DRUGINFO D0J3EA Theliatinib Investigative T59328 DRUGINFO D0ZH1U Tyrphostin ag-1478 Investigative T59328 DRUGINFO D0E5IP WHI-P154 Investigative T59328 DRUGINFO D0NJ3Q WZ-3146 Investigative T59328 KEGGPATH hsa04010:MAPK signaling pathway T59328 KEGGPATH hsa04012:ErbB signaling pathway T59328 KEGGPATH hsa04014:Ras signaling pathway T59328 KEGGPATH hsa04015:Rap1 signaling pathway T59328 KEGGPATH hsa04020:Calcium signaling pathway T59328 KEGGPATH hsa04060:Cytokine-cytokine receptor interaction T59328 KEGGPATH hsa04066:HIF-1 signaling pathway T59328 KEGGPATH hsa04068:FoxO signaling pathway T59328 KEGGPATH hsa04144:Endocytosis T59328 KEGGPATH hsa04151:PI3K-Akt signaling pathway T59328 KEGGPATH hsa04320:Dorso-ventral axis formation T59328 KEGGPATH hsa04510:Focal adhesion T59328 KEGGPATH hsa04520:Adherens junction T59328 KEGGPATH hsa04540:Gap junction T59328 KEGGPATH hsa04810:Regulation of actin cytoskeleton T59328 KEGGPATH hsa04912:GnRH signaling pathway T59328 KEGGPATH hsa04915:Estrogen signaling pathway T59328 KEGGPATH hsa04921:Oxytocin signaling pathway T59328 KEGGPATH hsa05120:Epithelial cell signaling in Helicobacter pylori infection T59328 KEGGPATH hsa05160:Hepatitis C T59328 KEGGPATH hsa05200:Pathways in cancer T59328 KEGGPATH hsa05205:Proteoglycans in cancer T59328 KEGGPATH hsa05206:MicroRNAs in cancer T59328 KEGGPATH hsa05212:Pancreatic cancer T59328 KEGGPATH hsa05213:Endometrial cancer T59328 KEGGPATH hsa05214:Glioma T59328 KEGGPATH hsa05215:Prostate cancer T59328 KEGGPATH hsa05218:Melanoma T59328 KEGGPATH hsa05219:Bladder cancer T59328 KEGGPATH hsa05223:Non-small cell lung cancer T59328 KEGGPATH hsa05230:Central carbon metabolism in cancer T59328 KEGGPATH hsa05231:Choline metabolism in cancer T59328 WIKIPATH WP1843:L1CAM interactions T59328 WIKIPATH WP1910:Signaling by EGFR T59328 WIKIPATH WP1984:Integrated Breast Cancer Pathway T59328 WIKIPATH WP2002:miR-targeted genes in epithelium - TarBase T59328 WIKIPATH WP2004:miR-targeted genes in lymphocytes - TarBase T59328 WIKIPATH WP2005:miR-targeted genes in muscle cell - TarBase T59328 WIKIPATH WP2100:Arylhydrocarbon receptor (AhR) signaling pathway T59328 WIKIPATH WP2261:Signaling Pathways in Glioblastoma T59328 WIKIPATH WP2324:AGE/RAGE pathway T59328 WIKIPATH WP2363:Gastric cancer network 2 T59328 WIKIPATH WP2377:Integrated Pancreatic Cancer Pathway T59328 WIKIPATH WP2431:Spinal Cord Injury T59328 WIKIPATH WP2586:Aryl Hydrocarbon Receptor T59328 WIKIPATH WP2643:Nanoparticle-mediated activation of receptor signaling T59328 WIKIPATH WP2653:PIP3 activates AKT signaling T59328 WIKIPATH WP2664:Gastrin-CREB signalling pathway via PKC and MAPK T59328 WIKIPATH WP2780:Signaling by ERBB2 T59328 WIKIPATH WP2781:Signaling by ERBB4 T59328 WIKIPATH WP2804:Hair Follicle Development: Induction (Part 1 of 3) T59328 WIKIPATH WP2828:Bladder Cancer T59328 WIKIPATH WP2840:Hair Follicle Development: Cytodifferentiation (Part 3 of 3) T59328 WIKIPATH WP2868:TCA Cycle Nutrient Utilization and Invasiveness of Ovarian Cancer T59328 WIKIPATH WP2870:Extracellular vesicle-mediated signaling in recipient cells T59328 WIKIPATH WP2873:Aryl Hydrocarbon Receptor Pathway T59328 WIKIPATH WP306:Focal Adhesion T59328 WIKIPATH WP382:MAPK Signaling Pathway T59328 WIKIPATH WP437:EGF/EGFR Signaling Pathway T59328 WIKIPATH WP51:Regulation of Actin Cytoskeleton T59328 WIKIPATH WP673:ErbB Signaling Pathway T59328 REACPATH R-HSA-1236382:Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants T59328 REACPATH R-HSA-1250196:SHC1 events in ERBB2 signaling T59328 REACPATH R-HSA-1251932:PLCG1 events in ERBB2 signaling T59328 REACPATH R-HSA-1257604:PIP3 activates AKT signaling T59328 REACPATH R-HSA-179812:GRB2 events in EGFR signaling T59328 REACPATH R-HSA-180292:GAB1 signalosome T59328 REACPATH R-HSA-180336:SHC1 events in EGFR signaling T59328 REACPATH R-HSA-182971:EGFR downregulation T59328 REACPATH R-HSA-1963640:GRB2 events in ERBB2 signaling T59328 REACPATH R-HSA-1963642:PI3K events in ERBB2 signaling T59328 REACPATH R-HSA-2179392:EGFR Transactivation by Gastrin T59328 REACPATH R-HSA-2219530:Constitutive Signaling by Aberrant PI3K in Cancer T59328 REACPATH R-HSA-5637810:Constitutive Signaling by EGFRvIII T59328 REACPATH R-HSA-5673001:RAF/MAP kinase cascade T59328 NET_PATH NetPath_16:IL4 Signaling Pathway T59328 NET_PATH NetPath_4:EGFR1 Signaling Pathway T59328 INTEPATH a6b1_a6b4_integrin_pathway:a6b1 and a6b4 Integrin signaling T59328 INTEPATH ajdiss_2pathway:Posttranslational regulation of adherens junction stability and dissassembly T59328 INTEPATH arf6_pathway:Arf6 signaling events T59328 INTEPATH ecadherin_keratinocyte_pathway:E-cadherin signaling in keratinocytes T59328 INTEPATH ecadherin_stabilization_pathway:Stabilization and expansion of the E-cadherin adherens junction T59328 INTEPATH erbb_network_pathway:ErbB receptor signaling network T59328 INTEPATH erbb1_downstream_pathway:ErbB1 downstream signaling T59328 INTEPATH erbb1_internalization_pathway:Internalization of ErbB1 T59328 INTEPATH erbb1_receptor_proximal_pathway:EGF receptor (ErbB1) signaling pathway T59328 INTEPATH et_egfrpathway:EGFR-dependent Endothelin signaling events T59328 INTEPATH lysophospholipid_pathway:LPA receptor mediated events T59328 INTEPATH p53downstreampathway:Direct p53 effectors T59328 INTEPATH ptp1bpathway:Signaling events mediated by PTP1B T59328 INTEPATH shp2_pathway:SHP2 signaling T59328 INTEPATH syndecan_3_pathway:Syndecan-3-mediated signaling events T59328 INTEPATH tcptp_pathway:Signaling events mediated by TCPTP T59328 INTEPATH telomerasepathway:Regulation of Telomerase T59328 INTEPATH txa2pathway:Thromboxane A2 receptor signaling T59328 INTEPATH upa_upar_pathway:Urokinase-type plasminogen activator (uPA) and uPAR-mediated signaling T59328 PANTPATH P00012:Cadherin signaling pathway T59328 PANTPATH P00018:EGF receptor signaling pathway T89515 TARGETID T89515 T89515 FORMERID TTDS00208 T89515 UNIPROID DEFM_HUMAN T89515 TARGNAME Polypeptide deformylase (PDF) T89515 GENENAME PDF T89515 TARGTYPE Successful target T89515 SYNONYMS PDF T89515 FUNCTION Bifunctional enzyme. Involved in de novo dTMP biosynthesis. Key enzyme in folate metabolism. Catalyzes an essential reaction for de novo glycine and purine synthesis, DNA precursor synthesis, and for the conversion of dUMP to dTMP. T89515 PDBSTRUC 3G5P; 3G5K T89515 BIOCLASS CH-NH donor oxidoreductase T89515 ECNUMBER EC 3.5.1.88 T89515 SEQUENCE MARLWGALSLWPLWAAVPWGGAAAVGVRACSSTAAPDGVEGPALRRSYWRHLRRLVLGPPEPPFSHVCQVGDPVLRGVAAPVERAQLGGPELQRLTQRLVQVMRRRRCVGLSAPQLGVPRQVLALELPEALCRECPPRQRALRQMEPFPLRVFVNPSLRVLDSRLVTFPEGCESVAGFLACVPRFQAVQISGLDPNGEQVVWQASGWAARIIQHEMDHLQGCLFIDKMDSRTFTNVYWMKVND T89515 DRUGINFO D0Y2DI Chlorproguanil Approved T89515 DRUGINFO D0E3SF MCB-3837 Approved T89515 DRUGINFO D0Y4AW Meprobamate Approved T89515 DRUGINFO D02LWU Pralatrexate Approved T89515 DRUGINFO D0P8RS Proguanil Approved T89515 DRUGINFO D0Y7TS Trimetrexate Approved T89515 DRUGINFO D0A2UV Ustekinumab Approved T89515 DRUGINFO D0W3LI LY333531 Phase 2 T89515 DRUGINFO D02AIM Metoprine Phase 2 T89515 DRUGINFO D0D2RN Aminopterin Withdrawn from market T89515 DRUGINFO D07KZA 2-(N-Morpholino)-Ethanesulfonic Acid Investigative T89515 DRUGINFO D03DRF 2-Allylthio-3-benzyl-6-nitro-quinazolin-4(3H)-one Investigative T89515 DRUGINFO D0S4ZT 2-Allylthio-6-amino-3-benzyl-quinazolin-4(3H)-one Investigative T89515 DRUGINFO D0J2FY 2'-Monophosphoadenosine 5'-Diphosphoribose Investigative T89515 DRUGINFO D0CH7U 2'-Monophosphoadenosine-5'-Diphosphate Investigative T89515 DRUGINFO D0Q5FV 2-Sulfhydryl-Ethanol Investigative T89515 DRUGINFO D01UOO 3-Benzyl-2-ethylthio-6-nitro-quinazolin-4(3H)-one Investigative T89515 DRUGINFO D0UR9D 3-benzyl-2-mercapto-6-nitroquinazolin-4(3H)-one Investigative T89515 DRUGINFO D0AT2Z 3-Phenylsulfanylmethyl-quinoxaline-5,7-diamine Investigative T89515 DRUGINFO D0U7CJ 4-(2,6-diamino-9H-purin-8-yl)-2,6-dimethoxyphenol Investigative T89515 DRUGINFO D02ZPZ 5-((E)-Styryl)-quinazoline-2,4-diamine Investigative T89515 DRUGINFO D0ME8Z 5-(2-fluorobenzyloxy)quinazoline-2,4-diamine Investigative T89515 DRUGINFO D0C1EF 5-(4-Methoxyphenoxy)-2,4-Quinazolinediamine Investigative T89515 DRUGINFO D0KY9B 5-Chloryl-2,4,6-Quinazolinetriamine Investigative T89515 DRUGINFO D0A9WT 5-Formyl-6-Hydrofolic Acid Investigative T89515 DRUGINFO D08GPU 5-Phenethyl-quinazoline-2,4-diamine Investigative T89515 DRUGINFO D02ZCP 5-Phenylsulfanyl-2,4-Quinazolinediamine Investigative T89515 DRUGINFO D0J4KJ 5-p-Tolylsulfanyl-quinazoline-2,4-diamine Investigative T89515 DRUGINFO D0V1UL 6-(2-Phenylsulfanyl-ethyl)-pteridine-2,4-diamine Investigative T89515 DRUGINFO D01ILN 6,7-Diphenyl-pteridine-2,4-diamine Investigative T89515 DRUGINFO D0A8HX 6-m-Tolyl-pteridine-2,4,7-triamine Investigative T89515 DRUGINFO D08CMW 6-Phenylaminomethyl-quinazoline-2,4-diamine Investigative T89515 DRUGINFO D0V9US 6-Phenylsulfanylmethyl-pteridine-2,4-diamine Investigative T89515 DRUGINFO D0Y3TU 7H-Pyrrolo[3,2-f]quinazoline-1,3-diamine Investigative T89515 DRUGINFO D06QEN 7-Methyl-7H-pyrrolo[3,2-f]quinazoline-1,3-diamine Investigative T89515 DRUGINFO D0Y5JB 8-(2,3,4-trimethoxyphenyl)-9H-purine-2,6-diamine Investigative T89515 DRUGINFO D05TPU 8-(2,4,5-trimethoxyphenyl)-9H-purine-2,6-diamine Investigative T89515 DRUGINFO D05KJX 8-(2,4,6-trimethoxyphenyl)-9H-purine-2,6-diamine Investigative T89515 DRUGINFO D0SB0W 8-(2,4-dimethoxyphenyl)-9H-purine-2,6-diamine Investigative T89515 DRUGINFO D0A5GM 8-(2,5-dimethoxyphenyl)-9H-purine-2,6-diamine Investigative T89515 DRUGINFO D0U0KY 8-(2,6-Dichloro-phenyl)-9H-purine-2,6-diamine Investigative T89515 DRUGINFO D07BKE 8-(3,4,5-trimethoxyphenyl)-9H-purine-2,6-diamine Investigative T89515 DRUGINFO D04UBQ 8-(3,4-dichlorophenyl)-9H-purine-2,6-diamine Investigative T89515 DRUGINFO D03POU 8-(3,4-dimethoxyphenyl)-9H-purine-2,6-diamine Investigative T89515 DRUGINFO D0S1VJ 8-(3,5-dimethoxyphenyl)-9H-purine-2,6-diamine Investigative T89515 DRUGINFO D0H2VY 8-benzyl-9H-purine-2,6-diamine Investigative T89515 DRUGINFO D0B9MY 8-Pyridin-4-yl-9H-purine-2,6-diamine Investigative T89515 DRUGINFO D0C9NE Biopterin Investigative T89515 DRUGINFO D0DT4R Brodimoprim-4,6-Dicarboxylate Investigative T89515 DRUGINFO D0A6CS Bromo-WR99210 Investigative T89515 DRUGINFO D0O9YG Cycloguanil Investigative T89515 DRUGINFO D06YIB DDATHF Investigative T89515 DRUGINFO D09YVN Dihydrofolic Acid Investigative T89515 DRUGINFO D05WHM Edatrexate Investigative T89515 DRUGINFO D06DIH Furo[2,3d]Pyrimidine Antifolate Investigative T89515 DRUGINFO D0LH5P GNF-PF-173 Investigative T89515 DRUGINFO D0H8AW GNF-PF-607 Investigative T89515 DRUGINFO D07XLJ N*6*-Benzyl-quinazoline-2,4,6-triamine Investigative T89515 DRUGINFO D04MOZ NB3178 Investigative T89515 DRUGINFO D0H4NN NB3322 Investigative T89515 DRUGINFO D0T1XE Pergularinine Investigative T89515 DRUGINFO D0UZ9U PREMETREXED Investigative T89515 DRUGINFO D0B1PE Ro 5-4864 Investigative T89515 DRUGINFO D06UPT Sri-9439 Investigative T89515 DRUGINFO D0D1ON Sri-9662 Investigative T89515 DRUGINFO D0C1UM Tylophorinidine Investigative T89515 WHIZPATH PW000024:Folate Metabolism T89515 WHIZPATH PW000140:Pterine Biosynthesis T89515 REACPATH R-HSA-113510:E2F mediated regulation of DNA replication T89515 REACPATH R-HSA-1474151:Tetrahydrobiopterin (BH4) synthesis, recycling, salvage and regulation T89515 REACPATH R-HSA-196757:Metabolism of folate and pterines T89515 REACPATH R-HSA-69205:G1/S-Specific Transcription T08391 TARGETID T08391 T08391 FORMERID TTDC00187 T08391 UNIPROID JAK2_HUMAN T08391 TARGNAME Janus kinase 2 (JAK-2) T08391 GENENAME JAK2 T08391 TARGTYPE Successful target T08391 SYNONYMS Tyrosine-protein kinase JAK2 T08391 FUNCTION Mediates essential signaling events in both innate and adaptive immunity. In the cytoplasm, plays a pivotal role in signal transduction via its association with type I receptors such as growth hormone (GHR), prolactin (PRLR), leptin (LEPR), erythropoietin (EPOR), thrombopoietin (THPO); or type II receptors including IFN-alpha, IFN-beta, IFN-gamma and multiple interleukins. Following ligand-binding to cell surface receptors, phosphorylates specific tyrosine residues on the cytoplasmic tails of the receptor, creating docking sites for STATs proteins. Subsequently, phosphorylates the STATs proteins once they are recruited to the receptor. Phosphorylated STATs then form homodimer or heterodimers and translocate to the nucleus to activate gene transcription. For example, cell stimulation with erythropoietin (EPO) during erythropoiesis leads to JAK2 autophosphorylation, activation, and its association with erythropoietin receptor (EPOR) that becomes phosphorylated in its cytoplasmic domain. Then, STAT5 (STAT5A or STAT5B) is recruited, phosphorylated and activated by JAK2. Once activated, dimerized STAT5 translocates into the nucleus and promotes the transcription of several essential genes involved in the modulation of erythropoiesis. Part of a signaling cascade that is activated by increased cellular retinol and that leads to the activation of STAT5 (STAT5A or STAT5B). In addition, JAK2 mediates angiotensin-2-induced ARHGEF1 phosphorylation. Plays a role in cell cycle by phosphorylating CDKN1B. Cooperates with TEC through reciprocal phosphorylation to mediate cytokine-driven activation of FOS transcription. In the nucleus, plays a key role in chromatin by specifically mediating phosphorylation of 'Tyr-41' of histone H3 (H3Y41ph), a specific tag that promotes exclusion of CBX5 (HP1 alpha) from chromatin. Non-receptor tyrosine kinase involved in various processes such as cell growth, development, differentiation or histone modifications. T08391 PDBSTRUC 6M9H; 6E2Q; 6E2P; 6DRW; 6BSS T08391 BIOCLASS Kinase T08391 ECNUMBER EC 2.7.10.2 T08391 SEQUENCE MGMACLTMTEMEGTSTSSIYQNGDISGNANSMKQIDPVLQVYLYHSLGKSEADYLTFPSGEYVAEEICIAASKACGITPVYHNMFALMSETERIWYPPNHVFHIDESTRHNVLYRIRFYFPRWYCSGSNRAYRHGISRGAEAPLLDDFVMSYLFAQWRHDFVHGWIKVPVTHETQEECLGMAVLDMMRIAKENDQTPLAIYNSISYKTFLPKCIRAKIQDYHILTRKRIRYRFRRFIQQFSQCKATARNLKLKYLINLETLQSAFYTEKFEVKEPGSGPSGEEIFATIIITGNGGIQWSRGKHKESETLTEQDLQLYCDFPNIIDVSIKQANQEGSNESRVVTIHKQDGKNLEIELSSLREALSFVSLIDGYYRLTADAHHYLCKEVAPPAVLENIQSNCHGPISMDFAISKLKKAGNQTGLYVLRCSPKDFNKYFLTFAVERENVIEYKHCLITKNENEEYNLSGTKKNFSSLKDLLNCYQMETVRSDNIIFQFTKCCPPKPKDKSNLLVFRTNGVSDVPTSPTLQRPTHMNQMVFHKIRNEDLIFNESLGQGTFTKIFKGVRREVGDYGQLHETEVLLKVLDKAHRNYSESFFEAASMMSKLSHKHLVLNYGVCVCGDENILVQEFVKFGSLDTYLKKNKNCINILWKLEVAKQLAWAMHFLEENTLIHGNVCAKNILLIREEDRKTGNPPFIKLSDPGISITVLPKDILQERIPWVPPECIENPKNLNLATDKWSFGTTLWEICSGGDKPLSALDSQRKLQFYEDRHQLPAPKWAELANLINNCMDYEPDFRPSFRAIIRDLNSLFTPDYELLTENDMLPNMRIGALGFSGAFEDRDPTQFEERHLKFLQQLGKGNFGSVEMCRYDPLQDNTGEVVAVKKLQHSTEEHLRDFEREIEILKSLQHDNIVKYKGVCYSAGRRNLKLIMEYLPYGSLRDYLQKHKERIDHIKLLQYTSQICKGMEYLGTKRYIHRDLATRNILVENENRVKIGDFGLTKVLPQDKEYYKVKEPGESPIFWYAPESLTESKFSVASDVWSFGVVLYELFTYIEKSKSPPAEFMRMIGNDKQGQMIVFHLIELLKNNGRLPRPDGCPDEIYMIMTECWNNNVNQRPSFRDLALRVDQIRDNMAG T08391 DRUGINFO D0Y7IC Baricitinib Approved T08391 DRUGINFO D0G8BM Fedratinib Approved T08391 DRUGINFO D04LKS Ruxolitinib Approved T08391 DRUGINFO D0GH3Q ITF2357 Phase 3 T08391 DRUGINFO D0D5ZJ Momelotinib Phase 3 T08391 DRUGINFO D0PN8H Pacritinib Phase 3 T08391 DRUGINFO D05AJT XL019 Phase 3 T08391 DRUGINFO D0MP0X AZD1480 Phase 2 T08391 DRUGINFO D0DK8X BMS-911543 Phase 2 T08391 DRUGINFO D0BI3N Cerdulatinib Phase 2 T08391 DRUGINFO D01UAU CTP-543 Phase 2 T08391 DRUGINFO DU10JI CTP-543 Phase 2 T08391 DRUGINFO D09AFI INCB039110 Phase 2 T08391 DRUGINFO D05TSJ LY2784544 Phase 2 T08391 DRUGINFO D00MYW NS-018 Phase 1/2 T08391 DRUGINFO D08CNP AC430 Phase 1 T08391 DRUGINFO D0S0NX Peginterferon beta Phase 1 T08391 DRUGINFO D00RYA SB-1578 Phase 1 T08391 DRUGINFO D07XYI 1,2,4-triazolo[1,5a]pyridine derivative 1 Patented T08391 DRUGINFO D0NP2W 1,2,4-triazolo[1,5a]pyridine derivative 2 Patented T08391 DRUGINFO D0JZ2B Alkynyl-substituted pyrimidinyl-pyrrole derivative 1 Patented T08391 DRUGINFO D05AXE Aminooxazole carboxamide derivative 1 Patented T08391 DRUGINFO D09ALF Aminotriazolopyridine derivative 1 Patented T08391 DRUGINFO D0QD5Y Aromatic bicyclic compound 1 Patented T08391 DRUGINFO D0VI7E Aromatic bicyclic compound 2 Patented T08391 DRUGINFO D0M5AG Aromatic bicyclic compound 3 Patented T08391 DRUGINFO D0M9YZ Aromatic bicyclic compound 4 Patented T08391 DRUGINFO D0Q5JV Aromatic bicyclic compound 5 Patented T08391 DRUGINFO D09RTW Aromatic bicyclic compound 6 Patented T08391 DRUGINFO D01CRX Benzimidazole derivative 7 Patented T08391 DRUGINFO D01FVC Bis-aminopyrimidine derivative 1 Patented T08391 DRUGINFO D0LR6J Bis-aminopyrimidine derivative 2 Patented T08391 DRUGINFO D0S6XT Bis-aminopyrimidine derivative 3 Patented T08391 DRUGINFO D0SJ1Q Bis-aminopyrimidine derivative 4 Patented T08391 DRUGINFO D0M2OK Bis-aminopyrimidine derivative 5 Patented T08391 DRUGINFO D0WD1Z Curcumin analog 1 Patented T08391 DRUGINFO D0IC8O Curcumin analog 2 Patented T08391 DRUGINFO D0K2RW Cyanomethyl pypazole carboxamide derivative 1 Patented T08391 DRUGINFO D05GEL Cyclic cyanoethypypazole derivative 1 Patented T08391 DRUGINFO D0V0KI Cycloalkyl nitrile pyrazole carboxamide derivative 1 Patented T08391 DRUGINFO D0PB5X Cycloalkyl nitrile pyrazolo pyridone derivative 1 Patented T08391 DRUGINFO D0S4TH Cycloalkyl nitrile pyrazolo pyridone derivative 2 Patented T08391 DRUGINFO D08WPB Five-and-six-membered heterocyclic compound 1 Patented T08391 DRUGINFO D0H6XN Geminally-substituted cyanoethylpypazolo pyridone derivative 1 Patented T08391 DRUGINFO D0KI5F Geminally-substituted cyanoethylpypazolo pyridone derivative 2 Patented T08391 DRUGINFO D0VJ1R Imidazo[4,5-c]pyridine derivative 2 Patented T08391 DRUGINFO D0G9MM Isoxazole derivative 1 Patented T08391 DRUGINFO D0TX2G Isoxazole derivative 2 Patented T08391 DRUGINFO D0Y2IM N-(cyanomethyl)-4-(2-(phenylamino)pyrimidin-4-yl)benzamide derivative 1 Patented T08391 DRUGINFO D0A8BV PMID27774822-Compound-Figure10Compound12 Patented T08391 DRUGINFO D0AE0M PMID27774822-Compound-Figure10Compound4 Patented T08391 DRUGINFO D0GH8D PMID27774822-Compound-Figure10Example1 Patented T08391 DRUGINFO D0W8DN PMID27774822-Compound-Figure10Example19 Patented T08391 DRUGINFO D0RJ3W PMID27774822-Compound-Figure11Example5 Patented T08391 DRUGINFO D0M3CB PMID27774822-Compound-Figure1Example20 Patented T08391 DRUGINFO D0E2WK PMID27774822-Compound-Figure2Example1-1left Patented T08391 DRUGINFO D0IQ6G PMID27774822-Compound-Figure2Example1-1right Patented T08391 DRUGINFO D0NY6M PMID27774822-Compound-Figure3CompoundI-165 Patented T08391 DRUGINFO D04OCD PMID27774822-Compound-Figure7Example63 Patented T08391 DRUGINFO D0B9TH PMID27774822-Compound-Figure8Example5 Patented T08391 DRUGINFO D0YR8S PMID27774824-Compound-Figure11Example1up Patented T08391 DRUGINFO D0A6RG PMID27774824-Compound-Figure2Example4 Patented T08391 DRUGINFO D0U1HA PMID27774824-Compound-Figure3Example18 Patented T08391 DRUGINFO D0GB7G PMID27774824-Compound-Figure6Example12 Patented T08391 DRUGINFO D0F3BK PMID27774824-Compound-Figure6Example6 Patented T08391 DRUGINFO D0PM8K PMID27774824-Compound-Figure7Example10 Patented T08391 DRUGINFO D0KF8H PMID27774824-Compound-Figure8Example22 Patented T08391 DRUGINFO D0HS2J PMID27774824-Compound-Figure8Example99 Patented T08391 DRUGINFO D01DBB PMID27774824-Compound-Figure9Example2down Patented T08391 DRUGINFO D0WZ8N PMID27774824-Compound-Figure9Example2up Patented T08391 DRUGINFO D09PIS Pyrazolo[4,3-c]pyridine derivative 2 Patented T08391 DRUGINFO D03QAY Pyrazolopyridine derivative 3 Patented T08391 DRUGINFO D09RUN Pyrazolopyridine derivative 4 Patented T08391 DRUGINFO D02VGC Pyrazolopyridine derivative 6 Patented T08391 DRUGINFO D0D1QH Pyrazolopyridine derivative 7 Patented T08391 DRUGINFO D0CD6Y Pyrimidopyridazinone derivative 1 Patented T08391 DRUGINFO D0WA1V Pyrimidopyridazinone derivative 2 Patented T08391 DRUGINFO D0YJ4D Pyrrole derivative 7 Patented T08391 DRUGINFO D09UBE Pyrrole six-membered heteroaryl ring derivative 1 Patented T08391 DRUGINFO D0VQ7P Pyrrolo[2,3-d]pyrimidine derivative 11 Patented T08391 DRUGINFO D0FQ4Z Pyrrolo[2,3-d]pyrimidine derivative 6 Patented T08391 DRUGINFO D0U5FZ Pyrrolo[2,3-d]pyrimidine derivative 7 Patented T08391 DRUGINFO D0KL3B Pyrrolo[2,3-d]pyrimidine derivative 8 Patented T08391 DRUGINFO D0VR6E Pyrrolo-pyridine derivative 3 Patented T08391 DRUGINFO D06MQB Pyrrolo-pyridone derivative 1 Patented T08391 DRUGINFO D03PBI Pyrrolo-pyridone derivative 2 Patented T08391 DRUGINFO D01EYJ Ruxolitinib derivative 2 Patented T08391 DRUGINFO D00JUI Triazolo-pyridine derivative 1 Patented T08391 DRUGINFO D0G0FK Tricyclic compound 1 Patented T08391 DRUGINFO D0LS1O Tricyclic compound 11 Patented T08391 DRUGINFO D0X1FD Tricyclic heterocycle derivative 1 Patented T08391 DRUGINFO D03TEE Tricyclic heterocycle derivative 2 Patented T08391 DRUGINFO D0M2WA Tricyclic heterocycle derivative 5 Patented T08391 DRUGINFO D04BOW Tricyclic pyrrolopyridine compound 1 Patented T08391 DRUGINFO D0GZ7B AG490 Terminated T08391 DRUGINFO DLW69V 1,2,3,4,5,6-hexabromocyclohexane Investigative T08391 DRUGINFO D0I3EY 5-phenyl-1H-indazol-3-amine Investigative T08391 DRUGINFO D00MAM AMG-JAK2-01 Investigative T08391 DRUGINFO D05MHL Atropisomer 1 Investigative T08391 DRUGINFO D0OP3D AZ960 Investigative T08391 DRUGINFO D0N8CN BVB-808 Investigative T08391 DRUGINFO D0IR6U CMP-6 Investigative T08391 DRUGINFO D0I6QN K-454 Investigative T08391 DRUGINFO D02UVS NSC-1771 Investigative T08391 DRUGINFO D0A7XQ ON-044580 Investigative T08391 DRUGINFO D02NNT PMID21493067C1d Investigative T08391 DRUGINFO D0US9O PMID24359159C19a Investigative T08391 DRUGINFO D09VZR SGI-1252 Investigative T08391 DRUGINFO D0E5IP WHI-P154 Investigative T08391 KEGGPATH hsa04062:Chemokine signaling pathway T08391 KEGGPATH hsa04151:PI3K-Akt signaling pathway T08391 KEGGPATH hsa04550:Signaling pathways regulating pluripotency of stem cells T08391 KEGGPATH hsa04630:Jak-STAT signaling pathway T08391 KEGGPATH hsa04725:Cholinergic synapse T08391 KEGGPATH hsa04917:Prolactin signaling pathway T08391 KEGGPATH hsa04920:Adipocytokine signaling pathway T08391 KEGGPATH hsa05140:Leishmaniasis T08391 KEGGPATH hsa05145:Toxoplasmosis T08391 KEGGPATH hsa05152:Tuberculosis T08391 KEGGPATH hsa05162:Measles T08391 KEGGPATH hsa05164:Influenza A T08391 KEGGPATH hsa05168:Herpes simplex infection T08391 WIKIPATH WP127:IL-5 Signaling Pathway T08391 WIKIPATH WP1815:Factors involved in megakaryocyte development and platelet production T08391 WIKIPATH WP1836:Interferon gamma signaling T08391 WIKIPATH WP1840:Interleukin-3, 5 and GM-CSF signaling T08391 WIKIPATH WP2032:TSH signaling pathway T08391 WIKIPATH WP2034:Leptin signaling pathway T08391 WIKIPATH WP2112:IL17 signaling pathway T08391 WIKIPATH WP2203:TSLP Signaling Pathway T08391 WIKIPATH WP2324:AGE/RAGE pathway T08391 WIKIPATH WP2332:Interleukin-11 Signaling Pathway T08391 WIKIPATH WP2374:Oncostatin M Signaling Pathway T08391 WIKIPATH WP2380:BDNF signaling pathway T08391 WIKIPATH WP2593:JAK/STAT T08391 WIKIPATH WP2657:Growth hormone receptor signaling T08391 WIKIPATH WP2678:Prolactin receptor signaling T08391 WIKIPATH WP2713:Signaling by SCF-KIT T08391 WIKIPATH WP2732:Interleukin-2 signaling T08391 WIKIPATH WP2857:Mesodermal Commitment Pathway T08391 WIKIPATH WP286:IL-3 Signaling Pathway T08391 WIKIPATH WP304:Kit receptor signaling pathway T08391 WIKIPATH WP364:IL-6 signaling pathway T08391 WIKIPATH WP395:IL-4 Signaling Pathway T08391 WIKIPATH WP437:EGF/EGFR Signaling Pathway T08391 WIKIPATH WP581:EPO Receptor Signaling T08391 WIKIPATH WP61:Notch Signaling Pathway T08391 WIKIPATH WP619:Type II interferon signaling (IFNG) T08391 WIKIPATH WP733:Serotonin Receptor 2 and STAT3 Signaling T08391 REACPATH R-HSA-1059683:Interleukin-6 signaling T08391 REACPATH R-HSA-110056:MAPK3 (ERK1) activation T08391 REACPATH R-HSA-112411:MAPK1 (ERK2) activation T08391 REACPATH R-HSA-114604:GPVI-mediated activation cascade T08391 REACPATH R-HSA-1170546:Prolactin receptor signaling T08391 REACPATH R-HSA-3214858:RMTs methylate histone arginines T08391 REACPATH R-HSA-392451:G beta:gamma signalling through PI3Kgamma T08391 REACPATH R-HSA-512988:Interleukin-3, 5 and GM-CSF signaling T08391 REACPATH R-HSA-5673000:RAF activation T08391 REACPATH R-HSA-5673001:RAF/MAP kinase cascade T08391 REACPATH R-HSA-877300:Interferon gamma signaling T08391 REACPATH R-HSA-877312:Regulation of IFNG signaling T08391 REACPATH R-HSA-912526:Interleukin receptor SHC signaling T08391 REACPATH R-HSA-982772:Growth hormone receptor signaling T08391 REACPATH R-HSA-983231:Factors involved in megakaryocyte development and platelet production T08391 INTEPATH cxcr4_pathway:CXCR4-mediated signaling events T08391 INTEPATH endothelinpathway:Endothelins T08391 INTEPATH epopathway:EPO signaling pathway T08391 INTEPATH erbb2erbb3pathway:ErbB2/ErbB3 signaling events T08391 INTEPATH erbb4_pathway:ErbB4 signaling events T08391 INTEPATH gmcsf_pathway:GMCSF-mediated signaling events T08391 INTEPATH hes_heypathway:Notch-mediated HES/HEY network T08391 INTEPATH ifngpathway:IFN-gamma pathway T08391 INTEPATH il12_2pathway:IL12-mediated signaling events T08391 INTEPATH il23pathway:IL23-mediated signaling events T08391 INTEPATH il27pathway:IL27-mediated signaling events T08391 INTEPATH il3_pathway:IL3-mediated signaling events T08391 INTEPATH il4_2pathway:IL4-mediated signaling events T08391 INTEPATH il5_pathway:IL5-mediated signaling events T08391 INTEPATH il6_7pathway:IL6-mediated signaling events T08391 INTEPATH kitpathway:Signaling events mediated by Stem cell factor receptor (c-Kit) T08391 INTEPATH pdgfrbpathway:PDGFR-beta signaling pathway T08391 INTEPATH ptp1bpathway:Signaling events mediated by PTP1B T08391 INTEPATH s1p_s1p3_pathway:S1P3 pathway T08391 INTEPATH shp2_pathway:SHP2 signaling T08391 PANTPATH P00031:Inflammation mediated by chemokine and cytokine signaling pathway T08391 PANTPATH P00035:Interferon-gamma signaling pathway T08391 PANTPATH P00038:JAK/STAT signaling pathway T08391 PANTPATH P00047:PDGF signaling pathway T08391 PANTPATH P00048:PI3 kinase pathway T08391 PANTPATH P06959:CCKR signaling map ST T07663 TARGETID T07663 T07663 FORMERID TTDS00296 T07663 UNIPROID PDE5A_HUMAN T07663 TARGNAME Phosphodiesterase 5A (PDE5A) T07663 GENENAME PDE5A T07663 TARGTYPE Successful target T07663 SYNONYMS cGMP-specific 3',5'-cyclic phosphodiesterase; PDE5A; CGMP-binding cGMP-specific phosphodiesterase; CGB-PDE T07663 FUNCTION Plays a role in signal transduction by regulating the intracellular concentration of cyclic nucleotides. This phosphodiesterase catalyzes the specific hydrolysis of cGMP to 5'-GMP. Specifically regulates nitric-oxide-generated cGMP. T07663 PDBSTRUC 6ACB; 5ZZ2; 5JO3; 4OEX; 4OEW T07663 BIOCLASS Phosphoric diester hydrolase T07663 ECNUMBER EC 3.1.4.35 T07663 SEQUENCE MERAGPSFGQQRQQQQPQQQKQQQRDQDSVEAWLDDHWDFTFSYFVRKATREMVNAWFAERVHTIPVCKEGIRGHTESCSCPLQQSPRADNSAPGTPTRKISASEFDRPLRPIVVKDSEGTVSFLSDSEKKEQMPLTPPRFDHDEGDQCSRLLELVKDISSHLDVTALCHKIFLHIHGLISADRYSLFLVCEDSSNDKFLISRLFDVAEGSTLEEVSNNCIRLEWNKGIVGHVAALGEPLNIKDAYEDPRFNAEVDQITGYKTQSILCMPIKNHREEVVGVAQAINKKSGNGGTFTEKDEKDFAAYLAFCGIVLHNAQLYETSLLENKRNQVLLDLASLIFEEQQSLEVILKKIAATIISFMQVQKCTIFIVDEDCSDSFSSVFHMECEELEKSSDTLTREHDANKINYMYAQYVKNTMEPLNIPDVSKDKRFPWTTENTGNVNQQCIRSLLCTPIKNGKKNKVIGVCQLVNKMEENTGKVKPFNRNDEQFLEAFVIFCGLGIQNTQMYEAVERAMAKQMVTLEVLSYHASAAEEETRELQSLAAAVVPSAQTLKITDFSFSDFELSDLETALCTIRMFTDLNLVQNFQMKHEVLCRWILSVKKNYRKNVAYHNWRHAFNTAQCMFAALKAGKIQNKLTDLEILALLIAALSHDLDHRGVNNSYIQRSEHPLAQLYCHSIMEHHHFDQCLMILNSPGNQILSGLSIEEYKTTLKIIKQAILATDLALYIKRRGEFFELIRKNQFNLEDPHQKELFLAMLMTACDLSAITKPWPIQQRIAELVATEFFDQGDRERKELNIEPTDLMNREKKNKIPSMQVGFIDAICLQLYEALTHVSEDCFPLLDGCRKNRQKWQALAEQQEKMLINGESGQAKRN T07663 DRUGINFO D0Y5JC Avanafil Approved T07663 DRUGINFO D0F9GE Dipyridamole Approved T07663 DRUGINFO D0NJ3V Papaverine Approved T07663 DRUGINFO D0Z7ZM Rhucin Approved T07663 DRUGINFO D05MQK Tadalafil Approved T07663 DRUGINFO D01GUS Udenafil Approved T07663 DRUGINFO D0C9SY Vardenafil Approved T07663 DRUGINFO D0M9VE EXISULIND Phase 3 T07663 DRUGINFO D05OQG ICARIIN Phase 3 T07663 DRUGINFO D0M9FQ PF-489791 Phase 2 T07663 DRUGINFO D09OCK UK-371800 Phase 1 T07663 DRUGINFO D0K2BQ BRL-61063 Discontinued in Phase 2 T07663 DRUGINFO D0K2QG DASANTAFIL Discontinued in Phase 2 T07663 DRUGINFO D00SPK E-4021 Discontinued in Phase 2 T07663 DRUGINFO D0X1LO EMR-62203 Discontinued in Phase 2 T07663 DRUGINFO D0D7XW SINITRODIL Discontinued in Phase 2 T07663 DRUGINFO D04NPP SLX-2101 Discontinued in Phase 2 T07663 DRUGINFO D0N5SC UK-369003 Discontinued in Phase 1/2 T07663 DRUGINFO D0W8QG FR-229934 Terminated T07663 DRUGINFO D09UMA IMAZODAN Terminated T07663 DRUGINFO D0W8OH SKF-96231 Terminated T07663 DRUGINFO D01FRF Trequinsin Terminated T07663 DRUGINFO D00YPW ZAPRINAST Terminated T07663 DRUGINFO D09WUP 3,7-Bis(2-hydroxyethyl)icaritin Investigative T07663 DRUGINFO D03BWH 7-(2-Hydroxyethyl)-3-O-rhamnosylicariin Investigative T07663 DRUGINFO D0X7SR 8-prenylapigenin Investigative T07663 DRUGINFO D0W2BI 8-prenylquercetin Investigative T07663 DRUGINFO D0V3BI Aom-0890 Investigative T07663 DRUGINFO D0O3QI Benzo[1,3]dioxol-5-ylmethyl-quinazolin-4-yl-amine Investigative T07663 DRUGINFO D0V1CL Cartazolate Investigative T07663 DRUGINFO D06URK CKD-533 Investigative T07663 DRUGINFO D08VGM Gamma-Glutamyl[S-(2-Iodobenzyl)Cysteinyl]Glycine Investigative T07663 DRUGINFO D04AWP Guanosine-5'-Monophosphate Investigative T07663 DRUGINFO D06TLQ Icariside II Investigative T07663 DRUGINFO D0R6MT isobutylmethylxanthine Investigative T07663 DRUGINFO D06GUJ KURAIDIN Investigative T07663 DRUGINFO D0W4ZU KURARINOL Investigative T07663 DRUGINFO D0YZ0L LORNEIC ACID A Investigative T07663 DRUGINFO D0T5PO ROLIPRAM Investigative T07663 DRUGINFO D0H6ZC RWJ-387273 Investigative T07663 DRUGINFO D02VHD SCH51866 Investigative T07663 DRUGINFO D0KD6S SCH-57726 Investigative T07663 DRUGINFO D00QCL SOPHOFLAVESCENOL Investigative T07663 DRUGINFO D0S8AV SOPHORAFLAVANONE B Investigative T07663 DRUGINFO D0LZ5R T0156 Investigative T07663 DRUGINFO D0XQ8A TPN-729 Investigative T07663 KEGGPATH hsa00230:Purine metabolism T07663 KEGGPATH hsa04022:cGMP-PKG signaling pathway T07663 REACPATH R-HSA-418457:cGMP effects T07663 NET_PATH NetPath_7:TGF_beta_Receptor Signaling Pathway T63505 TARGETID T63505 T63505 FORMERID TTDNS00592 T63505 UNIPROID ABL1_HUMAN T63505 TARGNAME Tyrosine-protein kinase ABL1 (ABL) T63505 GENENAME ABL1 T63505 TARGTYPE Successful target T63505 SYNONYMS p150; Proto-oncogene tyrosine-protein kinase ABL1; Proto-oncogene c-Abl; JTK7; C-ABL; Abl; Abelson tyrosine-protein kinase 1; Abelson murine leukemia viral oncogene homolog 1 T63505 FUNCTION Coordinates actin remodeling through tyrosine phosphorylation of proteins controlling cytoskeleton dynamics like WASF3 (involved in branch formation); ANXA1 (involved in membrane anchoring); DBN1, DBNL, CTTN, RAPH1 and ENAH (involved in signaling); or MAPT and PXN (microtubule-binding proteins). Phosphorylation of WASF3 is critical for the stimulation of lamellipodia formation and cell migration. Involved in the regulation of cell adhesion and motility through phosphorylation of key regulators of these processes such as BCAR1, CRK, CRKL, DOK1, EFS or NEDD9. Phosphorylates multiple receptor tyrosine kinases and more particularly promotes endocytosis of EGFR, facilitates the formation of neuromuscular synapses through MUSK, inhibits PDGFRB-mediated chemotaxis and modulates the endocytosis of activated B-cell receptor complexes. Other substrates which are involved in endocytosis regulation are the caveolin (CAV1) and RIN1. Moreover, ABL1 regulates the CBL family of ubiquitin ligases that drive receptor down-regulation and actin remodeling. Phosphorylation of CBL leads to increased EGFR stability. Involved in late-stage autophagy by regulating positively the trafficking and function of lysosomal components. ABL1 targets to mitochondria in response to oxidative stress and thereby mediates mitochondrial dysfunction and cell death. In response to oxidative stress, phosphorylates serine/threonine kinase PRKD2 at 'Tyr-717'. ABL1 is also translocated in the nucleus where it has DNA-binding activity and is involved in DNA-damage response and apoptosis. Many substrates are known mediators of DNA repair: DDB1, DDB2, ERCC3, ERCC6, RAD9A, RAD51, RAD52 or WRN. Activates the proapoptotic pathway when the DNA damage is too severe to be repaired. Phosphorylates TP73, a primary regulator for this type of damage-induced apoptosis. Phosphorylates the caspase CASP9 on 'Tyr-153' and regulates its processing in the apoptotic response to DNA damage. Phosphorylates PSMA7 that leads to an inhibition of proteasomal activity and cell cycle transition blocks. ABL1 acts also as a regulator of multiple pathological signaling cascades during infection. Several known tyrosine-phosphorylated microbial proteins have been identified as ABL1 substrates. This is the case of A36R of Vaccinia virus, Tir (translocated intimin receptor) of pathogenic E. coli and possibly Citrobacter, CagA (cytotoxin-associated gene A) of H. pylori, or AnkA (ankyrin repeat-containing protein A) of A. phagocytophilum. Pathogens can highjack ABL1 kinase signaling to reorganize the host actin cytoskeleton for multiple purposes, like facilitating intracellular movement and host cell exit. Finally, functions as its own regulator through autocatalytic activity as well as through phosphorylation of its inhibitor, ABI1. Regulates T-cell differentiation in a TBX21-dependent manner. Phosphorylates TBX21 on tyrosine residues leading to an enhancement of its transcriptional activator activity. Non-receptor tyrosine-protein kinase that plays a role in many key processes linked to cell growth and survival such as cytoskeleton remodeling in response to extracellular stimuli, cell motility and adhesion, receptor endocytosis, autophagy, DNA damage response and apoptosis. T63505 PDBSTRUC 6NPV; 6NPU; 6NPE; 6BL8; 6AMW T63505 BIOCLASS Kinase T63505 ECNUMBER EC 2.7.10.2 T63505 SEQUENCE MLEICLKLVGCKSKKGLSSSSSCYLEEALQRPVASDFEPQGLSEAARWNSKENLLAGPSENDPNLFVALYDFVASGDNTLSITKGEKLRVLGYNHNGEWCEAQTKNGQGWVPSNYITPVNSLEKHSWYHGPVSRNAAEYLLSSGINGSFLVRESESSPGQRSISLRYEGRVYHYRINTASDGKLYVSSESRFNTLAELVHHHSTVADGLITTLHYPAPKRNKPTVYGVSPNYDKWEMERTDITMKHKLGGGQYGEVYEGVWKKYSLTVAVKTLKEDTMEVEEFLKEAAVMKEIKHPNLVQLLGVCTREPPFYIITEFMTYGNLLDYLRECNRQEVNAVVLLYMATQISSAMEYLEKKNFIHRDLAARNCLVGENHLVKVADFGLSRLMTGDTYTAHAGAKFPIKWTAPESLAYNKFSIKSDVWAFGVLLWEIATYGMSPYPGIDLSQVYELLEKDYRMERPEGCPEKVYELMRACWQWNPSDRPSFAEIHQAFETMFQESSISDEVEKELGKQGVRGAVSTLLQAPELPTKTRTSRRAAEHRDTTDVPEMPHSKGQGESDPLDHEPAVSPLLPRKERGPPEGGLNEDERLLPKDKKTNLFSALIKKKKKTAPTPPKRSSSFREMDGQPERRGAGEEEGRDISNGALAFTPLDTADPAKSPKPSNGAGVPNGALRESGGSGFRSPHLWKKSSTLTSSRLATGEEEGGGSSSKRFLRSCSASCVPHGAKDTEWRSVTLPRDLQSTGRQFDSSTFGGHKSEKPALPRKRAGENRSDQVTRGTVTPPPRLVKKNEEAADEVFKDIMESSPGSSPPNLTPKPLRRQVTVAPASGLPHKEEAGKGSALGTPAAAEPVTPTSKAGSGAPGGTSKGPAEESRVRRHKHSSESPGRDKGKLSRLKPAPPPPPAASAGKAGGKPSQSPSQEAAGEAVLGAKTKATSLVDAVNSDAAKPSQPGEGLKKPVLPATPKPQSAKPSGTPISPAPVPSTLPSASSALAGDQPSSTAFIPLISTRVSLRKTRQPPERIASGAITKGVVLDSTEALCLAISRNSEQMASHSAVLEAGKNLYTFCVSYVDSIQQMRNKFAFREAINKLENNLRELQICPATAGSGPAATQDFSKLLSSVKEISDIVQR T63505 DRUGINFO D01BYB Adenosine triphosphate Approved T63505 DRUGINFO D0OB0F Bosutinib Approved T63505 DRUGINFO D0H0EQ Ponatinib Approved T63505 DRUGINFO D03MNN SKI-758 Approved T63505 DRUGINFO D06JHV Flumatinib Phase 2 T63505 DRUGINFO D0M0XB Saracatinib Phase 2 T63505 DRUGINFO D0E0NM DCC-2036 Phase 1/2 T63505 DRUGINFO D06CIJ ISIS-CRP Phase 1 T63505 DRUGINFO D00ABO KW-2449 Phase 1 T63505 DRUGINFO D0O0RB 6,6-fused nitrogenous heterocyclic compound 1 Patented T63505 DRUGINFO D0QD6T 6,6-fused nitrogenous heterocyclic compound 2 Patented T63505 DRUGINFO D0XL1M 6,6-fused nitrogenous heterocyclic compound 3 Patented T63505 DRUGINFO D0X9VH Azaindole derivative 1 Patented T63505 DRUGINFO D05TYI Azaindole derivative 2 Patented T63505 DRUGINFO D0F4AW Indol-5-ol derivative 1 Patented T63505 DRUGINFO D0X0VH PMID25656651-Compound-28a Patented T63505 DRUGINFO D0RT8M PMID25656651-Compound-28b Patented T63505 DRUGINFO D0TX1S PMID25656651-Compound-33a Patented T63505 DRUGINFO D0JD9Z PMID25656651-Compound-33b Patented T63505 DRUGINFO D06LHV PMID25656651-Compound-34a Patented T63505 DRUGINFO D0KM7V PMID25656651-Compound-34b Patented T63505 DRUGINFO D03JXD PMID25656651-Compound-34c Patented T63505 DRUGINFO D0ZH4I PMID25656651-Compound-42 Patented T63505 DRUGINFO D0Y0PE PMID25656651-Compound-46 Patented T63505 DRUGINFO D01DBB PMID27774824-Compound-Figure9Example2down Patented T63505 DRUGINFO D0WZ8N PMID27774824-Compound-Figure9Example2up Patented T63505 DRUGINFO D04GFO MC-2001 Preclinical T63505 DRUGINFO D03PLP [1,1':2',1'']-terphenyl-4,3'',5''-triol Investigative T63505 DRUGINFO D0A5RM 4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol Investigative T63505 DRUGINFO D0D8OY AP-24226 Investigative T63505 DRUGINFO D04QUI BAS-00387275 Investigative T63505 DRUGINFO D01GNF BAS-00387328 Investigative T63505 DRUGINFO D03GQI BAS-00387347 Investigative T63505 DRUGINFO D07LYJ BAS-00672722 Investigative T63505 DRUGINFO D0D8ZN BAS-01373578 Investigative T63505 DRUGINFO D09QKH BAS-0338872 Investigative T63505 DRUGINFO D0H3RD BAS-0338876 Investigative T63505 DRUGINFO D0A5MG BAS-09534324 Investigative T63505 DRUGINFO D0I3XZ Bis-(5-hydroxy-1H-indol-2-yl)-methanone Investigative T63505 DRUGINFO D0YZ7H JNJ-10198409 Investigative T63505 DRUGINFO D08OBF MYRISTIC ACID Investigative T63505 DRUGINFO D0P3JW PD-0166326 Investigative T63505 DRUGINFO D0GW4Q PD-0173956 Investigative T63505 DRUGINFO D0H1OK TG-100435 Investigative T63505 DRUGINFO D0O9NE TRISMETHOXYRESVERATROL Investigative T63505 KEGGPATH hsa04012:ErbB signaling pathway T63505 KEGGPATH hsa04014:Ras signaling pathway T63505 KEGGPATH hsa04110:Cell cycle T63505 KEGGPATH hsa04360:Axon guidance T63505 KEGGPATH hsa04722:Neurotrophin signaling pathway T63505 KEGGPATH hsa05130:Pathogenic Escherichia coli infection T63505 KEGGPATH hsa05131:Shigellosis T63505 KEGGPATH hsa05200:Pathways in cancer T63505 KEGGPATH hsa05206:MicroRNAs in cancer T63505 KEGGPATH hsa05220:Chronic myeloid leukemia T63505 KEGGPATH hsa05416:Viral myocarditis T63505 WIKIPATH WP1815:Factors involved in megakaryocyte development and platelet production T63505 WIKIPATH WP1865:Myogenesis T63505 WIKIPATH WP1918:Signaling by Robo receptor T63505 WIKIPATH WP1984:Integrated Breast Cancer Pathway T63505 WIKIPATH WP2038:Regulation of Microtubule Cytoskeleton T63505 WIKIPATH WP2272:Pathogenic Escherichia coli infection T63505 WIKIPATH WP2377:Integrated Pancreatic Cancer Pathway T63505 WIKIPATH WP2446:Retinoblastoma (RB) in Cancer T63505 WIKIPATH WP2516:ATM Signaling Pathway T63505 WIKIPATH WP2719:Fcgamma receptor (FCGR) dependent phagocytosis T63505 WIKIPATH WP2864:Apoptosis-related network due to altered Notch3 in ovarian cancer T63505 REACPATH R-HSA-2029482:Regulation of actin dynamics for phagocytic cup formation T63505 REACPATH R-HSA-375170:CDO in myogenesis T63505 REACPATH R-HSA-5663213:RHO GTPases Activate WASPs and WAVEs T63505 REACPATH R-HSA-5685938:HDR through Single Strand Annealing (SSA) T63505 REACPATH R-HSA-5693565:Recruitment and ATM-mediated phosphorylation of repair and signaling proteins at DNA double strand breaks T63505 REACPATH R-HSA-983231:Factors involved in megakaryocyte development and platelet production T63505 INTEPATH ajdiss_2pathway:Posttranslational regulation of adherens junction stability and dissassembly T63505 INTEPATH atm_pathway:ATM pathway T63505 INTEPATH lis1pathway:Lissencephaly gene (LIS1) in neuronal migration and development T63505 INTEPATH p53regulationpathway:p53 pathway T63505 INTEPATH p73pathway:p73 transcription factor network T63505 INTEPATH pdgfrbpathway:PDGFR-beta signaling pathway T63505 INTEPATH rb_1pathway:Regulation of retinoblastoma protein T63505 INTEPATH tap63pathway:Validated transcriptional targets of TAp63 isoforms T63505 INTEPATH telomerasepathway:Regulation of Telomerase T63505 INTEPATH trkrpathway:Neurotrophic factor-mediated Trk receptor signaling T63505 PANTPATH P00008:Axon guidance mediated by Slit/Robo T13201 TARGETID T13201 T13201 FORMERID TTDR01224 T13201 UNIPROID CAH1_HUMAN T13201 TARGNAME Carbonic anhydrase I (CA-I) T13201 GENENAME CA1 T13201 TARGTYPE Successful target T13201 SYNONYMS Carbonic anhydrase B; Carbonic anhydrase 1; Carbonate dehydratase I; CAB T13201 FUNCTION Can hydrates cyanamide to urea. Reversible hydration of carbon dioxide. T13201 PDBSTRUC 6HWZ; 6G3V; 6FAG; 6FAF; 6F3B T13201 BIOCLASS Alpha-carbonic anhydrase T13201 ECNUMBER EC 4.2.1.1 T13201 SEQUENCE MASPDWGYDDKNGPEQWSKLYPIANGNNQSPVDIKTSETKHDTSLKPISVSYNPATAKEIINVGHSFHVNFEDNDNRSVLKGGPFSDSYRLFQFHFHWGSTNEHGSEHTVDGVKYSAELHVAHWNSAKYSSLAEAASKADGLAVIGVLMKVGEANPKLQKVLDALQAIKTKGKRAPFTNFDPSTLLPSSLDFWTYPGSLTHPPLYESVTWIICKESISVSSEQLAQFRSLLSNVEGDNAVPMQHNNRPTQPLKGRTVRASF T13201 DRUGINFO D0E1SW Acetazolamide Approved T13201 DRUGINFO D0J4GO Dichlorphenamide Approved T13201 DRUGINFO D07INV Ethoxzolamide Approved T13201 DRUGINFO D0C2II Methazolamide Approved T13201 DRUGINFO D07HBX Salicyclic acid Approved T13201 DRUGINFO D0W2CX CG-100649 Phase 3 T13201 DRUGINFO D07SDQ Curcumin Phase 3 T13201 DRUGINFO D0A8JP PARABEN Phase 3 T13201 DRUGINFO D0L6HN PHENOL Phase 2/3 T13201 DRUGINFO D0Y6OA Coumate Phase 2 T13201 DRUGINFO D0V0UK SULFAMIDE Phase 1 T13201 DRUGINFO D03SLR FERULIC ACID Patented T13201 DRUGINFO D04JIN (2-bromophenyl)difluoromethanesulfonamide Investigative T13201 DRUGINFO D0IU3X (4-bromophenyl)difluoromethanesulfonamide Investigative T13201 DRUGINFO D0CM3O [Au(CN)2]- Investigative T13201 DRUGINFO D0L2GD [Cu(CN)2]- Investigative T13201 DRUGINFO D05RAB 1,4-Dihydro-1-methyl-4-oxo-3-pyridinesulfonamide Investigative T13201 DRUGINFO D00XIB 1-acetamido-5-sulfonamidoindane Investigative T13201 DRUGINFO D04SNH 1-Benzyl-1,4-dihydro-4-oxo-3-pyridinesulfonamide Investigative T13201 DRUGINFO D0G9NE 1-cyclohexylamido-5-sulfonamidoindane Investigative T13201 DRUGINFO D0O4KL 1-pentafluorophenylamido-5-sulfonamidoindane Investigative T13201 DRUGINFO D0KZ2D 1-valproylamido-5-sulfonamidoindane Investigative T13201 DRUGINFO D05BMD 2-(4-chlorobenzyloxyamino)-N-hydroxyacetamide Investigative T13201 DRUGINFO D06NDR 2-(4-chlorobenzyloxyamino)-N-hydroxyhexanamide Investigative T13201 DRUGINFO D0G0OP 2-(4-chlorobenzyloxyamino)-N-hydroxypropanamide Investigative T13201 DRUGINFO D0FD8G 2-(biphenyl-4-yl)vinylboronic acid Investigative T13201 DRUGINFO D0RK7J 2,2,2-Trifluoro-N-(4-sulfamoyl-phenyl)-acetamide Investigative T13201 DRUGINFO D0LC0F 2,3-dihydro-1H-indene-5-sulfonamide Investigative T13201 DRUGINFO D0S6CO 2,4-dichloro-5-sulfamoylbenzoic acid Investigative T13201 DRUGINFO D0M3PO 2,4-Disulfamyltrifluoromethylaniline Investigative T13201 DRUGINFO D00FGB 2-acetamido-5-sulfonamidoindane Investigative T13201 DRUGINFO D08TBP 2-Acetylamino-indan-5-sulfonic acid hydrate Investigative T13201 DRUGINFO D0C4QB 2-Amino-indan-5-sulfonic acid Investigative T13201 DRUGINFO D0SF3B 2-butylamido-5-sulfonamidoindane Investigative T13201 DRUGINFO D0HN0R 2-cyclohexylamido-5-sulfonamidoindane Investigative T13201 DRUGINFO D08AOA 2-ethylamido-5-sulfonamidoindane Investigative T13201 DRUGINFO D05WQF 2-Hydroxycinnamic acid Investigative T13201 DRUGINFO D01EEM 2-Mercapto-N-(4-sulfamoyl-phenyl)-benzamide Investigative T13201 DRUGINFO D0D0BO 2-Morpholin-4-yl-N-(4-sulfamoyl-phenyl)-acetamide Investigative T13201 DRUGINFO D07PNA 2-nonylamido-5-sulfonamidoindane Investigative T13201 DRUGINFO D0H3NS 2-oxo-2H-chromene-3-carboxylic acid Investigative T13201 DRUGINFO D0D6UR 2-oxo-2H-thiochromene-3-carboxylic acid Investigative T13201 DRUGINFO D0J3SP 2-pentafluorophenylamido-5-sulfonamidoindane Investigative T13201 DRUGINFO D0O8WV 2-propylamido-5-sulfonamidoindane Investigative T13201 DRUGINFO D07LYW 2-valproylamido-5-sulfonamidoindane Investigative T13201 DRUGINFO D06ZMH 3-(3-Phenyl-ureido)-benzenesulfonamide Investigative T13201 DRUGINFO D09CSP 3-(4-sulfamoylphenyl)propanoic acid Investigative T13201 DRUGINFO D01JTI 3-bromophenyl-difluoromethanesulfonamide Investigative T13201 DRUGINFO D01UDU 3-Chloro-4-hydrazino-benzenesulfonamide Investigative T13201 DRUGINFO D01YHK 3-Fluoro-4-hydrazino-benzenesulfonamide Investigative T13201 DRUGINFO D0DY9U 3-mercapto-N-(4-sulfamoyl-phenyl)-propionamide Investigative T13201 DRUGINFO D07OMY 3-phenyl-5-sulfamoyl-1H-indole-2-carboxamide Investigative T13201 DRUGINFO D04RCR 3-phenylprop-1-enylboronic acid Investigative T13201 DRUGINFO D04NSN 4-(2-AMINOETHYL)BENZENESULFONAMIDE Investigative T13201 DRUGINFO D0TY8X 4-(2-aminopyrimidin-4-ylamino)benzenesulfonamide Investigative T13201 DRUGINFO D05ETN 4-(2-Methyl-8-quinolinoxy)-3-pyridinesulfonamide Investigative T13201 DRUGINFO D0Z5GE 4-(2-Phenylacetamido)-3-bromobenzenesulfonamide Investigative T13201 DRUGINFO D0A3JR 4-(2-Phenylacetamido)-3-chlorobenzenesulfonamide Investigative T13201 DRUGINFO D0O9VU 4-(2-Phenylacetamido)-3-fluorobenzenesulfonamide Investigative T13201 DRUGINFO D0O0UE 4-(2-Phenylacetamido)benzenesulfonamide Investigative T13201 DRUGINFO D09LWR 4-(2-Phenylacetamidoethyl)benzenesulfonamide Investigative T13201 DRUGINFO D06XNT 4-(2-Phenylacetamidomethyl)benzenesulfonamide Investigative T13201 DRUGINFO D02BMV 4-(2-Propynylthio)pyridine-3-sulfonamide Investigative T13201 DRUGINFO D0N7WP 4-(2-Pyridin-2-ylacetamido)benzenesulfonamide Investigative T13201 DRUGINFO D00GVA 4-(2-Pyridin-4-ylacetamido)benzenesulfonamide Investigative T13201 DRUGINFO D05EBZ 4-(4-Cyanophenoxy)-3-pyridinesulfonamide Investigative T13201 DRUGINFO D08JCC 4-(4-Fluorophenoxy)-3-pyridinesulfonamide Investigative T13201 DRUGINFO D0R4KQ 4-(5-Methyl-2-pirazolino)-3-pyridinesulfonamide Investigative T13201 DRUGINFO D09TKG 4-(Allylamino)-3-pyridinesulfonamide Investigative T13201 DRUGINFO D0V5OW 4-(Carbamolymethylthio)pyridine-3-sulfonamide Investigative T13201 DRUGINFO D01OTW 4-(Cyanomethylthio)pyridine-3-sulfonamide Investigative T13201 DRUGINFO D05XZM 4-(hydroxymethyl)benzenesulfonamide Investigative T13201 DRUGINFO D0Q5VB 4-(Methylhydrazino)-3-pyridinesulfonamide Investigative T13201 DRUGINFO D02NQK 4-(N-Oxide-2-pyridylthio)pyridine-3-sulfonamide Investigative T13201 DRUGINFO D05JAJ 4-(Quinolinoxy)-3-pyridinesulfonamide Investigative T13201 DRUGINFO D03KRB 4,4'-thiodipyridine-3-sulfonamide Investigative T13201 DRUGINFO D0BR1D 4,6-Dinitro salicylic acid Investigative T13201 DRUGINFO D0W9VC 4-[2-(2-Thienyl)acetamido]benzenesulfonamide Investigative T13201 DRUGINFO D01ISX 4-[2-(2-Thienyl)acetamidoethyl]benzenesulfonamide Investigative T13201 DRUGINFO D09LUD 4-[2-(3-Phenyl-ureido)-ethyl]-benzenesulfonamide Investigative T13201 DRUGINFO D0P6AM 4-Amino-3-bromo-benzenesulfonamide Investigative T13201 DRUGINFO D0YU8J 4-Amino-3-chloro-benzenesulfonamide Investigative T13201 DRUGINFO D04CVC 4-Amino-3-fluoro-benzenesulfonamide Investigative T13201 DRUGINFO D01STY 4-Amino-3-iodo-benzenesulfonamide Investigative T13201 DRUGINFO D0Z1HY 4-amino-6-chlorobenzene-1,3-disulfonamide Investigative T13201 DRUGINFO D0X6IE 4-amino-N-(4-sulfamoylbenzyl)benzenesulfonamide Investigative T13201 DRUGINFO D0Z6TM 4-azidobenzenesulfonamide Investigative T13201 DRUGINFO D0YD9F 4-Benzenesulfonylamino-benzenesulfonamide Investigative T13201 DRUGINFO D06IOI 4-Benzythiopyridine-3-sulfonamide Investigative T13201 DRUGINFO D0Z1CL 4-bromophenylboronic acid Investigative T13201 DRUGINFO D05NFU 4-butylphenylboronic acid Investigative T13201 DRUGINFO D0A8HW 4-Chloro-N-(5-sulfamoyl-indan-2-yl)-benzamide Investigative T13201 DRUGINFO D04VSP 4-Ethoxy-3-pyridinesulfonamide Investigative T13201 DRUGINFO D0LJ5P 4-ethynyl benzene sulfonamide Investigative T13201 DRUGINFO D0X9LJ 4-fluoro-N-(4-sulfamoylbenzyl)benzenesulfonamide Investigative T13201 DRUGINFO D0UM1I 4-Hydrazino-3-pyridinesulfonamide Investigative T13201 DRUGINFO D0NN3Q 4-Hydrazino-benzenesulfonamide Investigative T13201 DRUGINFO D0Q0EK 4-Hydrazinocarbonyl-benzenesulfonamide Investigative T13201 DRUGINFO D0U1AN 4-isothiocyanatobenzenesulfonamide Investigative T13201 DRUGINFO D00NUK 4-Methanesulfonylamino-benzenesulfonamide Investigative T13201 DRUGINFO D00IKQ 4-Methoxy-3-pyridinesulfonamide Investigative T13201 DRUGINFO D0A4HS 4-methoxyphenylboronic acid Investigative T13201 DRUGINFO D06GPL 4-methylphenyl-difluoromethanesulfonamide Investigative T13201 DRUGINFO D0X0RE 4-methylstyrylboronic acid Investigative T13201 DRUGINFO D0J7GU 4-Methylthiopyridine-3-sulfonamide Investigative T13201 DRUGINFO D0T0YI 4-nitrophenyl phosphate Investigative T13201 DRUGINFO D0I5YQ 4-nitrophenyl-difluoromethanesulfonamide Investigative T13201 DRUGINFO D0D2JA 4-phenoxyphenylboronic acid Investigative T13201 DRUGINFO D0X1MY 5-Amino-[1,3,4]thiadiazole-2-thiol Investigative T13201 DRUGINFO D05FMD 5-Chlorosalicylic Acid Investigative T13201 DRUGINFO D06SME 5-hydroxy-1-tosyl-1H-pyrrol-2(5H)-one Investigative T13201 DRUGINFO D0D1HC 5-oxo-1-tosyl-2,5-dihydro-1Hpyrrol-2-yl acetate Investigative T13201 DRUGINFO D0N1AW 6-(aminomethyl)-2H-chromen-2-one Investigative T13201 DRUGINFO D0O1QT 6-Amino-benzothiazole-2-sulfonic acid amide Investigative T13201 DRUGINFO D0Q2LL 6-Hydroxy-benzothiazole-2-sulfonic acid amide Investigative T13201 DRUGINFO D00XJA 6-methoxy-2-oxo-2H-chromene-3-carboxylic acid Investigative T13201 DRUGINFO D0G3BI 6-methyl-2-oxo-2H-chromene-3-carboxylic acid Investigative T13201 DRUGINFO D0RB0D 7-methoxy-2-oxo-2H-chromene-4-carboxylic acid Investigative T13201 DRUGINFO D06DYP 8-methoxy-2-oxo-2H-chromene-3-carboxylic acid Investigative T13201 DRUGINFO D05QEK Aminobenzolamide derivative Investigative T13201 DRUGINFO D09JHA Azide Investigative T13201 DRUGINFO D09QHC BENZENESULFONAMIDE Investigative T13201 DRUGINFO D0E8CC BENZOLAMIDE Investigative T13201 DRUGINFO D0XL5K Benzothiazole-2-sulfonic acid amide Investigative T13201 DRUGINFO D0C8ZY Beta-naphthylboronic acid Investigative T13201 DRUGINFO D09OSN Biphenyl-4-ylboronic acid Investigative T13201 DRUGINFO D0Y6EL Carbamoyl phosphate disodium Investigative T13201 DRUGINFO D09PWX Carzenide Investigative T13201 DRUGINFO D0V7AA CATECHIN Investigative T13201 DRUGINFO D0VD7H CL-5343 Investigative T13201 DRUGINFO D03ZMQ COUMARIN Investigative T13201 DRUGINFO D04FXD CYANATE Investigative T13201 DRUGINFO D0T6VB Cynooxide anion Investigative T13201 DRUGINFO D00YEF Decane-1,10-diyl disulfamate Investigative T13201 DRUGINFO D09WSJ Decyl sulfamate Investigative T13201 DRUGINFO D0A1CM ELLAGIC ACID Investigative T13201 DRUGINFO D00ZUQ ETHYL 3-[4-(AMINOSULFONYL)PHENYL]PROPANOATE Investigative T13201 DRUGINFO D0Y3TZ GALLICACID Investigative T13201 DRUGINFO D0U4BB HERNIARIN Investigative T13201 DRUGINFO D09JPC Hexane-1,6-diamine Investigative T13201 DRUGINFO D0T6ZX HYDROSULFIDE Investigative T13201 DRUGINFO D08RKK IODIDE Investigative T13201 DRUGINFO D05EPY L-693612 Investigative T13201 DRUGINFO D0M4EV N-(4-cyanophenyl)sulfamide Investigative T13201 DRUGINFO D0KB6T N-(4-Sulfamoyl-phenyl)-benzamide Investigative T13201 DRUGINFO D0K3LN N-(4-Sulfamoyl-phenyl)-butyramide Investigative T13201 DRUGINFO D0N8LR N-(4-Sulfamoyl-phenyl)-propionamide Investigative T13201 DRUGINFO D07YSQ N-(4-sulfamoylphenylethyl)-4-sulfamoylbenzamide Investigative T13201 DRUGINFO D0S4NO N-(5-ethyl-1,3,4-thiadiazol-2-yl)sulfamide Investigative T13201 DRUGINFO D0J1PZ N-(5-Mercapto-[1,3,4]thiadiazol-2-yl)-acetamide Investigative T13201 DRUGINFO D06JVR N-(5-phenyl-1,3,4-thiadiazol-2-yl)sulfamide Investigative T13201 DRUGINFO D0T2VH N-(5-tert-butyl-1,3,4-thiadiazol-2-yl)sulfamide Investigative T13201 DRUGINFO D0PA5L N-(pentafluorophenyl)sulfamide Investigative T13201 DRUGINFO D0K5NQ N-[4-(trifluoromethyl)phenyl]sulfamide Investigative T13201 DRUGINFO D0E3VJ N-[5-(ethylthio)-1,3,4-thiadiazol-2-yl]sulfamide Investigative T13201 DRUGINFO D04PSK N-[5-(methylthio)-1,3,4-thiadiazol-2-yl]sulfamide Investigative T13201 DRUGINFO D0M7QA N-{2-[4-(AMINOSULFONYL)PHENYL]ETHYL}ACETAMIDE Investigative T13201 DRUGINFO D00BMI N-1,3,4-thiadiazol-2-ylsulfamide Investigative T13201 DRUGINFO D09CXX N-hydroxysulfamide Investigative T13201 DRUGINFO D03EAQ N-hydroxysulfonamides Investigative T13201 DRUGINFO D00RJT NITRATE Investigative T13201 DRUGINFO D01XFH N-propynyl amidebenzenesulphonide Investigative T13201 DRUGINFO D0B4IN NSC-654077 Investigative T13201 DRUGINFO D0D4OV Octane-1,8-diyl disulfamate Investigative T13201 DRUGINFO D05TLB Octyl sulfamate Investigative T13201 DRUGINFO D08XQI PARAOXON Investigative T13201 DRUGINFO D0AU0M P-Coumaric Acid Investigative T13201 DRUGINFO D02QGI Pentane-1,5-diamine Investigative T13201 DRUGINFO D0Q0XO Pentanoic acid (4-sulfamoyl-phenyl)-amide Investigative T13201 DRUGINFO D06ORV Phenethylboronic acid Investigative T13201 DRUGINFO D01GNQ Phenoxyarsonous acid Investigative T13201 DRUGINFO D0EJ9B Phenyl Boronic acid Investigative T13201 DRUGINFO D0UN0E PHENYLDIFLUOROMETHANESULFONAMIDE Investigative T13201 DRUGINFO D07SIA PHENYLMETHANESULFONAMIDE Investigative T13201 DRUGINFO D0L4FM PHENYLSULFAMATE Investigative T13201 DRUGINFO D00IAE Prop-2-ynyl 4-sulfamoylbenzoate Investigative T13201 DRUGINFO D0A0YX SACCHARIN Investigative T13201 DRUGINFO D0D5XC Sodium trithiocarbonate Investigative T13201 DRUGINFO D0F7QZ Styrylboronic acid Investigative T13201 DRUGINFO D03VDJ SULFAMATE Investigative T13201 DRUGINFO D07ZXR Sulfamic acid 12-sulfamoyloxy-dodecyl ester Investigative T13201 DRUGINFO D07CBA Sulfamic acid 16-sulfamoyloxy-hexadecyl ester Investigative T13201 DRUGINFO D07IHP Sulfamic acid 3-sulfamoyloxy-phenyl ester Investigative T13201 DRUGINFO D04BKU Sulfamic acid 4-sulfamoyloxy-butyl ester Investigative T13201 DRUGINFO D0X0PO Sulfamic acid 6-sulfamoyloxy-hexyl ester Investigative T13201 DRUGINFO D05FNN Sulfamic acid 7-sulfamoyloxy-heptyl ester Investigative T13201 DRUGINFO D03LWY SULFATE Investigative T13201 DRUGINFO D0Q7DJ Syringic Acid Investigative T13201 DRUGINFO D0I0RT Thioureido sulfonamide Investigative T13201 DRUGINFO D0S8RD Trecadrine Investigative T13201 KEGGPATH hsa00910:Nitrogen metabolism T13201 WIKIPATH WP2681:Uptake of Oxygen and Release of Carbon Dioxide by Erythrocytes T13201 WIKIPATH WP2744:Uptake of Carbon Dioxide and Release of Oxygen by Erythrocytes T13201 WIKIPATH WP2770:Reversible Hydration of Carbon Dioxide T13201 WHIZPATH PW000565:Gastric Acid Production T13201 REACPATH R-HSA-1237044:Erythrocytes take up carbon dioxide and release oxygen T13201 REACPATH R-HSA-1247673:Erythrocytes take up oxygen and release carbon dioxide T13201 REACPATH R-HSA-1475029:Reversible hydration of carbon dioxide T13201 INTEPATH cmyb_pathway:C-MYB transcription factor network T20401 TARGETID T20401 T20401 FORMERID TTDS00306 T20401 UNIPROID CAH2_HUMAN T20401 TARGNAME Carbonic anhydrase II (CA-II) T20401 GENENAME CA2 T20401 TARGTYPE Successful target T20401 SYNONYMS Carbonic anhydrase C; Carbonic anhydrase 2; Carbonate dehydratase II; CAC T20401 FUNCTION Reversible hydration of carbon dioxide. Can hydrate cyanamide to urea. Involved in the regulation of fluid secretion into the anterior chamber of the eye. Contributes to intracellular pH regulation in the duodenal upper villous epithelium during proton-coupled peptide absorption. Stimulates the chloride-bicarbonate exchange activity of SLC26A6. Essential for bone resorption and osteoclast differentiation. T20401 PDBSTRUC 9CA2; 8CA2; 7CA2; 6QEB; 6MBY T20401 BIOCLASS Alpha-carbonic anhydrase T20401 ECNUMBER EC 4.2.1.1 T20401 SEQUENCE MSHHWGYGKHNGPEHWHKDFPIAKGERQSPVDIDTHTAKYDPSLKPLSVSYDQATSLRILNNGHAFNVEFDDSQDKAVLKGGPLDGTYRLIQFHFHWGSLDGQGSEHTVDKKKYAAELHLVHWNTKYGDFGKAVQQPDGLAVLGIFLKVGSAKPGLQKVVDVLDSIKTKGKSADFTNFDPRGLLPESLDYWTYPGSLTTPPLLECVTWIVLKEPISVSSEQVLKFRKLNFNGEGEPEELMVDNWRPAQPLKNRQIKASFK T20401 DRUGINFO D0L2MX Benzthiazide Approved T20401 DRUGINFO D0M9WM Chlorothiazide Approved T20401 DRUGINFO D03CNS Cyclothiazide Approved T20401 DRUGINFO D0J4GO Dichlorphenamide Approved T20401 DRUGINFO D05UYW Dorzolamide Approved T20401 DRUGINFO D0CK3G Ethinamate Approved T20401 DRUGINFO D07INV Ethoxzolamide Approved T20401 DRUGINFO D07HBX Salicyclic acid Approved T20401 DRUGINFO D0K1QD Sulfamylon Approved T20401 DRUGINFO D0W2CX CG-100649 Phase 3 T20401 DRUGINFO D07SDQ Curcumin Phase 3 T20401 DRUGINFO D02JUW GUAIACOL Phase 3 T20401 DRUGINFO D0A8JP PARABEN Phase 3 T20401 DRUGINFO D06PII SULTHIAME Phase 3 T20401 DRUGINFO D0L6HN PHENOL Phase 2/3 T20401 DRUGINFO D0Y6OA Coumate Phase 2 T20401 DRUGINFO D07ZNI STX-140 Phase 2 T20401 DRUGINFO D0W1SL BUTYLATEDHYDROXYTOLUENE Phase 1 T20401 DRUGINFO D0V0UK SULFAMIDE Phase 1 T20401 DRUGINFO D03SLR FERULIC ACID Patented T20401 DRUGINFO D01KOO (2,2-dimethyl-1,3-dioxolan-4-yl)methyl sulfamate Investigative T20401 DRUGINFO D04JIN (2-bromophenyl)difluoromethanesulfonamide Investigative T20401 DRUGINFO D0IU3X (4-bromophenyl)difluoromethanesulfonamide Investigative T20401 DRUGINFO D09UQM 1-(3,4-dichlorophenyl)-3-hydroxyurea Investigative T20401 DRUGINFO D0OT2H 1,2,4-Triazole Investigative T20401 DRUGINFO D05RAB 1,4-Dihydro-1-methyl-4-oxo-3-pyridinesulfonamide Investigative T20401 DRUGINFO D0C6ED 1,4-phenylene disulfamate Investigative T20401 DRUGINFO D00XIB 1-acetamido-5-sulfonamidoindane Investigative T20401 DRUGINFO D04SNH 1-Benzyl-1,4-dihydro-4-oxo-3-pyridinesulfonamide Investigative T20401 DRUGINFO D0G9NE 1-cyclohexylamido-5-sulfonamidoindane Investigative T20401 DRUGINFO D0O4KL 1-pentafluorophenylamido-5-sulfonamidoindane Investigative T20401 DRUGINFO D06OVA 1-pentenyl-4-(aminosulfonyl)benzoate Investigative T20401 DRUGINFO D0KZ2D 1-valproylamido-5-sulfonamidoindane Investigative T20401 DRUGINFO D05BMD 2-(4-chlorobenzyloxyamino)-N-hydroxyacetamide Investigative T20401 DRUGINFO D06NDR 2-(4-chlorobenzyloxyamino)-N-hydroxyhexanamide Investigative T20401 DRUGINFO D0G0OP 2-(4-chlorobenzyloxyamino)-N-hydroxypropanamide Investigative T20401 DRUGINFO D09SFY 2-(4-hydroxybenzylideneamino)ethanesulfonamide Investigative T20401 DRUGINFO D08ORD 2-(4-tert-butylbenzylideneamino)ethanesulfonamide Investigative T20401 DRUGINFO D0U0QW 2-(benzylideneamino)ethanesulfonamide Investigative T20401 DRUGINFO D0Y1XM 2-(benzyloxyamino)-N-hydroxyhexanamide Investigative T20401 DRUGINFO D02KDH 2-(N''-Acetyl-hydrazino)-benzenesulfonamide Investigative T20401 DRUGINFO D0RK7J 2,2,2-Trifluoro-N-(4-sulfamoyl-phenyl)-acetamide Investigative T20401 DRUGINFO D03DAM 2,2-Dimethyl-N-(4-sulfamoyl-phenyl)-propionamide Investigative T20401 DRUGINFO D0LC0F 2,3-dihydro-1H-indene-5-sulfonamide Investigative T20401 DRUGINFO D0S6CO 2,4-dichloro-5-sulfamoylbenzoic acid Investigative T20401 DRUGINFO D0M3PO 2,4-Disulfamyltrifluoromethylaniline Investigative T20401 DRUGINFO D05DFJ 2,6-Difluorobenzenesulfonamide Investigative T20401 DRUGINFO D06MZK 2,6-di-t-butylphenol Investigative T20401 DRUGINFO D09ZUN 2,6-di-tert-butyl-4-methoxyphenol Investigative T20401 DRUGINFO D00FGB 2-acetamido-5-sulfonamidoindane Investigative T20401 DRUGINFO D08TBP 2-Acetylamino-indan-5-sulfonic acid hydrate Investigative T20401 DRUGINFO D0OI1H 2-Amino-benzenesulfonamide Investigative T20401 DRUGINFO D0C4QB 2-Amino-indan-5-sulfonic acid Investigative T20401 DRUGINFO D0SF3B 2-butylamido-5-sulfonamidoindane Investigative T20401 DRUGINFO D0HN0R 2-cyclohexylamido-5-sulfonamidoindane Investigative T20401 DRUGINFO D08AOA 2-ethylamido-5-sulfonamidoindane Investigative T20401 DRUGINFO D06KTD 2-Hydrazinocarbonyl-benzenesulfonamide Investigative T20401 DRUGINFO D0G0FJ 2-hydrazinylbenzenesulfonamide Investigative T20401 DRUGINFO D05WQF 2-Hydroxycinnamic acid Investigative T20401 DRUGINFO D01EEM 2-Mercapto-N-(4-sulfamoyl-phenyl)-benzamide Investigative T20401 DRUGINFO D04GDW 2-methoxyestradiol-17-O-sulfamate Investigative T20401 DRUGINFO D09PUF 2-methoxyestrrone-3-O-sulfamate Investigative T20401 DRUGINFO D0D0BO 2-Morpholin-4-yl-N-(4-sulfamoyl-phenyl)-acetamide Investigative T20401 DRUGINFO D07PNA 2-nonylamido-5-sulfonamidoindane Investigative T20401 DRUGINFO D0D6UR 2-oxo-2H-thiochromene-3-carboxylic acid Investigative T20401 DRUGINFO D0J3SP 2-pentafluorophenylamido-5-sulfonamidoindane Investigative T20401 DRUGINFO D0O8WV 2-propylamido-5-sulfonamidoindane Investigative T20401 DRUGINFO D07CQI 2-Sulfamoyl-benzoic acid methyl ester Investigative T20401 DRUGINFO D0Q5FV 2-Sulfhydryl-Ethanol Investigative T20401 DRUGINFO D07LYW 2-valproylamido-5-sulfonamidoindane Investigative T20401 DRUGINFO D0H4CF 3-((4-aminophenyl)diazenyl)benzenesulfonamide Investigative T20401 DRUGINFO D0C7WG 3-((4-hydroxyphenyl)diazenyl)benzenesulfonamide Investigative T20401 DRUGINFO D06ZMH 3-(3-Phenyl-ureido)-benzenesulfonamide Investigative T20401 DRUGINFO D0BD0K 3-(4'-Hydroxyphenyl)diazenylbenzenesulfonamide Investigative T20401 DRUGINFO D09CSP 3-(4-sulfamoylphenyl)propanoic acid Investigative T20401 DRUGINFO D0S6GK 3,5-Difluorobenzenesulfonamide Investigative T20401 DRUGINFO D0J2AE 3-Amino-benzenesulfonamide Investigative T20401 DRUGINFO D01JTI 3-bromophenyl-difluoromethanesulfonamide Investigative T20401 DRUGINFO D01UDU 3-Chloro-4-hydrazino-benzenesulfonamide Investigative T20401 DRUGINFO D01YHK 3-Fluoro-4-hydrazino-benzenesulfonamide Investigative T20401 DRUGINFO D0C9ZY 3-hydroxy-2-methoxybenzaldehyde Investigative T20401 DRUGINFO D0DY9U 3-mercapto-N-(4-sulfamoyl-phenyl)-propionamide Investigative T20401 DRUGINFO D0A2PD 3-Mercuri-4-Aminobenzenesulfonamide Investigative T20401 DRUGINFO D07ZHE 3-Nitro-benzenesulfonamide Investigative T20401 DRUGINFO D07OMY 3-phenyl-5-sulfamoyl-1H-indole-2-carboxamide Investigative T20401 DRUGINFO D04RCR 3-phenylprop-1-enylboronic acid Investigative T20401 DRUGINFO D04HRS 4-((4-hydroxyphenyl)diazenyl)benzenesulfonamide Investigative T20401 DRUGINFO D0I1XT 4-((benzylideneamino)methyl)benzenesulfonamide Investigative T20401 DRUGINFO D04NSN 4-(2-AMINOETHYL)BENZENESULFONAMIDE Investigative T20401 DRUGINFO D0TY8X 4-(2-aminopyrimidin-4-ylamino)benzenesulfonamide Investigative T20401 DRUGINFO D04VLI 4-(2-Hydroxy-ethyl)-benzenesulfonamide Investigative T20401 DRUGINFO D05ETN 4-(2-Methyl-8-quinolinoxy)-3-pyridinesulfonamide Investigative T20401 DRUGINFO D0Z5GE 4-(2-Phenylacetamido)-3-bromobenzenesulfonamide Investigative T20401 DRUGINFO D0A3JR 4-(2-Phenylacetamido)-3-chlorobenzenesulfonamide Investigative T20401 DRUGINFO D0O9VU 4-(2-Phenylacetamido)-3-fluorobenzenesulfonamide Investigative T20401 DRUGINFO D0O0UE 4-(2-Phenylacetamido)benzenesulfonamide Investigative T20401 DRUGINFO D09LWR 4-(2-Phenylacetamidoethyl)benzenesulfonamide Investigative T20401 DRUGINFO D06XNT 4-(2-Phenylacetamidomethyl)benzenesulfonamide Investigative T20401 DRUGINFO D02BMV 4-(2-Propynylthio)pyridine-3-sulfonamide Investigative T20401 DRUGINFO D0N7WP 4-(2-Pyridin-2-ylacetamido)benzenesulfonamide Investigative T20401 DRUGINFO D00GVA 4-(2-Pyridin-4-ylacetamido)benzenesulfonamide Investigative T20401 DRUGINFO D05EBZ 4-(4-Cyanophenoxy)-3-pyridinesulfonamide Investigative T20401 DRUGINFO D08JCC 4-(4-Fluorophenoxy)-3-pyridinesulfonamide Investigative T20401 DRUGINFO D03VUQ 4-(4-hydroxy-benzylideneamino)-benzenesulfonamide Investigative T20401 DRUGINFO D0R6JK 4-(4-hydroxybenzylideneamino)benzoic acid Investigative T20401 DRUGINFO D02DCD 4-(4-tert-butylbenzylideneamino)benzoic acid Investigative T20401 DRUGINFO D0R4KQ 4-(5-Methyl-2-pirazolino)-3-pyridinesulfonamide Investigative T20401 DRUGINFO D09TKG 4-(Allylamino)-3-pyridinesulfonamide Investigative T20401 DRUGINFO D0S2II 4-(benzylideneamino)benzenesulfonamide Investigative T20401 DRUGINFO D0K4IH 4-(benzylideneamino)benzoic acid Investigative T20401 DRUGINFO D0V5OW 4-(Carbamolymethylthio)pyridine-3-sulfonamide Investigative T20401 DRUGINFO D01OTW 4-(Cyanomethylthio)pyridine-3-sulfonamide Investigative T20401 DRUGINFO D07QHM 4-(Hydroxymercury)Benzoic Acid Investigative T20401 DRUGINFO D05XZM 4-(hydroxymethyl)benzenesulfonamide Investigative T20401 DRUGINFO D0Q5VB 4-(Methylhydrazino)-3-pyridinesulfonamide Investigative T20401 DRUGINFO D0M7VN 4-(N-Methyl-hydrazino)-benzenesulfonamide Investigative T20401 DRUGINFO D02NQK 4-(N-Oxide-2-pyridylthio)pyridine-3-sulfonamide Investigative T20401 DRUGINFO D05JAJ 4-(Quinolinoxy)-3-pyridinesulfonamide Investigative T20401 DRUGINFO D03KRB 4,4'-thiodipyridine-3-sulfonamide Investigative T20401 DRUGINFO D0BR1D 4,6-Dinitro salicylic acid Investigative T20401 DRUGINFO D0W9VC 4-[2-(2-Thienyl)acetamido]benzenesulfonamide Investigative T20401 DRUGINFO D01ISX 4-[2-(2-Thienyl)acetamidoethyl]benzenesulfonamide Investigative T20401 DRUGINFO D09LUD 4-[2-(3-Phenyl-ureido)-ethyl]-benzenesulfonamide Investigative T20401 DRUGINFO D0P6AM 4-Amino-3-bromo-benzenesulfonamide Investigative T20401 DRUGINFO D0YU8J 4-Amino-3-chloro-benzenesulfonamide Investigative T20401 DRUGINFO D04CVC 4-Amino-3-fluoro-benzenesulfonamide Investigative T20401 DRUGINFO D01STY 4-Amino-3-iodo-benzenesulfonamide Investigative T20401 DRUGINFO D0Z1HY 4-amino-6-chlorobenzene-1,3-disulfonamide Investigative T20401 DRUGINFO D0X6IE 4-amino-N-(4-sulfamoylbenzyl)benzenesulfonamide Investigative T20401 DRUGINFO D0Z6TM 4-azidobenzenesulfonamide Investigative T20401 DRUGINFO D0YD9F 4-Benzenesulfonylamino-benzenesulfonamide Investigative T20401 DRUGINFO D06IOI 4-Benzythiopyridine-3-sulfonamide Investigative T20401 DRUGINFO D0Z1CL 4-bromophenylboronic acid Investigative T20401 DRUGINFO D05NFU 4-butylphenylboronic acid Investigative T20401 DRUGINFO D0A8HW 4-Chloro-N-(5-sulfamoyl-indan-2-yl)-benzamide Investigative T20401 DRUGINFO D00IUB 4-CYANOPHENOL Investigative T20401 DRUGINFO D04VSP 4-Ethoxy-3-pyridinesulfonamide Investigative T20401 DRUGINFO D0LJ5P 4-ethynyl benzene sulfonamide Investigative T20401 DRUGINFO D00SJT 4-Flourobenzenesulfonamide Investigative T20401 DRUGINFO D0X9LJ 4-fluoro-N-(4-sulfamoylbenzyl)benzenesulfonamide Investigative T20401 DRUGINFO D0UM1I 4-Hydrazino-3-pyridinesulfonamide Investigative T20401 DRUGINFO D0NN3Q 4-Hydrazino-benzenesulfonamide Investigative T20401 DRUGINFO D0Q0EK 4-Hydrazinocarbonyl-benzenesulfonamide Investigative T20401 DRUGINFO D0U1AN 4-isothiocyanatobenzenesulfonamide Investigative T20401 DRUGINFO D00NUK 4-Methanesulfonylamino-benzenesulfonamide Investigative T20401 DRUGINFO D00IKQ 4-Methoxy-3-pyridinesulfonamide Investigative T20401 DRUGINFO D0A4HS 4-methoxyphenylboronic acid Investigative T20401 DRUGINFO D0T8SN 4-methoxyphenylsulfamide Investigative T20401 DRUGINFO D07AGM 4-Methylamino-benzenesulfonamide Investigative T20401 DRUGINFO D0KK4F 4-Methylimidazole Investigative T20401 DRUGINFO D06GPL 4-methylphenyl-difluoromethanesulfonamide Investigative T20401 DRUGINFO D0J7GU 4-Methylthiopyridine-3-sulfonamide Investigative T20401 DRUGINFO D06LVE 4-Nitro-benzenesulfonamide Investigative T20401 DRUGINFO D0T0YI 4-nitrophenyl phosphate Investigative T20401 DRUGINFO D0I5YQ 4-nitrophenyl-difluoromethanesulfonamide Investigative T20401 DRUGINFO D0I8DW 4-nitrophenylsulfamide Investigative T20401 DRUGINFO D0D2JA 4-phenoxyphenylboronic acid Investigative T20401 DRUGINFO D0O0HT 4-Sulfonamide-[1-(4-Aminobutane)]Benzamide Investigative T20401 DRUGINFO D05PRS 4-Thiocyanato-benzenesulfonamide Investigative T20401 DRUGINFO D0X1MY 5-Amino-[1,3,4]thiadiazole-2-thiol Investigative T20401 DRUGINFO D05FMD 5-Chlorosalicylic Acid Investigative T20401 DRUGINFO D06SME 5-hydroxy-1-tosyl-1H-pyrrol-2(5H)-one Investigative T20401 DRUGINFO D0N1AW 6-(aminomethyl)-2H-chromen-2-one Investigative T20401 DRUGINFO D0L5TZ 6-(hydroxymethyl)-2H-chromen-2-one Investigative T20401 DRUGINFO D0O1QT 6-Amino-benzothiazole-2-sulfonic acid amide Investigative T20401 DRUGINFO D0A6HS 6-HYDROXY-1,3-BENZOTHIAZOLE-2-SULFONAMIDE Investigative T20401 DRUGINFO D0M8UY 6-hydroxybenzo[d][1,3]oxathiol-2-one Investigative T20401 DRUGINFO D0Q2LL 6-Hydroxy-benzothiazole-2-sulfonic acid amide Investigative T20401 DRUGINFO D00XJA 6-methoxy-2-oxo-2H-chromene-3-carboxylic acid Investigative T20401 DRUGINFO D0G3BI 6-methyl-2-oxo-2H-chromene-3-carboxylic acid Investigative T20401 DRUGINFO D07JYF 6-Nitro-benzothiazole-2-sulfonic acid amide Investigative T20401 DRUGINFO D0F2ME Acetate Ion Investigative T20401 DRUGINFO D04POB ACETYLSULFANILAMIDE Investigative T20401 DRUGINFO D09HNP AL4623 Investigative T20401 DRUGINFO D08CNG AL5300 Investigative T20401 DRUGINFO D0D6UL AL5424 Investigative T20401 DRUGINFO D0M8HC AL5927 Investigative T20401 DRUGINFO D09LMH AL6528 Investigative T20401 DRUGINFO D04XMZ Al7089a Investigative T20401 DRUGINFO D0XX9C AL7099A Investigative T20401 DRUGINFO D0B8CU AL7182 Investigative T20401 DRUGINFO D05NAR Allyl 4-(aminosulfonyl)benzoate Investigative T20401 DRUGINFO D05QEK Aminobenzolamide derivative Investigative T20401 DRUGINFO D09JHA Azide Investigative T20401 DRUGINFO D0E8CC BENZOLAMIDE Investigative T20401 DRUGINFO D0XL5K Benzothiazole-2-sulfonic acid amide Investigative T20401 DRUGINFO D0C8ZY Beta-naphthylboronic acid Investigative T20401 DRUGINFO D09OSN Biphenyl-4-ylboronic acid Investigative T20401 DRUGINFO D09PWX Carzenide Investigative T20401 DRUGINFO D0V7AA CATECHIN Investigative T20401 DRUGINFO D07QJJ CATECHOL Investigative T20401 DRUGINFO D0VD7H CL-5343 Investigative T20401 DRUGINFO D03ZMQ COUMARIN Investigative T20401 DRUGINFO D0S7NH Dansylamide Investigative T20401 DRUGINFO D00YEF Decane-1,10-diyl disulfamate Investigative T20401 DRUGINFO D09WSJ Decyl sulfamate Investigative T20401 DRUGINFO D0A0RT Di(2,6-diisopropylphenol) Investigative T20401 DRUGINFO D04LNI Di(2,6-dimethylphenol) Investigative T20401 DRUGINFO D0C3SL Di(2,6-di-t-butylphenol) Investigative T20401 DRUGINFO D0A1CM ELLAGIC ACID Investigative T20401 DRUGINFO D0R7QY EMATE Investigative T20401 DRUGINFO D00ZUQ ETHYL 3-[4-(AMINOSULFONYL)PHENYL]PROPANOATE Investigative T20401 DRUGINFO D06EWG Formic Acid Investigative T20401 DRUGINFO D0Y3TZ GALLICACID Investigative T20401 DRUGINFO D0T6ZX HYDROSULFIDE Investigative T20401 DRUGINFO D08RKK IODIDE Investigative T20401 DRUGINFO D06CGS Mercuribenzoic Acid Investigative T20401 DRUGINFO D07AUN Methyl 4-(4-hydroxybenzylideneamino)benzoate Investigative T20401 DRUGINFO D05DIH Methyl 4-(4-tert-butylbenzylideneamino)benzoate Investigative T20401 DRUGINFO D09CZV Methyl Mercury Ion Investigative T20401 DRUGINFO D0A4TC MMI270 Investigative T20401 DRUGINFO D0M7DE N-(1-benzofuran-3-ylmethyl)sulfamide Investigative T20401 DRUGINFO D0A7ZH N-(2,3-DIFLUORO-BENZYL)-4-SULFAMOYL-BENZAMIDE Investigative T20401 DRUGINFO D0S5LS N-(2,6-Diflouro-Benzyl)-4-Sulfamoyl-Benzamide Investigative T20401 DRUGINFO D0U7GL N-(2-Flouro-Benzyl)-4-Sulfamoyl-Benzamide Investigative T20401 DRUGINFO D0L4KE N-(2-Thienylmethyl)-2,5-Thiophenedisulfonamide Investigative T20401 DRUGINFO D0M4EV N-(4-cyanophenyl)sulfamide Investigative T20401 DRUGINFO D0KB6T N-(4-Sulfamoyl-phenyl)-benzamide Investigative T20401 DRUGINFO D0K3LN N-(4-Sulfamoyl-phenyl)-butyramide Investigative T20401 DRUGINFO D0T2YZ N-(4-Sulfamoyl-phenyl)-isobutyramide Investigative T20401 DRUGINFO D0N8LR N-(4-Sulfamoyl-phenyl)-propionamide Investigative T20401 DRUGINFO D07YSQ N-(4-sulfamoylphenylethyl)-4-sulfamoylbenzamide Investigative T20401 DRUGINFO D0S4NO N-(5-ethyl-1,3,4-thiadiazol-2-yl)sulfamide Investigative T20401 DRUGINFO D0J1PZ N-(5-Mercapto-[1,3,4]thiadiazol-2-yl)-acetamide Investigative T20401 DRUGINFO D06JVR N-(5-phenyl-1,3,4-thiadiazol-2-yl)sulfamide Investigative T20401 DRUGINFO D0T2VH N-(5-tert-butyl-1,3,4-thiadiazol-2-yl)sulfamide Investigative T20401 DRUGINFO D0PA5L N-(pentafluorophenyl)sulfamide Investigative T20401 DRUGINFO D0L6CN N-(phosphonacetyl)-L-aspartate Investigative T20401 DRUGINFO D0LM8L N-[(4-bromo-1-benzothien-3-yl)methyl]sulfamide Investigative T20401 DRUGINFO D0GI2R N-[(5-chloro-1-benzothien-3-yl)methyl]sulfamide Investigative T20401 DRUGINFO D0N8RD N-[2-(1h-Indol-5-Yl)-Butyl]-4-Sulfamoyl-Benzamide Investigative T20401 DRUGINFO D0K5NQ N-[4-(trifluoromethyl)phenyl]sulfamide Investigative T20401 DRUGINFO D0E3VJ N-[5-(ethylthio)-1,3,4-thiadiazol-2-yl]sulfamide Investigative T20401 DRUGINFO D04PSK N-[5-(methylthio)-1,3,4-thiadiazol-2-yl]sulfamide Investigative T20401 DRUGINFO D0M7QA N-{2-[4-(AMINOSULFONYL)PHENYL]ETHYL}ACETAMIDE Investigative T20401 DRUGINFO D00BMI N-1,3,4-thiadiazol-2-ylsulfamide Investigative T20401 DRUGINFO D07RZN N-Benzyl-4-Sulfamoyl-Benzamide Investigative T20401 DRUGINFO D09CXX N-hydroxysulfamide Investigative T20401 DRUGINFO D03EAQ N-hydroxysulfonamides Investigative T20401 DRUGINFO D00RJT NITRATE Investigative T20401 DRUGINFO D01XFH N-propynyl amidebenzenesulphonide Investigative T20401 DRUGINFO D0B4IN NSC-654077 Investigative T20401 DRUGINFO D0D4OV Octane-1,8-diyl disulfamate Investigative T20401 DRUGINFO D05TLB Octyl sulfamate Investigative T20401 DRUGINFO D08XQI PARAOXON Investigative T20401 DRUGINFO D0AU0M P-Coumaric Acid Investigative T20401 DRUGINFO D02QGI Pentane-1,5-diamine Investigative T20401 DRUGINFO D0Q0XO Pentanoic acid (4-sulfamoyl-phenyl)-amide Investigative T20401 DRUGINFO D06ORV Phenethylboronic acid Investigative T20401 DRUGINFO D01GNQ Phenoxyarsonous acid Investigative T20401 DRUGINFO D0EJ9B Phenyl Boronic acid Investigative T20401 DRUGINFO D0UN0E PHENYLDIFLUOROMETHANESULFONAMIDE Investigative T20401 DRUGINFO D07SIA PHENYLMETHANESULFONAMIDE Investigative T20401 DRUGINFO D00CIW Phenyl-phosphonic acid Investigative T20401 DRUGINFO D0L4FM PHENYLSULFAMATE Investigative T20401 DRUGINFO D06IYU PHENYLSULFAMIDE Investigative T20401 DRUGINFO D0SV6C PRONTOCIL Investigative T20401 DRUGINFO D00IAE Prop-2-ynyl 4-sulfamoylbenzoate Investigative T20401 DRUGINFO D0ZC3W P-toluenesulfonamide Investigative T20401 DRUGINFO D0L8ZG P-tolylboronic acid Investigative T20401 DRUGINFO D0F7SO Quinoline-8-sulfonamide Investigative T20401 DRUGINFO D02DBP RESORCINOL Investigative T20401 DRUGINFO D0A0YX SACCHARIN Investigative T20401 DRUGINFO D0G6OW Sodium 2,3,5,6-tetrafluorobenzoate Investigative T20401 DRUGINFO D0F4ZW SODIUM PERFLUOROHEXANESULFONAMIDE Investigative T20401 DRUGINFO D0D5XC Sodium trithiocarbonate Investigative T20401 DRUGINFO D03VDJ SULFAMATE Investigative T20401 DRUGINFO D07ZXR Sulfamic acid 12-sulfamoyloxy-dodecyl ester Investigative T20401 DRUGINFO D07CBA Sulfamic acid 16-sulfamoyloxy-hexadecyl ester Investigative T20401 DRUGINFO D07IHP Sulfamic acid 3-sulfamoyloxy-phenyl ester Investigative T20401 DRUGINFO D04BKU Sulfamic acid 4-sulfamoyloxy-butyl ester Investigative T20401 DRUGINFO D0N5KX Sulfamic acid 4-sulfamoyloxymethyl-benzyl ester Investigative T20401 DRUGINFO D0X0PO Sulfamic acid 6-sulfamoyloxy-hexyl ester Investigative T20401 DRUGINFO D05FNN Sulfamic acid 7-sulfamoyloxy-heptyl ester Investigative T20401 DRUGINFO D0A5XB Sulfamic acid benzo[1,3]dioxol-2-ylmethyl ester Investigative T20401 DRUGINFO D04MAM Sulfamic acid chroman-2-ylmethyl ester Investigative T20401 DRUGINFO D0Q7DJ Syringic Acid Investigative T20401 DRUGINFO D0I0RT Thioureido sulfonamide Investigative T20401 DRUGINFO D0S8RD Trecadrine Investigative T20401 KEGGPATH hsa00910:Nitrogen metabolism T20401 KEGGPATH hsa04964:Proximal tubule bicarbonate reclamation T20401 KEGGPATH hsa04966:Collecting duct acid secretion T20401 KEGGPATH hsa04971:Gastric acid secretion T20401 KEGGPATH hsa04972:Pancreatic secretion T20401 KEGGPATH hsa04976:Bile secretion T20401 WIKIPATH WP2681:Uptake of Oxygen and Release of Carbon Dioxide by Erythrocytes T20401 WIKIPATH WP2744:Uptake of Carbon Dioxide and Release of Oxygen by Erythrocytes T20401 WIKIPATH WP2770:Reversible Hydration of Carbon Dioxide T20401 REACPATH R-HSA-1237044:Erythrocytes take up carbon dioxide and release oxygen T20401 REACPATH R-HSA-1247673:Erythrocytes take up oxygen and release carbon dioxide T20401 REACPATH R-HSA-1475029:Reversible hydration of carbon dioxide T20401 NET_PATH NetPath_16:IL4 Signaling Pathway T20401 NET_PATH NetPath_4:EGFR1 Signaling Pathway T89534 TARGETID T89534 T89534 FORMERID TTDS00242 T89534 UNIPROID ESR1_HUMAN T89534 TARGNAME Estrogen receptor (ESR) T89534 GENENAME ESR1 T89534 TARGTYPE Successful target T89534 SYNONYMS Nuclear receptor subfamily 3 group A member 1; NR3A1; Estradiol receptor; ESR; ER-alpha; ER T89534 FUNCTION Nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Ligand-dependent nuclear transactivation involves either direct homodimer binding to a palindromic estrogen response element (ERE) sequence or association with other DNA-binding transcription factors, such as AP-1/c-Jun, c-Fos, ATF-2, Sp1 and Sp3, to mediate ERE-independent signaling. Ligand binding induces a conformational change allowing subsequent or combinatorial association with multiprotein coactivator complexes through LXXLL motifs of their respective components. Mutual transrepression occurs between the estrogen receptor (ER) and NF-kappa-B in a cell-type specific manner. Decreases NF-kappa-B DNA-binding activity and inhibits NF-kappa-B-mediated transcription from the IL6 promoter and displace RELA/p65 and associated coregulators from the promoter. Recruited to the NF-kappa-B response element of the CCL2 and IL8 promoters and can displace CREBBP. Present with NF-kappa-B components RELA/p65 and NFKB1/p50 on ERE sequences. Can also act synergistically with NF-kappa-B to activate transcription involving respective recruitment adjacent response elements; the function involves CREBBP. Can activate the transcriptional activity of TFF1. Also mediates membrane-initiated estrogen signaling involving various kinase cascades. Isoform 3 is involved in activation of NOS3 and endothelial nitric oxide production. Isoforms lacking one or several functional domains are thought to modulate transcriptional activity by competitive ligand or DNA binding and/or heterodimerization with the full-length receptor. Essential for MTA1-mediated transcriptional regulation of BRCA1 and BCAS3. Isoform 3 can bind to ERE and inhibit isoform 1. T89534 PDBSTRUC 6IAR; 6HMU; 6HKF; 6HKB; 6HHP T89534 BIOCLASS Nuclear hormone receptor T89534 SEQUENCE MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALLDAEPPILYSEYDPTRPFSEASMMGLLTNLADRELVHMINWAKRVPGFVDLTLHDQVHLLECAWLEILMIGLVWRSMEHPGKLLFAPNLLLDRNQGKCVEGMVEIFDMLLATSSRFRMMNLQGEEFVCLKSIILLNSGVYTFLSSTLKSLEEKDHIHRVLDKITDTLIHLMAKAGLTLQQQHQRLAQLLLILSHIRHMSNKGMEHLYSMKCKNVVPLYDLLLEMLDAHRLHAPTSRGGASVEETDQSHLATAGSTSSHSLQKYYITGEAEGFPATV T89534 DRUGINFO D06LOQ ARZOXIFENE Approved T89534 DRUGINFO D0JY8T Bazedoxifene Approved T89534 DRUGINFO D0N6YV Cenestin Approved T89534 DRUGINFO D0CT9Y Clomifene Approved T89534 DRUGINFO D0I5WB Clomiphene Citrate Approved T89534 DRUGINFO D0A2RG Conjugated estrogens a Approved T89534 DRUGINFO D01ICU Conjugated estrogens b Approved T89534 DRUGINFO D0X1EZ Cyclofenil Approved T89534 DRUGINFO D09IPV Danazol Approved T89534 DRUGINFO D09ZQN Dienestrol Approved T89534 DRUGINFO D0Y2NE Diethylstilbestrol Approved T89534 DRUGINFO D0R6RE Esterified estrogens Approved T89534 DRUGINFO D08QMX Estradiol Approved T89534 DRUGINFO D0T7ZQ Estradiol Acetate Approved T89534 DRUGINFO D0U0XD Estradiol Cypionate Approved T89534 DRUGINFO D07VBA Estradiol Valerate Approved T89534 DRUGINFO D0Z1FX Estriol Approved T89534 DRUGINFO D0M8PD Estrogen Approved T89534 DRUGINFO D00ZFP Estrone Approved T89534 DRUGINFO D03IUY Estropipate Approved T89534 DRUGINFO D06NXY Ethinyl Estradiol Approved T89534 DRUGINFO D0JO8Z Fosfestrol Approved T89534 DRUGINFO D0JO7Y Fulvestrant Approved T89534 DRUGINFO D0M5RF Gestrinone Approved T89534 DRUGINFO D09NMD Lasofoxifene Approved T89534 DRUGINFO D0W9GA Levormeloxifene Approved T89534 DRUGINFO D0J1ML Mestranol Approved T89534 DRUGINFO D0Z5OE Mitotane Approved T89534 DRUGINFO D0V2JK Nomegestrol acetate Approved T89534 DRUGINFO D02CTS Ospemifene Approved T89534 DRUGINFO D0S1UW Premarin/Trimegestone Approved T89534 DRUGINFO D0C4NY Promestriene Approved T89534 DRUGINFO D04UZT Quinestrol Approved T89534 DRUGINFO D01XBA Raloxifene Approved T89534 DRUGINFO D07KSG Tamoxifen Approved T89534 DRUGINFO D04VFJ Toremifene Approved T89534 DRUGINFO D0XB0T Acolbifene Phase 3 T89534 DRUGINFO D0VF3C NPC-01 Phase 3 T89534 DRUGINFO D0G7IV Premarin/Pravachol Phase 3 T89534 DRUGINFO D07KUN RAD-1901 Phase 3 T89534 DRUGINFO D02BAE Synthetic conjugated estrogen Phase 3 T89534 DRUGINFO D0C6XR Trimegestone/ethinyl estradiol Phase 3 T89534 DRUGINFO D0IC7A TZTX-001 Phase 3 T89534 DRUGINFO D09NST Afimoxifene Phase 2 T89534 DRUGINFO D00JFE ARN-810 Phase 2 T89534 DRUGINFO DATO92 AZD9833 Phase 2 T89534 DRUGINFO D0W4EB Endoxifen Phase 2 T89534 DRUGINFO D0L3TR Estetrol Phase 2 T89534 DRUGINFO D0E7FM GTx-758 Phase 2 T89534 DRUGINFO D0L0BX ICARITIN Phase 2 T89534 DRUGINFO D02PYN SR 16234 Phase 2 T89534 DRUGINFO D0Z5VW H3B-6545 Phase 1/2 T89534 DRUGINFO DZ91HE OP-1250 Phase 1/2 T89534 DRUGINFO DJ1W5R ZN-c5 Phase 1/2 T89534 DRUGINFO D09BQO ATD transdermal gel Phase 1 T89534 DRUGINFO D0X1OW AZD9496 Phase 1 T89534 DRUGINFO D03YGP CC-8490 Phase 1 T89534 DRUGINFO D08OUV CHF-4227 Phase 1 T89534 DRUGINFO D09OJI D-0502 Phase 1 T89534 DRUGINFO DG38QS G1T-48 Phase 1 T89534 DRUGINFO DH4Y3O LY3484356 Phase 1 T89534 DRUGINFO DNTW18 SCO-120 Phase 1 T89534 DRUGINFO D0NZ3C TTC-352 Phase 1 T89534 DRUGINFO DT4WU3 TTC-352 Phase 1 T89534 DRUGINFO D0QQ1J BITHIONOL Withdrawn from market T89534 DRUGINFO D0X0KJ Chlorotrianisene Withdrawn from market T89534 DRUGINFO D0C4FT HEXESTROL Withdrawn from market T89534 DRUGINFO D0MU0S EM-800 Discontinued in Phase 3 T89534 DRUGINFO D0GR2J Idoxifene Discontinued in Phase 3 T89534 DRUGINFO D01OML IoGen Discontinued in Phase 3 T89534 DRUGINFO D02VFB Miproxifene Discontinued in Phase 3 T89534 DRUGINFO D0R2JS Droloxifene Discontinued in Phase 2 T89534 DRUGINFO D0R8TB ERA-923 Discontinued in Phase 2 T89534 DRUGINFO D01AXT NP-50301 Discontinued in Phase 2 T89534 DRUGINFO D04HVB Panomifene Discontinued in Phase 2 T89534 DRUGINFO D04MNL SERM-3339 Discontinued in Phase 2 T89534 DRUGINFO D04BIG SR-90067 Discontinued in Phase 2 T89534 DRUGINFO D08DZZ HE2100 Discontinued in Phase 1 T89534 DRUGINFO D0B6HS HRT Discontinued in Phase 1 T89534 DRUGINFO D05BCA MX-4509 Discontinued in Phase 1 T89534 DRUGINFO D0P5NU BN-AA-003-NY Preclinical T89534 DRUGINFO D01EXY BN-AO-014 Preclinical T89534 DRUGINFO D0QI9N BN-CB-045 Preclinical T89534 DRUGINFO D0N6YN BN-DF-037 Preclinical T89534 DRUGINFO D0QX9U BN-GU-005-DHP Preclinical T89534 DRUGINFO D06YGP BN-OD-026 Preclinical T89534 DRUGINFO D09AAM ICI-164384 Terminated T89534 DRUGINFO D0SM0J LY-117018 Terminated T89534 DRUGINFO D0J4ZH Tamoxifen methyl iodide Terminated T89534 DRUGINFO D0TR4Z Zindoxifene Terminated T89534 DRUGINFO D0H5CV ZK-119010 Terminated T89534 DRUGINFO D00HUB [1,1':2',1'']Terphenyl-4'-carbaldehyde oxime Investigative T89534 DRUGINFO D0Z0UC 1,2-Bis-(4-hydroxy-phenyl)-3H-inden-5-ol Investigative T89534 DRUGINFO D05FUY 1,8-Dichloro-6-(4-hydroxy-phenyl)-naphthalen-2-ol Investigative T89534 DRUGINFO D08JCJ 17-METHYL-17-ALPHA-DIHYDROEQUILENIN Investigative T89534 DRUGINFO D0S6NV 1-Bromo-6-(4-hydroxy-phenyl)-naphthalen-2-ol Investigative T89534 DRUGINFO D01KJU 1-CHLORO-6-(4-HYDROXYPHENYL)-2-NAPHTHOL Investigative T89534 DRUGINFO D0ZT4U 1-Fluoro-6-(4-hydroxy-phenyl)-naphthalen-2-ol Investigative T89534 DRUGINFO D0V7QZ 2-(2-Chloro-4-hydroxy-phenyl)-benzooxazol-5-ol Investigative T89534 DRUGINFO D0DK9S 2-(3-Butoxy-4-hydroxy-phenyl)-benzooxazol-6-ol Investigative T89534 DRUGINFO D0K1TW 2-(3-Chloro-4-hydroxy-phenyl)-benzooxazol-5-ol Investigative T89534 DRUGINFO D08HCF 2-(3-Chloro-4-hydroxy-phenyl)-benzooxazol-6-ol Investigative T89534 DRUGINFO D09TQE 2-(3-Fluoro-4-hydroxy-phenyl)-benzooxazol-5-ol Investigative T89534 DRUGINFO D0AD3U 2-(3-Fluoro-4-hydroxy-phenyl)-benzooxazol-6-ol Investigative T89534 DRUGINFO D01SWO 2-(3-hydroxyphenyl)-1,2'-spirobi[1H-indene]-5-ol Investigative T89534 DRUGINFO D03DVM 2-(3-hydroxyphenyl)-1,2'-spirobi[1H-indene]-6-ol Investigative T89534 DRUGINFO D0W3FF 2-(4-Hydroxy-naphthalen-1-yl)-benzooxazol-6-ol Investigative T89534 DRUGINFO D0X2VK 2-(4-hydroxyphenyl)-1,2'-spirobi[1H-indene]-5-ol Investigative T89534 DRUGINFO D0L6IQ 2-(4-Hydroxy-phenyl)-4-methoxy-quinolin-6-ol Investigative T89534 DRUGINFO D0K7HR 2-(4-Hydroxy-phenyl)-4-vinyl-quinolin-6-ol Investigative T89534 DRUGINFO D02LCC 2-(4-Hydroxy-phenyl)-7-isopropyl-benzooxazol-5-ol Investigative T89534 DRUGINFO D03XEU 2-(4-Hydroxy-phenyl)-7-methoxy-benzofuran-5-ol Investigative T89534 DRUGINFO D05JPW 2-(4-Hydroxy-phenyl)-7-methoxy-benzooxazol-5-ol Investigative T89534 DRUGINFO D0C6AP 2-(4-Hydroxy-phenyl)-7-methyl-benzofuran-5-ol Investigative T89534 DRUGINFO D07VPM 2-(4-Hydroxy-phenyl)-7-phenyl-benzooxazol-5-ol Investigative T89534 DRUGINFO D02EJM 2-(4-Hydroxy-phenyl)-7-propenyl-benzooxazol-5-ol Investigative T89534 DRUGINFO D04WHH 2-(4-Hydroxy-phenyl)-7-propyl-benzooxazol-5-ol Investigative T89534 DRUGINFO D0YW4C 2-(4-Hydroxy-phenyl)-7-vinyl-benzooxazol-5-ol Investigative T89534 DRUGINFO D01WCA 2-(4-HYDROXY-PHENYL)BENZOFURAN-5-OL Investigative T89534 DRUGINFO D0N0OY 2-(4-Hydroxy-phenyl)-benzooxazol-5-ol Investigative T89534 DRUGINFO D09CQC 2-(4-Hydroxy-phenyl)-benzooxazol-6-ol Investigative T89534 DRUGINFO D00CWN 2-(4-Hydroxy-phenyl)-quinolin-6-ol Investigative T89534 DRUGINFO D0U2VA 2-(5-Hydroxy-naphthalen-1-yl)-benzooxazol-6-ol Investigative T89534 DRUGINFO D01QXL 2-(6-Hydroxy-naphthalen-1-yl)-benzooxazol-5-ol Investigative T89534 DRUGINFO D0YH4T 2-(6-Hydroxy-naphthalen-1-yl)-benzooxazol-6-ol Investigative T89534 DRUGINFO D02JJU 2-(6-Hydroxy-naphthalen-2-yl)-benzooxazol-5-ol Investigative T89534 DRUGINFO D00HZT 2-(6-Hydroxy-naphthalen-2-yl)-benzooxazol-6-ol Investigative T89534 DRUGINFO D0P7PK 2,3-diphenyl-1H-indole Investigative T89534 DRUGINFO D03BOO 2,4-Dibenzylamino-6-isopentylpyrimidine Investigative T89534 DRUGINFO D02GLM 2,4-diisobutylamino-6-isopentylpyrimidine Investigative T89534 DRUGINFO D00ZAJ 2-AMINO-1-METHYL-6-PHENYLIMIDAZO[4,5-B]PYRIDINE Investigative T89534 DRUGINFO D0H1CO 2-Naphthalen-1-yl-benzooxazol-6-ol Investigative T89534 DRUGINFO D0O2KP 2-phenyl-1,2'-spirobi[1H-indene]-5'-ol Investigative T89534 DRUGINFO D04EAY 3-(2-Hydroxy-phenyl)-benzo[d]isoxazol-6-ol Investigative T89534 DRUGINFO D0GH1I 3-(4-Hydroxyphenyl)-7-isobutoxychromen-4-one Investigative T89534 DRUGINFO D0O9UY 3-(4-Hydroxyphenyl)-7-isopropoxychromen-4-one Investigative T89534 DRUGINFO D08FLV 3-(4-Hydroxy-phenyl)-benzo[d]isoxazol-5-ol Investigative T89534 DRUGINFO D0B1HP 3-(4-Hydroxy-phenyl)-benzo[d]isoxazol-6-ol Investigative T89534 DRUGINFO D0W2YR 3-(5-Hydroxy-benzooxazol-2-yl)-benzene-1,2-diol Investigative T89534 DRUGINFO D0S2ZJ 3-(6-Hydroxy-benzooxazol-2-yl)-benzene-1,2-diol Investigative T89534 DRUGINFO D0C5FY 3,8-dihydroxy-4-methyl-6H-benzo[c]chromen-6-one Investigative T89534 DRUGINFO D0HM8Y 3,8-dihydroxy-7-methyl-6H-benzo[c]chromen-6-one Investigative T89534 DRUGINFO D00AAU 3-[1-ethyl-2-(3-hydroxyphenyl)butyl]phenol Investigative T89534 DRUGINFO D01ZRX 3-CHLORO-2-(4-HYDROXYPHENYL)-2H-INDAZOL-5-OL Investigative T89534 DRUGINFO D01UAO 3-chloro-4-(4-hydroxyphenyl)salicylaldoxime Investigative T89534 DRUGINFO D0A8CS 3-ETHYL-2-(4-HYDROXYPHENYL)-2H-INDAZOL-5-OL Investigative T89534 DRUGINFO D0U0ZE 3-hydroxy-8,10-dimethyl-6H-benzo[c]chromen-6-one Investigative T89534 DRUGINFO D0A1JP 3'-Methoxy-4'Hydroxyclomiphene Investigative T89534 DRUGINFO D0V7OK 4-(1,2-Diphenyl-but-1-enyl)-phenol Investigative T89534 DRUGINFO D09WEK 4-(1-benzyl-7-chloro-1H-indazol-3-yl)phenol Investigative T89534 DRUGINFO D0Q4VG 4-(1-butyl-7-chloro-1H-indazol-3-yl)phenol Investigative T89534 DRUGINFO D0F8LS 4-(1-cyclopentyl-7-fluoro-1H-indazol-3-yl)phenol Investigative T89534 DRUGINFO D0I5HZ 4-(2-phenyl-1H-benzo[d]imidazol-1-yl)phenol Investigative T89534 DRUGINFO D0K0IC 4-(2-phenyl-1H-indol-3-yl)phenol Investigative T89534 DRUGINFO D0U7KV 4-(3-(4-hydroxyphenyl)-1H-indol-2-yl)phenol Investigative T89534 DRUGINFO D00NEK 4-(3-phenyl-1H-indol-2-yl)phenol Investigative T89534 DRUGINFO D0R7AG 4-(5-Hydroxy-benzooxazol-2-yl)-benzene-1,3-diol Investigative T89534 DRUGINFO D0K5LX 4-(6-HYDROXY-1H-INDAZOL-3-YL)BENZENE-1,3-DIOL Investigative T89534 DRUGINFO D0C9XK 4-(6-Hydroxy-benzooxazol-2-yl)-benzene-1,2-diol Investigative T89534 DRUGINFO D03RYU 4-(6-Hydroxy-benzooxazol-2-yl)-benzene-1,3-diol Investigative T89534 DRUGINFO D0H8ZT 4-(7-chloro-1-cyclohexyl-1H-indazol-3-yl)phenol Investigative T89534 DRUGINFO D0V7ZI 4-(7-chloro-1-cyclopentyl-1H-indazol-3-yl)phenol Investigative T89534 DRUGINFO D0C4VX 4-(7-chloro-1-propyl-1H-indazol-3-yl)phenol Investigative T89534 DRUGINFO D0J6KN 4-(7-methyl-1-propyl-1H-indazol-3-yl)phenol Investigative T89534 DRUGINFO D00URP 4,10-dimethyl-6H-benzo[c]chromene-3,8-diol Investigative T89534 DRUGINFO D0NN0V 4',5,7-trihydroxy-6,8-dimethylisoflavone Investigative T89534 DRUGINFO D0S8EB 4,6,10-trimethyl-6H-benzo[c]chromene-3,8-diol Investigative T89534 DRUGINFO D0H5HI 4,6,6,7-tetramethyl-6H-benzo[c]chromene-3,8-diol Investigative T89534 DRUGINFO D0O6FX 4,6,7,10-tetramethyl-6H-benzo[c]chromene-3,8-diol Investigative T89534 DRUGINFO D0O5KR 4,6,7-trimethyl-6H-benzo[c]chromene-3,8-diol Investigative T89534 DRUGINFO D09PXU 4,7-dimethyl-6H-benzo[c]chromene-3,8-diol Investigative T89534 DRUGINFO D0K8QD 4-[1-(4-hydroxyphenyl)-2-phenylbut-1-enyl]phenol Investigative T89534 DRUGINFO D0XC3V 4-[1-(4-hydroxyphenyl)-2-phenylhex-1-enyl]phenol Investigative T89534 DRUGINFO D0OV3S 4-[1-(4-hydroxyphenyl)-2-phenylpent-1-enyl]phenol Investigative T89534 DRUGINFO D0Q6MS 4-[1-(4-hydroxyphenyl)-2-phenylprop-1-enyl]phenol Investigative T89534 DRUGINFO D07TGS 4-[1-(4-hydroxyphenyl)-2-phenylvinyl]phenol Investigative T89534 DRUGINFO D0I1NX 4-[1,2-bis(4-hydroxyphenyl)but-1-enyl]phenol Investigative T89534 DRUGINFO D06DNN 4-[1,2-bis(4-hydroxyphenyl)hex-1-enyl]phenol Investigative T89534 DRUGINFO D02DVT 4-[1,2-bis(4-hydroxyphenyl)pent-1-enyl]phenol Investigative T89534 DRUGINFO D00OLH 4-[1,2-bis(4-hydroxyphenyl)vinyl]phenol Investigative T89534 DRUGINFO D03EOD 4-[2,2-bis(4-hydroxyphenyl)-1-methylvinyl]phenol Investigative T89534 DRUGINFO D08WDN 4-Benzo[d]isoxazol-3-yl-benzene-1,3-diol Investigative T89534 DRUGINFO D04TPC 4-benzyl-2,6-diisobutylamino-pyrimidine Investigative T89534 DRUGINFO D03CBX 4-Bromo-2-(4-hydroxy-phenyl)-quinolin-6-ol Investigative T89534 DRUGINFO D01TUB 4-Chloro-2-(4-hydroxy-phenyl)-quinolin-6-ol Investigative T89534 DRUGINFO D09FWS 4-Ethyl-2-(4-hydroxy-phenyl)-quinolin-6-ol Investigative T89534 DRUGINFO D08SJL 4-Ethynyl-2-(4-hydroxy-phenyl)-quinolin-6-ol Investigative T89534 DRUGINFO D0Z9ZY 4-hydroxy-N,N-diphenylbenzenesulfonamide Investigative T89534 DRUGINFO D0J3PM 4-hydroxy-N-isopropyl-N-phenylbenzenesulfonamide Investigative T89534 DRUGINFO D08LVT 4-hydroxy-N-neopentyl-N-phenylbenzenesulfonamide Investigative T89534 DRUGINFO D0L0RK 4-hydroxy-N-phenyl-N-propylbenzenesulfonamide Investigative T89534 DRUGINFO D0L3AX 4-Naphthalen-2-yl-phenol Investigative T89534 DRUGINFO D0J0AG 5-Bromo-2-(4-hydroxy-phenyl)-quinolin-6-ol Investigative T89534 DRUGINFO D01KSR 5-Chloro-2-(4-hydroxy-phenyl)-benzooxazol-6-ol Investigative T89534 DRUGINFO D02HGS 5-Chloro-2-(4-hydroxy-phenyl)-quinolin-6-ol Investigative T89534 DRUGINFO D0X6LK 5-hydroxy-2-phenylisoindoline-1,3-dione Investigative T89534 DRUGINFO D0X7DJ 6-(2,5-Difluoro-4-hydroxy-phenyl)-naphthalen-2-ol Investigative T89534 DRUGINFO D0V6KJ 6-(2,6-Difluoro-4-hydroxy-phenyl)-naphthalen-2-ol Investigative T89534 DRUGINFO D02OKF 6-(2-Chloro-4-hydroxy-phenyl)-naphthalen-2-ol Investigative T89534 DRUGINFO D0CC6R 6-(2-Fluoro-4-hydroxy-phenyl)-naphthalen-2-ol Investigative T89534 DRUGINFO D0MY8V 6-(3,5-Difluoro-4-hydroxy-phenyl)-naphthalen-2-ol Investigative T89534 DRUGINFO D0K6TE 6-(3-Chloro-4-hydroxy-phenyl)-naphthalen-2-ol Investigative T89534 DRUGINFO D0X4VN 6-(3-Fluoro-4-hydroxy-phenyl)-naphthalen-2-ol Investigative T89534 DRUGINFO D0HR8L 6-(3-Hydroxy-phenyl)-naphthalen-1-ol Investigative T89534 DRUGINFO D0P8PK 6-(3-Hydroxy-phenyl)-naphthalen-2-ol Investigative T89534 DRUGINFO D0P6FN 6-(4-Hydroxy-2-methoxy-phenyl)-naphthalen-2-ol Investigative T89534 DRUGINFO D01GPY 6-(4-Hydroxy-2-methyl-phenyl)-naphthalen-2-ol Investigative T89534 DRUGINFO D0M0XL 6-(4-Hydroxy-phenyl)-1-methoxy-naphthalen-2-ol Investigative T89534 DRUGINFO D07XBD 6-(4-Hydroxy-phenyl)-1-methyl-naphthalen-2-ol Investigative T89534 DRUGINFO D0H2FI 6-(4-Hydroxy-phenyl)-1-nitro-naphthalen-2-ol Investigative T89534 DRUGINFO D0VN2R 6-(4-Hydroxy-phenyl)-1-phenyl-naphthalen-2-ol Investigative T89534 DRUGINFO D0H8PI 6-(4-Hydroxy-phenyl)-naphthalen-1-ol Investigative T89534 DRUGINFO D07LUI 6-(4-Hydroxy-phenyl)-naphthalen-2-ol Investigative T89534 DRUGINFO D0C9XW 6-butyl-2,4-dipropylaminopyrimidine Investigative T89534 DRUGINFO D05JKC 6-Chloro-2-(4-hydroxy-phenyl)-benzooxazol-5-ol Investigative T89534 DRUGINFO D0H6MZ 6-ethyl-2,4-diisobutylaminopyrimidine Investigative T89534 DRUGINFO D00IXB 6-ethyl-4,7-dimethyl-6H-benzo[c]chromene-3,8-diol Investigative T89534 DRUGINFO D0UV9G 6-Phenyl-naphthalen-2-ol Investigative T89534 DRUGINFO D01IAT 7-(3-Hydroxy-phenyl)-naphthalen-2-ol Investigative T89534 DRUGINFO D09DEK 7-(4-Hydroxy-phenyl)-naphthalen-2-ol Investigative T89534 DRUGINFO D00ZBL 7-Allyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol Investigative T89534 DRUGINFO D0L2MU 7-Bromo-2-(4-hydroxy-phenyl)-benzofuran-5-ol Investigative T89534 DRUGINFO D03GYS 7-Butyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol Investigative T89534 DRUGINFO D05YIU 7-Chloro-2-(4-hydroxy-phenyl)-benzofuran-5-ol Investigative T89534 DRUGINFO D05QTG 7-Cyclopentyloxy-3-(4-hydroxyphenyl)chromen-4-one Investigative T89534 DRUGINFO D06OAL 7-Ethyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol Investigative T89534 DRUGINFO D0S0SZ 7-Ethynyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol Investigative T89534 DRUGINFO D0SR8Q 7-Phenyl-naphthalen-2-ol Investigative T89534 DRUGINFO D03QHG 8-(2,2-dimethylpropyl)naringenin Investigative T89534 DRUGINFO D0Y2LJ 8-(2-methylpropyl)naringenin Investigative T89534 DRUGINFO D09NOH 8-(3-methylbutyl)naringenin Investigative T89534 DRUGINFO D0D1LB 8-benzylnaringenin Investigative T89534 DRUGINFO D08VDX 8-Chloro-6-(4-hydroxy-phenyl)-naphthalen-2-ol Investigative T89534 DRUGINFO D0FD6Z 8-Fluoro-6-(4-hydroxy-phenyl)-naphthalen-2-ol Investigative T89534 DRUGINFO D07XUY 8-methylnaringenin Investigative T89534 DRUGINFO D0J2NG 8-n-heptylnaringenin Investigative T89534 DRUGINFO D0W5HT 8-n-nonylnaringenin Investigative T89534 DRUGINFO D0LI0M 8-n-pentylnaringenin Investigative T89534 DRUGINFO D0W0LG 8-n-propylnaringenin Investigative T89534 DRUGINFO D05KXP 8-n-undecylnaringenin Investigative T89534 DRUGINFO D06DDT BROUSSONIN A Investigative T89534 DRUGINFO D07KXE Carboron Cluster with phenol Investigative T89534 DRUGINFO D02DML COUMESTROL Investigative T89534 DRUGINFO D0L5IC CP-394531 Investigative T89534 DRUGINFO D0J7XZ CP-409069 Investigative T89534 DRUGINFO D0SY2M daidzein Investigative T89534 DRUGINFO D02VIW DIHYDRORALOXIFENE Investigative T89534 DRUGINFO D0RI6O Doxorubicin-Formaldehyde Conjugate Investigative T89534 DRUGINFO D0W4WF EFFUSOL Investigative T89534 DRUGINFO D0V4DH Estriol E3 Investigative T89534 DRUGINFO D0H6OS Geldanamycin-estradiol hybrid Investigative T89534 DRUGINFO D09NFD GSK-5182 Investigative T89534 DRUGINFO D04SAO GW7604 Investigative T89534 DRUGINFO D00DJX JNJ-17148066 Investigative T89534 DRUGINFO D09UQU JNJ-19398990 Investigative T89534 DRUGINFO D0X0RJ JNJ-26529126 Investigative T89534 DRUGINFO D02TPO JNJ-26529152 Investigative T89534 DRUGINFO D04PEM LTERHKILHRLLQEGSPSD Investigative T89534 DRUGINFO D0XF9F methyl-piperidino-pyrazole Investigative T89534 DRUGINFO D07TGW MPrP Investigative T89534 DRUGINFO D07HBQ N,N,N-Triisobutyl-pyrimidine-2,4,6-triamine Investigative T89534 DRUGINFO D00FUO Nafoxidine Investigative T89534 DRUGINFO D0AD8G N-allyl-4-hydroxy-N-phenylbenzenesulfonamide Investigative T89534 DRUGINFO D00XLU N-benzyl-4-hydroxy-N-phenylbenzenesulfonamide Investigative T89534 DRUGINFO D0M4LQ N-butyl-4-hydroxy-N-phenylbenzenesulfonamide Investigative T89534 DRUGINFO D01XCA N-cyclohexyl-4-hydroxy-N-phenylbenzenesulfonamide Investigative T89534 DRUGINFO D09ULU N-ethyl-4-hydroxy-N-phenylbenzenesulfonamide Investigative T89534 DRUGINFO D0I6QZ Org-37663 Investigative T89534 DRUGINFO D0Y8UF propylpyrazoletriol Investigative T89534 DRUGINFO D04SEX R,R-THC Investigative T89534 DRUGINFO D0E3UW RG6046 Investigative T89534 DRUGINFO D0GY3R SERMs Investigative T89534 DRUGINFO D09BDK SNG-163 Investigative T89534 DRUGINFO D01NDN SNG-8006 Investigative T89534 DRUGINFO D03NWC SNG-8023 Investigative T89534 DRUGINFO D03AVA SNG-8033 Investigative T89534 DRUGINFO D0S8AV SOPHORAFLAVANONE B Investigative T89534 DRUGINFO D0E6AP STX Investigative T89534 DRUGINFO D0S5RI Tamoxifen butyl bromide Investigative T89534 DRUGINFO D0C6UR Tamoxifen ethyl bromide Investigative T89534 DRUGINFO D08GWS Tamoxifen isopropyl bromide Investigative T89534 DRUGINFO D0B4VV Trans-hydroxytamoxifen Investigative T89534 DRUGINFO D0W1YZ TSERaM Investigative T89534 DRUGINFO D0Y9BO WAY-169916 Investigative T89534 DRUGINFO D06SCS WAY200070 Investigative T89534 DRUGINFO D0P0FN ZK-164015 Investigative T89534 KEGGPATH hsa04915:Estrogen signaling pathway T89534 KEGGPATH hsa04917:Prolactin signaling pathway T89534 KEGGPATH hsa04919:Thyroid hormone signaling pathway T89534 KEGGPATH hsa04961:Endocrine and other factor-regulated calcium reabsorption T89534 KEGGPATH hsa05205:Proteoglycans in cancer T89534 WIKIPATH WP170:Nuclear Receptors T89534 WIKIPATH WP1984:Integrated Breast Cancer Pathway T89534 WIKIPATH WP2005:miR-targeted genes in muscle cell - TarBase T89534 WIKIPATH WP2034:Leptin signaling pathway T89534 WIKIPATH WP2377:Integrated Pancreatic Cancer Pathway T89534 WIKIPATH WP2593:JAK/STAT T89534 WIKIPATH WP2781:Signaling by ERBB4 T89534 WIKIPATH WP2881:Estrogen Receptor Pathway T89534 WIKIPATH WP2882:Nuclear Receptors Meta-Pathway T89534 WIKIPATH WP712:Estrogen signaling pathway T89534 REACPATH R-HSA-1251985:Nuclear signaling by ERBB4 T89534 REACPATH R-HSA-383280:Nuclear Receptor transcription pathway T89534 NET_PATH NetPath_21:RANKL Signaling Pathway T89534 NET_PATH NetPath_25:FSH Signaling Pathway T89534 NET_PATH NetPath_4:EGFR1 Signaling Pathway T89534 INTEPATH ap1_pathway:AP-1 transcription factor network T89534 INTEPATH atf2_pathway:ATF-2 transcription factor network T89534 INTEPATH er_nongenomic_pathway:Plasma membrane estrogen receptor signaling T89534 INTEPATH era_genomic_pathway:Validated nuclear estrogen receptor alpha network T89534 INTEPATH foxm1pathway:FOXM1 transcription factor network T89534 INTEPATH hdac_classii_pathway:Signaling events mediated by HDAC Class II T89534 INTEPATH hnf3apathway:FOXA1 transcription factor network T89534 INTEPATH lkb1_pathway:LKB1 signaling events T89534 INTEPATH p38alphabetadownstreampathway:Signaling mediated by p38-alpha and p38-beta T89534 INTEPATH smad2_3nuclearpathway:Regulation of nuclear SMAD2/3 signaling T89534 INTEPATH telomerasepathway:Regulation of Telomerase T52450 TARGETID T52450 T52450 FORMERID TTDC00147 T52450 UNIPROID MMP1_HUMAN T52450 TARGNAME Matrix metalloproteinase-1 (MMP-1) T52450 GENENAME MMP1 T52450 TARGTYPE Successful target T52450 SYNONYMS Interstitial collagenase; Fibroblast collagenase; CLG T52450 FUNCTION Cleaves collagens of types VII and X. In case of HIV infection, interacts and cleaves the secreted viral Tat protein, leading to a decrease in neuronal Tat's mediated neurotoxicity. Cleaves collagens of types I, II, and III at one site in the helical domain. T52450 PDBSTRUC 966C; 4AYK; 4AUO; 3SHI; 3AYK T52450 BIOCLASS Peptidase T52450 ECNUMBER EC 3.4.24.7 T52450 SEQUENCE MHSFPPLLLLLFWGVVSHSFPATLETQEQDVDLVQKYLEKYYNLKNDGRQVEKRRNSGPVVEKLKQMQEFFGLKVTGKPDAETLKVMKQPRCGVPDVAQFVLTEGNPRWEQTHLTYRIENYTPDLPRADVDHAIEKAFQLWSNVTPLTFTKVSEGQADIMISFVRGDHRDNSPFDGPGGNLAHAFQPGPGIGGDAHFDEDERWTNNFREYNLHRVAAHELGHSLGLSHSTDIGALMYPSYTFSGDVQLAQDDIDGIQAIYGRSQNPVQPIGPQTPKACDSKLTFDAITTIRGEVMFFKDRFYMRTNPFYPEVELNFISVFWPQLPNGLEAAYEFADRDEVRFFKGNKYWAVQGQNVLHGYPKDIYSSFGFPRTVKHIDAALSEENTGKTYFFVANKYWRYDEYKRSMDPGYPKMIAHDFPGIGHKVDAVFMKDGFFYFFHGTRQYKFDPKTKRILTLQKANSWFNCRKN T52450 DRUGINFO D00MDP Prinomastat Approved T52450 DRUGINFO D0MW3H CIPEMASTAT Phase 3 T52450 DRUGINFO D05VZE Marimastat Phase 3 T52450 DRUGINFO D0HG5M Apratastat Phase 2 T52450 DRUGINFO D05GAP PMID29130358-Compound-Figure10(2a) Patented T52450 DRUGINFO D0X6GG PMID29130358-Compound-Figure18(14a) Patented T52450 DRUGINFO D01EUF BMS 275291 Discontinued in Phase 3 T52450 DRUGINFO D0T9HG GM6001 Discontinued in Phase 2 T52450 DRUGINFO D03BOZ RS-130830 Discontinued in Phase 2 T52450 DRUGINFO D0G4OT XL784 Discontinued in Phase 2 T52450 DRUGINFO D05VNG BB-1101 Terminated T52450 DRUGINFO D08WBF BB-3644 Terminated T52450 DRUGINFO D08CEE L-696418 Terminated T52450 DRUGINFO D0EF7V Ro-31-4724 Terminated T52450 DRUGINFO D0E5GY RO-319790 Terminated T52450 DRUGINFO D0Y1XT SC-44463 Terminated T52450 DRUGINFO D0N0FX 3-(4-Methoxy-benzenesulfonyl)-cyclohexanethiol Investigative T52450 DRUGINFO D09XUQ 3-(4-Methoxy-benzenesulfonyl)-hexane-1-thiol Investigative T52450 DRUGINFO D01OCR 3-(4-Methoxy-benzenesulfonyl)-pentane-1-thiol Investigative T52450 DRUGINFO D0K3RC 3-(4-Phenoxy-benzenesulfonyl)-cyclohexanethiol Investigative T52450 DRUGINFO D0D7UA 3-(4-Phenoxy-benzenesulfonyl)-propane-1-thiol Investigative T52450 DRUGINFO D02BTV 3-Benzenesulfinyl-heptanoic acid hydroxyamide Investigative T52450 DRUGINFO D08ELY 3-Benzenesulfonyl-heptanoic acid hydroxyamide Investigative T52450 DRUGINFO D0N6CD 3-Cyclohexanesulfonyl-heptanoic acid hydroxyamide Investigative T52450 DRUGINFO D0T4AN 4-(4-Butoxy-phenyl)-N-hydroxy-4-oxo-butyramide Investigative T52450 DRUGINFO D0XE4B 4-(4-Methoxy-benzenesulfonyl)-butane-2-thiol Investigative T52450 DRUGINFO D01QOB 4-Butoxy-N-hydroxycarbamoylmethyl-benzamide Investigative T52450 DRUGINFO D0R2BO METHYLAMINO-PHENYLALANYL-LEUCYL-HYDROXAMIC ACID Investigative T52450 DRUGINFO D0A4TC MMI270 Investigative T52450 DRUGINFO D0L7AY N-(Ethylphosphoryl)-L-isoleucyl-L-Trp-NHCH3 Investigative T52450 DRUGINFO D08ZDD N-Hydroxy-4-(4-methoxy-phenyl)-4-oxo-butyramide Investigative T52450 DRUGINFO D06BYR N-Hydroxy-4-oxo-4-(4-phenoxy-phenyl)-butyramide Investigative T52450 DRUGINFO D0P2OA N-Hydroxycarbamoylmethyl-4-methoxy-benzamide Investigative T52450 DRUGINFO D09SYW N-Hydroxycarbamoylmethyl-4-phenoxy-benzamide Investigative T52450 DRUGINFO D0H2PA PKF-242-484 Investigative T52450 DRUGINFO D0XL8K Ro-37-9790 Investigative T52450 DRUGINFO D0BI8T RS-39066 Investigative T52450 DRUGINFO D03AMR SR-973 Investigative T52450 KEGGPATH hsa03320:PPAR signaling pathway T52450 KEGGPATH hsa05200:Pathways in cancer T52450 KEGGPATH hsa05219:Bladder cancer T52450 KEGGPATH hsa05323:Rheumatoid arthritis T52450 WIKIPATH WP129:Matrix Metalloproteinases T52450 WIKIPATH WP1794:Cell surface interactions at the vascular wall T52450 WIKIPATH WP1971:Integrated Cancer pathway T52450 WIKIPATH WP1984:Integrated Breast Cancer Pathway T52450 WIKIPATH WP2263:Prostate Cancer T52450 WIKIPATH WP2374:Oncostatin M Signaling Pathway T52450 WIKIPATH WP2435:Quercetin and Nf-kB/ AP-1 Induced Cell Apoptosis T52450 WIKIPATH WP2708:Degradation of collagen T52450 WIKIPATH WP2769:Activation of Matrix Metalloproteinases T52450 WIKIPATH WP2828:Bladder Cancer T52450 WIKIPATH WP366:TGF beta Signaling Pathway T52450 REACPATH R-HSA-1442490:Collagen degradation T52450 REACPATH R-HSA-1474228:Degradation of the extracellular matrix T52450 REACPATH R-HSA-1592389:Activation of Matrix Metalloproteinases T52450 REACPATH R-HSA-210991:Basigin interactions T52450 REACPATH R-HSA-381426:Regulation of Insulin-like Growth Factor (IGF) transport and uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs) T52450 NET_PATH NetPath_13:IL1 Signaling Pathway T52450 NET_PATH NetPath_26:TWEAK Signaling Pathway T52450 NET_PATH NetPath_4:EGFR1 Signaling Pathway T52450 NET_PATH NetPath_8:Wnt Signaling Pathway T52450 INTEPATH ap1_pathway:AP-1 transcription factor network T52450 INTEPATH endothelinpathway:Endothelins T52450 INTEPATH fra_pathway:Validated transcriptional targets of AP1 family members Fra1 and Fra2 T52450 INTEPATH reg_gr_pathway:Glucocorticoid receptor regulatory network T52450 INTEPATH syndecan_1_pathway:Syndecan-1-mediated signaling events T52450 PANTPATH P00004:Alzheimer disease-presenilin pathway T52450 PANTPATH P00050:Plasminogen activating cascade T53585 TARGETID T53585 T53585 FORMERID TTDS00195 T53585 UNIPROID HMDH_HUMAN T53585 TARGNAME HMG-CoA reductase (HMGCR) T53585 GENENAME HMGCR T53585 TARGTYPE Successful target T53585 SYNONYMS 3-hydroxy-3-methylglutaryl-coenzyme A reductase T53585 FUNCTION Transmembrane glycoprotein that is the rate-limiting enzyme in cholesterol biosynthesis as well as in the biosynthesis of nonsterol isoprenoids that are essential for normal cell function including ubiquinone and geranylgeranyl proteins. T53585 PDBSTRUC 3CDB; 3CDA; 3CD7; 3CD5; 3CD0 T53585 BIOCLASS CH-OH donor oxidoreductase T53585 ECNUMBER EC 1.1.1.34 T53585 SEQUENCE MLSRLFRMHGLFVASHPWEVIVGTVTLTICMMSMNMFTGNNKICGWNYECPKFEEDVLSSDIIILTITRCIAILYIYFQFQNLRQLGSKYILGIAGLFTIFSSFVFSTVVIHFLDKELTGLNEALPFFLLLIDLSRASTLAKFALSSNSQDEVRENIARGMAILGPTFTLDALVECLVIGVGTMSGVRQLEIMCCFGCMSVLANYFVFMTFFPACVSLVLELSRESREGRPIWQLSHFARVLEEEENKPNPVTQRVKMIMSLGLVLVHAHSRWIADPSPQNSTADTSKVSLGLDENVSKRIEPSVSLWQFYLSKMISMDIEQVITLSLALLLAVKYIFFEQTETESTLSLKNPITSPVVTQKKVPDNCCRREPMLVRNNQKCDSVEEETGINRERKVEVIKPLVAETDTPNRATFVVGNSSLLDTSSVLVTQEPEIELPREPRPNEECLQILGNAEKGAKFLSDAEIIQLVNAKHIPAYKLETLMETHERGVSIRRQLLSKKLSEPSSLQYLPYRDYNYSLVMGACCENVIGYMPIPVGVAGPLCLDEKEFQVPMATTEGCLVASTNRGCRAIGLGGGASSRVLADGMTRGPVVRLPRACDSAEVKAWLETSEGFAVIKEAFDSTSRFARLQKLHTSIAGRNLYIRFQSRSGDAMGMNMISKGTEKALSKLHEYFPEMQILAVSGNYCTDKKPAAINWIEGRGKSVVCEAVIPAKVVREVLKTTTEAMIEVNINKNLVGSAMAGSIGGYNAHAANIVTAIYIACGQDAAQNVGSSNCITLMEASGPTNEDLYISCTMPSIEIGTVGGGTNLLPQQACLQMLGVQGACKDNPGENARQLARIVCGTVMAGELSLMAALAAGHLVKSHMIHNRSKINLQDLQGACTKKTA T53585 DRUGINFO D0GY5Z Aspirin Approved T53585 DRUGINFO D01QIN Atorvastatin Approved T53585 DRUGINFO D03KIA Cerivastatin Approved T53585 DRUGINFO D04XGU Crestor/TriLipix Approved T53585 DRUGINFO D08GHB Fluvastatin Approved T53585 DRUGINFO D06WTZ Lovastatin Approved T53585 DRUGINFO D0G1WL PITAVASTATIN CALCIUM Approved T53585 DRUGINFO D02RQU Pravastatin Approved T53585 DRUGINFO D0JE2E Rosuvastatin Approved T53585 DRUGINFO D0H0ND Simvastatin Approved T53585 DRUGINFO D07QFP Teriflunomide Approved T53585 DRUGINFO D03VFL TOCOTRIENOL Approved T53585 DRUGINFO D0WL5V LAROPIPRANT Phase 4 T53585 DRUGINFO D0G7IV Premarin/Pravachol Phase 3 T53585 DRUGINFO D0CC8L CRILVASTATIN Phase 2 T53585 DRUGINFO D06BBV XZK-monascus Phase 2 T53585 DRUGINFO D0H0FX NCX-6560 Phase 1 T53585 DRUGINFO D0LJ0M 2-cyclopropyl-4-substituted-phenoxy-quinoline derivative 1 Patented T53585 DRUGINFO D09ZXW Atorvastatin lactole derivative 1 Patented T53585 DRUGINFO D0L3BE Hexahydro naphthalene derivative 1 Patented T53585 DRUGINFO D0M9ZW Hexahydro naphthalene derivative 2 Patented T53585 DRUGINFO D05SOY Hexahydro naphthalene derivative 3 Patented T53585 DRUGINFO D0AY4N Lactol derivative 1 Patented T53585 DRUGINFO D0CM4R Lactol derivative 2 Patented T53585 DRUGINFO D0G8JX Pitavastatin derivative 1 Patented T53585 DRUGINFO D0YX0O PMID27537201-Compound-Figure11 Patented T53585 DRUGINFO D03HKN PMID27537201-Compound-Figure13b Patented T53585 DRUGINFO D0EF9J PMID27537201-Compound-Figure13c Patented T53585 DRUGINFO D00YVL PMID27537201-Compound-Figure15a Patented T53585 DRUGINFO D0SH0L PMID27537201-Compound-Figure15b Patented T53585 DRUGINFO D0S3BE PMID27537201-Compound-Figure17 Patented T53585 DRUGINFO D0RW8J Poly-substituted azoles statin lactone derivative 1 Patented T53585 DRUGINFO D0AP6V Poly-substituted azoles statin lactone derivative 2 Patented T53585 DRUGINFO D0CW2F Poly-substituted miazine derivative 1 Patented T53585 DRUGINFO D0KU2T Pravastatin derivative 1 Patented T53585 DRUGINFO D0U2CK Quinoline derivative 1 Patented T53585 DRUGINFO D0QW7F Quinoline derivative 16 Patented T53585 DRUGINFO D04MFJ Quinoline derivative 17 Patented T53585 DRUGINFO D08FMC Sterol derivative 1 Patented T53585 DRUGINFO D0YZ3U Sterol derivative 2 Patented T53585 DRUGINFO D0O0OD Sterol derivative 3 Patented T53585 DRUGINFO D0Y9XD Dalvastatin Discontinued in Phase 3 T53585 DRUGINFO D0L1LJ Bervastatin Discontinued in Phase 2 T53585 DRUGINFO D04NCJ BMY-21950 Discontinued in Phase 2 T53585 DRUGINFO D0U5NU GLENVASTATIN Discontinued in Phase 2 T53585 DRUGINFO D02GSA RBx10558 Discontinued in Phase 2 T53585 DRUGINFO D0MF7U PF-3052334 Discontinued in Phase 1 T53585 DRUGINFO D0E2CO BMY-22089 Terminated T53585 DRUGINFO D07QSA CP-83101 Terminated T53585 DRUGINFO D0YQ9G GT-16-239 Terminated T53585 DRUGINFO D0J9GD Mevastatin Terminated T53585 DRUGINFO D0Y3OR SQ-33600 Terminated T53585 DRUGINFO D0C7RV SR12813 Terminated T53585 DRUGINFO D0C8HK (E)-5-octadecen-7,9-diynoic acid Investigative T53585 DRUGINFO D0A6FX (E)-octadecan-9-ynoic acid Investigative T53585 DRUGINFO D03GRA (R)-Mevalonate Investigative T53585 DRUGINFO D0NU6K (Z)-5-octadecen-7,9-diynoic acid Investigative T53585 DRUGINFO D0CU3I (Z)-7-octedecan-9-ynoic acid Investigative T53585 DRUGINFO D01GMJ 1,4-Dithiothreitol Investigative T53585 DRUGINFO D0J2FY 2'-Monophosphoadenosine 5'-Diphosphoribose Investigative T53585 DRUGINFO D08SKU 3-(1,3 dodecadiynyl)-6-oxiranebutanoic acid Investigative T53585 DRUGINFO D0IJ7H 3-Hydroxy-3-Methyl-Glutaric Acid Investigative T53585 DRUGINFO D0I0IM 5-ketodihydromevinolin Investigative T53585 DRUGINFO D01YQX 6-hydroxy-7,9-octadecadiynoic acid Investigative T53585 DRUGINFO D0C5LO 7,9-octadecadiynoic acid Investigative T53585 DRUGINFO D09EBV 7,9-tetradecadiynoic acid Investigative T53585 DRUGINFO D09QIA 9-octadecynoic acid Investigative T53585 DRUGINFO D02SRB BPL-001 Investigative T53585 DRUGINFO D0Q2EH Brutieridin Investigative T53585 DRUGINFO D0W3NA Coenzyme A Investigative T53585 DRUGINFO D09CSQ DFGYVAE Investigative T53585 DRUGINFO D0X1VL F(4-Fluoro)VAE Investigative T53585 DRUGINFO D01WQF FPYVAE peptide Investigative T53585 DRUGINFO D03CYY GFPDGG Investigative T53585 DRUGINFO D0C1RY GFPEGG Investigative T53585 DRUGINFO D0S1LA GFPTGG Investigative T53585 DRUGINFO D0X0GV GLPDGG peptide Investigative T53585 DRUGINFO D0B2FM GLPTGG Investigative T53585 DRUGINFO D03ZIK MT-001 Investigative T53585 DRUGINFO D04XQG NCX-1067 Investigative T53585 DRUGINFO D0R6JE Nicotinamide-Adenine-Dinucleotide Investigative T53585 DRUGINFO D03TKT o-hydroxyatorvastatin Investigative T53585 DRUGINFO D0W5FM PMID1527791C29 Investigative T53585 DRUGINFO D07QAX PMID15686906C17 Investigative T53585 DRUGINFO D0Q6WP PMID15686906C29 Investigative T53585 DRUGINFO D06FRE PMID1656041C11dd Investigative T53585 DRUGINFO D0O2FD PMID1656041C11ff Investigative T53585 DRUGINFO D0T4PL PMID1656041C11jj Investigative T53585 DRUGINFO D0M9BZ PMID1656041C11nn Investigative T53585 DRUGINFO D00TIO PMID1656041C4ff Investigative T53585 DRUGINFO D0X0GG PMID1656041C4rr Investigative T53585 DRUGINFO D0R8YV PMID1656041C74 Investigative T53585 DRUGINFO D0O8XW PMID17560788C29f Investigative T53585 DRUGINFO D00RHH PMID17574411C41 Investigative T53585 DRUGINFO D0G6PS PMID17574411C42 Investigative T53585 DRUGINFO D00UOI PMID17574412C33 Investigative T53585 DRUGINFO D0L6HX PMID18072721C50 Investigative T53585 DRUGINFO D0O7AS PMID18155906C16f Investigative T53585 DRUGINFO D02TIT PMID18412317C13b Investigative T53585 DRUGINFO D06HNA PMID1875346C18 Investigative T53585 DRUGINFO D01XMY PMID1895299C1 Investigative T53585 DRUGINFO D02OET PMID1895299C4p Investigative T53585 DRUGINFO D0M4YT PMID1895299C6v Investigative T53585 DRUGINFO D0N7RK PMID19502059C25d Investigative T53585 DRUGINFO D0G2QW PMID1992138C8b Investigative T53585 DRUGINFO D00VMO PMID1992149C13 Investigative T53585 DRUGINFO D02ITS PMID1992149C9 Investigative T53585 DRUGINFO D06BIF PMID2153213C13b Investigative T53585 DRUGINFO D09TKN PMID2153213C13g Investigative T53585 DRUGINFO D0R1FP PMID2153213C1a Investigative T53585 DRUGINFO D03EAN PMID2153213C1e Investigative T53585 DRUGINFO D0RA8F PMID2153213C1f Investigative T53585 DRUGINFO D02MEX PMID2153213C2c Investigative T53585 DRUGINFO D05GWF PMID2153213C2d Investigative T53585 DRUGINFO D0G4ZG PMID2153213C2f Investigative T53585 DRUGINFO D0MU7C PMID2231594C3j Investigative T53585 DRUGINFO D00ZJG PMID2231594C3k Investigative T53585 DRUGINFO D0UQ6A PMID2231594C3q Investigative T53585 DRUGINFO D02EQL PMID2231594C3u Investigative T53585 DRUGINFO D0J9DY PMID2296027C25 Investigative T53585 DRUGINFO D0ZQ3B PMID2296027C29 Investigative T53585 DRUGINFO D0O1OC PMID2296036C2g Investigative T53585 DRUGINFO D05UQC PMID2296036C2t Investigative T53585 DRUGINFO D0I9TR PMID2296036C4d Investigative T53585 DRUGINFO D01ZAL PMID2296036C4i Investigative T53585 DRUGINFO D0J8BD PMID2909732C7 Investigative T53585 DRUGINFO D0K1MB PMID7932551C9 Investigative T53585 DRUGINFO D0S1ER PMID8246233C28 Investigative T53585 DRUGINFO D0NJ5U PMID8246233C35 Investigative T53585 DRUGINFO D00TBG PMID8246233C5ab Investigative T53585 DRUGINFO D07VEB PMID8246234C3h Investigative T53585 DRUGINFO D0FD8Q PMID8246237C18t Investigative T53585 DRUGINFO D05YUT PMID8426367C18 Investigative T53585 DRUGINFO D0Y6DJ rawsonol Investigative T53585 DRUGINFO D0W7VX Statin Investigative T53585 KEGGPATH hsa00900:Terpenoid backbone biosynthesis T53585 KEGGPATH hsa01100:Metabolic pathways T53585 KEGGPATH hsa01130:Biosynthesis of antibiotics T53585 KEGGPATH hsa04152:AMPK signaling pathway T53585 KEGGPATH hsa04976:Bile secretion T53585 WIKIPATH WP197:Cholesterol Biosynthesis T53585 WIKIPATH WP1982:SREBP signalling T53585 WIKIPATH WP1984:Integrated Breast Cancer Pathway T53585 WIKIPATH WP2011:SREBF and miR33 in cholesterol and lipid homeostasis T53585 WIKIPATH WP2706:Activation of Gene Expression by SREBP (SREBF) T53585 WIKIPATH WP2797:Regulation of Lipid Metabolism by Peroxisome proliferator-activated receptor alpha (PPARalpha) T53585 WIKIPATH WP430:Statin Pathway T53585 WHIZPATH PW000050:Steroid Biosynthesis T53585 NET_PATH NetPath_17:IL5 Signaling Pathway T53585 NET_PATH NetPath_23:TSH Signaling Pathway T53585 NET_PATH NetPath_7:TGF_beta_Receptor Signaling Pathway T53585 PANTPATH P00014:Cholesterol biosynthesis T53585 BIOCPATH PWY-5910:Superpathway of geranylgeranyldiphosphate biosynthesis I (via mevalonate) T53585 BIOCPATH PWY66-5:Superpathway of cholesterol biosynthesis T53585 BIOCPATH PWY-922:Mevalonate pathway T14597 TARGETID T14597 T14597 FORMERID TTDS00249 T14597 UNIPROID ERBB2_HUMAN T14597 TARGNAME Erbb2 tyrosine kinase receptor (HER2) T14597 GENENAME ERBB2 T14597 TARGTYPE Successful target T14597 SYNONYMS p185erbB2; Tyrosine kinase-type cell surface receptor HER2; Receptor tyrosine-protein kinase erbB-2; Proto-oncogene c-ErbB-2; Proto-oncogene Neu; NGL; NEU; Metastatic lymph node gene 19 protein; MLN19; MLN 19; HER2; CD340 T14597 FUNCTION Protein tyrosine kinase that is part of several cell surface receptor complexes, but that apparently needs a coreceptor for ligand binding. Essential component of a neuregulin-receptor complex, although neuregulins do not interact with it alone. GP30 is a potential ligand for this receptor. Regulates outgrowth and stabilization of peripheral microtubules (MTs). Upon ERBB2 activation, the MEMO1-RHOA-DIAPH1 signaling pathway elicits the phosphorylation and thus the inhibition of GSK3B at cell membrane. This prevents the phosphorylation of APC and CLASP2, allowing its association with the cell membrane. In turn, membrane-bound APC allows the localization of MACF1 to the cell membrane, which is required for microtubule capture and stabilization. T14597 PDBSTRUC 6OGE; 6J71; 6BGT; 6ATT; 5TQS T14597 BIOCLASS Kinase T14597 ECNUMBER EC 2.7.10.1 T14597 SEQUENCE MELAALCRWGLLLALLPPGAASTQVCTGTDMKLRLPASPETHLDMLRHLYQGCQVVQGNLELTYLPTNASLSFLQDIQEVQGYVLIAHNQVRQVPLQRLRIVRGTQLFEDNYALAVLDNGDPLNNTTPVTGASPGGLRELQLRSLTEILKGGVLIQRNPQLCYQDTILWKDIFHKNNQLALTLIDTNRSRACHPCSPMCKGSRCWGESSEDCQSLTRTVCAGGCARCKGPLPTDCCHEQCAAGCTGPKHSDCLACLHFNHSGICELHCPALVTYNTDTFESMPNPEGRYTFGASCVTACPYNYLSTDVGSCTLVCPLHNQEVTAEDGTQRCEKCSKPCARVCYGLGMEHLREVRAVTSANIQEFAGCKKIFGSLAFLPESFDGDPASNTAPLQPEQLQVFETLEEITGYLYISAWPDSLPDLSVFQNLQVIRGRILHNGAYSLTLQGLGISWLGLRSLRELGSGLALIHHNTHLCFVHTVPWDQLFRNPHQALLHTANRPEDECVGEGLACHQLCARGHCWGPGPTQCVNCSQFLRGQECVEECRVLQGLPREYVNARHCLPCHPECQPQNGSVTCFGPEADQCVACAHYKDPPFCVARCPSGVKPDLSYMPIWKFPDEEGACQPCPINCTHSCVDLDDKGCPAEQRASPLTSIISAVVGILLVVVLGVVFGILIKRRQQKIRKYTMRRLLQETELVEPLTPSGAMPNQAQMRILKETELRKVKVLGSGAFGTVYKGIWIPDGENVKIPVAIKVLRENTSPKANKEILDEAYVMAGVGSPYVSRLLGICLTSTVQLVTQLMPYGCLLDHVRENRGRLGSQDLLNWCMQIAKGMSYLEDVRLVHRDLAARNVLVKSPNHVKITDFGLARLLDIDETEYHADGGKVPIKWMALESILRRRFTHQSDVWSYGVTVWELMTFGAKPYDGIPAREIPDLLEKGERLPQPPICTIDVYMIMVKCWMIDSECRPRFRELVSEFSRMARDPQRFVVIQNEDLGPASPLDSTFYRSLLEDDDMGDLVDAEEYLVPQQGFFCPDPAPGAGGMVHHRHRSSSTRSGGGDLTLGLEPSEEEAPRSPLAPSEGAGSDVFDGDLGMGAAKGLQSLPTHDPSPLQRYSEDPTVPLPSETDGYVAPLTCSPQPEYVNQPDVRPQPPSPREGPLPAARPAGATLERPKTLSPGKNGVVKDVFAFGGAVENPEYLTPQGGAAPQPHPPPAFSPAFDNLYYWDQDPPERGAPPSTFKGTPTAENPEYLGLDVPV T14597 DRUGINFO D05UFG BIBW 2992 Approved T14597 DRUGINFO D06XXH Dacomitinib Approved T14597 DRUGINFO D08CDI Lapatinib Approved T14597 DRUGINFO D01YYP Margetuximab Approved T14597 DRUGINFO D0U3YB Masoprocol Approved T14597 DRUGINFO D0F0ZE Merimepodib Approved T14597 DRUGINFO D0U1ZV NERATINIB MALEATE Approved T14597 DRUGINFO D0CI4E Pertuzumab Approved T14597 DRUGINFO D04WFL Trastuzumab Approved T14597 DRUGINFO D09GRX Tucatinib Approved T14597 DRUGINFO D04SLF Bevacizumab + Trastuzumab Phase 3 T14597 DRUGINFO D0Q9CY HKI-272 Phase 3 T14597 DRUGINFO D0F8UV Nelipepimut S Phase 3 T14597 DRUGINFO D04VRB NeuVax Phase 3 T14597 DRUGINFO D0HR7Z PF-05280014 Phase 3 T14597 DRUGINFO D0J6PY Taxol/Paraplatin/Herceptin Phase 3 T14597 DRUGINFO D0P4TH Trastuzumab-DM1 Phase 3 T14597 DRUGINFO D00NYJ Varlitinib Phase 2/3 T14597 DRUGINFO D0P7KI Anti-CD3 and anti-Her2/neu bispecific antibody-armed activated T cells Phase 2 T14597 DRUGINFO D0BM7M AZD8931 Phase 2 T14597 DRUGINFO D0U4FF BMS-599626 Phase 2 T14597 DRUGINFO D0YB3W CI-1033 Phase 2 T14597 DRUGINFO D0CN9Q CP-724714 Phase 2 T14597 DRUGINFO D06KOM DN24-02 Phase 2 T14597 DRUGINFO D0O2JI Ertumaxomab Phase 2 T14597 DRUGINFO D09XHU HER-2 Protein AutoVac Phase 2 T14597 DRUGINFO D0QF7Z HER2/neu peptide vaccine Phase 2 T14597 DRUGINFO D0B1TL Her2-targeted autologous T-cell therapy Phase 2 T14597 DRUGINFO D00YER HM-78136B Phase 2 T14597 DRUGINFO DV2N5P KN026 Phase 2 T14597 DRUGINFO D0P1DI MCLA-128 Phase 2 T14597 DRUGINFO D0G5GB MGAH22 Phase 2 T14597 DRUGINFO D0Q2KM MM-111 Phase 2 T14597 DRUGINFO DM7WY2 MRG002 Phase 2 T14597 DRUGINFO D03UKJ Pazopanib + Tyverb/Tykerb Phase 2 T14597 DRUGINFO DUW81M Tarloxotinib Phase 2 T14597 DRUGINFO DD94ZN A166 Phase 1/2 T14597 DRUGINFO D08KCJ ABY-025 Phase 1/2 T14597 DRUGINFO D0G4AJ AGN-208397 Phase 1/2 T14597 DRUGINFO D08QZH Anti-HER2 CAR-T Phase 1/2 T14597 DRUGINFO D03TQB AU105 Phase 1/2 T14597 DRUGINFO D0F3MT AVX901 Phase 1/2 T14597 DRUGINFO D9FJ5V BDTX-189 Phase 1/2 T14597 DRUGINFO D0NN7P CART-HER-2 Phase 1/2 T14597 DRUGINFO D06KQG HER-2-targeting CAR T Cells Phase 1/2 T14597 DRUGINFO DNC79U ISB 1302 Phase 1/2 T14597 DRUGINFO D0FF2G Sym013 Phase 1/2 T14597 DRUGINFO DY13WU TAS-0728 Phase 1/2 T14597 DRUGINFO D6SL3N Zenocutuzomab Phase 1/2 T14597 DRUGINFO D0V4XY S-222611 Phase 1b T14597 DRUGINFO DEI07S AIP-303 Phase 1 T14597 DRUGINFO D0M8AI ARRY-380 Phase 1 T14597 DRUGINFO D6IOB5 BAY 2701439 Phase 1 T14597 DRUGINFO D06XWD CAR-T Cells targeting HER2 Phase 1 T14597 DRUGINFO D0JI4M CAR-T cells targeting HER2 Phase 1 T14597 DRUGINFO D08JAN Cipatinib Phase 1 T14597 DRUGINFO D0Z4RC CUDC-101 Phase 1 T14597 DRUGINFO D1C0WB DZD1516 Phase 1 T14597 DRUGINFO D0DBS7 GBR1302 Phase 1 T14597 DRUGINFO DSOE74 GQ1001 Phase 1 T14597 DRUGINFO D0TN5W HER2-CAR T Cells Phase 1 T14597 DRUGINFO D0U2PS HER2p63-71 peptide vaccine Phase 1 T14597 DRUGINFO D0YF6K HER2-specific CAR T cell Phase 1 T14597 DRUGINFO D06RCE HER2-specific T cells Phase 1 T14597 DRUGINFO D0U3XL JNJ-26483327 Phase 1 T14597 DRUGINFO D3FYE1 M802 Phase 1 T14597 DRUGINFO DU54BA MB-103 Phase 1 T14597 DRUGINFO DQ04FJ MBS301 Phase 1 T14597 DRUGINFO D08UDG MEDI4276 Phase 1 T14597 DRUGINFO D07USV MM-302 Phase 1 T14597 DRUGINFO DS60CK MT-5111 Phase 1 T14597 DRUGINFO D05ATQ MVA HER-2 AutoVac Phase 1 T14597 DRUGINFO DEX8D5 NJH395 Phase 1 T14597 DRUGINFO D0UL7L Recombinant human Erbb3 fragment therapeutic tumor vaccine Phase 1 T14597 DRUGINFO DUA7P2 SBT6050 Phase 1 T14597 DRUGINFO D02UFQ TAK-285 Phase 1 T14597 DRUGINFO D0O9HF TrasGEX Phase 1 T14597 DRUGINFO D0H7ZN VM-206 Phase 1 T14597 DRUGINFO D09UGG Zemab Phase 1 T14597 DRUGINFO DH09QZ ZW49 Phase 1 T14597 DRUGINFO D05YLO Her-2-Bi-armed ATC Discontinued in Phase 2 T14597 DRUGINFO D0A9OV TAK165 Discontinued in Phase 1 T14597 DRUGINFO DO6UE8 227Th-labelled HER2-TTC Preclinical T14597 DRUGINFO D02YAQ GW-974 Terminated T14597 DRUGINFO D0NX2G (1-Benzyl-1H-indazol-5-yl)-quinazolin-4-yl-amine Investigative T14597 DRUGINFO D02ARA (1-Benzyl-1H-indol-5-yl)-quinazolin-4-yl-amine Investigative T14597 DRUGINFO D0J2CP PF 5208766 Investigative T14597 DRUGINFO D0B1SW Redoxal Investigative T14597 DRUGINFO D0O5CR TA1-RTA Investigative T14597 KEGGPATH hsa04012:ErbB signaling pathway T14597 KEGGPATH hsa04020:Calcium signaling pathway T14597 KEGGPATH hsa04066:HIF-1 signaling pathway T14597 KEGGPATH hsa04510:Focal adhesion T14597 KEGGPATH hsa04520:Adherens junction T14597 KEGGPATH hsa05200:Pathways in cancer T14597 KEGGPATH hsa05205:Proteoglycans in cancer T14597 KEGGPATH hsa05206:MicroRNAs in cancer T14597 KEGGPATH hsa05212:Pancreatic cancer T14597 KEGGPATH hsa05213:Endometrial cancer T14597 KEGGPATH hsa05215:Prostate cancer T14597 KEGGPATH hsa05219:Bladder cancer T14597 KEGGPATH hsa05223:Non-small cell lung cancer T14597 KEGGPATH hsa05230:Central carbon metabolism in cancer T14597 WIKIPATH WP1907:Semaphorin interactions T14597 WIKIPATH WP2005:miR-targeted genes in muscle cell - TarBase T14597 WIKIPATH WP2034:Leptin signaling pathway T14597 WIKIPATH WP2261:Signaling Pathways in Glioblastoma T14597 WIKIPATH WP2377:Integrated Pancreatic Cancer Pathway T14597 WIKIPATH WP2780:Signaling by ERBB2 T14597 WIKIPATH WP2828:Bladder Cancer T14597 WIKIPATH WP2870:Extracellular vesicle-mediated signaling in recipient cells T14597 WIKIPATH WP306:Focal Adhesion T14597 WIKIPATH WP437:EGF/EGFR Signaling Pathway T14597 WIKIPATH WP673:ErbB Signaling Pathway T14597 WIKIPATH WP710:DNA Damage Response (only ATM dependent) T14597 WHIZPATH PW000168:Phosphatidylinositol Phosphate Metabolism T14597 REACPATH R-HSA-1250196:SHC1 events in ERBB2 signaling T14597 REACPATH R-HSA-1251932:PLCG1 events in ERBB2 signaling T14597 REACPATH R-HSA-1257604:PIP3 activates AKT signaling T14597 REACPATH R-HSA-1963640:GRB2 events in ERBB2 signaling T14597 REACPATH R-HSA-1963642:PI3K events in ERBB2 signaling T14597 REACPATH R-HSA-2219530:Constitutive Signaling by Aberrant PI3K in Cancer T14597 REACPATH R-HSA-416572:Sema4D induced cell migration and growth-cone collapse T14597 REACPATH R-HSA-5673001:RAF/MAP kinase cascade T14597 NET_PATH NetPath_11:TCR Signaling Pathway T14597 INTEPATH a6b1_a6b4_integrin_pathway:a6b1 and a6b4 Integrin signaling T14597 INTEPATH erbb_network_pathway:ErbB receptor signaling network T14597 INTEPATH erbb2erbb3pathway:ErbB2/ErbB3 signaling events T14597 INTEPATH erbb4_pathway:ErbB4 signaling events T14597 INTEPATH myc_represspathway:Validated targets of C-MYC transcriptional repression T14597 PANTPATH P00012:Cadherin signaling pathway T14597 PANTPATH P00018:EGF receptor signaling pathway T07173 TARGETID T07173 T07173 FORMERID TTDC00318 T07173 UNIPROID NTRK1_HUMAN T07173 TARGNAME Tropomyosin-related kinase A (TrkA) T07173 GENENAME NTRK1 T07173 TARGTYPE Successful target T07173 SYNONYMS gp140trk; Tyrosine kinase receptor A; Tyrosine kinase receptor; Trk-A; TRKA; TRK1-transforming tyrosine kinase protein; TRK1 transforming tyrosinekinase protein; TRK; P140-TrkA; Neurotrophic tyrosine kinase receptor type 1; NGF-trk receptor type A; MTC; High affinity nerve growth factor receptor T07173 FUNCTION High affinity receptor for NGF which is its primary ligand. Can also bind and be activated by NTF3/neurotrophin-3. However, NTF3 only supports axonal extension through NTRK1 but has no effect on neuron survival. Upon dimeric NGF ligand-binding, undergoes homodimerization, autophosphorylation and activation. Recruits, phosphorylates and/or activates several downstream effectors including SHC1, FRS2, SH2B1, SH2B2 and PLCG1 that regulate distinct overlapping signaling cascades driving cell survival and differentiation. Through SHC1 and FRS2 activates a GRB2-Ras-MAPK cascade that regulates cell differentiation and survival. Through PLCG1 controls NF-Kappa-B activation and the transcription of genes involved in cell survival. Through SHC1 and SH2B1 controls a Ras-PI3 kinase-AKT1 signaling cascade that is also regulating survival. In absence of ligand and activation, may promote cell death, making the survival of neurons dependent on trophic factors. Receptor tyrosine kinase involved in the development and the maturation of the central and peripheral nervous systems through regulation of proliferation, differentiation and survival of sympathetic and nervous neurons. T07173 PDBSTRUC 6NSS; 6NSP; 6NPT; 6DKW; 6DKI T07173 BIOCLASS Kinase T07173 ECNUMBER EC 2.7.10.1 T07173 SEQUENCE MLRGGRRGQLGWHSWAAGPGSLLAWLILASAGAAPCPDACCPHGSSGLRCTRDGALDSLHHLPGAENLTELYIENQQHLQHLELRDLRGLGELRNLTIVKSGLRFVAPDAFHFTPRLSRLNLSFNALESLSWKTVQGLSLQELVLSGNPLHCSCALRWLQRWEEEGLGGVPEQKLQCHGQGPLAHMPNASCGVPTLKVQVPNASVDVGDDVLLRCQVEGRGLEQAGWILTELEQSATVMKSGGLPSLGLTLANVTSDLNRKNVTCWAENDVGRAEVSVQVNVSFPASVQLHTAVEMHHWCIPFSVDGQPAPSLRWLFNGSVLNETSFIFTEFLEPAANETVRHGCLRLNQPTHVNNGNYTLLAANPFGQASASIMAAFMDNPFEFNPEDPIPVSFSPVDTNSTSGDPVEKKDETPFGVSVAVGLAVFACLFLSTLLLVLNKCGRRNKFGINRPAVLAPEDGLAMSLHFMTLGGSSLSPTEGKGSGLQGHIIENPQYFSDACVHHIKRRDIVLKWELGEGAFGKVFLAECHNLLPEQDKMLVAVKALKEASESARQDFQREAELLTMLQHQHIVRFFGVCTEGRPLLMVFEYMRHGDLNRFLRSHGPDAKLLAGGEDVAPGPLGLGQLLAVASQVAAGMVYLAGLHFVHRDLATRNCLVGQGLVVKIGDFGMSRDIYSTDYYRVGGRTMLPIRWMPPESILYRKFTTESDVWSFGVVLWEIFTYGKQPWYQLSNTEAIDCITQGRELERPRACPPEVYAIMRGCWQREPQQRHSIKDVHARLQALAQAPPVYLDVLG T07173 DRUGINFO D0O0LS Entrectinib Approved T07173 DRUGINFO D07TOK Larotrectinib Approved T07173 DRUGINFO D0C2OR MIM-D3 Phase 3 T07173 DRUGINFO D0B7OY CT 327 Phase 2 T07173 DRUGINFO D04QYS SNA-120 Phase 2 T07173 DRUGINFO D0QP8X ONO-7579 Phase 1/2 T07173 DRUGINFO D05NFR TPX-0005 Phase 1/2 T07173 DRUGINFO D0FA6S Altiratinib Phase 1 T07173 DRUGINFO D0N0DU DS-6051 Phase 1 T07173 DRUGINFO D03UDF LOXO-195 Phase 1 T07173 DRUGINFO D07PSL PLX7486 Phase 1 T07173 DRUGINFO D1ZD0N VMD-928 Phase 1 T07173 DRUGINFO D0AU4G 3-amino-5-benzyl-substituted indazole derivative 1 Patented T07173 DRUGINFO D0Y1NH Azaindazole amide derivative 1 Patented T07173 DRUGINFO D0T3TZ Benzimidazole derivative 6 Patented T07173 DRUGINFO D0HF1A Bicyclic heteroaryl benzamide derivative 1 Patented T07173 DRUGINFO D0F8BF Bicyclic heteroaryl benzamide derivative 2 Patented T07173 DRUGINFO D0O0GZ Bicyclic heteroaryl benzamide derivative 3 Patented T07173 DRUGINFO D0I9FU Bicyclic heteroaryl benzamide derivative 4 Patented T07173 DRUGINFO D0KC8X Bicyclic heteroaryl benzamide derivative 5 Patented T07173 DRUGINFO D07CPL Bicyclic heteroaryl benzamide derivative 6 Patented T07173 DRUGINFO D0N6NG Bicyclic heteroaryl benzamide derivative 7 Patented T07173 DRUGINFO D0DY5R Bicyclic heteroaryl benzamide derivative 8 Patented T07173 DRUGINFO D07AJO Bicyclic heteroaryl benzamide derivative 9 Patented T07173 DRUGINFO D0T4CF Five membered heterocyclic benzamide derivative 1 Patented T07173 DRUGINFO D04BRW Five membered heterocyclic benzamide derivative 2 Patented T07173 DRUGINFO D0CY3U Five membered heterocyclic benzamide derivative 3 Patented T07173 DRUGINFO D0WI7N Imidazo pyridine derivative 1 Patented T07173 DRUGINFO D0T8XD Imidazo[1,2-b]pyridazine derivative 1 Patented T07173 DRUGINFO D0M8UO Imidazo[1,2-b]pyridazine derivative 2 Patented T07173 DRUGINFO D0N1CF Imidazo[1,2-b]pyridazine derivative 3 Patented T07173 DRUGINFO D0FS4S Imidazo[1,2-b]pyridazine derivative 4 Patented T07173 DRUGINFO D0DO4I Imidazo[1,2-b]pyridazine derivative 5 Patented T07173 DRUGINFO D0W0UF Imidazo[1,2-b]pyridazine derivative 6 Patented T07173 DRUGINFO D04QHI Imidazo[1,2-b]pyridazine derivative 7 Patented T07173 DRUGINFO D0C3RK N-(phenylpyrazolyl)benzamide derivative 1 Patented T07173 DRUGINFO D0BP9B N,N-bis(5-pyrazoyl)urea derivative 1 Patented T07173 DRUGINFO D00XXZ N-acylpiperidine ether derivative 1 Patented T07173 DRUGINFO D04RXX N-acylpiperidine ether derivative 2 Patented T07173 DRUGINFO D0X1LP N-acylpiperidine ether derivative 3 Patented T07173 DRUGINFO D00FJH N-acylpiperidine ether derivative 4 Patented T07173 DRUGINFO D03BAY N-acylpiperidine ether derivative 5 Patented T07173 DRUGINFO D04GCC N-acylpiperidine ether derivative 6 Patented T07173 DRUGINFO D02OLJ N-acylpiperidine ether derivative 7 Patented T07173 DRUGINFO D0X4LA N-acylpyrrolidine ether derivative 1 Patented T07173 DRUGINFO D08BIH N-acylpyrrolidine ether derivative 2 Patented T07173 DRUGINFO D0I5DM N-arylmethyl-N-phenyl cyclic urea derivative 1 Patented T07173 DRUGINFO D02QWP N-arylmethyl-N-phenyl cyclic urea derivative 2 Patented T07173 DRUGINFO D05NBR PMID28270010-Compound-Figure16-a Patented T07173 DRUGINFO D0W9RH PMID28270010-Compound-Figure16-b-1 Patented T07173 DRUGINFO D0YM2S PMID28270010-Compound-Figure16-b-2 Patented T07173 DRUGINFO D0P3VK PMID28270010-Compound-Figure17-1 Patented T07173 DRUGINFO D0T5OF PMID28270010-Compound-Figure17-2 Patented T07173 DRUGINFO D0D7EG PMID28270010-Compound-Figure17-3 Patented T07173 DRUGINFO D0X9VS PMID28270010-Compound-Figure24-a Patented T07173 DRUGINFO D07RLB PMID28270010-Compound-Figure24-b Patented T07173 DRUGINFO D0J9ZG PMID28270010-Compound-Figure5-1 Patented T07173 DRUGINFO D0T2OX PMID28270010-Compound-Figure5-2 Patented T07173 DRUGINFO D0V5AG PMID28270010-Compound-Figure5-3 Patented T07173 DRUGINFO D0J4CA PMID28270021-Compound-WO2010077680 103 Patented T07173 DRUGINFO D0T0HM PMID28270021-Compound-WO2010077680 109 Patented T07173 DRUGINFO D0PY0G PMID28270021-Compound-WO2010077680 201 Patented T07173 DRUGINFO D0FL8A PMID28270021-Compound-WO2010077680 481 Patented T07173 DRUGINFO D0K6IM PMID28270021-Compound-WO2010077680 495 Patented T07173 DRUGINFO D0F2BF PMID28270021-Compound-WO2010077680 803 Patented T07173 DRUGINFO D07KVL PMID28270021-Compound-WO2010077680 811 Patented T07173 DRUGINFO D02ZQN PMID28270021-Compound-WO2013009582Example16 Patented T07173 DRUGINFO D0Y0XJ PMID28270021-Compound-WO2013009582Example76 Patented T07173 DRUGINFO D0I2OO PMID28270021-Compound-WO2013161919Example85-117 Patented T07173 DRUGINFO D05AQT PMID28270021-Compound-WO2014078408Example1 Patented T07173 DRUGINFO D0YN0I PMID28270021-Compound-WO2014078408Example26 Patented T07173 DRUGINFO D0QT8L PMID28270021-Compound-WO2014129431Example8-1 Patented T07173 DRUGINFO D02ETU PMID28270021-Compound-WO2014152663 701 Patented T07173 DRUGINFO D0U5XI PMID28270021-Compound-WO2015042088Example11 Patented T07173 DRUGINFO D0VD5J PMID28270021-Compound-WO2015042088Example12 Patented T07173 DRUGINFO D0M8VS PMID28270021-Compound-WO2015042088Example4 Patented T07173 DRUGINFO D00MGO PMID28270021-Compound-WO2016054807Example1 Patented T07173 DRUGINFO D0LK8E PMID28270021-Compound-WO2016054807Example112 Patented T07173 DRUGINFO D08CZY PMID28270021-Compound-WO2016054807Example71 Patented T07173 DRUGINFO D0BO1H PMID28270021-Compound-WO2016054807Example80 Patented T07173 DRUGINFO D00EUL PMID28270021-Compound-WO2016054807Example82 Patented T07173 DRUGINFO D0DN3Q Pyrazolo[1,5-a]pyridine derivative 1 Patented T07173 DRUGINFO D0V9ZJ Pyrazolo[1,5-a]pyridine derivative 2 Patented T07173 DRUGINFO D0H8XH Pyrazolo[1,5-a]pyrimidine derivative 14 Patented T07173 DRUGINFO D0BI5I Pyrazolo[1,5-a]pyrimidine derivative 15 Patented T07173 DRUGINFO D0BZ0T Pyrazolo[1,5-a]pyrimidine derivative 16 Patented T07173 DRUGINFO D00DIZ Pyrazolo[1,5-a]pyrimidine derivative 17 Patented T07173 DRUGINFO D05RKT Pyrazolo[1,5-a]pyrimidine derivative 18 Patented T07173 DRUGINFO D05KHT Pyrazolo[1,5-a]pyrimidine derivative 19 Patented T07173 DRUGINFO D0Z5PA Pyrazolo[1,5-a]pyrimidine derivative 20 Patented T07173 DRUGINFO D0D6UF Pyrazolo[1,5-a]pyrimidine derivative 21 Patented T07173 DRUGINFO D0U2GJ Pyrazolo[1,5-a]pyrimidine derivative 22 Patented T07173 DRUGINFO D06NPZ Pyrazolo[1,5-a]pyrimidine derivative 23 Patented T07173 DRUGINFO D04KQB Pyrazolo[1,5-a]pyrimidine derivative 24 Patented T07173 DRUGINFO D03USW Pyrazolo[1,5-a]pyrimidine derivative 25 Patented T07173 DRUGINFO D09SYD Pyrazolo[1,5-a]pyrimidine derivative 26 Patented T07173 DRUGINFO D08IWT Pyrazolo[1,5-a]pyrimidine derivative 27 Patented T07173 DRUGINFO D0RK6W Pyrazolo[4,3-c]pyridine derivative 1 Patented T07173 DRUGINFO D0O8SX Pyrazolo[4,3-h]quinazoline-3-carboxamide derivative 1 Patented T07173 DRUGINFO D0RR8O Pyrido[3,2-d]pyrimidine derivative 2 Patented T07173 DRUGINFO D0U3RD Pyrido[3,2-d]pyrimidine derivative 3 Patented T07173 DRUGINFO D0I8AY Pyrrolidinyl urea derivative 10 Patented T07173 DRUGINFO D00ICS Pyrrolidinyl urea derivative 11 Patented T07173 DRUGINFO D0K2GH Pyrrolidinyl urea derivative 12 Patented T07173 DRUGINFO D0Z6LB Pyrrolidinyl urea derivative 13 Patented T07173 DRUGINFO D0JJ0T Pyrrolidinyl urea derivative 2 Patented T07173 DRUGINFO D0LB7Z Pyrrolidinyl urea derivative 3 Patented T07173 DRUGINFO D0K3QT Pyrrolidinyl urea derivative 4 Patented T07173 DRUGINFO D0ME5D Pyrrolidinyl urea derivative 5 Patented T07173 DRUGINFO D0J5OO Pyrrolidinyl urea derivative 6 Patented T07173 DRUGINFO D0X0YJ Pyrrolidinyl urea derivative 7 Patented T07173 DRUGINFO D0A4YR Pyrrolidinyl urea derivative 8 Patented T07173 DRUGINFO D06YON Pyrrolidinyl urea derivative 9 Patented T07173 DRUGINFO D0P8SR Pyrrolo[2,3-b]pyridine derivative 1 Patented T07173 DRUGINFO D06GOT Pyrrolo[2,3-b]pyridine derivative 2 Patented T07173 DRUGINFO D02IBX Pyrrolo[2,3-b]pyridine derivative 3 Patented T07173 DRUGINFO D0S0II Pyrrolo[2,3-d]pyrimidine derivative 3 Patented T07173 DRUGINFO D0AG2A Pyrrolo[2,3-d]pyrimidine derivative 4 Patented T07173 DRUGINFO D0DQ5G Pyrrolo[3,2-c]pyridine derivative 1 Patented T07173 DRUGINFO D0ZE6H Six-membered heterocyclic benzamide derivative 1 Patented T07173 DRUGINFO D0H3ZG Six-membered heterocyclic benzamide derivative 2 Patented T07173 DRUGINFO D07VFQ Six-membered heterocyclic benzamide derivative 3 Patented T07173 DRUGINFO D0EC4Z Six-membered heterocyclic benzamide derivative 4 Patented T07173 DRUGINFO D0UN4M Six-membered heterocyclic benzamide derivative 5 Patented T07173 DRUGINFO D04JCD Six-membered heterocyclic benzamide derivative 6 Patented T07173 DRUGINFO D05MRY Six-membered heterocyclic benzamide derivative 7 Patented T07173 DRUGINFO D06STX Thiadiazolyl carboxamide derivative 1 Patented T07173 DRUGINFO D0JU4R Thiazole derivative 4 Patented T07173 DRUGINFO D0MZ7K Triazolo[4,3-b]pyridazine derivative 2 Patented T07173 DRUGINFO D0UQ2G Tri-substituted urea derivative 1 Patented T07173 DRUGINFO D0CG8N Tri-substituted urea derivative 2 Patented T07173 DRUGINFO D08SDJ Ureido-phenyl-substituted triazine derivative 1 Patented T07173 DRUGINFO D0V7QU Ureido-phenyl-substituted triazine derivative 2 Patented T07173 DRUGINFO D0LX8D AZD6918 Discontinued in Phase 1 T07173 DRUGINFO D07SYN FX-007 Preclinical T07173 DRUGINFO D09QBA CEP-5104 Investigative T07173 DRUGINFO D07IHM CEP-6331 Investigative T07173 DRUGINFO D0Z5TQ GW-5074 Investigative T07173 DRUGINFO D02RWK K-252a analogue Investigative T07173 KEGGPATH hsa04010:MAPK signaling pathway T07173 KEGGPATH hsa04144:Endocytosis T07173 KEGGPATH hsa04210:Apoptosis T07173 KEGGPATH hsa04722:Neurotrophin signaling pathway T07173 KEGGPATH hsa04750:Inflammatory mediator regulation of TRP channels T07173 KEGGPATH hsa05200:Pathways in cancer T07173 KEGGPATH hsa05202:Transcriptional misregulation in cancer T07173 KEGGPATH hsa05216:Thyroid cancer T07173 KEGGPATH hsa05230:Central carbon metabolism in cancer T07173 WIKIPATH WP1873:NGF signalling via TRKA from the plasma membrane T07173 WIKIPATH WP2377:Integrated Pancreatic Cancer Pathway T07173 WIKIPATH WP2380:BDNF signaling pathway T07173 WIKIPATH WP382:MAPK Signaling Pathway T07173 REACPATH R-HSA-170968:Frs2-mediated activation T07173 REACPATH R-HSA-170984:ARMS-mediated activation T07173 REACPATH R-HSA-187024:NGF-independant TRKA activation T07173 REACPATH R-HSA-198203:PI3K/AKT activation T07173 NET_PATH NetPath_14:IL2 Signaling Pathway T07173 INTEPATH trkrpathway:Neurotrophic factor-mediated Trk receptor signaling T85435 TARGETID T85435 T85435 FORMERID TTDS00292 T85435 UNIPROID INSR_HUMAN T85435 TARGNAME Insulin receptor (INSR) T85435 GENENAME INSR T85435 TARGTYPE Successful target T85435 SYNONYMS IR; CD220 antigen; CD220 T85435 FUNCTION Binding of insulin leads to phosphorylation of several intracellular substrates, including, insulin receptor substrates (IRS1, 2, 3, 4), SHC, GAB1, CBL and other signaling intermediates. Each of these phosphorylated proteins serve as docking proteins for other signaling proteins that contain Src-homology-2 domains (SH2 domain) that specifically recognize different phosphotyrosine residues, including the p85 regulatory subunit of PI3K and SHP2. Phosphorylation of IRSs proteins lead to the activation of two main signaling pathways: the PI3K-AKT/PKB pathway, which is responsible for most of the metabolic actions of insulin, and the Ras-MAPK pathway, which regulates expression of some genes and cooperates with the PI3K pathway to control cell growth and differentiation. Binding of the SH2 domains of PI3K to phosphotyrosines on IRS1 leads to the activation of PI3K and the generation of phosphatidylinositol-(3, 4, 5)-triphosphate (PIP3), a lipid second messenger, which activates several PIP3-dependent serine/threonine kinases, such as PDPK1 and subsequently AKT/PKB. The net effect of this pathway is to produce a translocation of the glucose transporter SLC2A4/GLUT4 from cytoplasmic vesicles to the cell membrane to facilitate glucose transport. Moreover, upon insulin stimulation, activated AKT/PKB is responsible for: anti-apoptotic effect of insulin by inducing phosphorylation of BAD; regulates the expression of gluconeogenic and lipogenic enzymes by controlling the activity of the winged helix or forkhead (FOX) class of transcription factors. Another pathway regulated by PI3K-AKT/PKB activation is mTORC1 signaling pathway which regulates cell growth and metabolism and integrates signals from insulin. AKT mediates insulin-stimulated protein synthesis by phosphorylating TSC2 thereby activating mTORC1 pathway. The Ras/RAF/MAP2K/MAPK pathway is mainly involved in mediating cell growth, survival and cellular differentiation of insulin. Phosphorylated IRS1 recruits GRB2/SOS complex, which triggers the activation of the Ras/RAF/MAP2K/MAPK pathway. In addition to binding insulin, the insulin receptor can bind insulin-like growth factors (IGFI and IGFII). Isoform Short has a higher affinity for IGFII binding. When present in a hybrid receptor with IGF1R, binds IGF1. shows that hybrid receptors composed of IGF1R and INSR isoform Long are activated with a high affinity by IGF1, with low affinity by IGF2 and not significantly activated by insulin, and that hybrid receptors composed of IGF1R and INSR isoform Short are activated by IGF1, IGF2 and insulin. In contrast, shows that hybrid receptors composed of IGF1R and INSR isoform Long and hybrid receptors composed of IGF1R and INSR isoform Short have similar binding characteristics, both bind IGF1 and have a low affinity for insulin. Receptor tyrosine kinase which mediates the pleiotropic actions of insulin. T85435 PDBSTRUC 6HN5; 6HN4; 5U1M; 5KQV; 5J3H T85435 BIOCLASS Kinase T85435 ECNUMBER EC 2.7.10.1 T85435 SEQUENCE MATGGRRGAAAAPLLVAVAALLLGAAGHLYPGEVCPGMDIRNNLTRLHELENCSVIEGHLQILLMFKTRPEDFRDLSFPKLIMITDYLLLFRVYGLESLKDLFPNLTVIRGSRLFFNYALVIFEMVHLKELGLYNLMNITRGSVRIEKNNELCYLATIDWSRILDSVEDNYIVLNKDDNEECGDICPGTAKGKTNCPATVINGQFVERCWTHSHCQKVCPTICKSHGCTAEGLCCHSECLGNCSQPDDPTKCVACRNFYLDGRCVETCPPPYYHFQDWRCVNFSFCQDLHHKCKNSRRQGCHQYVIHNNKCIPECPSGYTMNSSNLLCTPCLGPCPKVCHLLEGEKTIDSVTSAQELRGCTVINGSLIINIRGGNNLAAELEANLGLIEEISGYLKIRRSYALVSLSFFRKLRLIRGETLEIGNYSFYALDNQNLRQLWDWSKHNLTITQGKLFFHYNPKLCLSEIHKMEEVSGTKGRQERNDIALKTNGDQASCENELLKFSYIRTSFDKILLRWEPYWPPDFRDLLGFMLFYKEAPYQNVTEFDGQDACGSNSWTVVDIDPPLRSNDPKSQNHPGWLMRGLKPWTQYAIFVKTLVTFSDERRTYGAKSDIIYVQTDATNPSVPLDPISVSNSSSQIILKWKPPSDPNGNITHYLVFWERQAEDSELFELDYCLKGLKLPSRTWSPPFESEDSQKHNQSEYEDSAGECCSCPKTDSQILKELEESSFRKTFEDYLHNVVFVPRKTSSGTGAEDPRPSRKRRSLGDVGNVTVAVPTVAAFPNTSSTSVPTSPEEHRPFEKVVNKESLVISGLRHFTGYRIELQACNQDTPEERCSVAAYVSARTMPEAKADDIVGPVTHEIFENNVVHLMWQEPKEPNGLIVLYEVSYRRYGDEELHLCVSRKHFALERGCRLRGLSPGNYSVRIRATSLAGNGSWTEPTYFYVTDYLDVPSNIAKIIIGPLIFVFLFSVVIGSIYLFLRKRQPDGPLGPLYASSNPEYLSASDVFPCSVYVPDEWEVSREKITLLRELGQGSFGMVYEGNARDIIKGEAETRVAVKTVNESASLRERIEFLNEASVMKGFTCHHVVRLLGVVSKGQPTLVVMELMAHGDLKSYLRSLRPEAENNPGRPPPTLQEMIQMAAEIADGMAYLNAKKFVHRDLAARNCMVAHDFTVKIGDFGMTRDIYETDYYRKGGKGLLPVRWMAPESLKDGVFTTSSDMWSFGVVLWEITSLAEQPYQGLSNEQVLKFVMDGGYLDQPDNCPERVTDLMRMCWQFNPKMRPTFLEIVNLLKDDLHPSFPEVSFFHSEENKAPESEELEMEFEDMENVPLDRSSHCQREEAGGRDGGSSLGFKRSYEEHIPYTHMNGGKKNGRILTLPRSNPS T85435 DRUGINFO D02EHV Human neutral insulin Approved T85435 DRUGINFO D03VXG Insulin Lyspro recombinant Approved T85435 DRUGINFO D06SVW Insulin recombinant Approved T85435 DRUGINFO D05ELO Insulin, porcine Approved T85435 DRUGINFO D0M2XE Insulin-glulisine Approved T85435 DRUGINFO D0L6JE Insulin-lispro Approved T85435 DRUGINFO D07MEH Meglitinides Approved T85435 DRUGINFO D09PPG Metformin arginine-hemisuccinimide Approved T85435 DRUGINFO D0Y3VQ Ryzodeq Approved T85435 DRUGINFO D0U8YK NN5401 Phase 3 T85435 DRUGINFO D0U3LK Metformin glycinate Phase 2/3 T85435 DRUGINFO D0T5YX DM-71 Phase 2 T85435 DRUGINFO D06MOY DM-99 Phase 2 T85435 DRUGINFO D0D4ZW EGS-21 Phase 2 T85435 DRUGINFO D00SWQ Mitoglitazone Phase 2 T85435 DRUGINFO D00AUX MSDC-0602 Phase 2 T85435 DRUGINFO D03VCJ NP-01 Phase 2 T85435 DRUGINFO D02SXZ S-707106 Phase 2 T85435 DRUGINFO D0A6OS TAK-379 Phase 2 T85435 DRUGINFO D0ZK7B Tesofensine Phase 2 T85435 DRUGINFO D07NKZ VVP-808 Phase 2 T85435 DRUGINFO D07HPJ AEW-541 Phase 1 T85435 DRUGINFO D06HPP AGT-182 Phase 1 T85435 DRUGINFO D0D5EJ Insulin oral sublingual Phase 1 T85435 DRUGINFO D08TGG Insulin transdermal Phase 1 T85435 DRUGINFO D07DLA ISF-402 Phase 1 T85435 DRUGINFO D08XFJ NN-1218 Phase 1 T85435 DRUGINFO D05LSY AKP-020 Discontinued in Phase 2 T85435 DRUGINFO D0Z8UQ DM-83 Discontinued in Phase 2 T85435 DRUGINFO D0F1MU EML-336 Discontinued in Phase 2 T85435 DRUGINFO D0M3OR KW-2450 Discontinued in Phase 1/2 T85435 DRUGINFO D02IJP CLX-0900 Terminated T85435 DRUGINFO D03CMR TER-16998 Terminated T85435 DRUGINFO D0W9KO 4-((1H-indazol-6-ylamino)methyl)benzene-1,2-diol Investigative T85435 DRUGINFO D0L7MM 4-((naphthalen-2-ylamino)methyl)benzene-1,2-diol Investigative T85435 DRUGINFO D0KC9V AD10-1025 Investigative T85435 DRUGINFO D0XQ0V DC-9703 Investigative T85435 DRUGINFO D03BCE FPT-038 Investigative T85435 DRUGINFO D06PJW GSK-1838705A Investigative T85435 DRUGINFO D0UG4S L-betagamma-meATP Investigative T85435 DRUGINFO D0R2WK NVP-TAE684 Investigative T85435 DRUGINFO D0G4CS PMID24900237C15 Investigative T85435 DRUGINFO D08ZLL Quick-acting insulin Investigative T85435 DRUGINFO D0I4LQ RHIIP Investigative T85435 DRUGINFO D0YN9H VVP-100X Investigative T85435 DRUGINFO D02QOL XMetD Investigative T85435 DRUGINFO D0C7QW XMetS Investigative T85435 KEGGPATH hsa04014:Ras signaling pathway T85435 KEGGPATH hsa04015:Rap1 signaling pathway T85435 KEGGPATH hsa04022:cGMP-PKG signaling pathway T85435 KEGGPATH hsa04066:HIF-1 signaling pathway T85435 KEGGPATH hsa04068:FoxO signaling pathway T85435 KEGGPATH hsa04151:PI3K-Akt signaling pathway T85435 KEGGPATH hsa04152:AMPK signaling pathway T85435 KEGGPATH hsa04520:Adherens junction T85435 KEGGPATH hsa04910:Insulin signaling pathway T85435 KEGGPATH hsa04913:Ovarian steroidogenesis T85435 KEGGPATH hsa04930:Type II diabetes mellitus T85435 KEGGPATH hsa04932:Non-alcoholic fatty liver disease (NAFLD) T85435 KEGGPATH hsa04960:Aldosterone-regulated sodium reabsorption T85435 WIKIPATH WP1403:AMPK Signaling T85435 WIKIPATH WP15:Selenium Micronutrient Network T85435 WIKIPATH WP1533:Vitamin B12 Metabolism T85435 WIKIPATH WP1584:Type II diabetes mellitus T85435 WIKIPATH WP176:Folate Metabolism T85435 WIKIPATH WP1913:Signaling by Insulin receptor T85435 WIKIPATH WP2324:AGE/RAGE pathway T85435 WIKIPATH WP2509:Nanoparticle triggered autophagic cell death T85435 WIKIPATH WP481:Insulin Signaling T85435 WIKIPATH WP710:DNA Damage Response (only ATM dependent) T85435 WHIZPATH PW000454:Insulin Signalling T85435 WHIZPATH PW000659:Leucine Stimulation on Insulin Signaling T85435 REACPATH R-HSA-74713:IRS activation T85435 REACPATH R-HSA-74749:Signal attenuation T85435 REACPATH R-HSA-74751:Insulin receptor signalling cascade T85435 REACPATH R-HSA-77387:Insulin receptor recycling T85435 NET_PATH NetPath_7:TGF_beta_Receptor Signaling Pathway T85435 INTEPATH insulin_glucose_pathway:Insulin-mediated glucose transport T85435 INTEPATH insulin_pathway:Insulin Pathway T85435 INTEPATH ptp1bpathway:Signaling events mediated by PTP1B T85435 INTEPATH tcptp_pathway:Signaling events mediated by TCPTP T85435 PANTPATH P00032:Insulin/IGF pathway-mitogen activated protein kinase kinase/MAP kinase cascade T85435 PANTPATH P00033:Insulin/IGF pathway-protein kinase B signaling cascade T85435 PANTPATH P00048:PI3 kinase pathway T12499 TARGETID T12499 T12499 FORMERID TTDS00407 T12499 UNIPROID LCK_HUMAN T12499 TARGNAME LCK tyrosine protein kinase (LCK) T12499 GENENAME LCK T12499 TARGTYPE Successful target T12499 SYNONYMS p56-LCK; Tyrosine-protein kinase Lck; T cell-specific protein-tyrosine kinase; Proto-oncogene tyrosine-protein kinase LCK; Proto-oncogene Lck; Protein YT16; Lymphocyte cell-specific protein-tyrosine kinase; Leukocyte C-terminal Src kinase; LSK; LCK p59-Fyn; LCK Protooncogene Syn T12499 FUNCTION Plays a key role in T-cell antigen receptor (TCR)-linked signal transduction pathways. Constitutively associated with the cytoplasmic portions of the CD4 and CD8 surface receptors. Association of the TCR with a peptide antigen-bound MHC complex facilitates the interaction of CD4 and CD8 with MHC class II and class I molecules, respectively, thereby recruiting the associated LCK protein to the vicinity of the TCR/CD3 complex. LCK then phosphorylates tyrosine residues within the immunoreceptor tyrosine-based activation motifs (ITAM) of the cytoplasmic tails of the TCR-gamma chains and CD3 subunits, initiating the TCR/CD3 signaling pathway. Once stimulated, the TCR recruits the tyrosine kinase ZAP70, that becomes phosphorylated and activated by LCK. Following this, a large number of signaling molecules are recruited, ultimately leading to lymphokine production. LCK also contributes to signaling by other receptor molecules. Associates directly with the cytoplasmic tail of CD2, which leads to hyperphosphorylation and activation of LCK. Also plays a role in the IL2 receptor-linked signaling pathway that controls the T-cell proliferative response. Binding of IL2 to its receptor results in increased activity of LCK. Is expressed at all stages of thymocyte development and is required for the regulation of maturation events that are governed by both pre-TCR and mature alpha beta TCR. Phosphorylates other substrates including RUNX3, PTK2B/PYK2, the microtubule-associated protein MAPT, RHOH or TYROBP. Interacts with FYB2. Non-receptor tyrosine-protein kinase that plays an essential role in the selection and maturation of developing T-cells in the thymus and in the function of mature T-cells. T12499 PDBSTRUC 6H6A; 5MTN; 5MTM; 4D8K; 4C3F T12499 BIOCLASS Kinase T12499 ECNUMBER EC 2.7.10.2 T12499 SEQUENCE MGCGCSSHPEDDWMENIDVCENCHYPIVPLDGKGTLLIRNGSEVRDPLVTYEGSNPPASPLQDNLVIALHSYEPSHDGDLGFEKGEQLRILEQSGEWWKAQSLTTGQEGFIPFNFVAKANSLEPEPWFFKNLSRKDAERQLLAPGNTHGSFLIRESESTAGSFSLSVRDFDQNQGEVVKHYKIRNLDNGGFYISPRITFPGLHELVRHYTNASDGLCTRLSRPCQTQKPQKPWWEDEWEVPRETLKLVERLGAGQFGEVWMGYYNGHTKVAVKSLKQGSMSPDAFLAEANLMKQLQHQRLVRLYAVVTQEPIYIITEYMENGSLVDFLKTPSGIKLTINKLLDMAAQIAEGMAFIEERNYIHRDLRAANILVSDTLSCKIADFGLARLIEDNEYTAREGAKFPIKWTAPEAINYGTFTIKSDVWSFGILLTEIVTHGRIPYPGMTNPEVIQNLERGYRMVRPDNCPEELYQLMRLCWKERPEDRPTFDYLRSVLEDFFTATEGQYQPQP T12499 DRUGINFO D0E6XR Dasatinib Approved T12499 DRUGINFO D02XNW VX-680 Phase 2 T12499 DRUGINFO D06CIJ ISIS-CRP Phase 1 T12499 DRUGINFO D0U3XL JNJ-26483327 Phase 1 T12499 DRUGINFO D07AIB (4-Phenoxy-phenyl)-quinazolin-4-yl-amine Investigative T12499 DRUGINFO D02BUW 2-(3,4,5-Trihydroxy-benzylidene)-malononitrile Investigative T12499 DRUGINFO D08DVL 3-(4-(o-toluidino)pyrimidin-2-ylamino)benzamide Investigative T12499 DRUGINFO D08WOG 4-(3-Chloro-phenoxy)-6,7-dimethoxy-quinazoline Investigative T12499 DRUGINFO D0O1YH 4,5,6,7-tetrabromo-1H-benzo[d][1,2,3]triazole Investigative T12499 DRUGINFO D0M3CT 4-Phenylsulfanyl-7H-pyrrolo[2,3-d]pyrimidine Investigative T12499 DRUGINFO D09HXU 6-o-tolylquinazolin-2-amine Investigative T12499 DRUGINFO D0BS6R A-420983 Investigative T12499 DRUGINFO D03AER A-641359 Investigative T12499 DRUGINFO D06WGX A-770041 Investigative T12499 DRUGINFO D00ICA AMP-PNP Investigative T12499 DRUGINFO D0TO6S Bisindolylmaleimide-I Investigative T12499 DRUGINFO D0M4SY BMS-536924 Investigative T12499 DRUGINFO D09QBA CEP-5104 Investigative T12499 DRUGINFO D0A7FQ CGP-57380 Investigative T12499 DRUGINFO D0B9BU CI-1040 Investigative T12499 DRUGINFO D0C3AD GW-788388 Investigative T12499 DRUGINFO D0D5EW HKI-9924129 Investigative T12499 DRUGINFO D0YZ7H JNJ-10198409 Investigative T12499 DRUGINFO D0Y4BL JNJ-28312141 Investigative T12499 DRUGINFO D0N6ES KN-62 Investigative T12499 DRUGINFO D06WJA L-779450 Investigative T12499 DRUGINFO D0D9TU LAVENDUSTIN A Investigative T12499 DRUGINFO D0OZ2S Lck inhibitor Investigative T12499 DRUGINFO D0GT8N NM-PP1 Investigative T12499 DRUGINFO D0P3JW PD-0166326 Investigative T12499 DRUGINFO D0S1KJ PD-0173952 Investigative T12499 DRUGINFO D03NPX PD-0173955 Investigative T12499 DRUGINFO D0GW4Q PD-0173956 Investigative T12499 DRUGINFO D0Z7GH PD-0173958 Investigative T12499 DRUGINFO D0OH3J PD-0179483 Investigative T12499 DRUGINFO D08RZB PMID15546730C2 Investigative T12499 DRUGINFO D0D5KZ PMID17280833C30 Investigative T12499 DRUGINFO D04TLI PMID17600705C23 Investigative T12499 DRUGINFO D0IZ8M PMID21855335C19a Investigative T12499 DRUGINFO D0L8HO RO-316233 Investigative T12499 DRUGINFO D0M5FF Ro31-8220 Investigative T12499 DRUGINFO D0L4HJ RPR-108518A Investigative T12499 DRUGINFO D0GB4V STAUROSPORINONE Investigative T12499 DRUGINFO D0CE3R SU 6656 Investigative T12499 DRUGINFO D0H1OK TG-100435 Investigative T12499 DRUGINFO D0Y1SR WH-4-023 Investigative T12499 DRUGINFO D07ERV Y-c[D-Pen-(3,5-diI)Tyr-GSFC]KR-NH2 Investigative T12499 DRUGINFO D0A2LX Y-c[D-Pen-(3-I)Tyr-GSFC]KR-NH2 Investigative T12499 DRUGINFO D00NWF ZM-336372 Investigative T12499 KEGGPATH hsa04064:NF-kappa B signaling pathway T12499 KEGGPATH hsa04380:Osteoclast differentiation T12499 KEGGPATH hsa04650:Natural killer cell mediated cytotoxicity T12499 KEGGPATH hsa04660:T cell receptor signaling pathway T12499 KEGGPATH hsa05166:HTLV-I infection T12499 KEGGPATH hsa05340:Primary immunodeficiency T12499 WIKIPATH WP1799:Costimulation by the CD28 family T12499 WIKIPATH WP1927:TCR signaling T12499 WIKIPATH WP2203:TSLP Signaling Pathway T12499 WIKIPATH WP23:B Cell Receptor Signaling Pathway T12499 WIKIPATH WP2583:T-Cell Receptor and Co-stimulatory Signaling T12499 WIKIPATH WP2653:PIP3 activates AKT signaling T12499 WIKIPATH WP2684:Host Interactions of HIV factors T12499 WIKIPATH WP2694:DAP12 interactions T12499 WIKIPATH WP2713:Signaling by SCF-KIT T12499 WIKIPATH WP453:Inflammatory Response Pathway T12499 WIKIPATH WP49:IL-2 Signaling Pathway T12499 WIKIPATH WP585:Interferon type I signaling pathways T12499 WIKIPATH WP61:Notch Signaling Pathway T12499 REACPATH R-HSA-114604:GPVI-mediated activation cascade T12499 REACPATH R-HSA-1257604:PIP3 activates AKT signaling T12499 REACPATH R-HSA-1433559:Regulation of KIT signaling T12499 REACPATH R-HSA-202427:Phosphorylation of CD3 and TCR zeta chains T12499 REACPATH R-HSA-202430:Translocation of ZAP-70 to Immunological synapse T12499 REACPATH R-HSA-202433:Generation of second messenger molecules T12499 REACPATH R-HSA-210990:PECAM1 interactions T12499 REACPATH R-HSA-2219530:Constitutive Signaling by Aberrant PI3K in Cancer T12499 REACPATH R-HSA-2424491:DAP12 signaling T12499 REACPATH R-HSA-389356:CD28 co-stimulation T12499 REACPATH R-HSA-389357:CD28 dependent PI3K/Akt signaling T12499 REACPATH R-HSA-389359:CD28 dependent Vav1 pathway T12499 REACPATH R-HSA-389513:CTLA4 inhibitory signaling T12499 REACPATH R-HSA-389948:PD-1 signaling T12499 REACPATH R-HSA-451927:Interleukin-2 signaling T12499 NET_PATH NetPath_11:TCR Signaling Pathway T12499 NET_PATH NetPath_14:IL2 Signaling Pathway T12499 INTEPATH alphasynuclein_pathway:Alpha-synuclein signaling T12499 INTEPATH amb2_neutrophils_pathway:amb2 Integrin signaling T12499 INTEPATH cd8tcrpathway:TCR signaling in naïve CD8+ T cells T12499 INTEPATH cxcr4_pathway:CXCR4-mediated signaling events T12499 INTEPATH epha_fwdpathway:EPHA forward signaling T12499 INTEPATH ephrinbrevpathway:Ephrin B reverse signaling T12499 INTEPATH glypican_1pathway:Glypican 1 network T12499 INTEPATH il12_2pathway:IL12-mediated signaling events T12499 INTEPATH il2_1pathway:IL2-mediated signaling events T12499 INTEPATH il2_pi3kpathway:IL2 signaling events mediated by PI3K T12499 INTEPATH il2_stat5pathway:IL2 signaling events mediated by STAT5 T12499 INTEPATH nfkappabatypicalpathway:Atypical NF-kappaB pathway T12499 INTEPATH p38alphabetapathway:Regulation of p38-alpha and p38-beta T12499 INTEPATH pdgfrbpathway:PDGFR-beta signaling pathway T12499 INTEPATH pi3kcipathway:Class I PI3K signaling events T12499 INTEPATH ptp1bpathway:Signaling events mediated by PTP1B T12499 INTEPATH shp2_pathway:SHP2 signaling T12499 INTEPATH tcr_pathway:TCR signaling in naïve CD4+ T cells T12499 INTEPATH txa2pathway:Thromboxane A2 receptor signaling T12499 PANTPATH P00049:Parkinson disease T12499 PANTPATH P00053:T cell activation T60631 TARGETID T60631 T60631 FORMERID TTDS00348 T60631 UNIPROID RET_HUMAN T60631 TARGNAME Proto-oncogene c-Ret (RET) T60631 GENENAME RET T60631 TARGTYPE Successful target T60631 SYNONYMS RET51; RET receptor tyrosine kinase; RET mutant Y791F; RET mutant V804M; RET mutant V804L; RET mutant S891A; RET mutant M918T; RET mutant G691S; Proto-oncogene tyrosine-protein kinase receptor Ret; PTC; Cadherin family member 12; CDHR16; CDHF12; C-ret T60631 FUNCTION Phosphorylates PTK2/FAK1. Regulates both cell death/survival balance and positional information. Required for the molecular mechanisms orchestration during intestine organogenesis; involved in the development of enteric nervous system and renal organogenesis during embryonic life, and promotes the formation of Peyer's patch-like structures, a major component of the gut-associated lymphoid tissue. Modulates cell adhesion via its cleavage by caspase in sympathetic neurons and mediates cell migration in an integrin (e. g. ITGB1 and ITGB3)-dependent manner. Involved in the development of the neural crest. Active in the absence of ligand, triggering apoptosis through a mechanism that requires receptor intracellular caspase cleavage. Acts as a dependence receptor; in the presence of the ligand GDNF in somatotrophs (within pituitary), promotes survival and down regulates growth hormone (GH) production, but triggers apoptosis in absence of GDNF. Regulates nociceptor survival and size. Triggers the differentiation of rapidly adapting (RA) mechanoreceptors. Mediator of several diseases such as neuroendocrine cancers; these diseases are characterized by aberrant integrins-regulated cell migration. Mediates, through interaction with GDF15-receptor GFRAL, GDF15-induced cell-signaling in the brainstem which induces inhibition of food-intake. Activates MAPK- and AKT-signaling pathways. Isoform 1 in complex with GFRAL induces higher activation of MAPK-signaling pathway than isoform 2 in complex with GFRAL. Receptor tyrosine-protein kinase involved in numerous cellular mechanisms including cell proliferation, neuronal navigation, cell migration, and cell differentiation upon binding with glial cell derived neurotrophic factor family ligands. T60631 PDBSTRUC 6FEK; 5FM3; 5FM2; 5AMN; 4UX8 T60631 BIOCLASS Kinase T60631 ECNUMBER EC 2.7.10.1 T60631 SEQUENCE MAKATSGAAGLRLLLLLLLPLLGKVALGLYFSRDAYWEKLYVDQAAGTPLLYVHALRDAPEEVPSFRLGQHLYGTYRTRLHENNWICIQEDTGLLYLNRSLDHSSWEKLSVRNRGFPLLTVYLKVFLSPTSLREGECQWPGCARVYFSFFNTSFPACSSLKPRELCFPETRPSFRIRENRPPGTFHQFRLLPVQFLCPNISVAYRLLEGEGLPFRCAPDSLEVSTRWALDREQREKYELVAVCTVHAGAREEVVMVPFPVTVYDEDDSAPTFPAGVDTASAVVEFKRKEDTVVATLRVFDADVVPASGELVRRYTSTLLPGDTWAQQTFRVEHWPNETSVQANGSFVRATVHDYRLVLNRNLSISENRTMQLAVLVNDSDFQGPGAGVLLLHFNVSVLPVSLHLPSTYSLSVSRRARRFAQIGKVCVENCQAFSGINVQYKLHSSGANCSTLGVVTSAEDTSGILFVNDTKALRRPKCAELHYMVVATDQQTSRQAQAQLLVTVEGSYVAEEAGCPLSCAVSKRRLECEECGGLGSPTGRCEWRQGDGKGITRNFSTCSPSTKTCPDGHCDVVETQDINICPQDCLRGSIVGGHEPGEPRGIKAGYGTCNCFPEEEKCFCEPEDIQDPLCDELCRTVIAAAVLFSFIVSVLLSAFCIHCYHKFAHKPPISSAEMTFRRPAQAFPVSYSSSGARRPSLDSMENQVSVDAFKILEDPKWEFPRKNLVLGKTLGEGEFGKVVKATAFHLKGRAGYTTVAVKMLKENASPSELRDLLSEFNVLKQVNHPHVIKLYGACSQDGPLLLIVEYAKYGSLRGFLRESRKVGPGYLGSGGSRNSSSLDHPDERALTMGDLISFAWQISQGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSRDVYEEDSYVKRSQGRIPVKWMAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPPERLFNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRRDYLDLAASTPSDSLIYDDGLSEEETPLVDCNNAPLPRALPSTWIENKLYGMSDPNWPGESPVPLTRADGTNTGFPRYPNDSVYANWMLSPSAAKLMDTFDS T60631 DRUGINFO D0H0EQ Ponatinib Approved T60631 DRUGINFO D0OD2I Pralsetinib Approved T60631 DRUGINFO D09GDD Regorafenib Approved T60631 DRUGINFO D01PZD Romiplostim Approved T60631 DRUGINFO D01KOA Selpercatinib Approved T60631 DRUGINFO D0G6QF Vandetanib Approved T60631 DRUGINFO D05BLN MGCD516 Phase 2/3 T60631 DRUGINFO D04MXN CEP-32496 Phase 1/2 T60631 DRUGINFO DS7CY4 TPX-0046 Phase 1/2 T60631 DRUGINFO D1BG7C BOS172738 Phase 1 T60631 DRUGINFO D0AX4H GSK3179106 Phase 1 T60631 DRUGINFO D0S6TK tamatinib Clinical trial T60631 DRUGINFO D08LCQ Benzo(b)carbazol-11-one compound 1 Patented T60631 DRUGINFO D0O9JD Benzo(b)carbazol-11-one compound 2 Patented T60631 DRUGINFO D0MX7B Carboxamide derivative 4 Patented T60631 DRUGINFO D0A6RR Dihydropyridine compound 1 Patented T60631 DRUGINFO D0JY9S Dihydropyridine compound 2 Patented T60631 DRUGINFO D0YC7C Dihydropyridine compound 3 Patented T60631 DRUGINFO D03JZP Dihydropyridine compound 4 Patented T60631 DRUGINFO D0X7IS Dihydropyridine compound 5 Patented T60631 DRUGINFO D03ORX Dihydropyridine compound 6 Patented T60631 DRUGINFO D06BNK Pyrazolo[3,4-d]pyrimidine derivative 5 Patented T60631 DRUGINFO D03MMZ Pyrazolo[3,4-d]pyrimidine derivative 6 Patented T60631 DRUGINFO D05HYJ Pyrazolo[3,4-d]pyrimidine derivative 7 Patented T60631 DRUGINFO D01BMX Pyrazolo[3,4-d]pyrimidine derivative 8 Patented T60631 DRUGINFO D0AK1F Pyridine derivative 18 Patented T60631 DRUGINFO D0T7BE Pyridine derivative 19 Patented T60631 DRUGINFO D0NB1V Pyridine derivative 20 Patented T60631 DRUGINFO D0O0AW Pyridine derivative 21 Patented T60631 DRUGINFO D0O4TA Pyridine derivative 22 Patented T60631 DRUGINFO D0XR9O Pyrrolo-pyridinone derivative 1 Patented T60631 DRUGINFO D0QY6M Pyrrolo-pyridinone derivative 2 Patented T60631 DRUGINFO D05NBB Pyrrolo-pyridinone derivative 3 Patented T60631 DRUGINFO D07QKP Pyrrolo-pyridinone derivative 4 Patented T60631 DRUGINFO D09FBJ Pyrrolo-pyrimidine derivative 2 Patented T60631 DRUGINFO D0FU0I Pyrrolo-pyrimidine derivative 3 Patented T60631 DRUGINFO D0P1AH Pyrrolo-pyrimidine derivative 4 Patented T60631 DRUGINFO D0NH2H Pyrrolo-pyrimidine derivative 5 Patented T60631 DRUGINFO D07OLQ Pyrrolo-pyrimidine derivative 6 Patented T60631 DRUGINFO D0B3GX Quinazoline derivative 14 Patented T60631 DRUGINFO D05PRG Quinazoline derivative 15 Patented T60631 DRUGINFO D0DV4X Quinazoline derivative 16 Patented T60631 DRUGINFO D0J5TN CEP-751 Terminated T60631 DRUGINFO D0Y1UL (E)-3-(4-hydroxybenzylidene)indolin-2-one Investigative T60631 DRUGINFO D00ATA (Z)-3-((1H-pyrrol-2-yl)methylene)indolin-2-one Investigative T60631 DRUGINFO D0W4UQ (Z)-5-Amino-3-(4-methoxybenzylidene)indolin-2-one Investigative T60631 DRUGINFO D0N7AJ AST-487 Investigative T60631 DRUGINFO D02CFR GW-559768X Investigative T60631 DRUGINFO D0N5TB ITRI-305 Investigative T60631 DRUGINFO D02NNT PMID21493067C1d Investigative T60631 DRUGINFO D02BXJ PMID21561767C8h Investigative T60631 DRUGINFO D0H1OK TG-100435 Investigative T60631 KEGGPATH hsa04144:Endocytosis T60631 KEGGPATH hsa05200:Pathways in cancer T60631 KEGGPATH hsa05216:Thyroid cancer T60631 KEGGPATH hsa05230:Central carbon metabolism in cancer T60631 WIKIPATH WP2855:Dopaminergic Neurogenesis T60631 WIKIPATH WP706:SIDS Susceptibility Pathways T60631 INTEPATH ajdiss_2pathway:Posttranslational regulation of adherens junction stability and dissassembly T60631 INTEPATH ret_pathway:Signaling events regulated by Ret tyrosine kinase T68251 TARGETID T68251 T68251 FORMERID TTDC00104 T68251 UNIPROID MMP2_HUMAN T68251 TARGNAME Matrix metalloproteinase-2 (MMP-2) T68251 GENENAME MMP2 T68251 TARGTYPE Successful target T68251 SYNONYMS TBE-1; Matrix metalloproteinase 2; CLG4A; 72 kDa type IV collagenase; 72 kDa gelatinase T68251 FUNCTION As well as degrading extracellular matrix proteins, can also act on several nonmatrix proteins such as big endothelial 1 and beta-type CGRP promoting vasoconstriction. Also cleaves KISS at a Gly-|-Leu bond. Appears to have a role in myocardial cell death pathways. Contributes to myocardial oxidative stress by regulating the activity of GSK3beta. Cleaves GSK3beta in vitro. Involved in the formation of the fibrovascular tissues in association with MMP14. Ubiquitinous metalloproteinase that is involved in diverse functions such as remodeling of the vasculature, angiogenesis, tissue repair, tumor invasion, inflammation, and atherosclerotic plaque rupture. T68251 PDBSTRUC 3AYU; 1RTG; 1QIB; 1KS0; 1J7M T68251 BIOCLASS Peptidase T68251 ECNUMBER EC 3.4.24.24 T68251 SEQUENCE MEALMARGALTGPLRALCLLGCLLSHAAAAPSPIIKFPGDVAPKTDKELAVQYLNTFYGCPKESCNLFVLKDTLKKMQKFFGLPQTGDLDQNTIETMRKPRCGNPDVANYNFFPRKPKWDKNQITYRIIGYTPDLDPETVDDAFARAFQVWSDVTPLRFSRIHDGEADIMINFGRWEHGDGYPFDGKDGLLAHAFAPGTGVGGDSHFDDDELWTLGEGQVVRVKYGNADGEYCKFPFLFNGKEYNSCTDTGRSDGFLWCSTTYNFEKDGKYGFCPHEALFTMGGNAEGQPCKFPFRFQGTSYDSCTTEGRTDGYRWCGTTEDYDRDKKYGFCPETAMSTVGGNSEGAPCVFPFTFLGNKYESCTSAGRSDGKMWCATTANYDDDRKWGFCPDQGYSLFLVAAHEFGHAMGLEHSQDPGALMAPIYTYTKNFRLSQDDIKGIQELYGASPDIDLGTGPTPTLGPVTPEICKQDIVFDGIAQIRGEIFFFKDRFIWRTVTPRDKPMGPLLVATFWPELPEKIDAVYEAPQEEKAVFFAGNEYWIYSASTLERGYPKPLTSLGLPPDVQRVDAAFNWSKNKKTYIFAGDKFWRYNEVKKKMDPGFPKLIADAWNAIPDNLDAVVDLQGGGHSYFFKGAYYLKLENQSLKSVKFGSIKSDWLGC T68251 DRUGINFO D00MDP Prinomastat Approved T68251 DRUGINFO D0U2BH Epigallocatechin gallate Phase 3 T68251 DRUGINFO D05VZE Marimastat Phase 3 T68251 DRUGINFO D0IJ7O Metastat Phase 1 T68251 DRUGINFO D0T4BL Neovastat Phase 1 T68251 DRUGINFO D05GAP PMID29130358-Compound-Figure10(2a) Patented T68251 DRUGINFO D0Y1LO PMID29130358-Compound-Figure11(3) Patented T68251 DRUGINFO D0Q4QB PMID29130358-Compound-Figure13(4) Patented T68251 DRUGINFO D0LS4Y PMID29130358-Compound-Figure16(9a) Patented T68251 DRUGINFO D0A9ZW PMID29130358-Compound-Figure16(9b) Patented T68251 DRUGINFO D0S3PN PMID29130358-Compound-Figure16(9c) Patented T68251 DRUGINFO D0O8RQ PMID29130358-Compound-Figure18(14) Patented T68251 DRUGINFO D0X6GG PMID29130358-Compound-Figure18(14a) Patented T68251 DRUGINFO D0W7HO PMID29130358-Compound-LonimacranthoideVII Patented T68251 DRUGINFO D0DB0Z PMID29130358-Compound-SB-3CT Patented T68251 DRUGINFO D01EUF BMS 275291 Discontinued in Phase 3 T68251 DRUGINFO D0Q1CD Tanomastat Discontinued in Phase 3 T68251 DRUGINFO D05WTZ Galarubicin Discontinued in Phase 2 T68251 DRUGINFO D0T9HG GM6001 Discontinued in Phase 2 T68251 DRUGINFO D03BOZ RS-130830 Discontinued in Phase 2 T68251 DRUGINFO D0C0ME RO-26-2853 Preclinical T68251 DRUGINFO D05VNG BB-1101 Terminated T68251 DRUGINFO D08WBF BB-3644 Terminated T68251 DRUGINFO D02GYD CDP-845 Terminated T68251 DRUGINFO D08CEE L-696418 Terminated T68251 DRUGINFO D0Y1XT SC-44463 Terminated T68251 DRUGINFO D0G3YZ (+/-)5-(biphenyl-4-yl)-3-hydroxypentanoic acid Investigative T68251 DRUGINFO D07MJD [2-(Biphenyl-4-sulfonyl)phenyl]acetic Acid Investigative T68251 DRUGINFO D0E5MB 2-(4'-chloro-biphenyl-4-sulfonyl)-pentanoic acid Investigative T68251 DRUGINFO D05THD 2-(Biphenyl-4-ylsulfonyl)N-hydroxybenzamide Investigative T68251 DRUGINFO D0L4EO 3-(4-(2-phenylethynyl)benzoyl)pentanoic acid Investigative T68251 DRUGINFO D0A5MV 3-(4-Phenylethynylbenzoyl)nonanoic acid Investigative T68251 DRUGINFO D05JPV 4-(4-(dec-1-ynyl)phenyl)-4-oxobutanoic acid Investigative T68251 DRUGINFO D07LTB 5-(4-Phenoxy-phenyl)-pyrimidine-2,4,6-trione Investigative T68251 DRUGINFO D0Y7NV 5-Biphenyl-4-yl-5-ethyl-pyrimidine-2,4,6-trione Investigative T68251 DRUGINFO D0Q9LC 5-Biphenyl-4-yl-5-hexyl-pyrimidine-2,4,6-trione Investigative T68251 DRUGINFO D0K4TI 5-Hexyl-5-phenyl-pyrimidine-2,4,6-trione Investigative T68251 DRUGINFO D0T1FR Cis-2-aminocyclohexylcarbamoylphosphonic acid Investigative T68251 DRUGINFO D0H9BL Clinopodic acid C Investigative T68251 DRUGINFO D0P8EY Folate gamma-hydroxamic acid Investigative T68251 DRUGINFO D0ZB6O Folate gamma-L-proline-hydroxamic acid Investigative T68251 DRUGINFO D0W2UK IK-862 Investigative T68251 DRUGINFO D06ALC Lithospermic acid Investigative T68251 DRUGINFO D0B0UI Methotrexate gamma-hydroxamic acid Investigative T68251 DRUGINFO D01HKU Methotrexate gamma-L-proline-hydroxamic acid Investigative T68251 DRUGINFO D0A4TC MMI270 Investigative T68251 DRUGINFO D0S9OL N-Hydroxy-2-(4-phenoxy-benzenesulfonyl)benzamide Investigative T68251 DRUGINFO D00RNA N-hydroxy-3-(2-oxo-2H-chromen-3-yl)propanamide Investigative T68251 DRUGINFO D08ICI N-hydroxy-3-(6-methoxy-2-oxo-2H-chromen-3-yl) Investigative T68251 DRUGINFO D02EFQ PD-169469 Investigative T68251 DRUGINFO D0F7BE PNU-107859 Investigative T68251 DRUGINFO D0XL8K Ro-37-9790 Investigative T68251 DRUGINFO D0U7CD Roche 28-2653 Investigative T68251 DRUGINFO D08NSS SC-74020 Investigative T68251 DRUGINFO D03AMR SR-973 Investigative T68251 DRUGINFO D0NP8A UK-356618 Investigative T68251 KEGGPATH hsa04670:Leukocyte transendothelial migration T68251 KEGGPATH hsa04912:GnRH signaling pathway T68251 KEGGPATH hsa04915:Estrogen signaling pathway T68251 KEGGPATH hsa05200:Pathways in cancer T68251 KEGGPATH hsa05205:Proteoglycans in cancer T68251 KEGGPATH hsa05219:Bladder cancer T68251 WIKIPATH WP129:Matrix Metalloproteinases T68251 WIKIPATH WP2324:AGE/RAGE pathway T68251 WIKIPATH WP2769:Activation of Matrix Metalloproteinases T68251 REACPATH R-HSA-1442490:Collagen degradation T68251 REACPATH R-HSA-1474228:Degradation of the extracellular matrix T68251 REACPATH R-HSA-1592389:Activation of Matrix Metalloproteinases T68251 REACPATH R-HSA-381426:Regulation of Insulin-like Growth Factor (IGF) transport and uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs) T68251 REACPATH R-HSA-3928665:EPH-ephrin mediated repulsion of cells T68251 NET_PATH NetPath_11:TCR Signaling Pathway T68251 NET_PATH NetPath_22:Leptin Signaling Pathway T68251 NET_PATH NetPath_5:ID Signaling Pathway T68251 INTEPATH amb2_neutrophils_pathway:amb2 Integrin signaling T68251 INTEPATH angiopoietinreceptor_pathway:Angiopoietin receptor Tie2-mediated signaling T68251 INTEPATH atf2_pathway:ATF-2 transcription factor network T68251 INTEPATH avb3_opn_pathway:Osteopontin-mediated events T68251 INTEPATH betacatenin_nuc_pathway:Regulation of nuclear beta catenin signaling and target gene transcription T68251 INTEPATH er_nongenomic_pathway:Plasma membrane estrogen receptor signaling T68251 INTEPATH foxm1pathway:FOXM1 transcription factor network T68251 INTEPATH fra_pathway:Validated transcriptional targets of AP1 family members Fra1 and Fra2 T68251 INTEPATH lysophospholipid_pathway:LPA receptor mediated events T68251 INTEPATH p53downstreampathway:Direct p53 effectors T68251 INTEPATH syndecan_2_pathway:Syndecan-2-mediated signaling events T68251 PANTPATH P00004:Alzheimer disease-presenilin pathway T00140 TARGETID T00140 T00140 FORMERID TTDS00112 T00140 UNIPROID LOX5_HUMAN T00140 TARGNAME Arachidonate 5-lipoxygenase (5-LOX) T00140 GENENAME ALOX5 T00140 TARGTYPE Successful target T00140 SYNONYMS LOG5; 5-lipoxygenase; 5-LO T00140 FUNCTION Catalyzes the first step in leukotriene biosynthesis, and thereby plays a role in inflammatory processes. T00140 PDBSTRUC 3V99; 3V98; 3V92; 3O8Y; 2ABV T00140 BIOCLASS Oxygenase T00140 ECNUMBER EC 1.13.11.34 T00140 SEQUENCE MPSYTVTVATGSQWFAGTDDYIYLSLVGSAGCSEKHLLDKPFYNDFERGAVDSYDVTVDEELGEIQLVRIEKRKYWLNDDWYLKYITLKTPHGDYIEFPCYRWITGDVEVVLRDGRAKLARDDQIHILKQHRRKELETRQKQYRWMEWNPGFPLSIDAKCHKDLPRDIQFDSEKGVDFVLNYSKAMENLFINRFMHMFQSSWNDFADFEKIFVKISNTISERVMNHWQEDLMFGYQFLNGCNPVLIRRCTELPEKLPVTTEMVECSLERQLSLEQEVQQGNIFIVDFELLDGIDANKTDPCTLQFLAAPICLLYKNLANKIVPIAIQLNQIPGDENPIFLPSDAKYDWLLAKIWVRSSDFHVHQTITHLLRTHLVSEVFGIAMYRQLPAVHPIFKLLVAHVRFTIAINTKAREQLICECGLFDKANATGGGGHVQMVQRAMKDLTYASLCFPEAIKARGMESKEDIPYYFYRDDGLLVWEAIRTFTAEVVDIYYEGDQVVEEDPELQDFVNDVYVYGMRGRKSSGFPKSVKSREQLSEYLTVVIFTASAQHAAVNFGQYDWCSWIPNAPPTMRAPPPTAKGVVTIEQIVDTLPDRGRSCWHLGAVWALSQFQENELFLGMYPEEHFIEKPVKEAMARFRKNLEAIVSVIAERNKKKQLPYYYLSPDRIPNSVAI T00140 DRUGINFO D06RCB Diethylcarbamazine Approved T00140 DRUGINFO D09JUG Zileuton Approved T00140 DRUGINFO D0V9EN 3,4-Dihydroxycinnamic Acid Phase 4 T00140 DRUGINFO D0AZ8C Silymarin Phase 4 T00140 DRUGINFO D08PXR ABT-761 Phase 3 T00140 DRUGINFO D0C0NH Avastin+/-Tarceva Phase 3 T00140 DRUGINFO D0X8VV Flobufen Phase 3 T00140 DRUGINFO D02YEY FPL-62064 Phase 3 T00140 DRUGINFO D02RQT Tenidap Phase 3 T00140 DRUGINFO D0AL8T Darbufelone Phase 2/3 T00140 DRUGINFO D00YEV BAICALEIN Phase 2 T00140 DRUGINFO D04FNQ BIM23A760 Phase 2 T00140 DRUGINFO D0D5ZV CMI-392 Phase 2 T00140 DRUGINFO D0K9UK E-6700 Phase 2 T00140 DRUGINFO D0S2PY MK-866 Phase 2 T00140 DRUGINFO D0L5XG PF-4191834 Phase 2 T00140 DRUGINFO D05VVX PTC299 Phase 2 T00140 DRUGINFO DES36M Q301 Phase 2 T00140 DRUGINFO D00RJB Rilopirox Phase 2 T00140 DRUGINFO D0L4SL TA-270 Phase 2 T00140 DRUGINFO D04WMR Tepoxalin Phase 2 T00140 DRUGINFO D0Q7UG Tipelukast Phase 2 T00140 DRUGINFO D04JIM UCB-35440 Phase 2 T00140 DRUGINFO D0A7JH WY-50295-tromethamine Phase 2 T00140 DRUGINFO D0L6VH BF-389 Phase 1 T00140 DRUGINFO D0Y4OI SKF-105809 Phase 1 T00140 DRUGINFO D0U2CB Ibuproxam Withdrawn from market T00140 DRUGINFO D01DAD CJ-13610 Discontinued in Phase 2 T00140 DRUGINFO D0V3HG CV-6504 Discontinued in Phase 2 T00140 DRUGINFO D06UVO DuP-654 Discontinued in Phase 2 T00140 DRUGINFO D0JY4Y E-3040 Discontinued in Phase 2 T00140 DRUGINFO D00HFD E-6080 Discontinued in Phase 2 T00140 DRUGINFO D0H7GH ETH615 Discontinued in Phase 2 T00140 DRUGINFO D04QVN FPL-64170 Discontinued in Phase 2 T00140 DRUGINFO D0E8UV Linetastine Discontinued in Phase 2 T00140 DRUGINFO D0M0QX MK-591 Discontinued in Phase 2 T00140 DRUGINFO D0K2ER MK-886 Discontinued in Phase 2 T00140 DRUGINFO D0P1TZ MLN-977 Discontinued in Phase 2 T00140 DRUGINFO D08ORO OPC-21268 Discontinued in Phase 2 T00140 DRUGINFO D0G5GJ R-68151 Discontinued in Phase 2 T00140 DRUGINFO D0U5EU SC-45662 Discontinued in Phase 2 T00140 DRUGINFO D0P3KA TEBUFELONE Discontinued in Phase 2 T00140 DRUGINFO D0P3CF AZD-4407 Discontinued in Phase 1 T00140 DRUGINFO D0F5NB CD-581 Discontinued in Phase 1 T00140 DRUGINFO D0N1SU Licofelone Discontinued in Phase 1 T00140 DRUGINFO D0X9KE A-78773 Terminated T00140 DRUGINFO D0L1IH A-79175 Terminated T00140 DRUGINFO D0T4EL A-80263 Terminated T00140 DRUGINFO D06XRQ AA-861 Terminated T00140 DRUGINFO D0U6AL BI-L-357 Terminated T00140 DRUGINFO D0C9RZ BU-4601A Terminated T00140 DRUGINFO D05WPQ BW A4C Terminated T00140 DRUGINFO D0HJ1Y BW B70C Terminated T00140 DRUGINFO D0DP8P BW755C Terminated T00140 DRUGINFO D0QI8I CGS 8515 Terminated T00140 DRUGINFO D02QGM CGS-26529 Terminated T00140 DRUGINFO D0L8RG CI-986 Terminated T00140 DRUGINFO D0V4GT CMI-206 Terminated T00140 DRUGINFO D09JYF Epocarbazolin-A Terminated T00140 DRUGINFO D0SZ3B ER-34122 Terminated T00140 DRUGINFO D04APY KC-11404 Terminated T00140 DRUGINFO D01LXG KC-11425 Terminated T00140 DRUGINFO D01QAR LY-221068 Terminated T00140 DRUGINFO D0H2RB NAFAZATROM Terminated T00140 DRUGINFO D0J8RS PD-146176 Terminated T00140 DRUGINFO D0C5HV R zileuton Terminated T00140 DRUGINFO D0S5DY R-85355 Terminated T00140 DRUGINFO D0O8ZE REV-5901 Terminated T00140 DRUGINFO D08JKK RWJ-63556 Terminated T00140 DRUGINFO D06MPF Sch-40120 Terminated T00140 DRUGINFO D09SCI SKF-104351 Terminated T00140 DRUGINFO D0H0IA WY-28342 Terminated T00140 DRUGINFO D06YOD ZD-7717 Terminated T00140 DRUGINFO D0D8MD ZM-230487 Terminated T00140 DRUGINFO D0H6JC 1,2-Dihydro-indazol-3-one Investigative T00140 DRUGINFO D02YPE 1,2-Dihydroxy-10H-anthracen-9-one Investigative T00140 DRUGINFO D00BSX 1,3,8-Trihydroxy-6-methyl-10H-anthracen-9-one Investigative T00140 DRUGINFO D0Y0KF 1,5-Dihydroxy-10H-anthracen-9-one Investigative T00140 DRUGINFO D07OKS 1,8,9-Trimethoxy-9,10-dihydro-anthracene Investigative T00140 DRUGINFO D04MBD 1,8-Dichloro-10H-anthracen-9-one Investigative T00140 DRUGINFO D00ENR 1,8-Dihydroxy-2-propionyl-10H-anthracen-9-one Investigative T00140 DRUGINFO D08FPY 10-Acetyl-1,8-dihydroxy-10H-anthracen-9-one Investigative T00140 DRUGINFO D06XYZ 10-Benzoyl-1,8-dihydroxy-10H-anthracen-9-one Investigative T00140 DRUGINFO D01VLQ 15-hydroxyeicosatetraenoic acid Investigative T00140 DRUGINFO D04RQG 1-Benzyl-1,2-dihydro-indazol-3-one Investigative T00140 DRUGINFO D0B0XK 1-furan-2-yl-3-pyridin-2-yl-propenone (FPP-3) Investigative T00140 DRUGINFO D0P8IX 1-Hydroxy-10H-anthracen-9-one Investigative T00140 DRUGINFO D06CWX 1-Hydroxy-8-methoxy-10H-anthracen-9-one Investigative T00140 DRUGINFO D0A9HL 1-Methyl-1,2-dihydro-indazol-3-one Investigative T00140 DRUGINFO D0R1ER 2-(1H-Indol-3-ylmethyl)-1,2-dihydro-indazol-3-one Investigative T00140 DRUGINFO D0L4TM 2-(3-Phenyl-propyl)-1,2-dihydro-indazol-3-one Investigative T00140 DRUGINFO D0X8BS 2-(4-Butoxy-phenoxy)-N-hydroxy-acetamide Investigative T00140 DRUGINFO D0T0CY 2-(4-Butoxy-phenoxy)-N-hydroxy-N-methyl-acetamide Investigative T00140 DRUGINFO D0N6CN 2-(4-Butoxy-phenoxy)-N-hydroxy-propionamide Investigative T00140 DRUGINFO D0IF2H 2-(4-Butoxy-phenyl)-N-hydroxy-N-methyl-acetamide Investigative T00140 DRUGINFO D0WW1K 2-(4-hydroxylphenyl)-3-(3,5-dihydroxylphenyl) propenoic acid (NNU-hdpa) Investigative T00140 DRUGINFO D05PHI 2-(4-Methoxy-phenyl)-5-phenyl-thiazol-4-ol Investigative T00140 DRUGINFO D08MCE 2-(4-Phenyl-butyl)-1,2-dihydro-indazol-3-one Investigative T00140 DRUGINFO D0J7YU 2-Benzyl-1,2-dihydro-indazol-3-one Investigative T00140 DRUGINFO D02HQK 2-Biphenyl-4-yl-N-hydroxy-N-methyl-acetamide Investigative T00140 DRUGINFO D0SJ3W 2-Furan-2-ylmethyl-1,2-dihydro-indazol-3-one Investigative T00140 DRUGINFO D0U8CM 2-Methyl-1,2-dihydro-indazol-3-one Investigative T00140 DRUGINFO D0F1ZE 2-Naphthalen-1-ylmethyl-1,2-dihydro-indazol-3-one Investigative T00140 DRUGINFO D0X6SA 2-Naphthalen-2-ylmethyl-1,2-dihydro-indazol-3-one Investigative T00140 DRUGINFO D0PD7X 2'-Nitro-biphenyl-4-carboxylic acid hydroxyamide Investigative T00140 DRUGINFO D06HUQ 2-Phenethyl-1,2-dihydro-indazol-3-one Investigative T00140 DRUGINFO D0S0PB 2-Phenyl-1,2-dihydro-indazol-3-one Investigative T00140 DRUGINFO D05KCN 2-Pyridin-2-ylmethyl-1,2-dihydro-indazol-3-one Investigative T00140 DRUGINFO D0HZ9X 2-Pyridin-3-ylmethyl-1,2-dihydro-indazol-3-one Investigative T00140 DRUGINFO D0Z5XD 2-Pyridin-4-ylmethyl-1,2-dihydro-indazol-3-one Investigative T00140 DRUGINFO D0XQ8P 2-Thiazol-5-ylmethyl-1,2-dihydro-indazol-3-one Investigative T00140 DRUGINFO D0X9RM 2-Thiophen-2-ylmethyl-1,2-dihydro-indazol-3-one Investigative T00140 DRUGINFO D08UXT 3-(4-Butoxy-phenyl)-N-hydroxy-N-methyl-acrylamide Investigative T00140 DRUGINFO D0S8UP 3,4-Dihydroxy-10H-anthracen-9-one Investigative T00140 DRUGINFO D05RIE 3-Benzoyl-N-hydroxy-benzamide Investigative T00140 DRUGINFO D09WYM 3-Biphenyl-3-yl-N-hydroxy-N-methyl-acrylamide Investigative T00140 DRUGINFO D02TLZ 3-Biphenyl-4-yl-N-hydroxy-N-methyl-acrylamide Investigative T00140 DRUGINFO D08NDV 4-(1H-indol-3-yl)-1-morpholinobutan-1-one Investigative T00140 DRUGINFO D0S6XY 4,5-Dihydroxy-10H-anthracen-9-one Investigative T00140 DRUGINFO D08BNV 4,5-Dimethoxy-10H-anthracen-9-one Investigative T00140 DRUGINFO D0J7AM 4-Bromo-N-hydroxy-benzamide Investigative T00140 DRUGINFO D02RBU 4-Butoxy-N-hydroxy-N-methyl-benzamide Investigative T00140 DRUGINFO D01QDG 4-Hydroxy-5-methoxy-10H-anthracen-9-one Investigative T00140 DRUGINFO D0R2XE 4-Pentadeca-1,3,6-trienylsulfanyl-butyric acid Investigative T00140 DRUGINFO D0AS0V 5,8-Dihydroxy-1,4-naphthoquinone Investigative T00140 DRUGINFO D0U9UL 5-Chloro-N-(4-ethylphenyl)benzo[d]oxazol-2-amine Investigative T00140 DRUGINFO D08HFK 5-Chloro-N-phenylbenzo[d]oxazol-2-amine Investigative T00140 DRUGINFO D0XL5D 5-Methoxy-N-phenylbenzo[d]oxazol-2-amine Investigative T00140 DRUGINFO D04IFV 5-Methyl-2-p-tolyl-thiazol-4-ol Investigative T00140 DRUGINFO D0H4MV 5-Methyl-N-phenylbenzo[d]oxazol-2-amine Investigative T00140 DRUGINFO D07CJR 5S-HETE Investigative T00140 DRUGINFO D02COM 7-tert-butyl-2, 3-dihydro-3, 3-dimethyl substituted dihydrofuran 30 (DHDMBF30) Investigative T00140 DRUGINFO D0NS1S ACACETIN Investigative T00140 DRUGINFO D09CXQ Acanthus ilicifolius Linn Investigative T00140 DRUGINFO D0C1XI Acetic acid 2-phenyl-5-propyl-thiazol-4-yl ester Investigative T00140 DRUGINFO D0G3VE Acetic acid 5-butyl-2-phenyl-thiazol-4-yl ester Investigative T00140 DRUGINFO D0CT9V Anthracene-2-carboxylic acid hydroxyamide Investigative T00140 DRUGINFO D0C6BU ANTHRONE Investigative T00140 DRUGINFO D05QBX Biphenyl-3-carboxylic acid hydroxyamide Investigative T00140 DRUGINFO D04XPJ Biphenyl-4-carboxylic acid hydroxyamide Investigative T00140 DRUGINFO D0O7SM BUDDLEDIN A Investigative T00140 DRUGINFO D03QNE BW A360C Investigative T00140 DRUGINFO D0PU1J BW B218C Investigative T00140 DRUGINFO D0R2MQ BW-858C Investigative T00140 DRUGINFO D0M6UM BW-A137C Investigative T00140 DRUGINFO D0U2YL CGS-23885 Investigative T00140 DRUGINFO D0J5OV Chebulagic acid Investigative T00140 DRUGINFO D0K3AO CYLINDOL A Investigative T00140 DRUGINFO D00MIM FR-122788 Investigative T00140 DRUGINFO D0UU1I Heme Investigative T00140 DRUGINFO D0T8TS Hexanoic acid 2,5-diphenyl-thiazol-4-yl ester Investigative T00140 DRUGINFO D09VTJ Hyperforin Investigative T00140 DRUGINFO D0F4HT ICI-211965 Investigative T00140 DRUGINFO D00OWE L-652,343 Investigative T00140 DRUGINFO D0E3CO N-(2-Ethylphenyl)-5-methylbenzo[d]oxazol-2-amine Investigative T00140 DRUGINFO D0C4KD N-(3-Bromophenyl)-5-methoxybenzo[d]oxazol-2-amine Investigative T00140 DRUGINFO D07XMM N-(4-Ethylphenyl)-5-methylbenzo[d]oxazol-2-amine Investigative T00140 DRUGINFO D05GZI N-(4-Ethylphenyl)benzo[d]oxazol-2-amine Investigative T00140 DRUGINFO D04UJI Naphthalene-2-carboxylic acid hydroxyamide Investigative T00140 DRUGINFO D0I9RY N-Hydroxy-2-methyl-3-naphthalen-2-yl-acrylamide Investigative T00140 DRUGINFO D0KB6Q N-Hydroxy-2-naphthalen-2-yl-acetamide Investigative T00140 DRUGINFO D09PDD N-Hydroxy-3-naphthalen-2-yl-acrylamide Investigative T00140 DRUGINFO D0T1HY N-Hydroxy-3-naphthalen-2-yl-N-phenyl-acrylamide Investigative T00140 DRUGINFO D06AFD N-Hydroxy-3-naphthalen-2-yl-N-p-tolyl-acrylamide Investigative T00140 DRUGINFO D0H7UQ N-Hydroxy-3-naphthalen-2-yl-propionamide Investigative T00140 DRUGINFO D07MYE N-Hydroxy-3-phenyl-acrylamide Investigative T00140 DRUGINFO D03HNC N-hydroxy-4-(naphthalen-1-yl)benzamide Investigative T00140 DRUGINFO D06MUA N-Hydroxy-4-iodo-benzamide Investigative T00140 DRUGINFO D0L3BQ N-Hydroxy-4-isobutyl-benzamide Investigative T00140 DRUGINFO D0K7XU N-Hydroxy-4-naphthalen-2-yl-benzamide Investigative T00140 DRUGINFO D0K7XQ N-hydroxy-N-[1-(4-isobutylphenyl)ethyl]urea Investigative T00140 DRUGINFO D06GRW N-Hydroxy-N-methyl-2,3,3-triphenyl-acrylamide Investigative T00140 DRUGINFO D07PCS N-Hydroxy-N-methyl-2-naphthalen-2-yl-propionamide Investigative T00140 DRUGINFO D0V8UV N-Hydroxy-N-methyl-3-naphthalen-1-yl-acrylamide Investigative T00140 DRUGINFO D0E4JU N-Hydroxy-N-methyl-3-naphthalen-2-yl-acrylamide Investigative T00140 DRUGINFO D06KQD N-Hydroxy-N-methyl-3-naphthalen-2-yl-propionamide Investigative T00140 DRUGINFO D0C7GT N-Hydroxy-N-methyl-3-phenanthren-2-yl-acrylamide Investigative T00140 DRUGINFO D0E1NK N-Hydroxy-N-methyl-3-phenanthren-3-yl-acrylamide Investigative T00140 DRUGINFO D0O6OJ N-Hydroxy-N-methyl-3-phenanthren-9-yl-acrylamide Investigative T00140 DRUGINFO D0A2QP N-Hydroxy-N-methyl-benzamide Investigative T00140 DRUGINFO D00JPV N-Phenylbenzo[d]oxazol-2-amine Investigative T00140 DRUGINFO D0DP9F Phenanthrene-2-carboxylic acid hydroxyamide Investigative T00140 DRUGINFO D04ZGR Phenanthrene-3-carboxylic acid hydroxyamide Investigative T00140 DRUGINFO D0P1LP PHENIDONE Investigative T00140 DRUGINFO D06TPF PYROGALLOL Investigative T00140 DRUGINFO D0Z0ZM SB-202235 Investigative T00140 DRUGINFO D00XKA SC-41661A Investigative T00140 DRUGINFO D07LMV SK&F 107649 Investigative T00140 DRUGINFO D01SQY TZI-41127 Investigative T00140 KEGGPATH hsa00590:Arachidonic acid metabolism T00140 KEGGPATH hsa01100:Metabolic pathways T00140 KEGGPATH hsa04726:Serotonergic synapse T00140 KEGGPATH hsa04913:Ovarian steroidogenesis T00140 KEGGPATH hsa05145:Toxoplasmosis T00140 WIKIPATH WP15:Selenium Micronutrient Network T00140 WIKIPATH WP167:Eicosanoid Synthesis T00140 WIKIPATH WP2650:Arachidonic acid metabolism T00140 WIKIPATH WP2877:Vitamin D Receptor Pathway T00140 WHIZPATH PW000044:Arachidonic Acid Metabolism T00140 NET_PATH NetPath_16:IL4 Signaling Pathway T00140 BIOCPATH PWY66-375:Leukotriene biosynthesis T00140 BIOCPATH PWY66-392:Lipoxin biosynthesis T00140 BIOCPATH PWY66-393:Aspirin-triggered lipoxin biosynthesis T00140 BIOCPATH PWY66-394:Aspirin triggered resolvin E biosynthesis T00140 BIOCPATH PWY66-395:Aspirin triggered resolvin D biosynthesis T00140 BIOCPATH PWY66-397:Resolvin D biosynthesis T57700 TARGETID T57700 T57700 FORMERID TTDS00270 T57700 UNIPROID KIT_HUMAN T57700 TARGNAME Tyrosine-protein kinase Kit (KIT) T57700 GENENAME KIT T57700 TARGTYPE Successful target T57700 SYNONYMS v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog; p145 c-kit; Proto-oncogene tyrosine-protein kinase Kit; Proto-oncogene c-Kit; Piebald trait protein; PBT; Mast/stem cell growth factor receptor Kit; CD117 antigen; CD117; C-kit T57700 FUNCTION In response to KITLG/SCF binding, KIT can activate several signaling pathways. Phosphorylates PIK3R1, PLCG1, SH2B2/APS and CBL. Activates the AKT1 signaling pathway by phosphorylation of PIK3R1, the regulatory subunit of phosphatidylinositol 3-kinase. Activated KIT also transmits signals via GRB2 and activation of RAS, RAF1 and the MAP kinases MAPK1/ERK2 and/or MAPK3/ERK1. Promotes activation of STAT family members STAT1, STAT3, STAT5A and STAT5B. Activation of PLCG1 leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate. KIT signaling is modulated by protein phosphatases, and by rapid internalization and degradation of the receptor. Activated KIT promotes phosphorylation of the protein phosphatases PTPN6/SHP-1 and PTPRU, and of the transcription factors STAT1, STAT3, STAT5A and STAT5B. Promotes phosphorylation of PIK3R1, CBL, CRK (isoform Crk-II), LYN, MAPK1/ERK2 and/or MAPK3/ERK1, PLCG1, SRC and SHC1. Tyrosine-protein kinase that acts as cell-surface receptor for the cytokine KITLG/SCF and plays an essential role in the regulation of cell survival and proliferation, hematopoiesis, stem cell maintenance, gametogenesis, mast cell development, migration and function, and in melanogenesis. T57700 PDBSTRUC 6GQM; 6GQL; 6GQK; 6GQJ; 4U0I T57700 BIOCLASS Kinase T57700 ECNUMBER EC 2.7.10.1 T57700 SEQUENCE MRGARGAWDFLCVLLLLLRVQTGSSQPSVSPGEPSPPSIHPGKSDLIVRVGDEIRLLCTDPGFVKWTFEILDETNENKQNEWITEKAEATNTGKYTCTNKHGLSNSIYVFVRDPAKLFLVDRSLYGKEDNDTLVRCPLTDPEVTNYSLKGCQGKPLPKDLRFIPDPKAGIMIKSVKRAYHRLCLHCSVDQEGKSVLSEKFILKVRPAFKAVPVVSVSKASYLLREGEEFTVTCTIKDVSSSVYSTWKRENSQTKLQEKYNSWHHGDFNYERQATLTISSARVNDSGVFMCYANNTFGSANVTTTLEVVDKGFINIFPMINTTVFVNDGENVDLIVEYEAFPKPEHQQWIYMNRTFTDKWEDYPKSENESNIRYVSELHLTRLKGTEGGTYTFLVSNSDVNAAIAFNVYVNTKPEILTYDRLVNGMLQCVAAGFPEPTIDWYFCPGTEQRCSASVLPVDVQTLNSSGPPFGKLVVQSSIDSSAFKHNGTVECKAYNDVGKTSAYFNFAFKGNNKEQIHPHTLFTPLLIGFVIVAGMMCIIVMILTYKYLQKPMYEVQWKVVEEINGNNYVYIDPTQLPYDHKWEFPRNRLSFGKTLGAGAFGKVVEATAYGLIKSDAAMTVAVKMLKPSAHLTEREALMSELKVLSYLGNHMNIVNLLGACTIGGPTLVITEYCCYGDLLNFLRRKRDSFICSKQEDHAEAALYKNLLHSKESSCSDSTNEYMDMKPGVSYVVPTKADKRRSVRIGSYIERDVTPAIMEDDELALDLEDLLSFSYQVAKGMAFLASKNCIHRDLAARNILLTHGRITKICDFGLARDIKNDSNYVVKGNARLPVKWMAPESIFNCVYTFESDVWSYGIFLWELFSLGSSPYPGMPVDSKFYKMIKEGFRMLSPEHAPAEMYDIMKTCWDADPLKRPTFKQIVQLIEKQISESTNHIYSNLANCSPNRQKPVVDHSVRINSVGSTASSSQPLLVHDDV T57700 DRUGINFO D0AZ3C Imatinib Approved T57700 DRUGINFO D0F0ZY Pazopanib HCl Approved T57700 DRUGINFO D09TAB Pexidartinib Approved T57700 DRUGINFO D0H0EQ Ponatinib Approved T57700 DRUGINFO D09GDD Regorafenib Approved T57700 DRUGINFO D09AAK Ripretinib Approved T57700 DRUGINFO D01PZD Romiplostim Approved T57700 DRUGINFO D0W5HK Sorafenib Approved T57700 DRUGINFO D0Z6MT Famitinib Phase 2 T57700 DRUGINFO D0T1GF MP470 Phase 2 T57700 DRUGINFO D00NSD XL-820 Phase 2 T57700 DRUGINFO D03MDY PLX9486 Phase 1/2 T57700 DRUGINFO D05CFQ AMG-191 Phase 1 T57700 DRUGINFO D0E0SH CART-117 cells Phase 1 T57700 DRUGINFO D0N8RV OSI-930 Phase 1 T57700 DRUGINFO D0D3FB PMID25656651-Compound-21a Patented T57700 DRUGINFO D0XQ5F PMID25656651-Compound-21b Patented T57700 DRUGINFO D0AK1F Pyridine derivative 18 Patented T57700 DRUGINFO D0T7BE Pyridine derivative 19 Patented T57700 DRUGINFO D0NB1V Pyridine derivative 20 Patented T57700 DRUGINFO D0O0AW Pyridine derivative 21 Patented T57700 DRUGINFO D0O4TA Pyridine derivative 22 Patented T57700 DRUGINFO D00DQX Motesanib Discontinued in Phase 3 T57700 DRUGINFO D0TS2B CAR-T cells targeting CD117 Preclinical T57700 DRUGINFO D0Y9GK 4-(4-aminophenyl)-1H-indazol-3yl-amine Investigative T57700 DRUGINFO D05FFB 5,11-Dimethyl-6H-pyrido[4,3-b]carbazol-9-ol Investigative T57700 DRUGINFO D08ZWJ 9-Bromo-5,11-dimethyl-6H-pyrido[4,3-b]carbazole Investigative T57700 DRUGINFO D0T4SL 9-Methoxy-5,11-dimethyl-6H-pyrido[4,3-b]carbazole Investigative T57700 DRUGINFO D0T2UB APCK-110 Investigative T57700 DRUGINFO D0N7AJ AST-487 Investigative T57700 DRUGINFO D0I3XZ Bis-(5-hydroxy-1H-indol-2-yl)-methanone Investigative T57700 DRUGINFO D05QBZ CP-673451 Investigative T57700 DRUGINFO D0UN9O GTP-14564 Investigative T57700 DRUGINFO D0Y4BL JNJ-28312141 Investigative T57700 DRUGINFO D08BJR Ki-20227 Investigative T57700 DRUGINFO D0P3JW PD-0166326 Investigative T57700 DRUGINFO D0GW4Q PD-0173956 Investigative T57700 DRUGINFO D0T5OS Phosphonotyrosine Investigative T57700 DRUGINFO D0C2GE PMID22765894C8h Investigative T57700 DRUGINFO D0BL0O PMID23521020C7k Investigative T57700 DRUGINFO D03SGF WBZ-7 Investigative T57700 KEGGPATH hsa04014:Ras signaling pathway T57700 KEGGPATH hsa04015:Rap1 signaling pathway T57700 KEGGPATH hsa04060:Cytokine-cytokine receptor interaction T57700 KEGGPATH hsa04144:Endocytosis T57700 KEGGPATH hsa04151:PI3K-Akt signaling pathway T57700 KEGGPATH hsa04640:Hematopoietic cell lineage T57700 KEGGPATH hsa04916:Melanogenesis T57700 KEGGPATH hsa05200:Pathways in cancer T57700 KEGGPATH hsa05221:Acute myeloid leukemia T57700 KEGGPATH hsa05230:Central carbon metabolism in cancer T57700 WIKIPATH WP2002:miR-targeted genes in epithelium - TarBase T57700 WIKIPATH WP2004:miR-targeted genes in lymphocytes - TarBase T57700 WIKIPATH WP2005:miR-targeted genes in muscle cell - TarBase T57700 WIKIPATH WP2406:Cardiac Progenitor Differentiation T57700 WIKIPATH WP2653:PIP3 activates AKT signaling T57700 WIKIPATH WP2713:Signaling by SCF-KIT T57700 WIKIPATH WP2848:Differentiation Pathway T57700 WIKIPATH WP304:Kit receptor signaling pathway T57700 REACPATH R-HSA-1257604:PIP3 activates AKT signaling T57700 REACPATH R-HSA-1433559:Regulation of KIT signaling T57700 REACPATH R-HSA-2219530:Constitutive Signaling by Aberrant PI3K in Cancer T57700 REACPATH R-HSA-5673001:RAF/MAP kinase cascade T57700 NET_PATH NetPath_15:IL3 Signaling Pathway T57700 NET_PATH NetPath_16:IL4 Signaling Pathway T57700 NET_PATH NetPath_6:KitReceptor Signaling Pathway T57700 INTEPATH cmyb_pathway:C-MYB transcription factor network T57700 INTEPATH kitpathway:Signaling events mediated by Stem cell factor receptor (c-Kit) T85943 TARGETID T85943 T85943 FORMERID TTDS00247 T85943 UNIPROID SRC_HUMAN T85943 TARGNAME Proto-oncogene c-Src (SRC) T85943 GENENAME SRC T85943 TARGTYPE Successful target T85943 SYNONYMS pp60c-src; Tyrosine kinase (pp60(src)); Src tyrosine kinase; SRC1; Proto-oncogene tyrosine-protein kinase Src; Pp60(src); P60-Src; C-src TK; C-Src T85943 FUNCTION Participates in signaling pathways that control a diverse spectrum of biological activities including gene transcription, immune response, cell adhesion, cell cycle progression, apoptosis, migration, and transformation. Due to functional redundancy between members of the SRC kinase family, identification of the specific role of each SRC kinase is very difficult. SRC appears to be one of the primary kinases activated following engagement of receptors and plays a role in the activation of other protein tyrosine kinase (PTK) families. Receptor clustering or dimerization leads to recruitment of SRC to the receptor complexes where it phosphorylates the tyrosine residues within the receptor cytoplasmic domains. Plays an important role in the regulation of cytoskeletal organization through phosphorylation of specific substrates such as AFAP1. Phosphorylation of AFAP1 allows the SRC SH2 domain to bind AFAP1 and to localize to actin filaments. Cytoskeletal reorganization is also controlled through the phosphorylation of cortactin (CTTN). When cells adhere via focal adhesions to the extracellular matrix, signals are transmitted by integrins into the cell resulting in tyrosine phosphorylation of a number of focal adhesion proteins, including PTK2/FAK1 and paxillin (PXN). In addition to phosphorylating focal adhesion proteins, SRC is also active at the sites of cell-cell contact adherens junctions and phosphorylates substrates such as beta-catenin (CTNNB1), delta-catenin (CTNND1), and plakoglobin (JUP). Another type of cell-cell junction, the gap junction, is also a target for SRC, which phosphorylates connexin-43 (GJA1). SRC is implicated in regulation of pre-mRNA-processing and phosphorylates RNA-binding proteins such as KHDRBS1. Also plays a role in PDGF-mediated tyrosine phosphorylation of both STAT1 and STAT3, leading to increased DNA binding activity of these transcription factors. Involved in the RAS pathway through phosphorylation of RASA1 and RASGRF1. Plays a role in EGF-mediated calcium-activated chloride channel activation. Required for epidermal growth factor receptor (EGFR) internalization through phosphorylation of clathrin heavy chain (CLTC and CLTCL1) at 'Tyr-1477'. Involved in beta-arrestin (ARRB1 and ARRB2) desensitization through phosphorylation and activation of GRK2, leading to beta-arrestin phosphorylation and internalization. Has a critical role in the stimulation of the CDK20/MAPK3 mitogen-activated protein kinase cascade by epidermal growth factor. Might be involved not only in mediating the transduction of mitogenic signals at the level of the plasma membrane but also in controlling progression through the cell cycle via interaction with regulatory proteins in the nucleus. Plays an important role in osteoclastic bone resorption in conjunction with PTK2B/PYK2. Both the formation of a SRC-PTK2B/PYK2 complex and SRC kinase activity are necessary for this function. Recruited to activated integrins by PTK2B/PYK2, thereby phosphorylating CBL, which in turn induces the activation and recruitment of phosphatidylinositol 3-kinase to the cell membrane in a signaling pathway that is critical for osteoclast function. Promotes energy production in osteoclasts by activating mitochondrial cytochrome C oxidase. Phosphorylates DDR2 on tyrosine residues, thereby promoting its subsequent autophosphorylation. Phosphorylates RUNX3 and COX2 on tyrosine residues, TNK2 on 'Tyr-284' and CBL on 'Tyr-731'. Enhances DDX58/RIG-I-elicited antiviral signaling. Phosphorylates PDPK1 at 'Tyr-9', 'Tyr-373' and 'Tyr-376'. Phosphorylates BCAR1 at 'Tyr-128'. Phosphorylates CBLC at multiple tyrosine residues, phosphorylation at 'Tyr-341' activates CBLC E3 activity. Involved in anchorage-independent cell growth. Required for podosome formation. Non-receptor protein tyrosine kinase which is activated following engagement of many different classes of cellular receptors including immune response receptors, integrins and other adhesion receptors, receptor protein tyrosine kinases, G protein-coupled receptors as well as cytokine receptors. T85943 PDBSTRUC 6EHJ; 6C4S; 6ATE; 4MXZ; 4MXY T85943 BIOCLASS Kinase T85943 ECNUMBER EC 2.7.10.2 T85943 SEQUENCE MGSNKSKPKDASQRRRSLEPAENVHGAGGGAFPASQTPSKPASADGHRGPSAAFAPAAAEPKLFGGFNSSDTVTSPQRAGPLAGGVTTFVALYDYESRTETDLSFKKGERLQIVNNTEGDWWLAHSLSTGQTGYIPSNYVAPSDSIQAEEWYFGKITRRESERLLLNAENPRGTFLVRESETTKGAYCLSVSDFDNAKGLNVKHYKIRKLDSGGFYITSRTQFNSLQQLVAYYSKHADGLCHRLTTVCPTSKPQTQGLAKDAWEIPRESLRLEVKLGQGCFGEVWMGTWNGTTRVAIKTLKPGTMSPEAFLQEAQVMKKLRHEKLVQLYAVVSEEPIYIVTEYMSKGSLLDFLKGETGKYLRLPQLVDMAAQIASGMAYVERMNYVHRDLRAANILVGENLVCKVADFGLARLIEDNEYTARQGAKFPIKWTAPEAALYGRFTIKSDVWSFGILLTELTTKGRVPYPGMVNREVLDQVERGYRMPCPPECPESLHDLMCQCWRKEPEERPTFEYLQAFLEDYFTSTEPQYQPGENL T85943 DRUGINFO D0OB0F Bosutinib Approved T85943 DRUGINFO D0E6XR Dasatinib Approved T85943 DRUGINFO D07DIM Herbimycin A Approved T85943 DRUGINFO D03MNN SKI-758 Approved T85943 DRUGINFO D0G2CG AL3818 Phase 3 T85943 DRUGINFO D0J1GR CP-868596 Phase 3 T85943 DRUGINFO D0TY3L KX-01 Phase 3 T85943 DRUGINFO D0MW0N Masitinib Phase 3 T85943 DRUGINFO D0M0XB Saracatinib Phase 2 T85943 DRUGINFO DS7CY4 TPX-0046 Phase 1/2 T85943 DRUGINFO D06CIJ ISIS-CRP Phase 1 T85943 DRUGINFO D0RE4L KX2-361 Phase 1 T85943 DRUGINFO D05YEI SUN-K0706 Phase 1 T85943 DRUGINFO D7M8LI TPX-0022 Phase 1 T85943 DRUGINFO D0QD5Y Aromatic bicyclic compound 1 Patented T85943 DRUGINFO D0VI7E Aromatic bicyclic compound 2 Patented T85943 DRUGINFO D0M5AG Aromatic bicyclic compound 3 Patented T85943 DRUGINFO D0M9YZ Aromatic bicyclic compound 4 Patented T85943 DRUGINFO D0Q5JV Aromatic bicyclic compound 5 Patented T85943 DRUGINFO D09RTW Aromatic bicyclic compound 6 Patented T85943 DRUGINFO D02VDD Deuterated 3-cyanoquinoline derivative 1 Patented T85943 DRUGINFO D07QBF PMID28460551-Compound-6 Patented T85943 DRUGINFO D0AK1F Pyridine derivative 18 Patented T85943 DRUGINFO D09WPN AP22408 Terminated T85943 DRUGINFO D0H8KG PD166285 Terminated T85943 DRUGINFO D0R2AT 2-(4-CARCOXY-5-ISOPROPYLTHIAZOLYL)BENZOPIPERIDINE Investigative T85943 DRUGINFO D0P5ST 3-(3-aminobenzo[e][1,2,4]triazin-7-yl)phenol Investigative T85943 DRUGINFO D0OG1Q 4-Chloro-5,7-diphenyl-7H-pyrrolo[2,3-d]pyrimidine Investigative T85943 DRUGINFO D0H3XF 5,7-Diphenyl-7H-pyrrolo[2,3-d]pyrimidin-4-ol Investigative T85943 DRUGINFO D07RQB 7-(naphthalen-2-yl)benzo[e][1,2,4]triazin-3-amine Investigative T85943 DRUGINFO D0BS6R A-420983 Investigative T85943 DRUGINFO D06WGX A-770041 Investigative T85943 DRUGINFO D0K9TT Ac-Cys-Ile-cyclo[Phe-Lys]-Tyr-Tyr Investigative T85943 DRUGINFO D08AWZ Ac-Cys-Ile-Phe(4-NO2)-Lys-Phe(4-NO2)-Tyr Investigative T85943 DRUGINFO D0U1BA Ac-Cys-Ile-Phe(4-NO2)-Lys-Tyr-Phe(4-NO2) Investigative T85943 DRUGINFO D0A5IW Ac-Cys-Ile-Phe(4-NO2)-Lys-Tyr-Tyr Investigative T85943 DRUGINFO D00JID Ac-Cys-Ile-Tyr-Lys-Phe(4-Cl)-Tyr Investigative T85943 DRUGINFO D0O8BX Ac-Cys-Ile-Tyr-Lys-Phe(4-CN)-Tyr Investigative T85943 DRUGINFO D04QEW Ac-Cys-Ile-Tyr-Lys-Phe(4-I)-Tyr Investigative T85943 DRUGINFO D08YUQ Ac-Cys-Ile-Tyr-Lys-Phe(4-N3)-Tyr Investigative T85943 DRUGINFO D06MYD Ac-Cys-Ile-Tyr-Lys-Phe(4-NO2)-Phe(4-NO2) Investigative T85943 DRUGINFO D0GN1A Ac-Cys-Ile-Tyr-Lys-Phe(4-NO2)-Tyr-Phe Investigative T85943 DRUGINFO D0LK4J Ac-Cys-Ile-Tyr-Lys-Tyr-Phe(4-NO2) Investigative T85943 DRUGINFO D0D3RL AP-24163 Investigative T85943 DRUGINFO D0D8OY AP-24226 Investigative T85943 DRUGINFO D04QUI BAS-00387275 Investigative T85943 DRUGINFO D01GNF BAS-00387328 Investigative T85943 DRUGINFO D03GQI BAS-00387347 Investigative T85943 DRUGINFO D07LYJ BAS-00672722 Investigative T85943 DRUGINFO D0P2QG BAS-01047341 Investigative T85943 DRUGINFO D0LP2M BAS-01047655 Investigative T85943 DRUGINFO D0D8ZN BAS-01373578 Investigative T85943 DRUGINFO D08WEV BAS-0338868 Investigative T85943 DRUGINFO D09QKH BAS-0338872 Investigative T85943 DRUGINFO D0A5MG BAS-09534324 Investigative T85943 DRUGINFO D0J4RY BAS-450225 Investigative T85943 DRUGINFO D01IDD BAS-4844343 Investigative T85943 DRUGINFO D03OKV BMS-279700 Investigative T85943 DRUGINFO D06QUQ CGP 77675 Investigative T85943 DRUGINFO D0M9QM CGP-191 Investigative T85943 DRUGINFO D0BU6T CGP-62464 Investigative T85943 DRUGINFO D0W6WU Cyclo[Ac-Cys-Ile-Phe]-Lys-Tyr-Tyr Investigative T85943 DRUGINFO D0OB0M Cyclo[Ac-Cys-Ile-Tyr-Lys-Tyr-Phe] Investigative T85943 DRUGINFO D0MI2W Cyclo[Ac-Cys-Ile-Tyr-Lys-Tyr-Tyr] Investigative T85943 DRUGINFO D0V6UC Cysteine Sulfenic Acid Investigative T85943 DRUGINFO D0N4FS DPI59 Investigative T85943 DRUGINFO D00TVY Glu-Pro-Gln-F2Pmp-Glu-Glu-Ile-Pro-Ile-Tyr-Leu Investigative T85943 DRUGINFO D06CYG Glu-Pro-Gln-pTyr-Glu-Glu-Ile-Pro-Ile-Tyr-Leu Investigative T85943 DRUGINFO D0D5EW HKI-9924129 Investigative T85943 DRUGINFO D05YQC ISO24 Investigative T85943 DRUGINFO D0YZ7H JNJ-10198409 Investigative T85943 DRUGINFO D0Q7TO K00244 Investigative T85943 DRUGINFO D0N8TQ N-(4-(phenylamino)quinazolin-6-yl)acrylamide Investigative T85943 DRUGINFO D03DEX N6-Benzyl Adenosine-5'-Diphosphate Investigative T85943 DRUGINFO D0X7IC NG-25 Investigative T85943 DRUGINFO D0GT8N NM-PP1 Investigative T85943 DRUGINFO D0S3FW N-Phenyl-5-phenylimidazo[1,5-a]pyrazin-8-amine Investigative T85943 DRUGINFO D0U7BY Oxalic Acid Investigative T85943 DRUGINFO D07HBR PAS219 Investigative T85943 DRUGINFO D09WNM PASBN Investigative T85943 DRUGINFO D0P3JW PD-0166326 Investigative T85943 DRUGINFO D0S1KJ PD-0173952 Investigative T85943 DRUGINFO D03NPX PD-0173955 Investigative T85943 DRUGINFO D0GW4Q PD-0173956 Investigative T85943 DRUGINFO D0Z7GH PD-0173958 Investigative T85943 DRUGINFO D0OH3J PD-0179483 Investigative T85943 DRUGINFO D0VF6E PD173074 Investigative T85943 DRUGINFO D03XDN PD-174265 Investigative T85943 DRUGINFO D0S9LT Phenylphosphate Investigative T85943 DRUGINFO D0T5OS Phosphonotyrosine Investigative T85943 DRUGINFO D08RZB PMID15546730C2 Investigative T85943 DRUGINFO D0C2GE PMID22765894C8h Investigative T85943 DRUGINFO D03EHM PP121 Investigative T85943 DRUGINFO D0R7BX RU78191 Investigative T85943 DRUGINFO D0AJ4T RU78262 Investigative T85943 DRUGINFO D0D1FK RU78299 Investigative T85943 DRUGINFO D02HOG RU78300 Investigative T85943 DRUGINFO D0M5RA RU78783 Investigative T85943 DRUGINFO D0U8UH RU79072 Investigative T85943 DRUGINFO D0U5KF RU79073 Investigative T85943 DRUGINFO D09NGN RU79256 Investigative T85943 DRUGINFO D0KS2T RU81843 Investigative T85943 DRUGINFO D02IYN RU82129 Investigative T85943 DRUGINFO D03NCK RU82197 Investigative T85943 DRUGINFO D0TC1E RU82209 Investigative T85943 DRUGINFO D0R1PD RU83876 Investigative T85943 DRUGINFO D0L4NP RU84687 Investigative T85943 DRUGINFO D02TIO RU85053 Investigative T85943 DRUGINFO D05GYO RU85493 Investigative T85943 DRUGINFO D01JJR RU90395 Investigative T85943 DRUGINFO D03YUW SBB007833 Investigative T85943 DRUGINFO D0D9PD SKS-927 Investigative T85943 DRUGINFO D0CE3R SU 6656 Investigative T85943 DRUGINFO D0H1OK TG-100435 Investigative T85943 DRUGINFO D0Y1SR WH-4-023 Investigative T85943 DRUGINFO D01IZN Y-c[D-Pen-(2')Nal-GSFC]KR-NH2 Investigative T85943 DRUGINFO D09DVB Y-c[D-Pen-(2R,3R)-2-Me-(2')Nal-GSFC]KR-NH2 Investigative T85943 DRUGINFO D0B4PI Y-c[D-Pen-(2R,3S)-2-Me-(2')Nal-GSFC]KR-NH2 Investigative T85943 DRUGINFO D0Q2UZ Y-c[D-Pen-(2S,3R)-2-Me-(2')Nal-GSFC]KR-NH2 Investigative T85943 DRUGINFO D0W7LW Y-c[D-Pen-(2S,3S)-2-Me-(2')Nal-GSFC]KR-NH2 Investigative T85943 DRUGINFO D07ERV Y-c[D-Pen-(3,5-diI)Tyr-GSFC]KR-NH2 Investigative T85943 DRUGINFO D0A2LX Y-c[D-Pen-(3-I)Tyr-GSFC]KR-NH2 Investigative T85943 DRUGINFO D02SRA Y-c[D-Pen-D-(2')Nal-GSFC]KR-NH2 Investigative T85943 KEGGPATH hsa04012:ErbB signaling pathway T85943 KEGGPATH hsa04015:Rap1 signaling pathway T85943 KEGGPATH hsa04062:Chemokine signaling pathway T85943 KEGGPATH hsa04144:Endocytosis T85943 KEGGPATH hsa04370:VEGF signaling pathway T85943 KEGGPATH hsa04510:Focal adhesion T85943 KEGGPATH hsa04520:Adherens junction T85943 KEGGPATH hsa04530:Tight junction T85943 KEGGPATH hsa04540:Gap junction T85943 KEGGPATH hsa04611:Platelet activation T85943 KEGGPATH hsa04727:GABAergic synapse T85943 KEGGPATH hsa04750:Inflammatory mediator regulation of TRP channels T85943 KEGGPATH hsa04810:Regulation of actin cytoskeleton T85943 KEGGPATH hsa04912:GnRH signaling pathway T85943 KEGGPATH hsa04915:Estrogen signaling pathway T85943 KEGGPATH hsa04917:Prolactin signaling pathway T85943 KEGGPATH hsa04919:Thyroid hormone signaling pathway T85943 KEGGPATH hsa04921:Oxytocin signaling pathway T85943 KEGGPATH hsa05100:Bacterial invasion of epithelial cells T85943 KEGGPATH hsa05120:Epithelial cell signaling in Helicobacter pylori infection T85943 KEGGPATH hsa05131:Shigellosis T85943 KEGGPATH hsa05152:Tuberculosis T85943 KEGGPATH hsa05161:Hepatitis B T85943 KEGGPATH hsa05203:Viral carcinogenesis T85943 KEGGPATH hsa05205:Proteoglycans in cancer T85943 WIKIPATH WP138:Androgen receptor signaling pathway T85943 WIKIPATH WP1539:Angiogenesis T85943 WIKIPATH WP185:Integrin-mediated Cell Adhesion T85943 WIKIPATH WP2018:RANKL/RANK Signaling Pathway T85943 WIKIPATH WP2034:Leptin signaling pathway T85943 WIKIPATH WP2035:FSH signaling pathway T85943 WIKIPATH WP2038:Regulation of Microtubule Cytoskeleton T85943 WIKIPATH WP2100:Arylhydrocarbon receptor (AhR) signaling pathway T85943 WIKIPATH WP2203:TSLP Signaling Pathway T85943 WIKIPATH WP2261:Signaling Pathways in Glioblastoma T85943 WIKIPATH WP2324:AGE/RAGE pathway T85943 WIKIPATH WP2332:Interleukin-11 Signaling Pathway T85943 WIKIPATH WP2374:Oncostatin M Signaling Pathway T85943 WIKIPATH WP2377:Integrated Pancreatic Cancer Pathway T85943 WIKIPATH WP2380:BDNF signaling pathway T85943 WIKIPATH WP244:Alpha 6 Beta 4 signaling pathway T85943 WIKIPATH WP2571:Polycystic Kidney Disease Pathway T85943 WIKIPATH WP2643:Nanoparticle-mediated activation of receptor signaling T85943 WIKIPATH WP286:IL-3 Signaling Pathway T85943 WIKIPATH WP2873:Aryl Hydrocarbon Receptor Pathway T85943 WIKIPATH WP2876:Pregnane X Receptor pathway T85943 WIKIPATH WP304:Kit receptor signaling pathway T85943 WIKIPATH WP313:Signaling of Hepatocyte Growth Factor Receptor T85943 WIKIPATH WP366:TGF beta Signaling Pathway T85943 WIKIPATH WP437:EGF/EGFR Signaling Pathway T85943 WIKIPATH WP581:EPO Receptor Signaling T85943 WIKIPATH WP61:Notch Signaling Pathway T85943 WIKIPATH WP615:Senescence and Autophagy in Cancer T85943 WIKIPATH WP673:ErbB Signaling Pathway T85943 NET_PATH NetPath_14:IL2 Signaling Pathway T85943 INTEPATH ajdiss_2pathway:Posttranslational regulation of adherens junction stability and dissassembly T85943 INTEPATH alphasynuclein_pathway:Alpha-synuclein signaling T85943 INTEPATH amb2_neutrophils_pathway:amb2 Integrin signaling T85943 INTEPATH ar_nongenomic_pathway:Nongenotropic Androgen signaling T85943 INTEPATH ar_tf_pathway:Regulation of Androgen receptor activity T85943 INTEPATH arf6_pathway:Arf6 signaling events T85943 INTEPATH avb3_integrin_pathway:Integrins in angiogenesis T85943 INTEPATH cdc42_pathway:CDC42 signaling events T85943 INTEPATH cxcr3pathway:CXCR3-mediated signaling events T85943 INTEPATH cxcr4_pathway:CXCR4-mediated signaling events T85943 INTEPATH ecadherin_keratinocyte_pathway:E-cadherin signaling in keratinocytes T85943 INTEPATH ecadherin_nascentaj_pathway:E-cadherin signaling in the nascent adherens junction T85943 INTEPATH endothelinpathway:Endothelins T85943 INTEPATH epha_fwdpathway:EPHA forward signaling T85943 INTEPATH epha2_fwdpathway:EPHA2 forward signaling T85943 INTEPATH ephbfwdpathway:EPHB forward signaling T85943 INTEPATH ephrinbrevpathway:Ephrin B reverse signaling T85943 INTEPATH er_nongenomic_pathway:Plasma membrane estrogen receptor signaling T85943 INTEPATH erbb1_downstream_pathway:ErbB1 downstream signaling T85943 INTEPATH erbb1_internalization_pathway:Internalization of ErbB1 T85943 INTEPATH erbb1_receptor_proximal_pathway:EGF receptor (ErbB1) signaling pathway T85943 INTEPATH erbb2erbb3pathway:ErbB2/ErbB3 signaling events T85943 INTEPATH fak_pathway:Signaling events mediated by focal adhesion kinase T85943 INTEPATH faspathway:FAS (CD95) signaling pathway T85943 INTEPATH fgf_pathway:FGF signaling pathway T85943 INTEPATH glypican_1pathway:Glypican 1 network T85943 INTEPATH integrin_a4b1_pathway:Alpha4 beta1 integrin signaling events T85943 INTEPATH integrin_a9b1_pathway:Alpha9 beta1 integrin signaling events T85943 INTEPATH lysophospholipid_pathway:LPA receptor mediated events T85943 INTEPATH met_pathway:Signaling events mediated by Hepatocyte Growth Factor Receptor (c-Met) T85943 INTEPATH nectin_pathway:Nectin adhesion pathway T85943 INTEPATH netrin_pathway:Netrin-mediated signaling events T85943 INTEPATH nfkappabatypicalpathway:Atypical NF-kappaB pathway T85943 INTEPATH p38alphabetapathway:Regulation of p38-alpha and p38-beta T85943 INTEPATH pdgfrbpathway:PDGFR-beta signaling pathway T85943 INTEPATH pi3kciaktpathway:Class I PI3K signaling events mediated by Akt T85943 INTEPATH pi3kcipathway:Class I PI3K signaling events T85943 INTEPATH pi3kplctrkpathway:Trk receptor signaling mediated by PI3K and PLC-gamma T85943 INTEPATH prlsignalingeventspathway:Signaling events mediated by PRL T85943 INTEPATH ptp1bpathway:Signaling events mediated by PTP1B T85943 INTEPATH ret_pathway:Signaling events regulated by Ret tyrosine kinase T85943 INTEPATH s1p_s1p3_pathway:S1P3 pathway T85943 INTEPATH syndecan_2_pathway:Syndecan-2-mediated signaling events T85943 INTEPATH syndecan_3_pathway:Syndecan-3-mediated signaling events T85943 INTEPATH tcptp_pathway:Signaling events mediated by TCPTP T85943 INTEPATH txa2pathway:Thromboxane A2 receptor signaling T85943 INTEPATH upa_upar_pathway:Urokinase-type plasminogen activator (uPA) and uPAR-mediated signaling T85943 INTEPATH vegfr1_2_pathway:Signaling events mediated by VEGFR1 and VEGFR2 T85943 PANTPATH P00005:Angiogenesis T85943 PANTPATH P00012:Cadherin signaling pathway T85943 PANTPATH P00034:Integrin signalling pathway T85943 PANTPATH P00049:Parkinson disease T85943 PANTPATH P06959:CCKR signaling map ST T51408 TARGETID T51408 T51408 FORMERID TTDC00184 T51408 UNIPROID ADRB3_HUMAN T51408 TARGNAME Adrenergic receptor beta-3 (ADRB3) T51408 GENENAME ADRB3 T51408 TARGTYPE Successful target T51408 SYNONYMS Beta3AR; Beta3-AR; Beta-3 adrenoreceptor; Beta-3 adrenoceptor; Beta-3 adrenergic receptor; B3AR; ADRB3R T51408 FUNCTION Beta-3 is involved in the regulation of lipolysis and thermogenesis. Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. T51408 PDBSTRUC 2CDW T51408 BIOCLASS GPCR rhodopsin T51408 SEQUENCE MAPWPHENSSLAPWPDLPTLAPNTANTSGLPGVPWEAALAGALLALAVLATVGGNLLVIVAIAWTPRLQTMTNVFVTSLAAADLVMGLLVVPPAATLALTGHWPLGATGCELWTSVDVLCVTASIETLCALAVDRYLAVTNPLRYGALVTKRCARTAVVLVWVVSAAVSFAPIMSQWWRVGADAEAQRCHSNPRCCAFASNMPYVLLSSSVSFYLPLLVMLFVYARVFVVATRQLRLLRGELGRFPPEESPPAPSRSLAPAPVGTCAPPEGVPACGRRPARLLPLREHRALCTLGLIMGTFTLCWLPFFLANVLRALGGPSLVPGPAFLALNWLGYANSAFNPLIYCRSPDFRSAFRRLLCRCGRRLPPEPCAAARPALFPSGVPAARSSPAQPRLCQRLDGASWGVS T51408 DRUGINFO D0D0YM Amosulalol Approved T51408 DRUGINFO D06RUL Bitolterol Approved T51408 DRUGINFO D0H5MB Bopindolol Approved T51408 DRUGINFO D0O5YZ Mepindolol Approved T51408 DRUGINFO D0X5UN Mirabegron Approved T51408 DRUGINFO D09SSC Nipradilol Approved T51408 DRUGINFO D03NOS Rimiterol Approved T51408 DRUGINFO D09GFL Trihexyphenidyl Approved T51408 DRUGINFO D0DH5X Vibegron Approved T51408 DRUGINFO D00GZW ONO-2506 Phase 2/3 T51408 DRUGINFO D00NNI ASP-3652 Phase 2 T51408 DRUGINFO D09PYV AZ-40140 Phase 2 T51408 DRUGINFO D07WHS CL-316,243 Phase 2 T51408 DRUGINFO D03FLT CP-331684 Phase 2 T51408 DRUGINFO D0A5EF GW-427353 Phase 2 T51408 DRUGINFO D0D1FC LY-362884 Phase 2 T51408 DRUGINFO D06UKG LY-377604 Phase 2 T51408 DRUGINFO D0U7HL N-5984 Phase 2 T51408 DRUGINFO D01VAP YM-430 Phase 2 T51408 DRUGINFO D0V9IE ZD2079 Phase 2 T51408 DRUGINFO D0W3UH QLT-091568 Phase 1/2 T51408 DRUGINFO D07NFW BMS-196085 Phase 1 T51408 DRUGINFO D03QKW KUC-7483 Phase 1 T51408 DRUGINFO D04UNO KUL-7211 Phase 1 T51408 DRUGINFO D03INQ Laevo-Bambuterol Phase 1 T51408 DRUGINFO D05EPU ZD7114 Phase 1 T51408 DRUGINFO D0Y0GG Epanolol Discontinued in Preregistration T51408 DRUGINFO D01KKB PW-2101 Discontinued in Preregistration T51408 DRUGINFO D0E8CZ Amibegron Discontinued in Phase 3 T51408 DRUGINFO D0PU5L Adaprolol maleate-SME Discontinued in Phase 2 T51408 DRUGINFO D0D5DE ALPRENOXIME HYDROCHLORIDE Discontinued in Phase 2 T51408 DRUGINFO D02ZEM OBERADILOL MONOETHYL MALEATE Discontinued in Phase 2 T51408 DRUGINFO D02RHV PROXODOLOL Discontinued in Phase 2 T51408 DRUGINFO D01SWK Rafabegron Discontinued in Phase 2 T51408 DRUGINFO D06TVC Tienoxolol Discontinued in Phase 2 T51408 DRUGINFO D0X5ES NCX 950 Discontinued in Phase 1/2 T51408 DRUGINFO D0GT0Y MN-246 Discontinued in Phase 1 T51408 DRUGINFO D03ISE PAFENOLOL Discontinued in Phase 1 T51408 DRUGINFO D04NXR RO-16-8714 Discontinued in Phase 1 T51408 DRUGINFO D00BKV SB 418790 Discontinued in Phase 1 T51408 DRUGINFO D08SIR CL-314698 Preclinical T51408 DRUGINFO D00MIX CP-114271 Preclinical T51408 DRUGINFO D03VGW GCR-1087 Preclinical T51408 DRUGINFO D0MT5C L-742791 Preclinical T51408 DRUGINFO D0WS1V L-751250 Preclinical T51408 DRUGINFO D03GLM BMS-210285 Terminated T51408 DRUGINFO D04DZE BRL 26830A Terminated T51408 DRUGINFO D0Y1PG BRL 37344 Terminated T51408 DRUGINFO D06XAK H-216/44 Terminated T51408 DRUGINFO D0V4FK SM 11044 Terminated T51408 DRUGINFO D0I9QH SR-58878 Terminated T51408 DRUGINFO D00TVI SR-58894A Terminated T51408 DRUGINFO D07HTM (-)-Ro 363 Investigative T51408 DRUGINFO D0K6MI [125I]ICYP Investigative T51408 DRUGINFO D02VPW [3H](-)CGP 12177 Investigative T51408 DRUGINFO D03BZW [3H]CGP12177 Investigative T51408 DRUGINFO D0F7BV 1-(1H-Indol-4-yloxy)-3-phenethylamino-propan-2-ol Investigative T51408 DRUGINFO D0A4FU 1-(2-allylphenoxy)-3-morpholinopropan-2-ol Investigative T51408 DRUGINFO D04HXF 1-(2-isopropylphenoxy)-3-morpholinopropan-2-ol Investigative T51408 DRUGINFO D0A9ED Carazolol Investigative T51408 DRUGINFO D07ZZG cicloprolol Investigative T51408 DRUGINFO D0G6RK ER-23006 Investigative T51408 DRUGINFO D0C4NF FMP-825 Investigative T51408 DRUGINFO D0V5OS H87/07 Investigative T51408 DRUGINFO D0R2JT iodocyanopindolol Investigative T51408 DRUGINFO D0U5HS L748328 Investigative T51408 DRUGINFO D03VHK L-748337 Investigative T51408 DRUGINFO D02DKX LK 204-545 Investigative T51408 DRUGINFO D00PLX MystiLol Investigative T51408 DRUGINFO D04UNE NIHP Investigative T51408 DRUGINFO D0JK0I prenalterol Investigative T51408 DRUGINFO D0XR9Z SB251023 Investigative T51408 DRUGINFO D01OIV T-0509 Investigative T51408 DRUGINFO D0S8RD Trecadrine Investigative T51408 DRUGINFO D07KMN Trimetoquinol Investigative T51408 DRUGINFO D01OIK xamoterol Investigative T51408 DRUGINFO D0A0KP zinterol Investigative T51408 KEGGPATH hsa04020:Calcium signaling pathway T51408 KEGGPATH hsa04022:cGMP-PKG signaling pathway T51408 KEGGPATH hsa04080:Neuroactive ligand-receptor interaction T51408 KEGGPATH hsa04144:Endocytosis T51408 KEGGPATH hsa04970:Salivary secretion T51408 WIKIPATH WP1824:GPCR downstream signaling T51408 WIKIPATH WP1825:GPCR ligand binding T51408 WIKIPATH WP455:GPCRs, Class A Rhodopsin-like T51408 WIKIPATH WP536:Calcium Regulation in the Cardiac Cell T51408 WIKIPATH WP58:Monoamine GPCRs T51408 REACPATH R-HSA-390696:Adrenoceptors T51408 REACPATH R-HSA-418555:G alpha (s) signalling events T51408 PANTPATH P00026:Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway T51408 PANTPATH P04379:Beta3 adrenergic receptor signaling pathway T99089 TARGETID T99089 T99089 FORMERID TTDS00346 T99089 UNIPROID BRAF_HUMAN T99089 TARGNAME Serine/threonine-protein kinase B-raf (BRAF) T99089 GENENAME BRAF T99089 TARGTYPE Successful target T99089 SYNONYMS V-Raf murine sarcoma viral oncogene homolog B1; RAFB1; Proto-oncogene B-Raf; P94; BRAF1; BRAF(V599E); BRAF serine/threonine kinase; B-raf protein; B-Raf T99089 FUNCTION May play a role in the postsynaptic responses of hippocampal neuron. Phosphorylates MAP2K1, and thereby contributes to the MAP kinase signal transduction pathway. Protein kinase involved in the transduction of mitogenic signals from the cell membrane to the nucleus. T99089 PDBSTRUC 6CAD; 6B8U; 5VYK; 5VR3; 5VAM T99089 BIOCLASS Kinase T99089 ECNUMBER EC 2.7.11.1 T99089 SEQUENCE MAALSGGGGGGAEPGQALFNGDMEPEAGAGAGAAASSAADPAIPEEVWNIKQMIKLTQEHIEALLDKFGGEHNPPSIYLEAYEEYTSKLDALQQREQQLLESLGNGTDFSVSSSASMDTVTSSSSSSLSVLPSSLSVFQNPTDVARSNPKSPQKPIVRVFLPNKQRTVVPARCGVTVRDSLKKALMMRGLIPECCAVYRIQDGEKKPIGWDTDISWLTGEELHVEVLENVPLTTHNFVRKTFFTLAFCDFCRKLLFQGFRCQTCGYKFHQRCSTEVPLMCVNYDQLDLLFVSKFFEHHPIPQEEASLAETALTSGSSPSAPASDSIGPQILTSPSPSKSIPIPQPFRPADEDHRNQFGQRDRSSSAPNVHINTIEPVNIDDLIRDQGFRGDGGSTTGLSATPPASLPGSLTNVKALQKSPGPQRERKSSSSSEDRNRMKTLGRRDSSDDWEIPDGQITVGQRIGSGSFGTVYKGKWHGDVAVKMLNVTAPTPQQLQAFKNEVGVLRKTRHVNILLFMGYSTKPQLAIVTQWCEGSSLYHHLHIIETKFEMIKLIDIARQTAQGMDYLHAKSIIHRDLKSNNIFLHEDLTVKIGDFGLATVKSRWSGSHQFEQLSGSILWMAPEVIRMQDKNPYSFQSDVYAFGIVLYELMTGQLPYSNINNRDQIIFMVGRGYLSPDLSKVRSNCPKAMKRLMAECLKKKRDERPLFPQILASIELLARSLPKIHRSASEPSLNRAGFQTEDFSLYACASPKTPIQAGGYGAFPVH T99089 DRUGINFO D05ROI Dabrafenib Approved T99089 DRUGINFO D0TK7R LGX818 Approved T99089 DRUGINFO D0Y9EW Vemurafenib Approved T99089 DRUGINFO D05HTS PLX8394 Phase 2 T99089 DRUGINFO D0M5XN BGB-283 Phase 1/2 T99089 DRUGINFO D04MXN CEP-32496 Phase 1/2 T99089 DRUGINFO DIS4N5 ABM-1310 Phase 1 T99089 DRUGINFO D04AZM ARQ 736 Phase 1 T99089 DRUGINFO D0XL8W ASN003 Phase 1 T99089 DRUGINFO D0Z2FD BMS-908662 Phase 1 T99089 DRUGINFO D0G0PU RO-5212054 Phase 1 T99089 DRUGINFO D0RV7J RG-7256 Discontinued in Phase 1 T99089 DRUGINFO D03TTT AR-00341677 Investigative T99089 DRUGINFO D0C0ZC AZ-628 Investigative T99089 KEGGPATH hsa04010:MAPK signaling pathway T99089 KEGGPATH hsa04012:ErbB signaling pathway T99089 KEGGPATH hsa04015:Rap1 signaling pathway T99089 KEGGPATH hsa04024:cAMP signaling pathway T99089 KEGGPATH hsa04062:Chemokine signaling pathway T99089 KEGGPATH hsa04068:FoxO signaling pathway T99089 KEGGPATH hsa04150:mTOR signaling pathway T99089 KEGGPATH hsa04270:Vascular smooth muscle contraction T99089 KEGGPATH hsa04510:Focal adhesion T99089 KEGGPATH hsa04650:Natural killer cell mediated cytotoxicity T99089 KEGGPATH hsa04720:Long-term potentiation T99089 KEGGPATH hsa04722:Neurotrophin signaling pathway T99089 KEGGPATH hsa04726:Serotonergic synapse T99089 KEGGPATH hsa04730:Long-term depression T99089 KEGGPATH hsa04810:Regulation of actin cytoskeleton T99089 KEGGPATH hsa04910:Insulin signaling pathway T99089 KEGGPATH hsa04914:Progesterone-mediated oocyte maturation T99089 KEGGPATH hsa05034:Alcoholism T99089 KEGGPATH hsa05160:Hepatitis C T99089 KEGGPATH hsa05200:Pathways in cancer T99089 KEGGPATH hsa05205:Proteoglycans in cancer T99089 KEGGPATH hsa05210:Colorectal cancer T99089 KEGGPATH hsa05211:Renal cell carcinoma T99089 KEGGPATH hsa05212:Pancreatic cancer T99089 KEGGPATH hsa05213:Endometrial cancer T99089 KEGGPATH hsa05214:Glioma T99089 KEGGPATH hsa05215:Prostate cancer T99089 KEGGPATH hsa05216:Thyroid cancer T99089 KEGGPATH hsa05218:Melanoma T99089 KEGGPATH hsa05219:Bladder cancer T99089 KEGGPATH hsa05220:Chronic myeloid leukemia T99089 KEGGPATH hsa05221:Acute myeloid leukemia T99089 KEGGPATH hsa05223:Non-small cell lung cancer T99089 WIKIPATH WP185:Integrin-mediated Cell Adhesion T99089 WIKIPATH WP1873:NGF signalling via TRKA from the plasma membrane T99089 WIKIPATH WP1911:Signaling by FGFR T99089 WIKIPATH WP1984:Integrated Breast Cancer Pathway T99089 WIKIPATH WP2032:TSH signaling pathway T99089 WIKIPATH WP2261:Signaling Pathways in Glioblastoma T99089 WIKIPATH WP23:B Cell Receptor Signaling Pathway T99089 WIKIPATH WP2355:Corticotropin-releasing hormone T99089 WIKIPATH WP2571:Polycystic Kidney Disease Pathway T99089 WIKIPATH WP2754:Neurotransmitter Receptor Binding And Downstream Transmission In The Postsynaptic Cell T99089 WIKIPATH WP2828:Bladder Cancer T99089 WIKIPATH WP306:Focal Adhesion T99089 WIKIPATH WP382:MAPK Signaling Pathway T99089 WIKIPATH WP422:MAPK Cascade T99089 WIKIPATH WP437:EGF/EGFR Signaling Pathway T99089 WIKIPATH WP51:Regulation of Actin Cytoskeleton T99089 WIKIPATH WP615:Senescence and Autophagy in Cancer T99089 WIKIPATH WP712:Estrogen signaling pathway T99089 WIKIPATH WP722:Serotonin HTR1 Group and FOS Pathway T99089 WIKIPATH WP734:Serotonin Receptor 4/6/7 and NR3C Signaling T99089 WHIZPATH PW000445:Intracellular Signalling Through Adenosine Receptor A2a and Adenosine T99089 WHIZPATH PW000446:Intracellular Signalling Through Adenosine Receptor A2b and Adenosine T99089 REACPATH R-HSA-1295596:Spry regulation of FGF signaling T99089 REACPATH R-HSA-170968:Frs2-mediated activation T99089 REACPATH R-HSA-170984:ARMS-mediated activation T99089 REACPATH R-HSA-442742:CREB phosphorylation through the activation of Ras T99089 REACPATH R-HSA-5673000:RAF activation T99089 REACPATH R-HSA-5674135:MAP2K and MAPK activation T99089 REACPATH R-HSA-5674499:Negative feedback regulation of MAPK pathway T99089 REACPATH R-HSA-5675221:Negative regulation of MAPK pathway T99089 NET_PATH NetPath_19:IL-7 Signaling Pathway T99089 INTEPATH cdc42_pathway:CDC42 signaling events T99089 INTEPATH erbb1_downstream_pathway:ErbB1 downstream signaling T99089 INTEPATH mapktrkpathway:Trk receptor signaling mediated by the MAPK pathway T99089 INTEPATH mtor_4pathway:mTOR signaling pathway T99089 INTEPATH pdgfrbpathway:PDGFR-beta signaling pathway T99089 INTEPATH tcrraspathway:Ras signaling in the CD4+ TCR pathway T99089 INTEPATH vegfr1_2_pathway:Signaling events mediated by VEGFR1 and VEGFR2 T99089 PANTPATH P00005:Angiogenesis T99089 PANTPATH P00034:Integrin signalling pathway T99089 PANTPATH P00036:Interleukin signaling pathway T99089 PANTPATH P00047:PDGF signaling pathway T99089 PANTPATH P00053:T cell activation T99089 PANTPATH P00056:VEGF signaling pathway T99089 PANTPATH P04393:Ras Pathway T99089 PANTPATH P06959:CCKR signaling map ST T26623 TARGETID T26623 T26623 FORMERID TTDS00115 T26623 UNIPROID ALDR_HUMAN T26623 TARGNAME Aldose reductase (AKR1B1) T26623 GENENAME AKR1B1 T26623 TARGTYPE Successful target T26623 SYNONYMS Aldehyde reductase; AKR1B1 T26623 FUNCTION Catalyzes the NADPH-dependent reduction of a wide variety of carbonyl-containing compounds to their corresponding alcohols with a broad range of catalytic efficiencies. T26623 PDBSTRUC 6F8O; 6F84; 6F82; 6F81; 6F7R T26623 BIOCLASS Short-chain dehydrogenases reductase T26623 ECNUMBER EC 1.1.1.300 T26623 SEQUENCE MASRLLLNNGAKMPILGLGTWKSPPGQVTEAVKVAIDVGYRHIDCAHVYQNENEVGVAIQEKLREQVVKREELFIVSKLWCTYHEKGLVKGACQKTLSDLKLDYLDLYLIHWPTGFKPGKEFFPLDESGNVVPSDTNILDTWAAMEELVDEGLVKAIGISNFNHLQVEMILNKPGLKYKPAVNQIECHPYLTQEKLIQYCQSKGIVVTAYSPLGSPDRPWAKPEDPSLLEDPRIKAIAAKHNKTTAQVLIRFPMQRNLVVIPKSVTPERIAENFKVFDFELSSQDMTTLLSYNRNWRVCALLSCTSHKDYPFHEEF T26623 DRUGINFO D03KOZ Epalrestat Approved T26623 DRUGINFO D0Z5IU Sulindac Approved T26623 DRUGINFO D00EWR Fidarestat Phase 3 T26623 DRUGINFO D0K8TI Ranirestat Phase 3 T26623 DRUGINFO D4PL6G BNV-222 Phase 2/3 T26623 DRUGINFO D04PBH CONTIGOSIDE B Phase 2/3 T26623 DRUGINFO D0P7SO ADMVA Phase 2 T26623 DRUGINFO D04BFU LIDORESTAT Phase 2 T26623 DRUGINFO D0V4UO M-16209 Phase 2 T26623 DRUGINFO D0B4XX QR-333 Phase 2 T26623 DRUGINFO D00QKL T2c-003 Phase 1/2 T26623 DRUGINFO D07DIX ALO-1567 Phase 1 T26623 DRUGINFO D0Q7QY SSR-125047 Phase 1 T26623 DRUGINFO D0Q7AW IMIRESTAT Discontinued in Phase 3 T26623 DRUGINFO D0J6JZ MINALRESTAT Discontinued in Phase 3 T26623 DRUGINFO D0U9TM Ponalrestat Discontinued in Phase 3 T26623 DRUGINFO D0O2ET AD-5467 Discontinued in Phase 2 T26623 DRUGINFO D03PIB Alrestatin Discontinued in Phase 2 T26623 DRUGINFO D0E0FY CTL-102-GDEPT Discontinued in Phase 2 T26623 DRUGINFO D08VMO JTT-811 Discontinued in Phase 2 T26623 DRUGINFO D06EDT ZOPOLRESTAT Discontinued in Phase 2 T26623 DRUGINFO D0M9RE ARI-809 Preclinical T26623 DRUGINFO D0B0GC E-0722 Terminated T26623 DRUGINFO D0RZ0N FR-62765 Terminated T26623 DRUGINFO D02CGC Sorbinil Terminated T26623 DRUGINFO D0E6LC SPR-210 Terminated T26623 DRUGINFO D09BHF WF-2421 Terminated T26623 DRUGINFO D0C7KK Zenarestat Terminated T26623 DRUGINFO D0IF8Z (4-Methyl-2-oxo-2H-quinolin-1-yl)-acetic acid Investigative T26623 DRUGINFO D0F6TM (6-Hydroxy-2-oxo-2H-quinolin-1-yl)-acetic acid Investigative T26623 DRUGINFO D0J7MD (6-Methoxy-2-oxo-2H-quinolin-1-yl)-acetic acid Investigative T26623 DRUGINFO D07GTX (8-Hydroxy-2-oxo-2H-quinolin-1-yl)-acetic acid Investigative T26623 DRUGINFO D0A9NE 2-(3,4-Dihydroxy-benzyl)-7-hydroxy-chromen-4-one Investigative T26623 DRUGINFO D0YJ3Q 2-(3,4-Dihydroxy-phenyl)-7-hydroxy-chromen-4-one Investigative T26623 DRUGINFO D03LRQ 2-(3-benzoyl-1H-pyrrol-1-yl)acetic acid Investigative T26623 DRUGINFO D01UNC 2-(4-aminophenylsulfonamido)acetic acid Investigative T26623 DRUGINFO D04YIV 2-(Phenylsulfonamido)acetic Acid Investigative T26623 DRUGINFO D09PNQ 2,3-dihydroxypropanal Investigative T26623 DRUGINFO D04GYD 2-Benzhydryl-7-hydroxy-chromen-4-one Investigative T26623 DRUGINFO D0QP9D 2-Benzyl-7-hydroxy-chromen-4-one Investigative T26623 DRUGINFO D0J2FY 2'-Monophosphoadenosine 5'-Diphosphoribose Investigative T26623 DRUGINFO D0CX4E 3-(3-Benzoyl-1H-pyrrol-1-yl)propanoic acid Investigative T26623 DRUGINFO D06SPO 3,5-dichlorosalicylic acid Investigative T26623 DRUGINFO D0T2TW 3-[5-(3-nitrophenyl)thiophen-2-yl]propanoic acid Investigative T26623 DRUGINFO D0G4CJ 4-(3-Benzoyl-1H-pyrrol-1-yl)butanoic acid Investigative T26623 DRUGINFO D08ZZX 4-(3-Methoxy-phenyl)-isoxazolidine-3,5-dione Investigative T26623 DRUGINFO D0A2FM 6-(1H-Indole-2-sulfonyl)-2H-pyridazin-3-one Investigative T26623 DRUGINFO D0O9KV 6-(2-Bromo-benzenesulfonyl)-2H-pyridazin-3-one Investigative T26623 DRUGINFO D00EPD 6-(2-Chloro-benzenesulfonyl)-2H-pyridazin-3-one Investigative T26623 DRUGINFO D06YQS 6-(2-Fluoro-benzenesulfonyl)-2H-pyridazin-3-one Investigative T26623 DRUGINFO D0R7IJ 6-(3-Chloro-benzenesulfonyl)-2H-pyridazin-3-one Investigative T26623 DRUGINFO D0Y7PW 6-(4-Bromo-benzenesulfonyl)-2H-pyridazin-3-one Investigative T26623 DRUGINFO D02AAH 6-(4-Chloro-benzenesulfonyl)-2H-pyridazin-3-one Investigative T26623 DRUGINFO D0XD1Q 6-(4-Fluoro-benzenesulfonyl)-2H-pyridazin-3-one Investigative T26623 DRUGINFO D0P3AU 6-(4-Methoxy-benzenesulfonyl)-2H-pyridazin-3-one Investigative T26623 DRUGINFO D0R3MB 6-(Benzofuran-2-sulfonyl)-2H-pyridazin-3-one Investigative T26623 DRUGINFO D02WZA 6-(Benzothiazole-2-sulfonyl)-2H-pyridazin-3-one Investigative T26623 DRUGINFO D07XXK 6-(Biphenyl-2-sulfonyl)-2H-pyridazin-3-one Investigative T26623 DRUGINFO D0P1ZM 6-(Naphthalene-1-sulfonyl)-2H-pyridazin-3-one Investigative T26623 DRUGINFO D08JEI 6-(Naphthalene-2-sulfonyl)-2H-pyridazin-3-one Investigative T26623 DRUGINFO D0IB8C 6-(Toluene-4-sulfonyl)-2H-pyridazin-3-one Investigative T26623 DRUGINFO D05HBF 6,7-Dihydroxy-2-phenyl-chromen-4-one Investigative T26623 DRUGINFO D0OZ4C 6-Benzenesulfonyl-2H-pyridazin-3-one Investigative T26623 DRUGINFO D08MHU 6-Hydroxy-2-(4-hydroxy-benzyl)-chromen-4-one Investigative T26623 DRUGINFO D03NEF 6-methoxykaempferol 3-O-beta-D-robinobioside Investigative T26623 DRUGINFO D03YBR 6-Phenylmethanesulfonyl-2H-pyridazin-3-one Investigative T26623 DRUGINFO D00WFB 7-Hydroxy-2-(4-hydroxy-benzyl)-chromen-4-one Investigative T26623 DRUGINFO D05SLZ 7-Hydroxy-2-(4-methoxy-benzyl)-chromen-4-one Investigative T26623 DRUGINFO D0OC4B 7-Hydroxy-4-phenylcoumarin Investigative T26623 DRUGINFO D0L7MI 7-Hydroxy-6-nitro-2-phenyl-chromen-4-one Investigative T26623 DRUGINFO D0K8NO AK198 Investigative T26623 DRUGINFO D01AWD Alpha-D-Glucose-6-Phosphate Investigative T26623 DRUGINFO D00RIX APIGENIN Investigative T26623 DRUGINFO D01LWJ Apigenin-7-O-beta-D-glucuronide Investigative T26623 DRUGINFO D0BH6B Apigenin-7-O-beta-D-glucuronide methyl ester Investigative T26623 DRUGINFO D08BFU ASTRAGALIN Investigative T26623 DRUGINFO D0R3OQ BNV-222 Investigative T26623 DRUGINFO D01UYI Chrysin Investigative T26623 DRUGINFO D0SY2M daidzein Investigative T26623 DRUGINFO D0A4LM EPALRESTATE Investigative T26623 DRUGINFO D00KCB Fidarestat(Stereoisomer) Investigative T26623 DRUGINFO D06YEV Hydroxydimethylarsine Oxide Investigative T26623 DRUGINFO D07JEY IDD552 Investigative T26623 DRUGINFO D0FJ7G IDD594 Investigative T26623 DRUGINFO D00VHG Inhibitor Idd 384 Investigative T26623 DRUGINFO D08NKL Isorhamnetin 3,7-disulfate Investigative T26623 DRUGINFO D0J7VA Isorhamnetin 3-O-rhamnoside Investigative T26623 DRUGINFO D0G3TK KAEMPFEROL Investigative T26623 DRUGINFO D04UYB MANGIFERIN Investigative T26623 DRUGINFO D09MYF N-Acetylalanine Investigative T26623 DRUGINFO D01KKU NSC-94258 Investigative T26623 DRUGINFO D08OYH O5-Acetyl-O7-nitrooxyethyl chrysin Investigative T26623 DRUGINFO D01KAM O7-Nitrooxyethyl chrysin Investigative T26623 DRUGINFO D03DEO PALBINONE Investigative T26623 DRUGINFO D0Z3FX Patuletin 3-O-beta-D-galactoside Investigative T26623 DRUGINFO D08DRD Patuletin 3-O-beta-D-robinobioside Investigative T26623 DRUGINFO D0G1OW Quercetin 3-O-neohesperidoside Investigative T26623 DRUGINFO D07DJS QUERCITRIN Investigative T26623 DRUGINFO D0U8GZ Tamarixetin 3-glucoside-7-sulfate Investigative T26623 DRUGINFO D0BU5K TINGENIN B Investigative T26623 DRUGINFO D0F6AI TINGENONE Investigative T26623 DRUGINFO D02DYB TRIPTOCALLINE A Investigative T26623 KEGGPATH hsa00040:Pentose and glucuronate interconversions T26623 KEGGPATH hsa00051:Fructose and mannose metabolism T26623 KEGGPATH hsa00052:Galactose metabolism T26623 KEGGPATH hsa00561:Glycerolipid metabolism T26623 KEGGPATH hsa01100:Metabolic pathways T26623 WIKIPATH WP2749:Metabolism of steroid hormones and vitamin D T26623 WIKIPATH WP690:Polyol Pathway T26623 WIKIPATH WP702:Metapathway biotransformation T26623 WHIZPATH PW000025:Fructose and Mannose Degradation T26623 WHIZPATH PW000054:Pyruvate Metabolism T26623 WHIZPATH PW000140:Pterine Biosynthesis T26623 WHIZPATH PW000144:Glycerolipid Metabolism T26623 WHIZPATH PW000159:Galactose Metabolism T26623 NET_PATH NetPath_13:IL1 Signaling Pathway T26623 NET_PATH NetPath_7:TGF_beta_Receptor Signaling Pathway T26623 BIOCPATH PWY-5451:Acetone degradation I (to methylglyoxal) T26623 BIOCPATH PWY-5453:Methylglyoxal degradation III T53524 TARGETID T53524 T53524 FORMERID TTDC00311 T53524 UNIPROID PGFRA_HUMAN T53524 TARGNAME Platelet-derived growth factor receptor alpha (PDGFRA) T53524 GENENAME PDGFRA T53524 TARGTYPE Successful target T53524 SYNONYMS RHEPDGFRA; Platelet-derived growth factor receptor 2; Platelet-derived growth factor alpha receptor; PDGFR2; PDGFR-alpha; PDGFR-2; PDGF-R-alpha; CD140a antigen; CD140a; CD140 antigen-like family member A; Alpha-type platelet-derived growth factor receptor; Alpha platelet-derived growth factor receptor T53524 FUNCTION Depending on the context, promotes or inhibits cell proliferation and cell migration. Plays an important role in the differentiation of bone marrow-derived mesenchymal stem cells. Required for normal skeleton development and cephalic closure during embryonic development. Required for normal development of the mucosa lining the gastrointestinal tract, and for recruitment of mesenchymal cells and normal development of intestinal villi. Plays a role in cell migration and chemotaxis in wound healing. Plays a role in platelet activation, secretion of agonists from platelet granules, and in thrombin-induced platelet aggregation. Binding of its cognate ligands - homodimeric PDGFA, homodimeric PDGFB, heterodimers formed by PDGFA and PDGFB or homodimeric PDGFC -leads to the activation of several signaling cascades; the response depends on the nature of the bound ligand and is modulated by the formation of heterodimers between PDGFRA and PDGFRB. Phosphorylates PIK3R1, PLCG1, and PTPN11. Activation of PLCG1 leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate, mobilization of cytosolic Ca(2+) and the activation of protein kinase C. Phosphorylates PIK3R1, the regulatory subunit of phosphatidylinositol 3-kinase, and thereby mediates activation of the AKT1 signaling pathway. Mediates activation of HRAS and of the MAP kinases MAPK1/ERK2 and/or MAPK3/ERK1. Promotes activation of STAT family members STAT1, STAT3 and STAT5A and/or STAT5B. Receptor signaling is down-regulated by protein phosphatases that dephosphorylate the receptor and its down-stream effectors, and by rapid internalization of the activated receptor. Tyrosine-protein kinase that acts as a cell-surface receptor for PDGFA, PDGFB and PDGFC and plays an essential role in the regulation of embryonic development, cell proliferation, survival and chemotaxis. T53524 PDBSTRUC 5K5X; 5GRN; 1GQ5 T53524 BIOCLASS Kinase T53524 ECNUMBER EC 2.7.10.1 T53524 SEQUENCE MGTSHPAFLVLGCLLTGLSLILCQLSLPSILPNENEKVVQLNSSFSLRCFGESEVSWQYPMSEEESSDVEIRNEENNSGLFVTVLEVSSASAAHTGLYTCYYNHTQTEENELEGRHIYIYVPDPDVAFVPLGMTDYLVIVEDDDSAIIPCRTTDPETPVTLHNSEGVVPASYDSRQGFNGTFTVGPYICEATVKGKKFQTIPFNVYALKATSELDLEMEALKTVYKSGETIVVTCAVFNNEVVDLQWTYPGEVKGKGITMLEEIKVPSIKLVYTLTVPEATVKDSGDYECAARQATREVKEMKKVTISVHEKGFIEIKPTFSQLEAVNLHEVKHFVVEVRAYPPPRISWLKNNLTLIENLTEITTDVEKIQEIRYRSKLKLIRAKEEDSGHYTIVAQNEDAVKSYTFELLTQVPSSILDLVDDHHGSTGGQTVRCTAEGTPLPDIEWMICKDIKKCNNETSWTILANNVSNIITEIHSRDRSTVEGRVTFAKVEETIAVRCLAKNLLGAENRELKLVAPTLRSELTVAAAVLVLLVIVIISLIVLVVIWKQKPRYEIRWRVIESISPDGHEYIYVDPMQLPYDSRWEFPRDGLVLGRVLGSGAFGKVVEGTAYGLSRSQPVMKVAVKMLKPTARSSEKQALMSELKIMTHLGPHLNIVNLLGACTKSGPIYIITEYCFYGDLVNYLHKNRDSFLSHHPEKPKKELDIFGLNPADESTRSYVILSFENNGDYMDMKQADTTQYVPMLERKEVSKYSDIQRSLYDRPASYKKKSMLDSEVKNLLSDDNSEGLTLLDLLSFTYQVARGMEFLASKNCVHRDLAARNVLLAQGKIVKICDFGLARDIMHDSNYVSKGSTFLPVKWMAPESIFDNLYTTLSDVWSYGILLWEIFSLGGTPYPGMMVDSTFYNKIKSGYRMAKPDHATSEVYEIMVKCWNSEPEKRPSFYHLSEIVENLLPGQYKKSYEKIHLDFLKSDHPAVARMRVDSDNAYIGVTYKNEEDKLKDWEGGLDEQRLSADSGYIIPLPDIDPVPEEEDLGKRNRHSSQTSEESAIETGSSSSTFIKREDETIEDIDMMDDIGIDSSDLVEDSFL T53524 DRUGINFO D0UO2P Avapritinib Approved T53524 DRUGINFO D09QZS Olaratumab Approved T53524 DRUGINFO D09AAK Ripretinib Approved T53524 DRUGINFO D01PZD Romiplostim Approved T53524 DRUGINFO D0J1GR CP-868596 Phase 3 T53524 DRUGINFO D02WVT E-3810 Phase 3 T53524 DRUGINFO D0Z6MT Famitinib Phase 2 T53524 DRUGINFO D0AG7N MEDI-575 Phase 2 T53524 DRUGINFO D0T1GF MP470 Phase 2 T53524 DRUGINFO D00NSD XL-820 Phase 2 T53524 DRUGINFO D0IH3I PMID28460551-Compound-1 Patented T53524 DRUGINFO D0AK1F Pyridine derivative 18 Patented T53524 DRUGINFO D0T7BE Pyridine derivative 19 Patented T53524 DRUGINFO D0NB1V Pyridine derivative 20 Patented T53524 DRUGINFO D0O0AW Pyridine derivative 21 Patented T53524 DRUGINFO D0O4TA Pyridine derivative 22 Patented T53524 DRUGINFO D00QCB SRI-62-834 Discontinued in Phase 2 T53524 DRUGINFO D0KX1E CEP-2563 Discontinued in Phase 1 T53524 DRUGINFO D06GBK AG1295 Terminated T53524 DRUGINFO D03WTT RG-13022 Terminated T53524 DRUGINFO D09OLH (1H-indol-2-yl)(5-methoxy-1H-indol-2-yl)methanone Investigative T53524 DRUGINFO D0G0KQ (1H-indol-2-yl)(5-phenoxy-1H-indol-2-yl)methanone Investigative T53524 DRUGINFO D0D7ZL (1H-indol-2-yl)(6-methoxy-1H-indol-2-yl)methanone Investigative T53524 DRUGINFO D0H7MF (5-fluoro-1H-indol-2-yl)-(1H-indol-2-yl)methanone Investigative T53524 DRUGINFO D0XS9E (5-hydroxy-1H-indol-2-yl)(1H-indol-2-yl)methanone Investigative T53524 DRUGINFO D00YCU 1-Phenyl-1H-benzoimidazol-5-ol Investigative T53524 DRUGINFO D01FWD 1-Phenyl-1H-benzoimidazole Investigative T53524 DRUGINFO D07JDY 3-((E)-Styryl)-quinoline Investigative T53524 DRUGINFO D06MCJ 3-(1H-Indol-3-yl)-6,7-dimethoxy-quinoline Investigative T53524 DRUGINFO D0GN3E 3-(1H-Indol-3-yl)-quinoline Investigative T53524 DRUGINFO D0K9ON 3-(2-Cyclohexyl-ethyl)-6,7-dimethoxy-quinoline Investigative T53524 DRUGINFO D0P0RD 3-(3,4-Dichloro-phenyl)-6,7-dimethoxy-quinoline Investigative T53524 DRUGINFO D0AO6T 3-(3,4-Difluoro-phenyl)-6,7-dimethoxy-quinoline Investigative T53524 DRUGINFO D08SUH 3-(3,4-Dimethoxy-phenyl)-6,7-dimethoxy-quinoline Investigative T53524 DRUGINFO D0A6YP 3-(3-Fluoro-phenyl)-6,7-dimethoxy-quinoline Investigative T53524 DRUGINFO D0I0GL 3-(4-Fluoro-phenyl)-6,7-dimethoxy-quinoline Investigative T53524 DRUGINFO D06VNR 3-Benzyloxy-6,7-dimethoxy-quinoline Investigative T53524 DRUGINFO D08KWL 3-Cyclohexylethynyl-6,7-dimethoxy-quinoline Investigative T53524 DRUGINFO D0KF3N 3-Cyclopent-1-enyl-6,7-dimethoxy-quinoline Investigative T53524 DRUGINFO D00LRC 3-Cyclopentyl-6,7-dimethoxy-quinoline Investigative T53524 DRUGINFO D0IR5I 3-Pyridin-3-yl-quinoline-6,7-diol Investigative T53524 DRUGINFO D0H9TO 3-Pyridin-4-yl-quinolin-7-ol Investigative T53524 DRUGINFO D0Q3DS 3-Pyridin-4-yl-quinoline Investigative T53524 DRUGINFO D0K9VE 3-Pyridin-4-yl-quinoline-5,7-diol Investigative T53524 DRUGINFO D05GBY 3-Thiophen-3-yl-quinoline Investigative T53524 DRUGINFO D0YE1X 4-(3,4-Dimethoxy-phenoxy)-6,7-dimethoxy-quinoline Investigative T53524 DRUGINFO D0K2YG 4-(5-Methoxy-benzoimidazol-1-yl)-phenylamine Investigative T53524 DRUGINFO D03MQI 4-(6,7-Dimethoxy-quinolin-3-yl)-benzoic acid Investigative T53524 DRUGINFO D0H4JB 4-(6,7-Dimethoxy-quinolin-3-yl)-phenol Investigative T53524 DRUGINFO D01MUN 4-Benzoimidazol-1-yl-phenylamine Investigative T53524 DRUGINFO D01UYS 5-(6,7-Dimethoxy-quinolin-3-yl)-1H-pyridin-2-one Investigative T53524 DRUGINFO D05FFB 5,11-Dimethyl-6H-pyrido[4,3-b]carbazol-9-ol Investigative T53524 DRUGINFO D0SG0G 5,6,7-Trimethoxy-3-pyridin-4-yl-quinoline Investigative T53524 DRUGINFO D0P0WT 5,7-Dimethoxy-3-pyridin-4-yl-quinoline Investigative T53524 DRUGINFO D0RD5S 5,7-Dimethoxy-3-thiophen-3-yl-quinoline Investigative T53524 DRUGINFO D07ZWN 5,7-Dimethyl-3-thiophen-3-yl-quinoline Investigative T53524 DRUGINFO D0N4VR 5-Fluoro-3-thiophen-3-yl-quinoline Investigative T53524 DRUGINFO D02XKJ 5-Methoxy-1-phenyl-1H-benzoimidazole Investigative T53524 DRUGINFO D0CF9B 6,7-Dichloro-3-thiophen-3-yl-quinoline Investigative T53524 DRUGINFO D0QT4X 6,7-Difluoro-3-thiophen-3-yl-quinoline Investigative T53524 DRUGINFO D06LLF 6,7-Dimethoxy-3-((E)-styryl)-quinoline Investigative T53524 DRUGINFO D05EDW 6,7-Dimethoxy-3-(2-methoxy-phenyl)-quinoline Investigative T53524 DRUGINFO D07CFT 6,7-Dimethoxy-3-(3-methoxy-phenyl)-quinoline Investigative T53524 DRUGINFO D0G0KN 6,7-Dimethoxy-3-(4-methoxy-phenyl)-quinoline Investigative T53524 DRUGINFO D08JGS 6,7-Dimethoxy-3-(4-nitro-phenyl)-quinoline Investigative T53524 DRUGINFO D0WW8M 6,7-Dimethoxy-3-phenylethynyl-quinoline Investigative T53524 DRUGINFO D0G6SA 6,7-Dimethoxy-3-phenyl-quinoline Investigative T53524 DRUGINFO D0C1BE 6,7-Dimethoxy-3-p-tolyl-quinoline Investigative T53524 DRUGINFO D00RBV 6,7-Dimethoxy-3-pyridin-3-yl-quinoline Investigative T53524 DRUGINFO D0T9FQ 6,7-Dimethoxy-3-pyridin-4-yl-quinoline Investigative T53524 DRUGINFO D0G0ZQ 6,7-Dimethoxy-3-thiophen-2-yl-quinoline Investigative T53524 DRUGINFO D04PQX 6-Methoxy-3-pyridin-4-yl-quinoline Investigative T53524 DRUGINFO D0W7IN 6-Methoxy-3-thiophen-3-yl-quinoline Investigative T53524 DRUGINFO D0Z4HV 7-Chloro-3-pyridin-4-yl-quinoline Investigative T53524 DRUGINFO D05SNG 7-Fluoro-3-thiophen-3-yl-quinoline Investigative T53524 DRUGINFO D02PZZ 7-Methoxy-3-pyridin-4-yl-quinoline Investigative T53524 DRUGINFO D0V8QI 7-Methoxy-3-thiophen-3-yl-quinoline Investigative T53524 DRUGINFO D0A6AA 7-Thiophen-3-yl-[1,3]dioxolo[4,5-g]quinoline Investigative T53524 DRUGINFO D02CUF Benzyl-(6,7-dimethoxy-quinolin-3-yl)-amine Investigative T53524 DRUGINFO D0I3XZ Bis-(5-hydroxy-1H-indol-2-yl)-methanone Investigative T53524 DRUGINFO D0M4SY BMS-536924 Investigative T53524 DRUGINFO D05QBZ CP-673451 Investigative T53524 DRUGINFO D03DJR D-65476 Investigative T53524 DRUGINFO D0G5YI Di(1H-indol-2-yl)methanone Investigative T53524 DRUGINFO D0D5EW HKI-9924129 Investigative T53524 DRUGINFO D0YZ7H JNJ-10198409 Investigative T53524 DRUGINFO D0P3JW PD-0166326 Investigative T53524 DRUGINFO D0S1KJ PD-0173952 Investigative T53524 DRUGINFO D03NPX PD-0173955 Investigative T53524 DRUGINFO D0GW4Q PD-0173956 Investigative T53524 DRUGINFO D0Z7GH PD-0173958 Investigative T53524 DRUGINFO D0OH3J PD-0179483 Investigative T53524 DRUGINFO D02BXJ PMID21561767C8h Investigative T53524 DRUGINFO D0C2GE PMID22765894C8h Investigative T53524 DRUGINFO D03EHM PP121 Investigative T53524 DRUGINFO D09XIL Ro-4396686 Investigative T53524 DRUGINFO D0W9BF RPR-101511 Investigative T53524 DRUGINFO D0FH3M RPR-108514A Investigative T53524 DRUGINFO D09LPL SU-11652 Investigative T53524 KEGGPATH hsa04010:MAPK signaling pathway T53524 KEGGPATH hsa04014:Ras signaling pathway T53524 KEGGPATH hsa04015:Rap1 signaling pathway T53524 KEGGPATH hsa04020:Calcium signaling pathway T53524 KEGGPATH hsa04060:Cytokine-cytokine receptor interaction T53524 KEGGPATH hsa04144:Endocytosis T53524 KEGGPATH hsa04151:PI3K-Akt signaling pathway T53524 KEGGPATH hsa04510:Focal adhesion T53524 KEGGPATH hsa04540:Gap junction T53524 KEGGPATH hsa04810:Regulation of actin cytoskeleton T53524 KEGGPATH hsa05166:HTLV-I infection T53524 KEGGPATH hsa05200:Pathways in cancer T53524 KEGGPATH hsa05206:MicroRNAs in cancer T53524 KEGGPATH hsa05214:Glioma T53524 KEGGPATH hsa05215:Prostate cancer T53524 KEGGPATH hsa05218:Melanoma T53524 KEGGPATH hsa05230:Central carbon metabolism in cancer T53524 KEGGPATH hsa05231:Choline metabolism in cancer T53524 WIKIPATH WP1539:Angiogenesis T53524 WIKIPATH WP1916:Signaling by PDGF T53524 WIKIPATH WP2261:Signaling Pathways in Glioblastoma T53524 WIKIPATH WP2328:Allograft Rejection T53524 WIKIPATH WP2377:Integrated Pancreatic Cancer Pathway T53524 WIKIPATH WP2406:Cardiac Progenitor Differentiation T53524 WIKIPATH WP2653:PIP3 activates AKT signaling T53524 WIKIPATH WP2839:Hair Follicle Development: Organogenesis (Part 2 of 3) T53524 WIKIPATH WP306:Focal Adhesion T53524 WIKIPATH WP322:Osteoblast Signaling T53524 WIKIPATH WP51:Regulation of Actin Cytoskeleton T53524 REACPATH R-HSA-1257604:PIP3 activates AKT signaling T53524 REACPATH R-HSA-2219530:Constitutive Signaling by Aberrant PI3K in Cancer T53524 REACPATH R-HSA-5673001:RAF/MAP kinase cascade T53524 NET_PATH NetPath_7:TGF_beta_Receptor Signaling Pathway T53524 INTEPATH atf2_pathway:ATF-2 transcription factor network T53524 INTEPATH pdgf_pathway:PDGF receptor signaling network T53524 INTEPATH pdgfrapathway:PDGFR-alpha signaling pathway T53524 PANTPATH P00005:Angiogenesis T53524 PANTPATH P00047:PDGF signaling pathway T83875 TARGETID T83875 T83875 FORMERID TTDS00289 T83875 UNIPROID AOFA_HUMAN T83875 TARGNAME Monoamine oxidase type A (MAO-A) T83875 GENENAME MAOA T83875 TARGTYPE Successful target T83875 SYNONYMS Monoamine oxidase A; Amine oxidase [flavin-containing] A T83875 FUNCTION MAOA preferentially oxidizes biogenic amines such as 5-hydroxytryptamine (5-HT), norepinephrine and epinephrine. Catalyzes the oxidative deamination of biogenic and xenobiotic amines and has important functions in the metabolism of neuroactive and vasoactive amines in the central nervous system and peripheral tissues. T83875 PDBSTRUC 2Z5Y; 2Z5X; 2BXS; 2BXR; 1H8Q T83875 BIOCLASS CH-NH(2) donor oxidoreductase T83875 ECNUMBER EC 1.4.3.4 T83875 SEQUENCE MENQEKASIAGHMFDVVVIGGGISGLSAAKLLTEYGVSVLVLEARDRVGGRTYTIRNEHVDYVDVGGAYVGPTQNRILRLSKELGIETYKVNVSERLVQYVKGKTYPFRGAFPPVWNPIAYLDYNNLWRTIDNMGKEIPTDAPWEAQHADKWDKMTMKELIDKICWTKTARRFAYLFVNINVTSEPHEVSALWFLWYVKQCGGTTRIFSVTNGGQERKFVGGSGQVSERIMDLLGDQVKLNHPVTHVDQSSDNIIIETLNHEHYECKYVINAIPPTLTAKIHFRPELPAERNQLIQRLPMGAVIKCMMYYKEAFWKKKDYCGCMIIEDEDAPISITLDDTKPDGSLPAIMGFILARKADRLAKLHKEIRKKKICELYAKVLGSQEALHPVHYEEKNWCEEQYSGGCYTAYFPPGIMTQYGRVIRQPVGRIFFAGTETATKWSGYMEGAVEAGERAAREVLNGLGKVTEKDIWVQEPESKDVPAVEITHTFWERNLPSVSGLLKIIGFSTSVTALGFVLYKYKLLPRS T83875 DRUGINFO D09QDP Clorgyline Approved T83875 DRUGINFO D0I2VK Isocarboxazid Approved T83875 DRUGINFO D01ZSO Moclobemide Approved T83875 DRUGINFO D0H0HJ Tranylcypromine Approved T83875 DRUGINFO D00VUI Psoralen Phase 3 T83875 DRUGINFO D08CJK TRYPTAMINE Phase 3 T83875 DRUGINFO D04RCT CHF-3381 Phase 2 T83875 DRUGINFO D00RWQ CX157 Phase 2 T83875 DRUGINFO D0C3UC Ladostigil Phase 2 T83875 DRUGINFO D0H7PW PIPERINE Phase 1/2 T83875 DRUGINFO D0T5AW Desoxypeganine Phase 1 T83875 DRUGINFO D0XY6I AphanamgrandiolA Patented T83875 DRUGINFO D04OEV Cyclic peptide derivative 1 Patented T83875 DRUGINFO D03YOU GypensapogeninA Patented T83875 DRUGINFO D0R2YC GypensapogeninB Patented T83875 DRUGINFO D00OWF Harmine Patented T83875 DRUGINFO D07NTA Heteroaryl-cyclopropylamine derivative 1 Patented T83875 DRUGINFO D0P1PC HouttuynoidA Patented T83875 DRUGINFO D0LZ2M IncarviatoneA Patented T83875 DRUGINFO D0G3TH KadcoccitoneA Patented T83875 DRUGINFO D0I9CK MyriberineA Patented T83875 DRUGINFO D08IOP N-(2-phenylcyclopropyl) amino acid derivative 3 Patented T83875 DRUGINFO D07MEE PhyllanthoidA Patented T83875 DRUGINFO D0TX9E PMID25399762-Compound-Figure1-Aphanamixoid A Patented T83875 DRUGINFO D0K3UV PMID25399762-Compound-Figure1-Chukrasone A Patented T83875 DRUGINFO D0Y9VB PMID25399762-Compound-Figure1-Chukrasone B Patented T83875 DRUGINFO D0N1CG PMID25399762-Compound-Figure1-Eryngiolide A Patented T83875 DRUGINFO D0V6TF PMID25399762-Compound-Figure1-Neonectrolide A Patented T83875 DRUGINFO D05GWJ PMID25399762-Compound-Figure1-Sarcaboside A Patented T83875 DRUGINFO D05MYL PMID25399762-Compound-Figure1-Sarcaboside B Patented T83875 DRUGINFO D03QMA PMID25399762-Compound-Figure2-Artoxanthochromane Patented T83875 DRUGINFO D0I5DV PMID25399762-Compound-Figure2-Spirooliganone B Patented T83875 DRUGINFO D08HOV PMID25399762-Compound-Figure3-Aspeverin Patented T83875 DRUGINFO D0KW7O PMID25399762-Compound-Figure3-Fluevirosine A Patented T83875 DRUGINFO D0M0EP PMID25399762-Compound-Figure3-Lycojaponicumin A Patented T83875 DRUGINFO D0E7OQ PMID25399762-Compound-Figure3-Lycojaponicumin B Patented T83875 DRUGINFO D0H7HH PMID25399762-Compound-Figure3-Lycojaponicumin C Patented T83875 DRUGINFO D03EHC PMID25399762-Compound-Table 5-8 Patented T83875 DRUGINFO D03VGN PMID25399762-Compound-Table 5-O-methyl-M30 Patented T83875 DRUGINFO D0AH9P PMID29324067-Compound-25 Patented T83875 DRUGINFO D0AA7U PMID29757691-Compound-4 Patented T83875 DRUGINFO D05RJG Schiff base compound 1 Patented T83875 DRUGINFO D01OGR Secondary and tertiary (hetero)arylamide derivative 2 Patented T83875 DRUGINFO D0T9JB Tacrine-coumarin hybrid derivative 1 Patented T83875 DRUGINFO D04OHC Tarnylcypromine derivative 2 Patented T83875 DRUGINFO D0O7IH Tarnylcypromine derivative 3 Patented T83875 DRUGINFO D04AXC Tetra-hydro-isoquinoline derivative 1 Patented T83875 DRUGINFO D0NB7Z Tetra-hydro-isoquinoline derivative 2 Patented T83875 DRUGINFO D02EME Tetra-hydro-isoquinoline derivative 3 Patented T83875 DRUGINFO D0R6RT Tetra-hydro-isoquinoline derivative 4 Patented T83875 DRUGINFO D05WEP Befloxatone Discontinued in Phase 3 T83875 DRUGINFO D0IZ1D Brofaromine Discontinued in Phase 2 T83875 DRUGINFO D0H9DE CS-722 Discontinued in Phase 2 T83875 DRUGINFO D0ZM5W Esuprone Discontinued in Phase 2 T83875 DRUGINFO D06QOJ RS-8359 Discontinued in Phase 2 T83875 DRUGINFO D01OLO AS602868 Discontinued in Phase 1 T83875 DRUGINFO D0E8UJ BW-1370U87 Discontinued in Phase 1 T83875 DRUGINFO D02CGY Bifemelane Terminated T83875 DRUGINFO D0G9AP E-2011 Terminated T83875 DRUGINFO D0D6OR (+/-)-2-(4'-Benzyloxyphenyl)thiomorpholine Investigative T83875 DRUGINFO D0M4GR (+/-)-2-(4'-Butoxyphenyl)thiomorpholin-5-one Investigative T83875 DRUGINFO D0T3XC (+/-)-2-(4'-Butoxyphenyl)thiomorpholine Investigative T83875 DRUGINFO D0D5KD (+/-)-2-(4'-Ethoxyphenyl)thiomorpholin-5-one Investigative T83875 DRUGINFO D0J0QW (+/-)-2-(4'-Ethoxyphenyl)thiomorpholine Investigative T83875 DRUGINFO D0ID3Y (+/-)-2-(4'-Methoxyphenyl)thiomorpholin-5-one Investigative T83875 DRUGINFO D08TFN (+/-)-2-(4'-Methoxyphenyl)thiomorpholine Investigative T83875 DRUGINFO D0Z5BU (+/-)-2-(4'-Propoxyphenyl)thiomorpholin-5-one Investigative T83875 DRUGINFO D08FXH (+/-)-2-(4'-Propoxyphenyl)thiomorpholine Investigative T83875 DRUGINFO D04FLL (+/-)-2-Phenylthiomorpholin-5-one Investigative T83875 DRUGINFO D0HU4J (+/-)-2-Phenylthiomorpholine Investigative T83875 DRUGINFO D03HXD (6-Benzyloxy-2-naphthyl)-2-aminopropane Investigative T83875 DRUGINFO D0V7RM (6-Butoxy-2-naphthyl)-2-aminopropane Investigative T83875 DRUGINFO D0L5EW (6-Ethoxy-2-naphthyl)-2-aminopropane Investigative T83875 DRUGINFO D02IDM (6-Methoxy-2-naphthyl)-2-aminopropane Investigative T83875 DRUGINFO D0R4TI (6-methylthio-2-naphthyl)isopropylamine Investigative T83875 DRUGINFO D0IP7L (6-Propoxy-2-naphthyl)-2-aminopropane Investigative T83875 DRUGINFO D02TFD (7-Benzyloxy-2-oxo-2H-chromen-4-yl)acetonitrile Investigative T83875 DRUGINFO D06AJP (E)-5-(3-Chlorostyryl)isatin Investigative T83875 DRUGINFO D0X8HH (E)-5-(3-Fluorostyryl)isatin Investigative T83875 DRUGINFO D09XSB (E)-5-Styrylisatin Investigative T83875 DRUGINFO D0S7FP (R)-Indan-1-yl-methyl-prop-2-ynyl-amine Investigative T83875 DRUGINFO D04UYZ (R,S)-N-(R-phenylethyl)-1H-pyrrole-2-carboxamide Investigative T83875 DRUGINFO D0M0XR (R/R)BEFLOXATONE Investigative T83875 DRUGINFO D0Z0ZU (S)-2-amino-1-(4-butylthiophenyl)-propane Investigative T83875 DRUGINFO D02ZZA (S)-2-amino-1-(4-ethylthiophenyl)-propane Investigative T83875 DRUGINFO D0Q2QA (S)-2-amino-1-(4-methylthiophenyl)-propane Investigative T83875 DRUGINFO D08SSS (S)-2-amino-1-(4-propylthiophenyl)-propane Investigative T83875 DRUGINFO D0BE0S 1-(1-Naphthyl)-2-aminopropane Investigative T83875 DRUGINFO D00YVE 1-(2-Naphthyl)-2-aminopropane Investigative T83875 DRUGINFO D0B5CR 1-(3-(4-chlorobenzyl)quinoxalin-2-yl)hydrazine Investigative T83875 DRUGINFO D0WI3V 1-(3-benzyl-6,7-dichloroquinoxalin-2-yl)hydrazine Investigative T83875 DRUGINFO D0O4XF 1-(3-benzylquinoxalin-2-yl)hydrazine Investigative T83875 DRUGINFO D01SBZ 1-(4-(benzyloxy)phenyl)propan-2-amine Investigative T83875 DRUGINFO D00KQB 1-(4-butoxyphenyl)propan-2-amine Investigative T83875 DRUGINFO D0X0PA 1-(4-ethoxyphenyl)propan-2-amine Investigative T83875 DRUGINFO D0H6UA 1-(4-propoxyphenyl)propan-2-amine Investigative T83875 DRUGINFO D0C1SE 1,2,3,4-Tetrahydro-pyrazino[1,2-a]indole Investigative T83875 DRUGINFO D0Q1IP 2-(2-cycloheptylidenehydrazinyl)-4-phenylthiazole Investigative T83875 DRUGINFO D00WVG 2-(2-cyclopentylidenehydrazinyl)-4-phenylthiazole Investigative T83875 DRUGINFO D0C0MP 2-(3,4-dimethoxyphenyl)-4,5-dihydro-1H-imidazole Investigative T83875 DRUGINFO D0H1GQ 2-(3-benzylquinoxalin-2-ylamino)ethanol Investigative T83875 DRUGINFO D0A4AB 2-(4,5-dihydro-1H-imidazol-2-yl)quinoline Investigative T83875 DRUGINFO D0K8SK 2-(4-methoxyphenyl)-4,5-dihydro-1H-imidazole Investigative T83875 DRUGINFO D0P1UC 2-(5-phenyl-furan-2-yl)-4,5-dihydro-1H-imidazole Investigative T83875 DRUGINFO D04ZPU 2-(naphthalen-2-yl)-4,5-dihydro-1H-imidazole Investigative T83875 DRUGINFO D0M7WE 2,3,4,5-Tetrahydro-1H-pyrido[4,3-b]indole Investigative T83875 DRUGINFO D0S3QN 2-[7-(Benzyloxy)-2-oxo-2H-chromen-4-yl]acetamide Investigative T83875 DRUGINFO D08SCH 2-Amino-1-(4-methylthiophenyl)propane Investigative T83875 DRUGINFO D0LI3J 2-BFi Investigative T83875 DRUGINFO D02BBT 2-Bromo-N-(2-morpholinoethyl)nicotinamide Investigative T83875 DRUGINFO D0R5EW 2-Chloro-N-(2-morpholinoethyl)nicotinamide Investigative T83875 DRUGINFO D0NS9X 2-Chloro-N-(3-morpholinopropyl)nicotinamide Investigative T83875 DRUGINFO D09ZDQ 2-Furan-2-yl-4,5-dihydro-1H-imidazole Investigative T83875 DRUGINFO D00WSM 2-oxo-N-m-tolyl-2H-chromene-3-carboxamide Investigative T83875 DRUGINFO D03PXS 2-oxo-N-phenyl-2H-chromene-3-carboxamide Investigative T83875 DRUGINFO D0H0GZ 2-oxo-N-p-tolyl-2H-chromene-3-carboxamide Investigative T83875 DRUGINFO D0Z7NC 2-Phenethyl-4,5-dihydro-1H-imidazole Investigative T83875 DRUGINFO D0N9FH 2-Phenoxymethyl-4,5-dihydro-1H-imidazole Investigative T83875 DRUGINFO D0W3BX 2-phenyl-5H-indeno[1,2-d]pyrimidine Investigative T83875 DRUGINFO D0Q9NC 2-phenyl-9H-indeno[2,1-d]pyrimidine Investigative T83875 DRUGINFO D0P4GF 3,4-Benzo-7-(beta-bromoallyloxy)-8-methylcoumarin Investigative T83875 DRUGINFO D0TL3S 3,4-Benzo-7-acetonyloxy-8-methoxycoumarin Investigative T83875 DRUGINFO D0Y1XS 3,4-Benzo-7-acetonyloxy-8-methylcoumarin Investigative T83875 DRUGINFO D09NNZ 3,4-Dichloro-N-(2-methyl-1H-indol-5-yl)benzamide Investigative T83875 DRUGINFO D0O0QN 3-aminoacetamido-4'-methylfuro[3,2-g]coumarin Investigative T83875 DRUGINFO D0KW6V 3-benzyl-N-(2-morpholinoethyl)quinoxalin-2-amine Investigative T83875 DRUGINFO D0D6QI 3-Chloro-N-(2-methyl-1H-indol-5-yl)benzamide Investigative T83875 DRUGINFO D0P0XO 3-methyl-2(1H)-thioxo-4(3H)-quinazolinone Investigative T83875 DRUGINFO D0E8IE 4-(2-oxo-2H-chromene-3-carboxamido)benzoic acid Investigative T83875 DRUGINFO D0T1FJ 4-(Aminomethyl)-7-(benzyloxy)-2H-chromen-2-one Investigative T83875 DRUGINFO D01LUB 4,8-Dimethyl-7-(2'-oxocyclohexyloxy)coumarin Investigative T83875 DRUGINFO D0G8BT 4,9-Dihydro-3H-beta-carboline Investigative T83875 DRUGINFO D0S9JC 4-Chloro-N-(2-morpholinoethyl)nicotinamide Investigative T83875 DRUGINFO D06IAE 4-Chloro-N-(3-morpholinopropyl)nicotinamide Investigative T83875 DRUGINFO D00JUD 4-methyl-2H-benzofuro[3,2-g]chromen-2-one Investigative T83875 DRUGINFO D0A1RE 4-methyl-7-(2-oxocyclopentyloxy)-2H-chromen-2-one Investigative T83875 DRUGINFO D0J3IA 5,6-Dichloro-N-(2-morpholinoethyl)nicotinamide Investigative T83875 DRUGINFO D0ZA4J 5,6-Dichloro-N-(3-morpholinopropyl)nicotinamide Investigative T83875 DRUGINFO D07LCW 5-Azidomethyl-3-pyrrol-1-yl-oxazolidin-2-one Investigative T83875 DRUGINFO D0L8ND 5-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline Investigative T83875 DRUGINFO D08HAM 5-Bromo-4,9-dihydro-3H-beta-carboline Investigative T83875 DRUGINFO D08QVY 5-Hydroxymethyl-3-pyrrol-1-yl-oxazolidin-2-one Investigative T83875 DRUGINFO D00NSA 5-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Investigative T83875 DRUGINFO D0V6XA 5-Methoxy-4,9-dihydro-3H-beta-carboline Investigative T83875 DRUGINFO D06FXI 5-Methoxymethyl-3-pyrrol-1-yl-oxazolidin-2-one Investigative T83875 DRUGINFO D0E5VT 6,11-dihydro-5H-benzo[a]carbazole Investigative T83875 DRUGINFO D0S0JH 6-amino-9-methoxy-7H-furo[3,2-g]chromen-7-one Investigative T83875 DRUGINFO D05GQQ 6-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline Investigative T83875 DRUGINFO D04GVX 6-Bromo-4,9-dihydro-3H-beta-carboline Investigative T83875 DRUGINFO D05GGH 6-Chloro-N-(2-morpholinoethyl)nicotinamide Investigative T83875 DRUGINFO D04SJC 6-Chloro-N-(3-morpholinopropyl)nicotinamide Investigative T83875 DRUGINFO D04EDK 6-Fluoro-N-(2-morpholinoethyl)nicotinamide Investigative T83875 DRUGINFO D0D0SC 6-Hydroxy-N-(2-morpholinoethyl)nicotinamide Investigative T83875 DRUGINFO D0J3SN 6-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Investigative T83875 DRUGINFO D0C7PD 6-Methoxy-4,9-dihydro-3H-beta-carboline Investigative T83875 DRUGINFO D0C9WW 7-(3-chlorobenzyloxy)-4-carboxaldehyde-coumarin Investigative T83875 DRUGINFO D08FFH 7-Acetonyloxy-3,4-cyclohexene-8-methylcoumarin Investigative T83875 DRUGINFO D00OQL 7-Acetonyloxy-3,4-cyclopentene-8-methylcoumarin Investigative T83875 DRUGINFO D0R4PR 7-acetonyloxy-3-acetylamino-8-methoxycoumarin Investigative T83875 DRUGINFO D02UVG 7-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline Investigative T83875 DRUGINFO D0W4TW 7-Bromo-4,9-dihydro-3H-beta-carboline Investigative T83875 DRUGINFO D05GDP 7-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Investigative T83875 DRUGINFO D05FQN 7-Methoxy-9H-beta-carboline Investigative T83875 DRUGINFO D07NBB 8-(3-Bromobenzyloxy)caffeine Investigative T83875 DRUGINFO D08YCE 8-(3-Chlorobenzyloxy)caffeine Investigative T83875 DRUGINFO D04LPY 8-(3-Fluorobenzyloxy)caffeine Investigative T83875 DRUGINFO D0B6MV 8-(3-Methoxybenzyloxy)caffeine Investigative T83875 DRUGINFO D00OLX 8-(3-Methylbenzyloxy)caffeine Investigative T83875 DRUGINFO D02FJX 8-[(3-Trifluoromethyl)benzyloxy]caffeine Investigative T83875 DRUGINFO D0JN9R 8-Benzyloxycaffeine Investigative T83875 DRUGINFO D06BAC 8-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline Investigative T83875 DRUGINFO D0G2EF 8-Bromo-4,9-dihydro-3H-beta-carboline Investigative T83875 DRUGINFO D0Q3VI 8-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Investigative T83875 DRUGINFO D0Y1GL 8-Methoxy-4,9-dihydro-3H-beta-carboline Investigative T83875 DRUGINFO D0U9VX 9-(3-aminopropoxy)-7H-furo[3,2-g]chromen-7-one Investigative T83875 DRUGINFO D0D2YR 9-Methyl-2,3,4,9-tetrahydro-1H-beta-carboline Investigative T83875 DRUGINFO D0R7ZC Beta-methoxyamphetamine Investigative T83875 DRUGINFO D05FMZ C-(1H-Indol-3-yl)-methylamine Investigative T83875 DRUGINFO D0D1PE CGS-19281A Investigative T83875 DRUGINFO D0H1VT Cis-(+/-)-2-Fluoro-1,2-diphenylcyclopropylamine Investigative T83875 DRUGINFO D0X8RN Cis-2-phenylcyclopropylamine Investigative T83875 DRUGINFO D0B0JK DECYL(DIMETHYL)PHOSPHINE OXIDE Investigative T83875 DRUGINFO D05HJT Ethyl 4-(2-oxo-2H-chromene-3-carboxamido)benzoate Investigative T83875 DRUGINFO D01UPT FA-70 Investigative T83875 DRUGINFO D00IMW Flavin-Adenine Dinucleotide Investigative T83875 DRUGINFO D0A4IY HYDRAZINECARBOXAMIDE Investigative T83875 DRUGINFO D08CNS IPRONIAZIDE Investigative T83875 DRUGINFO D0I4ME MMDA Investigative T83875 DRUGINFO D08QZP N-((1H-indol-2-yl)methyl)(phenyl)methanamine Investigative T83875 DRUGINFO D0Y0LQ N-((1H-indol-2-yl)methyl)-2-phenylethanamine Investigative T83875 DRUGINFO D08PEW N-(1H-Indol-2-ylmethyl)-N-(4-phenylbutyl)amine Investigative T83875 DRUGINFO D00KDZ N-(1H-Indol-2-ylmethyl)-N-methyl-N-phenylamine Investigative T83875 DRUGINFO D01PES N-(1H-Indol-2-ylmethyl)-N-phenylamine Investigative T83875 DRUGINFO D0KB2R N-(1-Methyl-1H-indol-2-ylmethyl)-N-phenylamine Investigative T83875 DRUGINFO D0C9RO N-(2-benzyl),N-(1-methylpyrrol-2-ylmethyl)amine Investigative T83875 DRUGINFO D05WQN N-(2-Methyl-1H-indol-5-yl)cyclohexanecarboxamide Investigative T83875 DRUGINFO D02PSR N'-(2-phenylallyl)hydrazine hydrochloride Investigative T83875 DRUGINFO D0N8UE N-(2-phenylethyl),N-(pyrrol-2-ylmethyl)amine Investigative T83875 DRUGINFO D0YO7C N-(2-Phenylethyl)-1H-indole-2-carboxamide Investigative T83875 DRUGINFO D07LCU N-(3-Phenylpropyl)-1H-indole-2-carboxamide Investigative T83875 DRUGINFO D0Y4JQ N-(3-phenylpropyl)-1H-pyrrole-2-carboxamide Investigative T83875 DRUGINFO D0B1WD N-(4-Ethylphenyl)-2-oxo-2H-chromene-3-carboxamide Investigative T83875 DRUGINFO D08HNJ N-(4-Phenylbutyl)-1H-indole-2-carboxamide Investigative T83875 DRUGINFO D0P3DV N-(4-phenylbutyl)-1H-pyrrole-2-carboxamide Investigative T83875 DRUGINFO D0O2UK N-(benzyl),N-(pyrrol-2-ylmethyl)amine Investigative T83875 DRUGINFO D0G4BG N-(propargyl),N-(pyrrol-2-ylmethyl)amine Investigative T83875 DRUGINFO D0T6XC N2-[4-(benzyloxy)benzyl]glycinamide Investigative T83875 DRUGINFO D02QBV N2-{4-[(3-fluorobenzyl)oxy]benzyl}glycinamide Investigative T83875 DRUGINFO D03XKJ N2-{4-[(4-chlorobenzyl)oxy]benzyl}glycinamide Investigative T83875 DRUGINFO D0SN3L N-2-phenylethyl-1H-pyrrole-2-carboxamide Investigative T83875 DRUGINFO D02AQG N-Benzyl-(6-butoxy-2-naphthyl)-2-aminopropane Investigative T83875 DRUGINFO D0M0HM N-Benzyl-(6-methoxy-2-naphthyl)-2-aminopropane Investigative T83875 DRUGINFO D0V0TN N-Benzyl,N-methyl-1H-indole-2-carboxamide Investigative T83875 DRUGINFO D0C8RD N-benzyl,N-methyl-1H-pyrrole-2-carboxamide Investigative T83875 DRUGINFO D0Z5YO N-Benzyl-1H-indole-2-carboxamide Investigative T83875 DRUGINFO D0A4FA N-benzyl-1H-pyrrole-2-carboxamide Investigative T83875 DRUGINFO D05ANK N-Benzyl-N-(1H-indol-2-ylmethyl)-N-methylamine Investigative T83875 DRUGINFO D0MO1O N-methyl,N-(benzyl),N-(pyrrol-2-ylmethyl)amine Investigative T83875 DRUGINFO D03KDD N-methyl,N-(propargyl),N-(pyrrol-2-ylmethyl)amine Investigative T83875 DRUGINFO D0F7JK N-Methyl,N-phenyl-1H-indole-2-carboxamide Investigative T83875 DRUGINFO D07ULQ N-methyl-N-(prop-2-ynyl)-1H-pyrrole-2-carboxamide Investigative T83875 DRUGINFO D0K9UN N-Phenyl-1H-indole-2-carboxamide Investigative T83875 DRUGINFO D0KU2D N-phenyl-1H-pyrrole-2-carboxamide Investigative T83875 DRUGINFO D05OXR N-Phenyl-1-methyl-1H-indole-2-carboxamide Investigative T83875 DRUGINFO D0H5MV N-propargyl-1H-pyrrole-2-carboxamide Investigative T83875 DRUGINFO D0B4CA NSC-656158 Investigative T83875 DRUGINFO D08SRB Phenyl 4-(4,5-dihydro-1H-imidazol-2-yl)benzoate Investigative T83875 DRUGINFO D04QRS PNU-22394 Investigative T83875 DRUGINFO D0V3NT TOLOXATONE Investigative T83875 DRUGINFO D09BIV TRACIZOLINE Investigative T83875 DRUGINFO D07WFU Trans-(+/-)-2-Fluoro-1,2-diphenylcyclopropylamine Investigative T83875 DRUGINFO D03LGV Trans-2-(4-chlorophenyl)-2-fluorocyclopropanamine Investigative T83875 DRUGINFO D08PHY Trans-2-fluoro-2-(4-fluorophenyl)cyclopropanamine Investigative T83875 DRUGINFO D09HBX Trans-2-fluoro-2-phenylcyclopropylamin Investigative T83875 DRUGINFO D0F2DC Trans-2-fluoro-2-p-tolylcyclopropanamine Investigative T83875 DRUGINFO D03LPH TRYPTOLINE Investigative T83875 KEGGPATH hsa00260:Glycine, serine and threonine metabolism T83875 KEGGPATH hsa00330:Arginine and proline metabolism T83875 KEGGPATH hsa00340:Histidine metabolism T83875 KEGGPATH hsa00350:Tyrosine metabolism T83875 KEGGPATH hsa00360:Phenylalanine metabolism T83875 KEGGPATH hsa00380:Tryptophan metabolism T83875 KEGGPATH hsa00982:Drug metabolism - cytochrome P450 T83875 KEGGPATH hsa01100:Metabolic pathways T83875 KEGGPATH hsa04726:Serotonergic synapse T83875 KEGGPATH hsa04728:Dopaminergic synapse T83875 KEGGPATH hsa05030:Cocaine addiction T83875 KEGGPATH hsa05031:Amphetamine addiction T83875 KEGGPATH hsa05034:Alcoholism T83875 WIKIPATH WP1455:Serotonin Transporter Activity T83875 WIKIPATH WP1870:Neurotransmitter Clearance In The Synaptic Cleft T83875 WIKIPATH WP1871:Neurotransmitter Release Cycle T83875 WIKIPATH WP1879:Phase 1 - Functionalization of compounds T83875 WIKIPATH WP2436:Dopamine metabolism T83875 WIKIPATH WP408:Oxidative Stress T83875 WIKIPATH WP550:Biogenic Amine Synthesis T83875 WIKIPATH WP706:SIDS Susceptibility Pathways T83875 WHIZPATH PW000043:Histidine Metabolism T83875 WHIZPATH PW000142:Tyrosine Metabolism T83875 WHIZPATH PW000157:Glycine and Serine Metabolism T83875 REACPATH R-HSA-181430:Norepinephrine Neurotransmitter Release Cycle T83875 NET_PATH NetPath_16:IL4 Signaling Pathway T83875 PANTPATH P00001:Adrenaline and noradrenaline biosynthesis T83875 PANTPATH P04372:5-Hydroxytryptamine degredation T83875 PANTPATH P05912:Dopamine receptor mediated signaling pathway T83875 BIOCPATH PWY-0:Putrescine degradation III T83875 BIOCPATH PWY-6313:Serotonin degradation T83875 BIOCPATH PWY-6342:Noradrenaline and adrenaline degradation T83875 BIOCPATH PWY-6399:Melatonin degradation II T83875 BIOCPATH PWY-6402:Superpathway of melatonin degradation T83875 BIOCPATH PWY66-401:Superpathway of tryptophan utilization T83875 BIOCPATH PWY6666-2:Dopamine degradation T58454 TARGETID T58454 T58454 FORMERID TTDS00171 T58454 UNIPROID FGFR2_HUMAN T58454 TARGNAME Fibroblast growth factor receptor 2 (FGFR2) T58454 GENENAME FGFR2 T58454 TARGTYPE Successful target T58454 SYNONYMS Keratinocyte growth factor receptor 2; Keratinocyte growth factor receptor; KSAM; KGFR; K-sam; FGFR-2; FGF-2 receptor; CD332; BEK T58454 FUNCTION Required for normal embryonic patterning, trophoblast function, limb bud development, lung morphogenesis, osteogenesis and skin development. Plays an essential role in the regulation of osteoblast differentiation, proliferation and apoptosis, and is required for normal skeleton development. Promotes cell proliferation in keratinocytes and immature osteoblasts, but promotes apoptosis in differentiated osteoblasts. Phosphorylates PLCG1, FRS2 and PAK4. Ligand binding leads to the activation of several signaling cascades. Activation of PLCG1 leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate. Phosphorylation of FRS2 triggers recruitment of GRB2, GAB1, PIK3R1 and SOS1, and mediates activation of RAS, MAPK1/ERK2, MAPK3/ERK1 and the MAP kinase signaling pathway, as well as of the AKT1 signaling pathway. FGFR2 signaling is down-regulated by ubiquitination, internalization and degradation. Mutations that lead to constitutive kinase activation or impair normal FGFR2 maturation, internalization and degradation lead to aberrant signaling. Over-expressed FGFR2 promotes activation of STAT1. Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of cell proliferation, differentiation, migration and apoptosis, and in the regulation of embryonic development. T58454 PDBSTRUC 5UI0; 5UHN; 5UGX; 5UGL; 5EG3 T58454 BIOCLASS Kinase T58454 ECNUMBER EC 2.7.10.1 T58454 SEQUENCE MVSWGRFICLVVVTMATLSLARPSFSLVEDTTLEPEEPPTKYQISQPEVYVAAPGESLEVRCLLKDAAVISWTKDGVHLGPNNRTVLIGEYLQIKGATPRDSGLYACTASRTVDSETWYFMVNVTDAISSGDDEDDTDGAEDFVSENSNNKRAPYWTNTEKMEKRLHAVPAANTVKFRCPAGGNPMPTMRWLKNGKEFKQEHRIGGYKVRNQHWSLIMESVVPSDKGNYTCVVENEYGSINHTYHLDVVERSPHRPILQAGLPANASTVVGGDVEFVCKVYSDAQPHIQWIKHVEKNGSKYGPDGLPYLKVLKAAGVNTTDKEIEVLYIRNVTFEDAGEYTCLAGNSIGISFHSAWLTVLPAPGREKEITASPDYLEIAIYCIGVFLIACMVVTVILCRMKNTTKKPDFSSQPAVHKLTKRIPLRRQVTVSAESSSSMNSNTPLVRITTRLSSTADTPMLAGVSEYELPEDPKWEFPRDKLTLGKPLGEGCFGQVVMAEAVGIDKDKPKEAVTVAVKMLKDDATEKDLSDLVSEMEMMKMIGKHKNIINLLGACTQDGPLYVIVEYASKGNLREYLRARRPPGMEYSYDINRVPEEQMTFKDLVSCTYQLARGMEYLASQKCIHRDLAARNVLVTENNVMKIADFGLARDINNIDYYKKTTNGRLPVKWMAPEALFDRVYTHQSDVWSFGVLMWEIFTLGGSPYPGIPVEELFKLLKEGHRMDKPANCTNELYMMMRDCWHAVPSQRPTFKQLVEDLDRILTLTTNEEYLDLSQPLEQYSPSYPDTRSSCSSGDDSVFSPDPMPYEPCLPQYPHINGSVKT T58454 DRUGINFO D09PMV Interferon Alfa-2a, Recombinant Approved T58454 DRUGINFO D0O7GU Palifermin Approved T58454 DRUGINFO D0O6UY Pemigatinib Approved T58454 DRUGINFO D02WVT E-3810 Phase 3 T58454 DRUGINFO D0KV1Q Trafermin Phase 3 T58454 DRUGINFO D0XT0W Debio 1347 Phase 2 T58454 DRUGINFO D0D4VV LY2874455 Phase 2 T58454 DRUGINFO D0G2QH AEE-788 Phase 1/2 T58454 DRUGINFO D00DRL MK-2461 Phase 1/2 T58454 DRUGINFO D47MOS Alofanib Phase 1 T58454 DRUGINFO D0L6RF BAY1179470 Phase 1 T58454 DRUGINFO DU1DL0 RLY-4008 Phase 1 T58454 DRUGINFO D0Z0KD PD-0183812 Terminated T58454 DRUGINFO D0R6OM ACTB-1003 Investigative T58454 DRUGINFO D02VPS Anti-FGFR2 humanized mab Investigative T58454 DRUGINFO D0VN4K PK 11195 Investigative T58454 DRUGINFO D0IE6Z Platelet factor 4 (PF-4) Investigative T58454 DRUGINFO D09XIL Ro-4396686 Investigative T58454 DRUGINFO D0H1OK TG-100435 Investigative T58454 KEGGPATH hsa04010:MAPK signaling pathway T58454 KEGGPATH hsa04014:Ras signaling pathway T58454 KEGGPATH hsa04015:Rap1 signaling pathway T58454 KEGGPATH hsa04144:Endocytosis T58454 KEGGPATH hsa04151:PI3K-Akt signaling pathway T58454 KEGGPATH hsa04550:Signaling pathways regulating pluripotency of stem cells T58454 KEGGPATH hsa04810:Regulation of actin cytoskeleton T58454 KEGGPATH hsa05200:Pathways in cancer T58454 KEGGPATH hsa05215:Prostate cancer T58454 KEGGPATH hsa05230:Central carbon metabolism in cancer T58454 WIKIPATH WP1539:Angiogenesis T58454 WIKIPATH WP1544:MicroRNAs in cardiomyocyte hypertrophy T58454 WIKIPATH WP1911:Signaling by FGFR T58454 WIKIPATH WP2064:Neural Crest Differentiation T58454 WIKIPATH WP2261:Signaling Pathways in Glioblastoma T58454 WIKIPATH WP2795:Cardiac Hypertrophic Response T58454 WIKIPATH WP2804:Hair Follicle Development: Induction (Part 1 of 3) T58454 WIKIPATH WP2839:Hair Follicle Development: Organogenesis (Part 2 of 3) T58454 WIKIPATH WP2858:Ectoderm Differentiation T58454 WIKIPATH WP51:Regulation of Actin Cytoskeleton T58454 REACPATH R-HSA-2033519:Activated point mutants of FGFR2 T58454 NET_PATH NetPath_13:IL1 Signaling Pathway T58454 INTEPATH fgf_pathway:FGF signaling pathway T58454 PANTPATH P00021:FGF signaling pathway T30082 TARGETID T30082 T30082 FORMERID TTDS00140 T30082 UNIPROID ACES_HUMAN T30082 TARGNAME Acetylcholinesterase (AChE) T30082 GENENAME ACHE T30082 TARGTYPE Successful target T30082 SYNONYMS YT; N-ACHE; ARACHE T30082 FUNCTION Role in neuronal apoptosis. Terminates signal transduction at the neuromuscular junction by rapid hydrolysis of the acetylcholine released into the synaptic cleft. T30082 PDBSTRUC 6O69; 6F25; 6CQZ; 6CQY; 6CQX T30082 BIOCLASS Carboxylic ester hydrolase T30082 ECNUMBER EC 3.1.1.7 T30082 SEQUENCE MRPPQCLLHTPSLASPLLLLLLWLLGGGVGAEGREDAELLVTVRGGRLRGIRLKTPGGPVSAFLGIPFAEPPMGPRRFLPPEPKQPWSGVVDATTFQSVCYQYVDTLYPGFEGTEMWNPNRELSEDCLYLNVWTPYPRPTSPTPVLVWIYGGGFYSGASSLDVYDGRFLVQAERTVLVSMNYRVGAFGFLALPGSREAPGNVGLLDQRLALQWVQENVAAFGGDPTSVTLFGESAGAASVGMHLLSPPSRGLFHRAVLQSGAPNGPWATVGMGEARRRATQLAHLVGCPPGGTGGNDTELVACLRTRPAQVLVNHEWHVLPQESVFRFSFVPVVDGDFLSDTPEALINAGDFHGLQVLVGVVKDEGSYFLVYGAPGFSKDNESLISRAEFLAGVRVGVPQVSDLAAEAVVLHYTDWLHPEDPARLREALSDVVGDHNVVCPVAQLAGRLAAQGARVYAYVFEHRASTLSWPLWMGVPHGYEIEFIFGIPLDPSRNYTAEEKIFAQRLMRYWANFARTGDPNEPRDPKAPQWPPYTAGAQQYVSLDLRPLEVRRGLRAQACAFWNRFLPKLLSATDTLDEAERQWKAEFHRWSSYMVHWKNQFDHYSKQDRCSDL T30082 DRUGINFO D06IAQ Ambenonium Approved T30082 DRUGINFO D06IDT Demecarium bromide Approved T30082 DRUGINFO D0NS6H Donepezil Approved T30082 DRUGINFO D0U8AT Echothiophate Iodide Approved T30082 DRUGINFO D0S5LH Edrophonium Approved T30082 DRUGINFO D0R9VR Galantamine Approved T30082 DRUGINFO D06XWB Huperzine A Approved T30082 DRUGINFO D0B2OT Isoflurophate Approved T30082 DRUGINFO D0K3LW Malathion Approved T30082 DRUGINFO D08USJ Neostigmine Approved T30082 DRUGINFO D0X7NU Pralidoxime Chloride Approved T30082 DRUGINFO D0O2WB Pyridostigmine Approved T30082 DRUGINFO D0WY5Q Rivastigmine Approved T30082 DRUGINFO D0E6YQ Tacrine Approved T30082 DRUGINFO D00WVW YM443 Approved T30082 DRUGINFO D07CIN (-)-Phenserine Phase 3 T30082 DRUGINFO D0SH2X Amocarzine Phase 3 T30082 DRUGINFO D01LYX Eptastigmine Phase 3 T30082 DRUGINFO D05UXU INM-176 Phase 3 T30082 DRUGINFO D0MZ9A Suronacrine maleate Phase 3 T30082 DRUGINFO D0C3UC Ladostigil Phase 2 T30082 DRUGINFO D0W3BA Methanesulfonyl fluoride Phase 2 T30082 DRUGINFO D0O5GK R-phenserine Phase 2 T30082 DRUGINFO D0PC1V T-82 Phase 2 T30082 DRUGINFO D0X1XK CPC-212 Phase 1 T30082 DRUGINFO D0WI9W CPC-250 Phase 1 T30082 DRUGINFO D0T5AW Desoxypeganine Phase 1 T30082 DRUGINFO D01KDM GTP-004 Phase 1 T30082 DRUGINFO D08ZRR KW-5092 Phase 1 T30082 DRUGINFO D0JA7V PRX-105 Phase 1 T30082 DRUGINFO D05REB ZT-1 Phase 1 T30082 DRUGINFO D0C0LQ 2-PAM derivative 1 Patented T30082 DRUGINFO D0G4YS 4-PAM derivative 1 Patented T30082 DRUGINFO D01RZG Amidine oxime derivative 1 Patented T30082 DRUGINFO D0Y4CG Decyle nelycorine dibromo salt derivative 1 Patented T30082 DRUGINFO D0K3EB Di-substituted piperidine derivative 2 Patented T30082 DRUGINFO D03DIQ Egonol compound 1 Patented T30082 DRUGINFO D0XS3N Fluorinated donepezil derivative 1 Patented T30082 DRUGINFO D0AH3R Fluorinated donepezil derivative 2 Patented T30082 DRUGINFO D0W9ZU Galantamine analog 1 Patented T30082 DRUGINFO D0J3OD Indoline derivative 1 Patented T30082 DRUGINFO D0OE6G Isochroman-4-ketone derivative 1 Patented T30082 DRUGINFO D03VUN Lycorine dimer salt derivative 1 Patented T30082 DRUGINFO D0QJ5H PMID27967267-Compound-12 Patented T30082 DRUGINFO D02SQQ PMID27967267-Compound-13 Patented T30082 DRUGINFO D0UX5I PMID27967267-Compound-14 Patented T30082 DRUGINFO D01FRI PMID27967267-Compound-15 Patented T30082 DRUGINFO D0I6UA PMID27967267-Compound-27 Patented T30082 DRUGINFO D0ZX8C PMID27967267-Compound-28 Patented T30082 DRUGINFO D04TGJ PMID27967267-Compound-3 Patented T30082 DRUGINFO D00AQW PMID27967267-Compound-36 Patented T30082 DRUGINFO D04XHE PMID27967267-Compound-39 Patented T30082 DRUGINFO D07HNU PMID27967267-Compound-42 Patented T30082 DRUGINFO D0YF7A PMID27967267-Compound-43 Patented T30082 DRUGINFO D01EGC PMID27967267-Compound-47 Patented T30082 DRUGINFO D0HI1R PMID27967267-Compound-48 Patented T30082 DRUGINFO D0OG8Z PMID27967267-Compound-49 Patented T30082 DRUGINFO D0X5KA PMID27967267-Compound-51 Patented T30082 DRUGINFO D06GSR PMID27967267-Compound-52 Patented T30082 DRUGINFO D0T0CB PMID27967267-Compound-7 Patented T30082 DRUGINFO D03WGA PMID27967267-Compound-neostenine Patented T30082 DRUGINFO D0V2JR PMID27967267-Compound-neotuberostemonine Patented T30082 DRUGINFO D02GCZ PMID27967267-Compound-stenine Patented T30082 DRUGINFO D0X9CR PMID29757691-Compound-10 Patented T30082 DRUGINFO D0H3YG PMID29757691-Compound-2a Patented T30082 DRUGINFO D0WD0M PMID29757691-Compound-2a-i Patented T30082 DRUGINFO D0AA7U PMID29757691-Compound-4 Patented T30082 DRUGINFO D0W9OC PMID29757691-Compound-7 Patented T30082 DRUGINFO D0RS6O PMID29757691-Compound-8a Patented T30082 DRUGINFO D04FAS PMID29757691-Compound-8b Patented T30082 DRUGINFO D0VQ2N PMID29757691-Compound-8c Patented T30082 DRUGINFO D0B9TI PMID29757691-Compound-8d Patented T30082 DRUGINFO D01SQO Quinazoline alkaloid derivative 1 Patented T30082 DRUGINFO D0CB1C Tacrine heterodimer derivative 1 Patented T30082 DRUGINFO D05WPG Tacrine-caffeic acid hybrid derivative 1 Patented T30082 DRUGINFO D0SW0V Tacrine-caffeic acid hybrid derivative 2 Patented T30082 DRUGINFO D0C1UA Tacrine-dihydropyridine hybrid derivative 1 Patented T30082 DRUGINFO D0G9HY Tacrine-indole hybrid derivative 1 Patented T30082 DRUGINFO D0I7KU Tacrine-indole hybrid derivative 2 Patented T30082 DRUGINFO D05QVX Tacrine-indole hybrid derivative 3 Patented T30082 DRUGINFO D0I2FM Tacrine-phenothiazine hybrid derivative 1 Patented T30082 DRUGINFO D04AXC Tetra-hydro-isoquinoline derivative 1 Patented T30082 DRUGINFO D0NB7Z Tetra-hydro-isoquinoline derivative 2 Patented T30082 DRUGINFO D02EME Tetra-hydro-isoquinoline derivative 3 Patented T30082 DRUGINFO D0R6RT Tetra-hydro-isoquinoline derivative 4 Patented T30082 DRUGINFO D0L8QQ VELNACRINE Discontinued in Phase 3 T30082 DRUGINFO D0AM8W Zanapezil Discontinued in Phase 3 T30082 DRUGINFO D0R5UZ Caracemide Discontinued in Phase 2 T30082 DRUGINFO D09PTA HP-290 Discontinued in Phase 2 T30082 DRUGINFO D0B2BQ Icopezil maleate Discontinued in Phase 2 T30082 DRUGINFO D09JVV Physostigmine Discontinued in Phase 2 T30082 DRUGINFO D0F3FB S-9977 Discontinued in Phase 2 T30082 DRUGINFO D05UHJ SM-10888 Discontinued in Phase 2 T30082 DRUGINFO D03GAX TAK-802 Discontinued in Phase 2 T30082 DRUGINFO D0F1VQ ZIFROSILONE Discontinued in Phase 2 T30082 DRUGINFO D04UKJ NP-61 Discontinued in Phase 1 T30082 DRUGINFO D0SR4T PHENSERINE TARTRATE Preclinical T30082 DRUGINFO D0V7FG SPH-1285 Preclinical T30082 DRUGINFO D0S1VV 7-methoxytacrine Terminated T30082 DRUGINFO D02UQU ABS-301 Terminated T30082 DRUGINFO D0M2GI CI-1002 Terminated T30082 DRUGINFO D09IUG F-3796 Terminated T30082 DRUGINFO D0J4GQ FR-152558 Terminated T30082 DRUGINFO D06ZAM MF268 Terminated T30082 DRUGINFO D0K0XG MF-8615 Terminated T30082 DRUGINFO D03DFY NP-7557 Terminated T30082 DRUGINFO D0TK0W Ro-46-5934 Terminated T30082 DRUGINFO D04ZJO (-)-huperzine B Investigative T30082 DRUGINFO D04FHZ (-)-Tolserine Investigative T30082 DRUGINFO D07EMX (1R)-1,2,2-TRIMETHYLPROPYL (S)-METHYLPHOSPHINATE Investigative T30082 DRUGINFO D01GWN (24S)-ethylcholesta-7,9(11),22(E)-triene-3b-ol Investigative T30082 DRUGINFO D0SE8T (2-Butyryloxy-ethyl)-trimethyl-ammonium iodide Investigative T30082 DRUGINFO D0J3EU (2-Chloro-ethyl)-trimethyl-ammonium chloride Investigative T30082 DRUGINFO D08TRN (2-Ethoxy-ethyl)-trimethyl-ammonium iodide Investigative T30082 DRUGINFO D0GT6I (2-Mercapto-ethyl)-trimethyl-ammonium iodide Investigative T30082 DRUGINFO D00RLO (3-Bromo-propyl)-trimethyl-ammonium Investigative T30082 DRUGINFO D08JOR (3-Hydroxy-2-methyl-phenyl)-trimethyl-ammonium Investigative T30082 DRUGINFO D0R1FR (3R)-9-amino-3-methyl-1,2,3,4-tetrahydroacridine Investigative T30082 DRUGINFO D03FZK (4-Bromo-butyl)-trimethyl-ammonium Investigative T30082 DRUGINFO D0P8KQ (4-Iodo-butyl)-trimethyl-ammonium iodide Investigative T30082 DRUGINFO D05KZH (5-Bromo-pentyl)-trimethyl-ammonium Investigative T30082 DRUGINFO D0A9IM (R)-tacrine(10)-hupyridone Investigative T30082 DRUGINFO D09FAU (RS)-tacrine(10)-hupyridone Investigative T30082 DRUGINFO D0T4UO (S)-tacrine(10)-hupyridone Investigative T30082 DRUGINFO D0Y3LO (S,S)-(-)-bis(10)-hupyridone Investigative T30082 DRUGINFO D09DJX (S,S)-(-)-bis(12)-hupyridone Investigative T30082 DRUGINFO D0D5QT 1-(3-Bromomethyl-phenyl)-2,2,2-trifluoro-ethanone Investigative T30082 DRUGINFO D0Z6WU 1,10-bis(pyridinium)-decane dibromide Investigative T30082 DRUGINFO D07YJG 1,11-bis(pyridinium)-undecane dibromide Investigative T30082 DRUGINFO D0K2FQ 1,2-Di(berberine-9-O-yl)ethane dibromide Investigative T30082 DRUGINFO D0W9VA 1,2-NAPHTHOQUINONE Investigative T30082 DRUGINFO D05QXU 1,3-Bis-(3-imidazolidin-2-yl-phenyl)-urea Investigative T30082 DRUGINFO D0P5BT 1,3-Di(berberine-9-O-yl)ethane dibromide Investigative T30082 DRUGINFO D00FPI 1,4-Di(berberine-9-O-yl)ethane dibromide Investigative T30082 DRUGINFO D0L5QJ 1,9-bis(pyridinium)-nonane dibromide Investigative T30082 DRUGINFO D0FI9G 10-Hydroxy-infractopicrin Investigative T30082 DRUGINFO D03KMG 1-benzene sulfonyl-cis-2,6-dimethyl piperidine Investigative T30082 DRUGINFO D04OUJ 1-Deoxy-1-Thio-Heptaethylene Glycol Investigative T30082 DRUGINFO D0L3IS 1-ETHOXY-2-(2-ETHOXYETHOXY)ETHANE Investigative T30082 DRUGINFO D06IEN 2-(Acetylamino)-2-Deoxy-a-D-Glucopyranose Investigative T30082 DRUGINFO D07KZA 2-(N-Morpholino)-Ethanesulfonic Acid Investigative T30082 DRUGINFO D0MV0T 2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-imine Investigative T30082 DRUGINFO D0V3LC 24-ethylcholest-6-ene-3,5-diol Investigative T30082 DRUGINFO D0J4LR 24-ethyl-cholest-7-ene-3,5,6-triol Investigative T30082 DRUGINFO D09ZGN 2-Hex-5-enyl-5-non-8-enyl-3,4-dihydro-2H-pyrrole Investigative T30082 DRUGINFO D0C6QF 2-Hex-5-enyl-5-non-8-enyl-pyrrolidine Investigative T30082 DRUGINFO D0O1JC 2-Hex-5-enyl-5-nonyl-pyrrolidine Investigative T30082 DRUGINFO D0K8AU 2-morpholino-N-phenethylpyrimidin-4-amine Investigative T30082 DRUGINFO D02AFZ 2-Propyl-beta-carboline-2-ium iodide Investigative T30082 DRUGINFO D09JAB 3-(2,5-Dioxo-pyrrolidin-1-yl)-benzoic acid Investigative T30082 DRUGINFO D07VIO 3-(2-Diethylamino-acetamino)-rutaecarpine Investigative T30082 DRUGINFO D03DIP 3-(2-Diethylamino-propionamino)-rutaecarpine Investigative T30082 DRUGINFO D0E0ZV 3-(2-N-Piperidyl-acetamino)-rutaecarpine Investigative T30082 DRUGINFO D0C3IS 3-(2-N-Piperidyl-propionamino)-rutaecarpine Investigative T30082 DRUGINFO D0LT0T 3-(2-N-Pyrrolyl-acetamino)-rutaecarpine Investigative T30082 DRUGINFO D0F6VM 3-(2-N-Pyrrolyl-propionamino)-rutaecarpine Investigative T30082 DRUGINFO D0H5XD 3-(3-Carboxy-propionylamino)-benzoic acid Investigative T30082 DRUGINFO D0V7EA 3-(4-Benzoylpiperazine-1-carbonyl)coumarin Investigative T30082 DRUGINFO D08WRG 3-(4-o-Tolylpiperazine-1-carbonyl)coumarin Investigative T30082 DRUGINFO D0S7HC 3-(4-Phenylpiperazin-1-carbonyl)coumarin Investigative T30082 DRUGINFO D01OND 3-(dimethylamino)phenyl phenylcarbamate Investigative T30082 DRUGINFO D0N0HK 3,4,5,6-Tetrachloro-[1,2]benzoquinone Investigative T30082 DRUGINFO D02DWE 3,6,9,12,15-Pentaoxaheptadecane Investigative T30082 DRUGINFO D05CCT 3,7-BIS(DIMETHYLAMINO)PHENOTHIAZIN-5-IUM Investigative T30082 DRUGINFO D0J9FT 3-[(1s)-1-(Dimethylamino)Ethyl]Phenol Investigative T30082 DRUGINFO D0E2LR 3-[2-(1-Benzyl-piperidin-4-yl)-ethyl]-1H-indazole Investigative T30082 DRUGINFO D0L9YJ 3-[3-(benzylmethylamino)propoxy]xanthen-9-one Investigative T30082 DRUGINFO D01EZC 3-[4-(benzylmethylamino)butoxy]xanthen-9-one Investigative T30082 DRUGINFO D0H3BC 3-[5-(benzylmethylamino)pentyloxy]xanthen-9-one Investigative T30082 DRUGINFO D0O8DZ 3-[6-(benzylmethylamino)hexyloxy]xanthen-9-one Investigative T30082 DRUGINFO D09GXM 3-[7-(benzylmethylamino)-heptyloxy]xanthen-9-one Investigative T30082 DRUGINFO D0B4DT 3-[8-(benzylmethylamino)octyloxy]xanthen-9-one Investigative T30082 DRUGINFO D03PQH 3-hydroxy-N,N,N-trimethylbenzenaminium iodide Investigative T30082 DRUGINFO D0T2RY 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Investigative T30082 DRUGINFO D0R2QC 4-[4-(benzhydryloxy)piperidino]butyl benzoate Investigative T30082 DRUGINFO D0C0NS 4ALPHA-(HYDROXYMETHYL)-4ALPHA-DEMETHYLTERRITREM B Investigative T30082 DRUGINFO D02ELG 4-formylphenyl-O-beta-Dglucopyranoside Investigative T30082 DRUGINFO D0FS3L 4-formylphenyl-O-beta-D-ribopyranoside Investigative T30082 DRUGINFO D0O2OH 4-ISOPROPYLPHENSERINE Investigative T30082 DRUGINFO D0WX6R 5,6-dinitroacenaphthoquinone Investigative T30082 DRUGINFO D03WOS 5-Chloro-1,2,3,4-tetrahydro-acridin-9-ylamine Investigative T30082 DRUGINFO D0D3TG 5-Hex-5-enyl-2-nonyl-3,4-dihydro-2H-pyrrole Investigative T30082 DRUGINFO D0D4SK 6,8-Dichloro-1,2,3,4-tetrahydro-acridin-9-ylamine Investigative T30082 DRUGINFO D0M0BM 6-chlorotacrine hydrochloride Investigative T30082 DRUGINFO D0G5TL 6-hydroxy-1,2,9-trimethyl-9H-beta-carbolin-2-ium Investigative T30082 DRUGINFO D09CGV 6-hydroxy-1,2-dimethyl-9H-beta-carbolin-2-ium Investigative T30082 DRUGINFO D0ER5C 6-hydroxy-2,9-dimethyl-9H-beta-carbolin-2-ium Investigative T30082 DRUGINFO D02LWX 6-hydroxy-2-methyl-9H-beta-carbolin-2-ium Investigative T30082 DRUGINFO D00MFR 6-methoxy-1,2-dimethyl-9H-beta-carbolin-2-ium Investigative T30082 DRUGINFO D0ZI7F 6-methoxy-1,9-dimethyl-9H-pyrido[3,4-b]indole Investigative T30082 DRUGINFO D0DV9Z 6-methoxy-2,9-dimethyl-9H-beta-carbolin-2-ium Investigative T30082 DRUGINFO D0XI4U 6-methoxy-2-methyl-9H-beta-carbolin-2-ium Investigative T30082 DRUGINFO D09NEH 6-Methyl-4-(4-benzoylpiperazin-1-yl)coumarin Investigative T30082 DRUGINFO D04JAX 6-Methyl-4-(4-o-tolylpiperazin-1-yl)coumarin Investigative T30082 DRUGINFO D03XXV 6-Methyl-4-(4-phenylpiperazin-1-yl)coumarin Investigative T30082 DRUGINFO D0MB3S 7-Chloro-1,2,3,4-tetrahydro-acridin-9-ylamine Investigative T30082 DRUGINFO D0I3UA 7-Oxo-7H-dibenzo[de,g]quinoline Investigative T30082 DRUGINFO D0X4EV 8-Chloro-1,2,3,4-tetrahydro-acridin-9-ylamine Investigative T30082 DRUGINFO D0V0PS 9-Amino-1,2,3,4-tetrahydro-acridine-1,7-diol Investigative T30082 DRUGINFO D0N9DB 9-amino-7H-dibenzo[de,h]quinolin-7-one Investigative T30082 DRUGINFO D0W8NK 9-Ethyl-2-methyl-beta-carboline-2-ium iodide Investigative T30082 DRUGINFO D0H4DW 9-Ethyl-beta-carboline Investigative T30082 DRUGINFO D08XPP 9-hydrazino-1,2,3,4-tetrahydroacridine Investigative T30082 DRUGINFO D01DHW 9-O-[2-(Phenylol-1-yloxy)ethyl]berberine bromide Investigative T30082 DRUGINFO D02WKB 9-O-[2-(Phenylol-1-yloxy)hexyl]berberine bromide Investigative T30082 DRUGINFO D02QMU 9-O-[3-(2-Pyridinoxyl)butyl]-berberine bromide Investigative T30082 DRUGINFO D0ZL9I 9-O-[3-(4-Bromo-phenoxyl)butyl]-berberine bromide Investigative T30082 DRUGINFO D0P2VL 9-O-[3-(4-Nitro-phenoxyl)butyl]-berberine bromide Investigative T30082 DRUGINFO D00NIX 9-O-[3-(Phenylamino)propyl]-berberine bromide Investigative T30082 DRUGINFO D0W7XL 9-O-[3-(Phenylol-1-yloxy)propyl]berberine bromide Investigative T30082 DRUGINFO D01TLN 9-O-[4-(Phenylol-1-yloxy)butyl]berberine bromide Investigative T30082 DRUGINFO D09XSI 9-O-[5-(Phenylol-1-yloxy)pentyl]berberine bromide Investigative T30082 DRUGINFO D0M1CG Allyl-trimethyl-ammonium Investigative T30082 DRUGINFO D0S2DW AP-2238 Investigative T30082 DRUGINFO D0S1MC AP-2243 Investigative T30082 DRUGINFO D0M2EM BENZOQUINONE Investigative T30082 DRUGINFO D08QQR Beta-L-fucose Investigative T30082 DRUGINFO D06EJS BIS(12)-HUPERZINE B Investigative T30082 DRUGINFO D04KWA Bis(14)-Huperzine B Investigative T30082 DRUGINFO D0P5CV BIS(16)-HUPERZINE B Investigative T30082 DRUGINFO D03EPB BIS(18)-HUPERZINE B Investigative T30082 DRUGINFO D04ZJK BIS(20)-HUPERZINE B Investigative T30082 DRUGINFO D0N8EC BIS(8)-HUPERZINE B Investigative T30082 DRUGINFO D0UF9K BIS(9)-HUPERZINE B Investigative T30082 DRUGINFO D0M4IE Bis-7-tacrine Investigative T30082 DRUGINFO D04ZQL But-3-enyl-trimethyl-ammonium bromide Investigative T30082 DRUGINFO D0O1QB BW284C51 Investigative T30082 DRUGINFO D06ACI BZYX Investigative T30082 DRUGINFO D0NJ5W CAPROCTAMINE Investigative T30082 DRUGINFO D07FFB Carinatumins B (2) Investigative T30082 DRUGINFO D04GTP CHF-2819 Investigative T30082 DRUGINFO D0D0BI CHLORANIL Investigative T30082 DRUGINFO D0W6PT Chlorphrifos oxon Investigative T30082 DRUGINFO D0M5ES CHLORPYRIFOS Investigative T30082 DRUGINFO D0Q2DE CHOLINE IODIDE Investigative T30082 DRUGINFO D09JZY Cis-2,6-dimethyl-1-methyl sulfonyl piperidine Investigative T30082 DRUGINFO D0A2BE CLEBOPRIDE Investigative T30082 DRUGINFO D04XXE CORONARIDINE Investigative T30082 DRUGINFO D0G2WI CP-126998 Investigative T30082 DRUGINFO D01XRG CRYPTADINE B Investigative T30082 DRUGINFO D02VFM DECIDIUM Investigative T30082 DRUGINFO D0T7ZN Dimethyl-pent-4-enyl-ammonium bromide Investigative T30082 DRUGINFO D0K6GY Ethyl octylfluorophosphonate Investigative T30082 DRUGINFO D0XL1R ETHYLPHENSERINE Investigative T30082 DRUGINFO D0G6XS Fucose Investigative T30082 DRUGINFO D0ST5U Galanthamine derivative Investigative T30082 DRUGINFO D0L4OW GANSTIGMINE Investigative T30082 DRUGINFO D02DUJ GENESERINE Investigative T30082 DRUGINFO D0G5SM HALOXYSTEROL A Investigative T30082 DRUGINFO D0X3FF HALOXYSTEROL B Investigative T30082 DRUGINFO D0E0LL Haloxysterol C Investigative T30082 DRUGINFO D09MCN Haloxysterol D Investigative T30082 DRUGINFO D0U1SE Hexyl-trimethyl-ammonium Investigative T30082 DRUGINFO D09RJH Huprine X Investigative T30082 DRUGINFO D0A0FK Huprine Y Investigative T30082 DRUGINFO D09JCF Huprine-Tacrine Heterodimer Investigative T30082 DRUGINFO D0XN8A Infractopicrin Investigative T30082 DRUGINFO D09QDC Iso-OMPA Investigative T30082 DRUGINFO D0HQ4M Isopropyl dodecylfluorophosphonate Investigative T30082 DRUGINFO D0K8BT Isosorbide-2-(methylcarbamate)-5-benzoate Investigative T30082 DRUGINFO D04SYM Isosorbide-2-(methylcarbamate)-5-mononitrate Investigative T30082 DRUGINFO D01QRR Isosorbide-2-benzylcarbamate-5-cyclopentanoate Investigative T30082 DRUGINFO D0T5MD Isosorbide-2-benzylcarbamate-5-cyclopropanoate Investigative T30082 DRUGINFO D0VI6N Isosorbide-2-benzylcarbamate-5-tosylate Investigative T30082 DRUGINFO D05EPI Isosorbide-di-(4-nitrophenyl carbamate) Investigative T30082 DRUGINFO D01AJQ Isosorbide-di-(benzylcarbamate) Investigative T30082 DRUGINFO D0O8AQ Isosorbide-di-(ethylcarbamate) Investigative T30082 DRUGINFO D06LRC Isosorbide-di-phenylcarbamate Investigative T30082 DRUGINFO D0Z6RT LAWSARITOL Investigative T30082 DRUGINFO D0F5EJ LIPOCRINE Investigative T30082 DRUGINFO D01RUH LYSICAMINE Investigative T30082 DRUGINFO D01KVT MEMOQUIN Investigative T30082 DRUGINFO D03FHV MESUAGENIN A Investigative T30082 DRUGINFO D0A6MF MESUAGENIN B Investigative T30082 DRUGINFO D00FEH Mesuagenin D Investigative T30082 DRUGINFO D0J4QH Methyl Phosphinic Acid Investigative T30082 DRUGINFO D04LMJ MMB-4 Investigative T30082 DRUGINFO D0W8RP Monoisopropylphosphorylserine Investigative T30082 DRUGINFO D00YHI N-(14-methylallyl)norgalanthamine Investigative T30082 DRUGINFO D0MC3U N,N'-(1',10'-decylene)-bis-(-)-nor-MEP Investigative T30082 DRUGINFO D02JXK N,N'-(1',11'-undecydene)-bis-(-)-nor-MEP Investigative T30082 DRUGINFO D0F0PY N,N'-(1',12'-dodecydene)-bis-(-)-nor-MEP Investigative T30082 DRUGINFO D0A8OX N,N'-(1',5'-pentylene)-bis-(-)-nor-MEP Investigative T30082 DRUGINFO D0Y7UG N,N'-(1',6-hexylene)-bis-(-)-nor-MEP Investigative T30082 DRUGINFO D0EX1R N,N'-(1',7'-heptylene)-bis-(-)-nor-MEP Investigative T30082 DRUGINFO D0Y0VQ N,N'-(1',8'-octylene)-bis-(-)-nor-MEP Investigative T30082 DRUGINFO D05QNR N,N'-(1',9'-nonylene)-bis-(-)-nor-MEP Investigative T30082 DRUGINFO D0D3TB N-ALLYLNORGALANTHAMINE Investigative T30082 DRUGINFO D0H7OP N-allylnorlitebamine Investigative T30082 DRUGINFO D0Z6GG N-benzyl-2-(pyrrolidin-1-yl)pyrimidin-4-amine Investigative T30082 DRUGINFO D0Z4OS N-benzyl-2-morpholinopyrimidin-4-amine Investigative T30082 DRUGINFO D0E4BT N-benzyl-2-thiomorpholinopyrimidin-4-amine Investigative T30082 DRUGINFO D07YQY N-benzylnorlitebamine Investigative T30082 DRUGINFO D08LBC N-butylnorlitebamine Investigative T30082 DRUGINFO D0O9OW N-isobutylnorlitebamine Investigative T30082 DRUGINFO D01ZHK N-isopropylnorlitebamine Investigative T30082 DRUGINFO D0PF3Z N-isopropylnorlitebamineN-methoiodide Investigative T30082 DRUGINFO D0G0GZ N-Methyl-1'H-phenothiazine-1'-carboxamide Investigative T30082 DRUGINFO D03JRX N-n-dodecyl-7-methoxytacrine hydrochloride Investigative T30082 DRUGINFO D0C0XU N-n-heptyl-7-methoxytacrine hydrochloride Investigative T30082 DRUGINFO D0O9YQ N-n-hexyl-7-methoxytacrine hydrochloride Investigative T30082 DRUGINFO D0H2UG N-n-nonyl-7-methoxytacrine hydrochloride Investigative T30082 DRUGINFO D0Q3EV N-n-octyl-7-methoxytacrine hydrochloride Investigative T30082 DRUGINFO D05UJV N-n-pentyl-7-methoxytacrine hydrochloride Investigative T30082 DRUGINFO D08PWL N-n-propyl-7-methoxytacrine hydrochloride Investigative T30082 DRUGINFO D0ZY4C N-phenethyl-2-(pyrrolidin-1-yl)pyrimidin-4-amine Investigative T30082 DRUGINFO D0B2JV N-propylnorlitebamine Investigative T30082 DRUGINFO D0FY2N NPRx-30 Investigative T30082 DRUGINFO D0F5VY NSC-23180 Investigative T30082 DRUGINFO D0E3OZ OBIDOXIME Investigative T30082 DRUGINFO D08XQI PARAOXON Investigative T30082 DRUGINFO D0M9JF Petrosamine Investigative T30082 DRUGINFO D08UET Propidium Investigative T30082 DRUGINFO D0RA5T Pseudocolumbamine trifluoroacetate Investigative T30082 DRUGINFO D0L8UL Pseudopalmatine trifluoroacetate Investigative T30082 DRUGINFO D01MVX TACRINE(8)-4-AMINOQUINOLINE Investigative T30082 DRUGINFO D0L0ZH TASPINE Investigative T30082 DRUGINFO D0P5YS TERRITREM B Investigative T30082 DRUGINFO D0D9PI Tetraethylene Glycol Investigative T30082 DRUGINFO D0P6PQ THIOCTIC ACID Investigative T30082 DRUGINFO D0PF7F TOLSERINE Investigative T30082 DRUGINFO D0G5QX TRIMEDOXIME Investigative T30082 DRUGINFO D0M8SQ Trimethyl-(3-nitro-phenyl)-ammonium iodide Investigative T30082 DRUGINFO D0O6AH Trimethyl-(4-oxo-pentyl)-ammonium iodide Investigative T30082 DRUGINFO D0I0EN TURBINATINE Investigative T30082 DRUGINFO D00AJB Voacangine Investigative T30082 DRUGINFO D0X4HG XANTHOSTIGMINE Investigative T30082 KEGGPATH hsa00564:Glycerophospholipid metabolism T30082 KEGGPATH hsa04725:Cholinergic synapse T30082 WIKIPATH WP2377:Integrated Pancreatic Cancer Pathway T30082 WIKIPATH WP528:Acetylcholine Synthesis T30082 WIKIPATH WP550:Biogenic Amine Synthesis T30082 WIKIPATH WP727:Monoamine Transport T30082 WHIZPATH PW000048:Phospholipid Biosynthesis T30082 INTEPATH atf2_pathway:ATF-2 transcription factor network T30082 PANTPATH P00042:Muscarinic acetylcholine receptor 1 and 3 signaling pathway T30082 PANTPATH P00043:Muscarinic acetylcholine receptor 2 and 4 signaling pathway T30082 PANTPATH P00044:Nicotinic acetylcholine receptor signaling pathway T53378 TARGETID T53378 T53378 FORMERID TTDR00209 T53378 UNIPROID CAH4_HUMAN T53378 TARGNAME Carbonic anhydrase IV (CA-IV) T53378 GENENAME CA4 T53378 TARGTYPE Successful target T53378 SYNONYMS Carbonic anhydrase 4; Carbonate dehydratase IV; CAIV T53378 FUNCTION May stimulate the sodium/bicarbonate transporter activity of SLC4A4 that acts in pH homeostasis. It is essential for acid overload removal from the retina and retina epithelium, and acid release in the choriocapillaris in the choroid. Reversible hydration of carbon dioxide. T53378 PDBSTRUC 5KU6; 5JNC; 5JNA; 5JN9; 5JN8 T53378 BIOCLASS Alpha-carbonic anhydrase T53378 ECNUMBER EC 4.2.1.1 T53378 SEQUENCE MRMLLALLALSAARPSASAESHWCYEVQAESSNYPCLVPVKWGGNCQKDRQSPINIVTTKAKVDKKLGRFFFSGYDKKQTWTVQNNGHSVMMLLENKASISGGGLPAPYQAKQLHLHWSDLPYKGSEHSLDGEHFAMEMHIVHEKEKGTSRNVKEAQDPEDEIAVLAFLVEAGTQVNEGFQPLVEALSNIPKPEMSTTMAESSLLDLLPKEEKLRHYFRYLGSLTTPTCDEKVVWTVFREPIQLHREQILAFSQKLYYDKEQTVSMKDNVRPLQQLGQRTVIKSGAPGRPLPWALPALLGPMLACLLAGFLR T53378 DRUGINFO D01MUR Brinzolamide Approved T53378 DRUGINFO D07HBX Salicyclic acid Approved T53378 DRUGINFO D0K1QD Sulfamylon Approved T53378 DRUGINFO D07SDQ Curcumin Phase 3 T53378 DRUGINFO D0A8JP PARABEN Phase 3 T53378 DRUGINFO D0L6HN PHENOL Phase 2/3 T53378 DRUGINFO D0Y6OA Coumate Phase 2 T53378 DRUGINFO D02ECG Sodium pyruvate Phase 1/2 T53378 DRUGINFO D0V0UK SULFAMIDE Phase 1 T53378 DRUGINFO D03SLR FERULIC ACID Patented T53378 DRUGINFO D0LD9S SPERMINE Terminated T53378 DRUGINFO D0L2GD [Cu(CN)2]- Investigative T53378 DRUGINFO D01ENA [Fe(CN)6]4- Investigative T53378 DRUGINFO D09UQM 1-(3,4-dichlorophenyl)-3-hydroxyurea Investigative T53378 DRUGINFO D0M3PO 2,4-Disulfamyltrifluoromethylaniline Investigative T53378 DRUGINFO D0H3NS 2-oxo-2H-chromene-3-carboxylic acid Investigative T53378 DRUGINFO D0EX9Q 2-Propyl-pentanoic acid 4-sulfamoyl-benzyl ester Investigative T53378 DRUGINFO D0S1OY 2-Propyl-pentanoic acid 4-sulfamoyl-benzylamide Investigative T53378 DRUGINFO D0J2AE 3-Amino-benzenesulfonamide Investigative T53378 DRUGINFO D04NSN 4-(2-AMINOETHYL)BENZENESULFONAMIDE Investigative T53378 DRUGINFO D0P6AM 4-Amino-3-bromo-benzenesulfonamide Investigative T53378 DRUGINFO D0YU8J 4-Amino-3-chloro-benzenesulfonamide Investigative T53378 DRUGINFO D04CVC 4-Amino-3-fluoro-benzenesulfonamide Investigative T53378 DRUGINFO D01STY 4-Amino-3-iodo-benzenesulfonamide Investigative T53378 DRUGINFO D0NN3Q 4-Hydrazino-benzenesulfonamide Investigative T53378 DRUGINFO D0N1AW 6-(aminomethyl)-2H-chromen-2-one Investigative T53378 DRUGINFO D0L5TZ 6-(hydroxymethyl)-2H-chromen-2-one Investigative T53378 DRUGINFO D0G3BI 6-methyl-2-oxo-2H-chromene-3-carboxylic acid Investigative T53378 DRUGINFO D00RNZ 7-(benzyloxy)-2H-chromen-2-one Investigative T53378 DRUGINFO D0H0PQ Aminocarbonyl dihydrogen phosphate Investigative T53378 DRUGINFO D0E8CC BENZOLAMIDE Investigative T53378 DRUGINFO D0Y6EL Carbamoyl phosphate disodium Investigative T53378 DRUGINFO D0V7AA CATECHIN Investigative T53378 DRUGINFO D07QJJ CATECHOL Investigative T53378 DRUGINFO D0VD7H CL-5343 Investigative T53378 DRUGINFO D03ZMQ COUMARIN Investigative T53378 DRUGINFO D00YEF Decane-1,10-diyl disulfamate Investigative T53378 DRUGINFO D09WSJ Decyl sulfamate Investigative T53378 DRUGINFO D0A1CM ELLAGIC ACID Investigative T53378 DRUGINFO D07TAJ Ethyl 7-methoxy-2-oxo-2H-chromene-3-carboxylate Investigative T53378 DRUGINFO D0Y3TZ GALLICACID Investigative T53378 DRUGINFO D0U4BB HERNIARIN Investigative T53378 DRUGINFO D09JPC Hexane-1,6-diamine Investigative T53378 DRUGINFO D03MXZ Malonate sodium Investigative T53378 DRUGINFO D0S4NO N-(5-ethyl-1,3,4-thiadiazol-2-yl)sulfamide Investigative T53378 DRUGINFO D06JVR N-(5-phenyl-1,3,4-thiadiazol-2-yl)sulfamide Investigative T53378 DRUGINFO D04HQK N-(5-Sulfamoyl-[1,3,4]thiadiazol-2-yl)-benzamide Investigative T53378 DRUGINFO D0T2VH N-(5-tert-butyl-1,3,4-thiadiazol-2-yl)sulfamide Investigative T53378 DRUGINFO D0L6CN N-(phosphonacetyl)-L-aspartate Investigative T53378 DRUGINFO D0E3VJ N-[5-(ethylthio)-1,3,4-thiadiazol-2-yl]sulfamide Investigative T53378 DRUGINFO D04PSK N-[5-(methylthio)-1,3,4-thiadiazol-2-yl]sulfamide Investigative T53378 DRUGINFO D0X5HL N1-(naphthalen-1-yl)ethane-1,2-diamine Investigative T53378 DRUGINFO D00BMI N-1,3,4-thiadiazol-2-ylsulfamide Investigative T53378 DRUGINFO D03EAQ N-hydroxysulfonamides Investigative T53378 DRUGINFO D0D4OV Octane-1,8-diyl disulfamate Investigative T53378 DRUGINFO D05TLB Octyl sulfamate Investigative T53378 DRUGINFO D0AU0M P-Coumaric Acid Investigative T53378 DRUGINFO D02QGI Pentane-1,5-diamine Investigative T53378 DRUGINFO D0EJ9B Phenyl Boronic acid Investigative T53378 DRUGINFO D0M6RM Phenylarsonic acid Investigative T53378 DRUGINFO D00CIW Phenyl-phosphonic acid Investigative T53378 DRUGINFO D05KTE SODIUM CITRATE Investigative T53378 DRUGINFO D0GQ9A Sodium phenylarsonate Investigative T53378 DRUGINFO D0Q4VO SODIUM PHOSPHATE, DIBASIC, ANHYDROUS Investigative T53378 DRUGINFO D0H7JJ Sodium sulfamate Investigative T53378 DRUGINFO D0D5XC Sodium trithiocarbonate Investigative T53378 DRUGINFO D03VDJ SULFAMATE Investigative T53378 DRUGINFO D0R3DQ SYL-040003 Investigative T53378 DRUGINFO D0Q7DJ Syringic Acid Investigative T53378 DRUGINFO D0S8RD Trecadrine Investigative T53378 DRUGINFO D01DOW Trisodium phosphate Investigative T53378 KEGGPATH hsa00910:Nitrogen metabolism T53378 KEGGPATH hsa04964:Proximal tubule bicarbonate reclamation T53378 WIKIPATH WP2681:Uptake of Oxygen and Release of Carbon Dioxide by Erythrocytes T53378 WIKIPATH WP2744:Uptake of Carbon Dioxide and Release of Oxygen by Erythrocytes T53378 WIKIPATH WP2770:Reversible Hydration of Carbon Dioxide T53378 REACPATH R-HSA-1237044:Erythrocytes take up carbon dioxide and release oxygen T53378 REACPATH R-HSA-1247673:Erythrocytes take up oxygen and release carbon dioxide T53378 REACPATH R-HSA-1475029:Reversible hydration of carbon dioxide T80975 TARGETID T80975 T80975 FORMERID TTDS00008 T80975 UNIPROID VGFR2_HUMAN T80975 TARGNAME Vascular endothelial growth factor receptor 2 (KDR) T80975 GENENAME KDR T80975 TARGTYPE Successful target T80975 SYNONYMS VEGFR2; VEGFR-2; VEGF-2 receptor; Protein-tyrosine kinase receptor flk-1; Kinase insert domain receptor; Fetal liver kinase 1; FLK1; FLK-1; CD309 T80975 FUNCTION Plays an essential role in the regulation of angiogenesis, vascular development, vascular permeability, and embryonic hematopoiesis. Promotes proliferation, survival, migration and differentiation of endothelial cells. Promotes reorganization of the actin cytoskeleton. Isoforms lacking a transmembrane domain, such as isoform 2 and isoform 3, may function as decoy receptors for VEGFA, VEGFC and/or VEGFD. Isoform 2 plays an important role as negative regulator of VEGFA- and VEGFC-mediated lymphangiogenesis by limiting the amount of free VEGFA and/or VEGFC and preventing their binding to FLT4. Modulates FLT1 and FLT4 signaling by forming heterodimers. Binding of vascular growth factors to isoform 1 leads to the activation of several signaling cascades. Activation of PLCG1 leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate and the activation of protein kinase C. Mediates activation of MAPK1/ERK2, MAPK3/ERK1 and the MAP kinase signaling pathway, as well as of the AKT1 signaling pathway. Mediates phosphorylation of PIK3R1, the regulatory subunit of phosphatidylinositol 3-kinase, reorganization of the actin cytoskeleton and activation of PTK2/FAK1. Required for VEGFA-mediated induction of NOS2 and NOS3, leading to the production of the signaling molecule nitric oxide (NO) by endothelial cells. Phosphorylates PLCG1. Promotes phosphorylation of FYN, NCK1, NOS3, PIK3R1, PTK2/FAK1 and SRC. Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFA, VEGFC and VEGFD. T80975 PDBSTRUC 6GQQ; 6GQP; 6GQO; 5OYJ; 5EW3 T80975 BIOCLASS Kinase T80975 ECNUMBER EC 2.7.10.1 T80975 SEQUENCE MQSKVLLAVALWLCVETRAASVGLPSVSLDLPRLSIQKDILTIKANTTLQITCRGQRDLDWLWPNNQSGSEQRVEVTECSDGLFCKTLTIPKVIGNDTGAYKCFYRETDLASVIYVYVQDYRSPFIASVSDQHGVVYITENKNKTVVIPCLGSISNLNVSLCARYPEKRFVPDGNRISWDSKKGFTIPSYMISYAGMVFCEAKINDESYQSIMYIVVVVGYRIYDVVLSPSHGIELSVGEKLVLNCTARTELNVGIDFNWEYPSSKHQHKKLVNRDLKTQSGSEMKKFLSTLTIDGVTRSDQGLYTCAASSGLMTKKNSTFVRVHEKPFVAFGSGMESLVEATVGERVRIPAKYLGYPPPEIKWYKNGIPLESNHTIKAGHVLTIMEVSERDTGNYTVILTNPISKEKQSHVVSLVVYVPPQIGEKSLISPVDSYQYGTTQTLTCTVYAIPPPHHIHWYWQLEEECANEPSQAVSVTNPYPCEEWRSVEDFQGGNKIEVNKNQFALIEGKNKTVSTLVIQAANVSALYKCEAVNKVGRGERVISFHVTRGPEITLQPDMQPTEQESVSLWCTADRSTFENLTWYKLGPQPLPIHVGELPTPVCKNLDTLWKLNATMFSNSTNDILIMELKNASLQDQGDYVCLAQDRKTKKRHCVVRQLTVLERVAPTITGNLENQTTSIGESIEVSCTASGNPPPQIMWFKDNETLVEDSGIVLKDGNRNLTIRRVRKEDEGLYTCQACSVLGCAKVEAFFIIEGAQEKTNLEIIILVGTAVIAMFFWLLLVIILRTVKRANGGELKTGYLSIVMDPDELPLDEHCERLPYDASKWEFPRDRLKLGKPLGRGAFGQVIEADAFGIDKTATCRTVAVKMLKEGATHSEHRALMSELKILIHIGHHLNVVNLLGACTKPGGPLMVIVEFCKFGNLSTYLRSKRNEFVPYKTKGARFRQGKDYVGAIPVDLKRRLDSITSSQSSASSGFVEEKSLSDVEEEEAPEDLYKDFLTLEHLICYSFQVAKGMEFLASRKCIHRDLAARNILLSEKNVVKICDFGLARDIYKDPDYVRKGDARLPLKWMAPETIFDRVYTIQSDVWSFGVLLWEIFSLGASPYPGVKIDEEFCRRLKEGTRMRAPDYTTPEMYQTMLDCWHGEPSQRPTFSELVEHLGNLLQANAQQDGKDYIVLPISETLSMEEDSGLSLPTSPVSCMEEEEVCDPKFHYDNTAGISQYLQNSKRKSRPVSVKTFEDIPLEEPEVKVIPDDNQTDSGMVLASEELKTLEDRTKLSPSFGGMVPSKSRESVASEGSNQTSGYQSGYHSDDTDTTVYSSEEAELLKLIEIGVQTGSTAQILQPDSGTTLSSPPV T80975 DRUGINFO D01ZRI Axitinib Approved T80975 DRUGINFO D0IQ6P Cabozantinib Approved T80975 DRUGINFO D0R0FO Lenvatinib Approved T80975 DRUGINFO D0F0ZY Pazopanib HCl Approved T80975 DRUGINFO D09HVD Ramucirumab Approved T80975 DRUGINFO D09GDD Regorafenib Approved T80975 DRUGINFO D01PZD Romiplostim Approved T80975 DRUGINFO D0W5HK Sorafenib Approved T80975 DRUGINFO D0R0MW Sunitinib Approved T80975 DRUGINFO D0W7JZ Tivozanib Approved T80975 DRUGINFO D0G6QF Vandetanib Approved T80975 DRUGINFO D0SZ6E YN-968D1 Approved T80975 DRUGINFO D0HS5V Brivanib Phase 3 T80975 DRUGINFO D09VMI Cediranib Phase 3 T80975 DRUGINFO D02WVT E-3810 Phase 3 T80975 DRUGINFO D03JTG Fruquintinib Phase 3 T80975 DRUGINFO D0Q9CY HKI-272 Phase 3 T80975 DRUGINFO D0D7BX Rivoceranib Phase 3 T80975 DRUGINFO D0A1AQ Rosiglitazone + metformin Phase 3 T80975 DRUGINFO D05PWX Sulfatinib Phase 3 T80975 DRUGINFO D05BLN MGCD516 Phase 2/3 T80975 DRUGINFO D0HN7I Alacizumab pegol Phase 2 T80975 DRUGINFO D07NOI BAY-57-9352 Phase 2 T80975 DRUGINFO D0R6UV BMS-690514 Phase 2 T80975 DRUGINFO D00YPR CP-547632 Phase 2 T80975 DRUGINFO D0ZN1R Delphinidin Phase 2 T80975 DRUGINFO D0Z6MT Famitinib Phase 2 T80975 DRUGINFO DN3Z5D L-DOS47 Phase 2 T80975 DRUGINFO D03AND RAF265 Phase 2 T80975 DRUGINFO D09LOZ TTAC-0001 Phase 2 T80975 DRUGINFO D0P6DJ VATALANIB Phase 2 T80975 DRUGINFO D0D1GF XL880 Phase 2 T80975 DRUGINFO D0U6BQ Anti-VEGFR2 CD8 cell therapy Phase 1/2 T80975 DRUGINFO D0Q0HZ Elpamotide Phase 1/2 T80975 DRUGINFO D00DRL MK-2461 Phase 1/2 T80975 DRUGINFO D04NOE OTSGC-A24 Phase 1/2 T80975 DRUGINFO D0FA6S Altiratinib Phase 1 T80975 DRUGINFO D0FD6D CEP-11981 Phase 1 T80975 DRUGINFO D0CY1B CYC116 Phase 1 T80975 DRUGINFO D09ETH E-7050 Phase 1 T80975 DRUGINFO D07HRU KRN633 Phase 1 T80975 DRUGINFO D0N8RV OSI-930 Phase 1 T80975 DRUGINFO D0GM6E Pegdinetanib Phase 1 T80975 DRUGINFO D0ZI5A PF-00337210 Phase 1 T80975 DRUGINFO D0F5JZ PLX-4720 Phase 1 T80975 DRUGINFO D0T2ER TAK-593 Phase 1 T80975 DRUGINFO D07PNT XL999 Phase 1 T80975 DRUGINFO D01AXK Antibodie derivative 10 Patented T80975 DRUGINFO D08XAY Antibodie derivative 6 Patented T80975 DRUGINFO D0AK1F Pyridine derivative 18 Patented T80975 DRUGINFO D0JU8E Pyrimidine derivative 12 Patented T80975 DRUGINFO D0G1YI Pyrimidine derivative 13 Patented T80975 DRUGINFO D06BTN Pyrimidine derivative 14 Patented T80975 DRUGINFO D06HEO Pyrimidine derivative 4 Patented T80975 DRUGINFO D05PRG Quinazoline derivative 15 Patented T80975 DRUGINFO D0DV4X Quinazoline derivative 16 Patented T80975 DRUGINFO D08OXH Quinoline and quinazoline derivative 1 Patented T80975 DRUGINFO D00DQX Motesanib Discontinued in Phase 3 T80975 DRUGINFO D09DJU SU-14813 Discontinued in Phase 2 T80975 DRUGINFO D0E8VF IMC-1C11 Discontinued in Phase 1 T80975 DRUGINFO D06GBK AG1295 Terminated T80975 DRUGINFO D0H4GI CEP-5214 Terminated T80975 DRUGINFO D06GJO (2-Methoxy-phenyl)-(5-phenyl-oxazol-2-yl)-amine Investigative T80975 DRUGINFO D0A9ZQ (3-Phenoxy-phenyl)-(5-phenyl-oxazol-2-yl)-amine Investigative T80975 DRUGINFO D07AIB (4-Phenoxy-phenyl)-quinazolin-4-yl-amine Investigative T80975 DRUGINFO D0D3YL (5-Phenyl-oxazol-2-yl)-m-tolyl-amine Investigative T80975 DRUGINFO D0V9DQ [3-(5-Phenyl-oxazol-2-ylamino)-phenyl]-methanol Investigative T80975 DRUGINFO D0XC6G 2-(1H-indazol-3-yl)-1H-benzo[d]imidazole Investigative T80975 DRUGINFO D03HQK 2-(5-Phenyl-oxazol-2-ylamino)-benzonitrile Investigative T80975 DRUGINFO D0E9DI 2-(p-toluidino)-4-phenylpyrimidine-5-carbonitrile Investigative T80975 DRUGINFO D0J3OZ 2-(pyrimidin-4-ylamino)thiazole-5-carbonitrile Investigative T80975 DRUGINFO D01LEV 3-((3-bromothiophen-2-yl)methylene)indolin-2-one Investigative T80975 DRUGINFO D0M9OF 3-(1H-Indol-2-yl)-1H-quinolin-2-one Investigative T80975 DRUGINFO D00YWZ 3-(4-aminophenyl)thieno[3,2-c]pyridin-4-amine Investigative T80975 DRUGINFO D0EK0G 3-(4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione Investigative T80975 DRUGINFO D0J2XD 3-(5-Phenyl-oxazol-2-ylamino)-benzonitrile Investigative T80975 DRUGINFO D0UX3T 3-(5-Thiophen-3-yl-pyridin-3-yl)-1H-indole Investigative T80975 DRUGINFO D00NYT 3,4-di-(4-methoxyphenyl)-1H-pyrrole-2,5-dione Investigative T80975 DRUGINFO D0C3WY 3,4-diphenyl-1H-pyrrole-2,5-dione Investigative T80975 DRUGINFO D0YN1E 3,6-Di-pyridin-4-yl-pyrazolo[1,5-a]pyrimidine Investigative T80975 DRUGINFO D07QMC 3-Benzimidazol-2-ylhydroquinolin-2-one Investigative T80975 DRUGINFO D0F0AU 3-methyl-1H-thieno[2,3-c]pyrazole-5-carboxamide Investigative T80975 DRUGINFO D09TQP 3-phenyl-1,4-dihydroindeno[1,2-c]pyrazole Investigative T80975 DRUGINFO D0Y9GK 4-(4-aminophenyl)-1H-indazol-3yl-amine Investigative T80975 DRUGINFO D09AKX 4-(4-m-Tolylamino-phthalazin-1-yl)-benzamide Investigative T80975 DRUGINFO D08JSJ 4-(4-p-Tolylamino-phthalazin-1-yl)-benzamide Investigative T80975 DRUGINFO D09LEK 4-(5-Phenyl-oxazol-2-ylamino)-benzenesulfonamide Investigative T80975 DRUGINFO D0D3QA 4-(isoquinolin-5-yl)-N-m-tolylphthalazin-1-amine Investigative T80975 DRUGINFO D03HTT 4-(isoquinolin-5-yl)-N-o-tolylphthalazin-1-amine Investigative T80975 DRUGINFO D0KH5T 4-[3-Hydroxyanilino]-6,7-Dimethoxyquinazoline Investigative T80975 DRUGINFO D0UZ5W 4-Chloro-N-(2-chloro-benzoyl)-benzenesulfonamide Investigative T80975 DRUGINFO D0V4BR 4-Chloro-N-(2-methyl-benzoyl)-benzenesulfonamide Investigative T80975 DRUGINFO D05THI 4-Chloro-N-(3-chloro-benzoyl)-benzenesulfonamide Investigative T80975 DRUGINFO D09MSA 4-Chloro-N-(4-chloro-benzoyl)-benzenesulfonamide Investigative T80975 DRUGINFO D0C6OD 4-Chloro-N-(4-nitro-benzoyl)-benzenesulfonamide Investigative T80975 DRUGINFO D06BVH 4-phenyl-2-(phenylamino)pyrimidine-5-carbonitrile Investigative T80975 DRUGINFO D0U3ZP 5-(4-Methoxy-phenyl)-1-phenyl-1H-benzoimidazole Investigative T80975 DRUGINFO D00MCJ 6-(1H-Benzoimidazol-2-yl)-benzocyclohepten-7-one Investigative T80975 DRUGINFO D09HXU 6-o-tolylquinazolin-2-amine Investigative T80975 DRUGINFO D04RQU 8-methyl-4H,7H-indolo[6,5,4-cd]indol-5-one Investigative T80975 DRUGINFO D0EE6A AAL-993 Investigative T80975 DRUGINFO D07SRX AG-E-85378 Investigative T80975 DRUGINFO D0AK4H AMG-429 Investigative T80975 DRUGINFO D0N7AJ AST-487 Investigative T80975 DRUGINFO D05GMB BIBF-1202 Investigative T80975 DRUGINFO D0M4SY BMS-536924 Investigative T80975 DRUGINFO D0Z7TM BMS-645737 Investigative T80975 DRUGINFO D0RG0Z BX-795 Investigative T80975 DRUGINFO D0IX7Y BX-912 Investigative T80975 DRUGINFO D0C6KI CB-676475 Investigative T80975 DRUGINFO D09QBA CEP-5104 Investigative T80975 DRUGINFO D0R3IK EPI-0030 Investigative T80975 DRUGINFO D0ST4P IM-023911 Investigative T80975 DRUGINFO D0Z8TR IM-094261 Investigative T80975 DRUGINFO D0A9ZP IM-094882 Investigative T80975 DRUGINFO D00GVV Indolin-2-one deriv. 4b Investigative T80975 DRUGINFO D02AOT Isoindolinone Urea derivative Investigative T80975 DRUGINFO D0Q4EQ JNJ-38158471 Investigative T80975 DRUGINFO D02RWK K-252a analogue Investigative T80975 DRUGINFO D08BJR Ki-20227 Investigative T80975 DRUGINFO D0E3HC L000021649 Investigative T80975 DRUGINFO D07XBW N-(2,4-Dichloro-benzoyl)-benzenesulfonamide Investigative T80975 DRUGINFO D0M2QA N-(3-Bromo-benzoyl)-4-chloro-benzenesulfonamide Investigative T80975 DRUGINFO D0BM4F Phenyl-(5-phenyl-oxazol-2-yl)-amine Investigative T80975 DRUGINFO D0C2GE PMID22765894C8h Investigative T80975 DRUGINFO D0PP6Y PMID23639540C13a Investigative T80975 DRUGINFO D03EHM PP121 Investigative T80975 DRUGINFO D09LKM Pyrazolo[1,5-a]pyrimidine 3G Investigative T80975 DRUGINFO D07OIZ R-84 Investigative T80975 DRUGINFO D09XIL Ro-4396686 Investigative T80975 DRUGINFO D09LPL SU-11652 Investigative T80975 DRUGINFO D0H1OK TG-100435 Investigative T80975 DRUGINFO D07OSK VEGF receptor 2 kinase inhibitor I Investigative T80975 KEGGPATH hsa04014:Ras signaling pathway T80975 KEGGPATH hsa04015:Rap1 signaling pathway T80975 KEGGPATH hsa04060:Cytokine-cytokine receptor interaction T80975 KEGGPATH hsa04144:Endocytosis T80975 KEGGPATH hsa04151:PI3K-Akt signaling pathway T80975 KEGGPATH hsa04370:VEGF signaling pathway T80975 KEGGPATH hsa04510:Focal adhesion T80975 KEGGPATH hsa05205:Proteoglycans in cancer T80975 WIKIPATH WP1539:Angiogenesis T80975 WIKIPATH WP1919:Signaling by VEGF T80975 WIKIPATH WP2406:Cardiac Progenitor Differentiation T80975 WIKIPATH WP259:Nifedipine Activity T80975 WIKIPATH WP306:Focal Adhesion T80975 REACPATH R-HSA-194306:Neurophilin interactions with VEGF and VEGFR T80975 REACPATH R-HSA-195399:VEGF binds to VEGFR leading to receptor dimerization T80975 REACPATH R-HSA-216083:Integrin cell surface interactions T80975 REACPATH R-HSA-3928663:EPHA-mediated growth cone collapse T80975 REACPATH R-HSA-4420097:VEGFA-VEGFR2 Pathway T80975 REACPATH R-HSA-5218921:VEGFR2 mediated cell proliferation T80975 NET_PATH NetPath_14:IL2 Signaling Pathway T80975 INTEPATH avb3_integrin_pathway:Integrins in angiogenesis T80975 INTEPATH hes_heypathway:Notch-mediated HES/HEY network T80975 INTEPATH hif2pathway:HIF-2-alpha transcription factor network T80975 INTEPATH integrin3_pathway:Beta3 integrin cell surface interactions T80975 INTEPATH s1p_s1p1_pathway:S1P1 pathway T80975 INTEPATH shp2_pathway:SHP2 signaling T80975 INTEPATH tcptp_pathway:Signaling events mediated by TCPTP T80975 INTEPATH vegf_vegfr_pathway:VEGF and VEGFR signaling network T80975 INTEPATH vegfr1_2_pathway:Signaling events mediated by VEGFR1 and VEGFR2 T80975 PANTPATH P00005:Angiogenesis T80975 PANTPATH P00056:VEGF signaling pathway T74312 TARGETID T74312 T74312 FORMERID TTDS00090 T74312 UNIPROID FLT3_HUMAN T74312 TARGNAME Fms-like tyrosine kinase 3 (FLT-3) T74312 GENENAME FLT3 T74312 TARGTYPE Successful target T74312 SYNONYMS Stem cell tyrosine kinase 1; STK1; STK-1; Receptor-type tyrosine-protein kinase FLT3; Fetal liver kinase-2; FLT-3; FLK2; FLK-2; FL cytokine receptor; CD135 T74312 FUNCTION Tyrosine-protein kinase that acts as cell-surface receptor for the cytokine FLT3LG and regulates differentiation, proliferation and survival of hematopoietic progenitor cells and of dendritic cells. Promotes phosphorylation of SHC1 and AKT1, and activation of the downstream effector MTOR. Promotes activation of RAS signaling and phosphorylation of downstream kinases, including MAPK1/ERK2 and/or MAPK3/ERK1. Promotes phosphorylation of FES, FER, PTPN6/SHP, PTPN11/SHP-2, PLCG1, and STAT5A and/or STAT5B. Activation of wild-type FLT3 causes only marginal activation of STAT5A or STAT5B. Mutations that cause constitutive kinase activity promote cell proliferation and resistance to apoptosis via the activation of multiple signaling pathways. T74312 PDBSTRUC 6IL3; 5X02; 4XUF; 4RT7; 3QS9 T74312 BIOCLASS Kinase T74312 ECNUMBER EC 2.7.10.1 T74312 SEQUENCE MPALARDGGQLPLLVVFSAMIFGTITNQDLPVIKCVLINHKNNDSSVGKSSSYPMVSESPEDLGCALRPQSSGTVYEAAAVEVDVSASITLQVLVDAPGNISCLWVFKHSSLNCQPHFDLQNRGVVSMVILKMTETQAGEYLLFIQSEATNYTILFTVSIRNTLLYTLRRPYFRKMENQDALVCISESVPEPIVEWVLCDSQGESCKEESPAVVKKEEKVLHELFGTDIRCCARNELGRECTRLFTIDLNQTPQTTLPQLFLKVGEPLWIRCKAVHVNHGFGLTWELENKALEEGNYFEMSTYSTNRTMIRILFAFVSSVARNDTGYYTCSSSKHPSQSALVTIVEKGFINATNSSEDYEIDQYEEFCFSVRFKAYPQIRCTWTFSRKSFPCEQKGLDNGYSISKFCNHKHQPGEYIFHAENDDAQFTKMFTLNIRRKPQVLAEASASQASCFSDGYPLPSWTWKKCSDKSPNCTEEITEGVWNRKANRKVFGQWVSSSTLNMSEAIKGFLVKCCAYNSLGTSCETILLNSPGPFPFIQDNISFYATIGVCLLFIVVLTLLICHKYKKQFRYESQLQMVQVTGSSDNEYFYVDFREYEYDLKWEFPRENLEFGKVLGSGAFGKVMNATAYGISKTGVSIQVAVKMLKEKADSSEREALMSELKMMTQLGSHENIVNLLGACTLSGPIYLIFEYCCYGDLLNYLRSKREKFHRTWTEIFKEHNFSFYPTFQSHPNSSMPGSREVQIHPDSDQISGLHGNSFHSEDEIEYENQKRLEEEEDLNVLTFEDLLCFAYQVAKGMEFLEFKSCVHRDLAARNVLVTHGKVVKICDFGLARDIMSDSNYVVRGNARLPVKWMAPESLFEGIYTIKSDVWSYGILLWEIFSLGVNPYPGIPVDANFYKLIQNGFKMDQPFYATEEIYIIMQSCWAFDSRKRPSFPNLTSFLGCQLADAEEAMYQNVDGRVSECPHTYQNRRPFSREMDLGLLSPQAQVEDS T74312 DRUGINFO D04KZY Gilteritinib Approved T74312 DRUGINFO D09HNV Intedanib Approved T74312 DRUGINFO D0V9WF Lestaurtinib Approved (orphan drug) T74312 DRUGINFO D07NVU Midostaurin Approved T74312 DRUGINFO D09TAB Pexidartinib Approved T74312 DRUGINFO D0H0EQ Ponatinib Approved T74312 DRUGINFO D01XYJ Zidovudine Approved T74312 DRUGINFO D07KYT AC220 Phase 3 T74312 DRUGINFO D0PN8H Pacritinib Phase 3 T74312 DRUGINFO D0R6UV BMS-690514 Phase 2 T74312 DRUGINFO D0Q8CV CDX-301 Phase 2 T74312 DRUGINFO D0Z6MT Famitinib Phase 2 T74312 DRUGINFO D06KTJ TAK-659 Phase 2 T74312 DRUGINFO D28HJI FF-10101 Phase 1/2 T74312 DRUGINFO DI1VM3 HM43239 Phase 1/2 T74312 DRUGINFO D00DRL MK-2461 Phase 1/2 T74312 DRUGINFO D0V2ZC SEL24 Phase 1/2 T74312 DRUGINFO D0X8ID SEL-24 Phase 1/2 T74312 DRUGINFO D07UUB 4SC-203 Phase 1 T74312 DRUGINFO D91CMX AMG 427 Phase 1 T74312 DRUGINFO D0YQ9I FF-10101-01 Phase 1 T74312 DRUGINFO DKCU40 FN-1501 Phase 1 T74312 DRUGINFO D07ZNF IMC-EB10 Phase 1 T74312 DRUGINFO D0D1HS Ki23819 Phase 1 T74312 DRUGINFO D00ABO KW-2449 Phase 1 T74312 DRUGINFO D10LNV MRX-2843 Phase 1 T74312 DRUGINFO DIA08F SKI-G-801 Phase 1 T74312 DRUGINFO D0MX7B Carboxamide derivative 4 Patented T74312 DRUGINFO D0AK1F Pyridine derivative 18 Patented T74312 DRUGINFO D0IT6Q Tandutinib Discontinued in Phase 2 T74312 DRUGINFO D04GFO MC-2001 Preclinical T74312 DRUGINFO D06GBK AG1295 Terminated T74312 DRUGINFO D01MIP SU5614 Terminated T74312 DRUGINFO D09OLH (1H-indol-2-yl)(5-methoxy-1H-indol-2-yl)methanone Investigative T74312 DRUGINFO D0G0KQ (1H-indol-2-yl)(5-phenoxy-1H-indol-2-yl)methanone Investigative T74312 DRUGINFO D0D7ZL (1H-indol-2-yl)(6-methoxy-1H-indol-2-yl)methanone Investigative T74312 DRUGINFO D0H7MF (5-fluoro-1H-indol-2-yl)-(1H-indol-2-yl)methanone Investigative T74312 DRUGINFO D0XS9E (5-hydroxy-1H-indol-2-yl)(1H-indol-2-yl)methanone Investigative T74312 DRUGINFO D0I7QX (benzo[b]furan-2-yl)-(1H-indol-2-yl)methanone Investigative T74312 DRUGINFO D0ZO8Z 2-(3,4-dimethoxybenzamido)thiophene-3-carboxamide Investigative T74312 DRUGINFO D0Y9GK 4-(4-aminophenyl)-1H-indazol-3yl-amine Investigative T74312 DRUGINFO D0D0TQ AKN-028 Investigative T74312 DRUGINFO D0N7AJ AST-487 Investigative T74312 DRUGINFO D0L0MZ Bis(5-acetoxybenzo[b]furan-2-yl)methanone Investigative T74312 DRUGINFO D07AXL Bis(5-aminobenzo[b]furan-2-yl)methanone Investigative T74312 DRUGINFO D0I3XZ Bis-(5-hydroxy-1H-indol-2-yl)-methanone Investigative T74312 DRUGINFO D02OBA Bis(5-hydroxybenzo[b]furan-2-yl)methanone Investigative T74312 DRUGINFO D03VAA Bis(6-hydroxybenzo[b]furan-2-yl)methanone Investigative T74312 DRUGINFO D0Z3DW Bis(benzo[b]furan-2-yl)methanone Investigative T74312 DRUGINFO D0G5YI Di(1H-indol-2-yl)methanone Investigative T74312 DRUGINFO D0N3XP G749 Investigative T74312 DRUGINFO D0UN9O GTP-14564 Investigative T74312 DRUGINFO D0X1JO IN1479 Investigative T74312 DRUGINFO D0Y4BL JNJ-28312141 Investigative T74312 DRUGINFO D0X6KS N-[4-(3-amino-1H-indazol-4-yl)phenyl]benzamide Investigative T74312 DRUGINFO D06UKS PMID21982499C14k Investigative T74312 DRUGINFO D0C2GE PMID22765894C8h Investigative T74312 DRUGINFO D0E7VO PMID24900538C2c Investigative T74312 DRUGINFO D0X7JK TCS-359 Investigative T74312 DRUGINFO D07ADX URMC-099 Investigative T74312 KEGGPATH hsa04060:Cytokine-cytokine receptor interaction T74312 KEGGPATH hsa04640:Hematopoietic cell lineage T74312 KEGGPATH hsa05200:Pathways in cancer T74312 KEGGPATH hsa05202:Transcriptional misregulation in cancer T74312 KEGGPATH hsa05221:Acute myeloid leukemia T74312 KEGGPATH hsa05230:Central carbon metabolism in cancer T75243 TARGETID T75243 T75243 FORMERID TTDS00265 T75243 UNIPROID MTOR_HUMAN T75243 TARGNAME Serine/threonine-protein kinase mTOR (mTOR) T75243 GENENAME MTOR T75243 TARGTYPE Successful target T75243 SYNONYMS Target of rapamycin; TOR kinase; Rapamycin target protein 1; Rapamycin target protein; Rapamycin and FKBP12 target 1; RAPT1; RAFT1; Mechanistic target of rapamycin; Mammalian target of rapamycin; FRAP2; FRAP1; FRAP; FKBP12-rapamycin complex-associated protein; FKBP-rapamycin associated protein; FK506-binding protein 12-rapamycin complex-associated protein 1 T75243 FUNCTION MTOR directly or indirectly regulates the phosphorylation of at least 800 proteins. Functions as part of 2 structurally and functionally distinct signaling complexes mTORC1 and mTORC2 (mTOR complex 1 and 2). Activated mTORC1 up-regulates protein synthesis by phosphorylating key regulators of mRNA translation and ribosome synthesis. This includes phosphorylation of EIF4EBP1 and release of its inhibition toward the elongation initiation factor 4E (eiF4E). Moreover, phosphorylates and activates RPS6KB1 and RPS6KB2 that promote protein synthesis by modulating the activity of their downstream targets including ribosomal protein S6, eukaryotic translation initiation factor EIF4B, and the inhibitor of translation initiation PDCD4. Stimulates the pyrimidine biosynthesis pathway, both by acute regulation through RPS6KB1-mediated phosphorylation of the biosynthetic enzyme CAD, and delayed regulation, through transcriptional enhancement of the pentose phosphate pathway which produces 5-phosphoribosyl-1-pyrophosphate (PRPP), an allosteric activator of CAD at a later step in synthesis, this function is dependent on the mTORC1 complex. Regulates ribosome synthesis by activating RNA polymerase III-dependent transcription through phosphorylation and inhibition of MAF1 an RNA polymerase III-repressor. In parallel to protein synthesis, also regulates lipid synthesis through SREBF1/SREBP1 and LPIN1. To maintain energy homeostasis mTORC1 may also regulate mitochondrial biogenesis through regulation of PPARGC1A. mTORC1 also negatively regulates autophagy through phosphorylation of ULK1. Under nutrient sufficiency, phosphorylates ULK1 at 'Ser-758', disrupting the interaction with AMPK and preventing activation of ULK1. Also prevents autophagy through phosphorylation of the autophagy inhibitor DAP. Also prevents autophagy by phosphorylating RUBCNL/Pacer under nutrient-rich conditions. mTORC1 exerts a feedback control on upstream growth factor signaling that includes phosphorylation and activation of GRB10 a INSR-dependent signaling suppressor. Among other potential targets mTORC1 may phosphorylate CLIP1 and regulate microtubules. As part of the mTORC2 complex MTOR may regulate other cellular processes including survival and organization of the cytoskeleton. Plays a critical role in the phosphorylation at 'Ser-473' of AKT1, a pro-survival effector of phosphoinositide 3-kinase, facilitating its activation by PDK1. mTORC2 may regulate the actin cytoskeleton, through phosphorylation of PRKCA, PXN and activation of the Rho-type guanine nucleotide exchange factors RHOA and RAC1A or RAC1B. mTORC2 also regulates the phosphorylation of SGK1 at 'Ser-422'. Regulates osteoclastogenesis by adjusting the expression of CEBPB isoforms. Plays an important regulatory role in the circadian clock function; regulates period length and rhythm amplitude of the suprachiasmatic nucleus (SCN) and liver clocks. Serine/threonine protein kinase which is a central regulator of cellular metabolism, growth and survival in response to hormones, growth factors, nutrients, energy and stress signals. T75243 PDBSTRUC 6BCX; 6BCU; 5ZCS; 5WBY; 5WBU T75243 BIOCLASS Kinase T75243 ECNUMBER EC 2.7.11.1 T75243 SEQUENCE MLGTGPAAATTAATTSSNVSVLQQFASGLKSRNEETRAKAAKELQHYVTMELREMSQEESTRFYDQLNHHIFELVSSSDANERKGGILAIASLIGVEGGNATRIGRFANYLRNLLPSNDPVVMEMASKAIGRLAMAGDTFTAEYVEFEVKRALEWLGADRNEGRRHAAVLVLRELAISVPTFFFQQVQPFFDNIFVAVWDPKQAIREGAVAALRACLILTTQREPKEMQKPQWYRHTFEEAEKGFDETLAKEKGMNRDDRIHGALLILNELVRISSMEGERLREEMEEITQQQLVHDKYCKDLMGFGTKPRHITPFTSFQAVQPQQSNALVGLLGYSSHQGLMGFGTSPSPAKSTLVESRCCRDLMEEKFDQVCQWVLKCRNSKNSLIQMTILNLLPRLAAFRPSAFTDTQYLQDTMNHVLSCVKKEKERTAAFQALGLLSVAVRSEFKVYLPRVLDIIRAALPPKDFAHKRQKAMQVDATVFTCISMLARAMGPGIQQDIKELLEPMLAVGLSPALTAVLYDLSRQIPQLKKDIQDGLLKMLSLVLMHKPLRHPGMPKGLAHQLASPGLTTLPEASDVGSITLALRTLGSFEFEGHSLTQFVRHCADHFLNSEHKEIRMEAARTCSRLLTPSIHLISGHAHVVSQTAVQVVADVLSKLLVVGITDPDPDIRYCVLASLDERFDAHLAQAENLQALFVALNDQVFEIRELAICTVGRLSSMNPAFVMPFLRKMLIQILTELEHSGIGRIKEQSARMLGHLVSNAPRLIRPYMEPILKALILKLKDPDPDPNPGVINNVLATIGELAQVSGLEMRKWVDELFIIIMDMLQDSSLLAKRQVALWTLGQLVASTGYVVEPYRKYPTLLEVLLNFLKTEQNQGTRREAIRVLGLLGALDPYKHKVNIGMIDQSRDASAVSLSESKSSQDSSDYSTSEMLVNMGNLPLDEFYPAVSMVALMRIFRDQSLSHHHTMVVQAITFIFKSLGLKCVQFLPQVMPTFLNVIRVCDGAIREFLFQQLGMLVSFVKSHIRPYMDEIVTLMREFWVMNTSIQSTIILLIEQIVVALGGEFKLYLPQLIPHMLRVFMHDNSPGRIVSIKLLAAIQLFGANLDDYLHLLLPPIVKLFDAPEAPLPSRKAALETVDRLTESLDFTDYASRIIHPIVRTLDQSPELRSTAMDTLSSLVFQLGKKYQIFIPMVNKVLVRHRINHQRYDVLICRIVKGYTLADEEEDPLIYQHRMLRSGQGDALASGPVETGPMKKLHVSTINLQKAWGAARRVSKDDWLEWLRRLSLELLKDSSSPSLRSCWALAQAYNPMARDLFNAAFVSCWSELNEDQQDELIRSIELALTSQDIAEVTQTLLNLAEFMEHSDKGPLPLRDDNGIVLLGERAAKCRAYAKALHYKELEFQKGPTPAILESLISINNKLQQPEAAAGVLEYAMKHFGELEIQATWYEKLHEWEDALVAYDKKMDTNKDDPELMLGRMRCLEALGEWGQLHQQCCEKWTLVNDETQAKMARMAAAAAWGLGQWDSMEEYTCMIPRDTHDGAFYRAVLALHQDLFSLAQQCIDKARDLLDAELTAMAGESYSRAYGAMVSCHMLSELEEVIQYKLVPERREIIRQIWWERLQGCQRIVEDWQKILMVRSLVVSPHEDMRTWLKYASLCGKSGRLALAHKTLVLLLGVDPSRQLDHPLPTVHPQVTYAYMKNMWKSARKIDAFQHMQHFVQTMQQQAQHAIATEDQQHKQELHKLMARCFLKLGEWQLNLQGINESTIPKVLQYYSAATEHDRSWYKAWHAWAVMNFEAVLHYKHQNQARDEKKKLRHASGANITNATTAATTAATATTTASTEGSNSESEAESTENSPTPSPLQKKVTEDLSKTLLMYTVPAVQGFFRSISLSRGNNLQDTLRVLTLWFDYGHWPDVNEALVEGVKAIQIDTWLQVIPQLIARIDTPRPLVGRLIHQLLTDIGRYHPQALIYPLTVASKSTTTARHNAANKILKNMCEHSNTLVQQAMMVSEELIRVAILWHEMWHEGLEEASRLYFGERNVKGMFEVLEPLHAMMERGPQTLKETSFNQAYGRDLMEAQEWCRKYMKSGNVKDLTQAWDLYYHVFRRISKQLPQLTSLELQYVSPKLLMCRDLELAVPGTYDPNQPIIRIQSIAPSLQVITSKQRPRKLTLMGSNGHEFVFLLKGHEDLRQDERVMQLFGLVNTLLANDPTSLRKNLSIQRYAVIPLSTNSGLIGWVPHCDTLHALIRDYREKKKILLNIEHRIMLRMAPDYDHLTLMQKVEVFEHAVNNTAGDDLAKLLWLKSPSSEVWFDRRTNYTRSLAVMSMVGYILGLGDRHPSNLMLDRLSGKILHIDFGDCFEVAMTREKFPEKIPFRLTRMLTNAMEVTGLDGNYRITCHTVMEVLREHKDSVMAVLEAFVYDPLLNWRLMDTNTKGNKRSRTRTDSYSAGQSVEILDGVELGEPAHKKTGTTVPESIHSFIGDGLVKPEALNKKAIQIINRVRDKLTGRDFSHDDTLDVPTQVELLIKQATSHENLCQCYIGWCPFW T75243 DRUGINFO D0K3QS Everolimus Approved T75243 DRUGINFO D03FCF Novolimus Approved T75243 DRUGINFO D0S5LO PF-04449913 Approved T75243 DRUGINFO D03LJR Sirolimus Approved T75243 DRUGINFO D0ES1Q Temsirolimus Approved T75243 DRUGINFO D0V7WS Zotarolimus Approved T75243 DRUGINFO D0O3CV Ridaforolimus Phase 3 T75243 DRUGINFO D0W3UV ABI-009 Phase 2 T75243 DRUGINFO D0Z2UQ AZD2014 Phase 2 T75243 DRUGINFO D0VG0D BEZ235 Phase 2 T75243 DRUGINFO D0O6VZ GDC-0980/RG7422 Phase 2 T75243 DRUGINFO D03DPZ INK128 Phase 2 T75243 DRUGINFO D0H1WC LY3023414 Phase 2 T75243 DRUGINFO D00BUO MM-141 Phase 2 T75243 DRUGINFO D0H7XL OSI-027 Phase 2 T75243 DRUGINFO D0N5JZ PF-04691502 Phase 2 T75243 DRUGINFO D0D8JB PF-05212384 Phase 2 T75243 DRUGINFO D0TU7B PQR309 Phase 2 T75243 DRUGINFO D00KTV Salirasib Phase 2 T75243 DRUGINFO D01PGR SAR245409 Phase 2 T75243 DRUGINFO D03NJY SF1126 Phase 2 T75243 DRUGINFO D0X7IN BGT226 Phase 1/2 T75243 DRUGINFO D05EXN CC-223 Phase 1/2 T75243 DRUGINFO D03IXK ME-344 Phase 1/2 T75243 DRUGINFO D08PSC BI 860585 Phase 1 T75243 DRUGINFO D0R9VX DS-3078 Phase 1 T75243 DRUGINFO D0X4RT DS-7423 Phase 1 T75243 DRUGINFO D0U8QH GDC-0349 Phase 1 T75243 DRUGINFO D0QN5M LAM-001 Phase 1 T75243 DRUGINFO D0Y0FE PWT-33597 Phase 1 T75243 DRUGINFO D0U3DP VS-5584 Phase 1 T75243 DRUGINFO D0X5VI PMID25726713-Compound-47 Patented T75243 DRUGINFO D0WJ3W PMID25726713-Compound-48 Patented T75243 DRUGINFO D07TVO PMID25726713-Compound-49 Patented T75243 DRUGINFO D0Y8JF PMID25726713-Compound-50 Patented T75243 DRUGINFO D0KH7Q PMID25726713-Compound-51 Patented T75243 DRUGINFO D0K1VK AZD8055 Discontinued in Phase 1/2 T75243 DRUGINFO D0H5MX TAFA-93 Discontinued in Phase 1 T75243 DRUGINFO D05SXC SCR-44001 Terminated T75243 DRUGINFO D00GQM (4-(6-morpholino-9H-purin-2-yl)phenyl)methanol Investigative T75243 DRUGINFO D0X7TB 2-(2-Methyl-morpholin-4-yl)-benzo[h]chromen-4-one Investigative T75243 DRUGINFO D07JKB 2-(6-morpholino-9H-purin-2-yl)phenol Investigative T75243 DRUGINFO D0P0UV 2-chloro-N-(6-cyanopyridin-3-yl)propanamide Investigative T75243 DRUGINFO D0T0BY 2-Morpholin-4-yl-pyrimido[2,1-a]isoquinolin-4-one Investigative T75243 DRUGINFO D0TC5H 3-(6-morpholino-9H-purin-2-yl)phenol Investigative T75243 DRUGINFO D0Y1DR 4-(2-(1H-indol-6-yl)-9H-purin-6-yl)morpholine Investigative T75243 DRUGINFO D0AH8Q 4-(2-(thiophen-2-yl)-9H-purin-6-yl)morpholine Investigative T75243 DRUGINFO D0F1SI 4-(2-(thiophen-3-yl)-9H-purin-6-yl)morpholine Investigative T75243 DRUGINFO D09FBN 4-(6-morpholino-9H-purin-2-yl)phenol Investigative T75243 DRUGINFO D0U8GR AP-21967 Investigative T75243 DRUGINFO D0N9TK AR-mTOR-26 Investigative T75243 DRUGINFO D02TCF C-16-(S)-3-methylindolerapamycin Investigative T75243 DRUGINFO D0JD4S CU-906 Investigative T75243 DRUGINFO D0H4KF EC-0565 Investigative T75243 DRUGINFO D0A8ES EC-0845 Investigative T75243 DRUGINFO D09VHS EM-101 Investigative T75243 DRUGINFO D0W1ST Ethyl 1-[(1H-benzimidazol-2(3H)one-5-yl)sulfonyl]-1H-pyrrole-2-carboxylate Investigative T75243 DRUGINFO D02ELN HM-5016699 Investigative T75243 DRUGINFO D0J9PK OXA-01 Investigative T75243 DRUGINFO D07NFT P-2281 Investigative T75243 DRUGINFO D0QE9F P-6915 Investigative T75243 DRUGINFO D05RSS PF-03772304 Investigative T75243 DRUGINFO D03XRZ PF-05094037 Investigative T75243 DRUGINFO D03EHM PP121 Investigative T75243 DRUGINFO D0H2CM PP-242 Investigative T75243 DRUGINFO D01AQN Rapamycin complexed with immunophilin FKBP12 Investigative T75243 DRUGINFO D0E1YN SB-2280 Investigative T75243 DRUGINFO D05SOW SX-MTR1 Investigative T75243 DRUGINFO D0H0HR torin 1 Investigative T75243 DRUGINFO D2B7WM Torin2 Investigative T75243 DRUGINFO D08BTX X-387 Investigative T75243 KEGGPATH hsa04012:ErbB signaling pathway T75243 KEGGPATH hsa04066:HIF-1 signaling pathway T75243 KEGGPATH hsa04150:mTOR signaling pathway T75243 KEGGPATH hsa04151:PI3K-Akt signaling pathway T75243 KEGGPATH hsa04152:AMPK signaling pathway T75243 KEGGPATH hsa04910:Insulin signaling pathway T75243 KEGGPATH hsa04919:Thyroid hormone signaling pathway T75243 KEGGPATH hsa04920:Adipocytokine signaling pathway T75243 KEGGPATH hsa04930:Type II diabetes mellitus T75243 KEGGPATH hsa05200:Pathways in cancer T75243 KEGGPATH hsa05205:Proteoglycans in cancer T75243 KEGGPATH hsa05206:MicroRNAs in cancer T75243 KEGGPATH hsa05214:Glioma T75243 KEGGPATH hsa05215:Prostate cancer T75243 KEGGPATH hsa05221:Acute myeloid leukemia T75243 KEGGPATH hsa05230:Central carbon metabolism in cancer T75243 KEGGPATH hsa05231:Choline metabolism in cancer T75243 WIKIPATH WP1403:AMPK Signaling T75243 WIKIPATH WP1471:TOR Signaling T75243 WIKIPATH WP1544:MicroRNAs in cardiomyocyte hypertrophy T75243 WIKIPATH WP1584:Type II diabetes mellitus T75243 WIKIPATH WP1799:Costimulation by the CD28 family T75243 WIKIPATH WP1913:Signaling by Insulin receptor T75243 WIKIPATH WP1982:SREBP signalling T75243 WIKIPATH WP1984:Integrated Breast Cancer Pathway T75243 WIKIPATH WP2011:SREBF and miR33 in cholesterol and lipid homeostasis T75243 WIKIPATH WP2018:RANKL/RANK Signaling Pathway T75243 WIKIPATH WP2032:TSH signaling pathway T75243 WIKIPATH WP2034:Leptin signaling pathway T75243 WIKIPATH WP2035:FSH signaling pathway T75243 WIKIPATH WP2203:TSLP Signaling Pathway T75243 WIKIPATH WP2263:Prostate Cancer T75243 WIKIPATH WP2374:Oncostatin M Signaling Pathway T75243 WIKIPATH WP2380:BDNF signaling pathway T75243 WIKIPATH WP244:Alpha 6 Beta 4 signaling pathway T75243 WIKIPATH WP2571:Polycystic Kidney Disease Pathway T75243 WIKIPATH WP2653:PIP3 activates AKT signaling T75243 WIKIPATH WP2677:Signaling by Type 1 Insulin-like Growth Factor 1 Receptor (IGF1R) T75243 WIKIPATH WP2795:Cardiac Hypertrophic Response T75243 WIKIPATH WP2870:Extracellular vesicle-mediated signaling in recipient cells T75243 WIKIPATH WP363:Wnt Signaling Pathway Netpath T75243 WIKIPATH WP437:EGF/EGFR Signaling Pathway T75243 WIKIPATH WP481:Insulin Signaling T75243 WIKIPATH WP585:Interferon type I signaling pathways T75243 WIKIPATH WP615:Senescence and Autophagy in Cancer T75243 WIKIPATH WP673:ErbB Signaling Pathway T75243 WHIZPATH PW000659:Leucine Stimulation on Insulin Signaling T75243 REACPATH R-HSA-1257604:PIP3 activates AKT signaling T75243 REACPATH R-HSA-1632852:Macroautophagy T75243 REACPATH R-HSA-166208:mTORC1-mediated signalling T75243 REACPATH R-HSA-3371571:HSF1-dependent transactivation T75243 REACPATH R-HSA-389357:CD28 dependent PI3K/Akt signaling T75243 REACPATH R-HSA-5218920:VEGFR2 mediated vascular permeability T75243 REACPATH R-HSA-5628897:TP53 Regulates Metabolic Genes T75243 REACPATH R-HSA-5674400:Constitutive Signaling by AKT1 E17K in Cancer T75243 INTEPATH cdc42_pathway:CDC42 signaling events T75243 INTEPATH cxcr3pathway:CXCR3-mediated signaling events T75243 INTEPATH cxcr4_pathway:CXCR4-mediated signaling events T75243 INTEPATH erbb1_downstream_pathway:ErbB1 downstream signaling T75243 INTEPATH erbb2erbb3pathway:ErbB2/ErbB3 signaling events T75243 INTEPATH et_egfrpathway:EGFR-dependent Endothelin signaling events T75243 INTEPATH ifngpathway:IFN-gamma pathway T75243 INTEPATH il12_2pathway:IL12-mediated signaling events T75243 INTEPATH il2_pi3kpathway:IL2 signaling events mediated by PI3K T75243 INTEPATH il4_2pathway:IL4-mediated signaling events T75243 INTEPATH lkb1_pathway:LKB1 signaling events T75243 INTEPATH met_pathway:Signaling events mediated by Hepatocyte Growth Factor Receptor (c-Met) T75243 INTEPATH mtor_4pathway:mTOR signaling pathway T75243 INTEPATH pi3kciaktpathway:Class I PI3K signaling events mediated by Akt T75243 INTEPATH telomerasepathway:Regulation of Telomerase T75243 PANTPATH P00030:Hypoxia response via HIF activation T75243 PANTPATH P00036:Interleukin signaling pathway T25005 TARGETID T25005 T25005 FORMERID TTDR00233 T25005 UNIPROID BTK_HUMAN T25005 TARGNAME Tyrosine-protein kinase BTK (ATK) T25005 GENENAME BTK T25005 TARGTYPE Successful target T25005 SYNONYMS Bruton's tyrosine kinase; Bruton tyrosine kinase; BPK; B-cell progenitor kinase; B cell progenitor kinase; Agammaglobulinemia tyrosine kinase; Agammaglobulinaemia tyrosine kinase; AGMX1 T25005 FUNCTION Binding of antigen to the B-cell antigen receptor (BCR) triggers signaling that ultimately leads to B-cell activation. After BCR engagement and activation at the plasma membrane, phosphorylates PLCG2 at several sites, igniting the downstream signaling pathway through calcium mobilization, followed by activation of the protein kinase C (PKC) family members. PLCG2 phosphorylation is performed in close cooperation with the adapter protein B-cell linker protein BLNK. BTK acts as a platform to bring together a diverse array of signaling proteins and is implicated in cytokine receptor signaling pathways. Plays an important role in the function of immune cells of innate as well as adaptive immunity, as a component of the Toll-like receptors (TLR) pathway. The TLR pathway acts as a primary surveillance system for the detection of pathogens and are crucial to the activation of host defense. Especially, is a critical molecule in regulating TLR9 activation in splenic B-cells. Within the TLR pathway, induces tyrosine phosphorylation of TIRAP which leads to TIRAP degradation. BTK plays also a critical role in transcription regulation. Induces the activity of NF-kappa-B, which is involved in regulating the expression of hundreds of genes. BTK is involved on the signaling pathway linking TLR8 and TLR9 to NF-kappa-B. Transiently phosphorylates transcription factor GTF2I on tyrosine residues in response to BCR. GTF2I then translocates to the nucleus to bind regulatory enhancer elements to modulate gene expression. ARID3A and NFAT are other transcriptional target of BTK. BTK is required for the formation of functional ARID3A DNA-binding complexes. There is however no evidence that BTK itself binds directly to DNA. BTK has a dual role in the regulation of apoptosis. Non-receptor tyrosine kinase indispensable for B lymphocyte development, differentiation and signaling. T25005 PDBSTRUC 6O8I; 6NFI; 6NFH; 6N9P; 6HRT T25005 BIOCLASS Kinase T25005 ECNUMBER EC 2.7.10.2 T25005 SEQUENCE MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVFAKSTGDPQGVIRHYVVCSTPQSQYYLAEKHLFSTIPELINYHQHNSAGLISRLKYPVSQQNKNAPSTAGLGYGSWEIDPKDLTFLKELGTGQFGVVKYGKWRGQYDVAIKMIKEGSMSEDEFIEEAKVMMNLSHEKLVQLYGVCTKQRPIFIITEYMANGCLLNYLREMRHRFQTQQLLEMCKDVCEAMEYLESKQFLHRDLAARNCLVNDQGVVKVSDFGLSRYVLDDEYTSSVGSKFPVRWSPPEVLMYSKFSSKSDIWAFGVLMWEIYSLGKMPYERFTNSETAEHIAQGLRLYRPHLASEKVYTIMYSCWHEKADERPTFKILLSNILDVMDEES T25005 DRUGINFO D09PQZ Acalabrutinib Approved T25005 DRUGINFO D09KTS Ibrutinib Approved T25005 DRUGINFO D0UT4W Zanubrutinib Approved T25005 DRUGINFO D0A9PN GDC-0853 Phase 3 T25005 DRUGINFO DUTJ12 ICP-022 Phase 3 T25005 DRUGINFO DXP04H Pirtobrutinib Phase 3 T25005 DRUGINFO D0KQ7M ARQ 531 Phase 2 T25005 DRUGINFO D0E8PG BGB-3112 Phase 2 T25005 DRUGINFO D08AOZ BMS-986142 Phase 2 T25005 DRUGINFO D04BFC CC-292 Phase 2 T25005 DRUGINFO DVS81T DTRM-555 Phase 2 T25005 DRUGINFO D0H0KH GS-4059 Phase 2 T25005 DRUGINFO D0C0OB LOU064 Phase 2 T25005 DRUGINFO D0QX8X M2951 Phase 2 T25005 DRUGINFO D0GH7L PRN1008 Phase 2 T25005 DRUGINFO D0UF0N ACP-319 Phase 1/2 T25005 DRUGINFO DT3BA1 CG-806 Phase 1/2 T25005 DRUGINFO D0YI4F Vecabrutinib Phase 1/2 T25005 DRUGINFO D0KT8D AC0058TA Phase 1 T25005 DRUGINFO D05SGI BGB-3113 Phase 1 T25005 DRUGINFO D0WP9A BIIB068 Phase 1 T25005 DRUGINFO D3Q4SZ DTRMWXHS-12 Phase 1 T25005 DRUGINFO DTF20P HM71224 Phase 1 T25005 DRUGINFO DBO39X JNJ-64264681 Phase 1 T25005 DRUGINFO D08SGE M7583 Phase 1 T25005 DRUGINFO D02MRX ONO-4059 Phase 1 T25005 DRUGINFO D09NVR PRN2246 Phase 1 T25005 DRUGINFO D0VS3U TAK-020 Phase 1 T25005 DRUGINFO DQ21NM TG-1701 Phase 1 T25005 DRUGINFO D0P3UH Imidazopyridine derivative 4 Patented T25005 DRUGINFO D0NK1R PMID27774824-Compound-Figure12Example1 Patented T25005 DRUGINFO D0UH8J PMID27774824-Compound-Figure12Example10 Patented T25005 DRUGINFO D00BYK PMID27774824-Compound-Figure12Example61 Patented T25005 DRUGINFO D09PIS Pyrazolo[4,3-c]pyridine derivative 2 Patented T25005 DRUGINFO D0QW4H Pyrrolo[2,3-d]pyrimidine derivative 12 Patented T25005 DRUGINFO D03ULH Pyrrolo[2,3-d]pyrimidine derivative 13 Patented T25005 DRUGINFO D00KEX Pyrrolo[2,3-d]pyrimidine derivative 14 Patented T25005 DRUGINFO D09TKO Pyrrolo[2,3-d]pyrimidine derivative 15 Patented T25005 DRUGINFO D06ZNU Pyrrolo[2,3-d]pyrimidine derivative 16 Patented T25005 DRUGINFO D0V8JZ Pyrrolo[2,3-d]pyrimidine derivative 17 Patented T25005 DRUGINFO D0WN2X Pyrrolo[2,3-d]pyrimidine derivative 18 Patented T25005 DRUGINFO D00KPQ Pyrrolo[2,3-d]pyrimidine derivative 19 Patented T25005 DRUGINFO D0Q1BE Pyrrolo[2,3-d]pyrimidine derivative 20 Patented T25005 DRUGINFO D0TI0R Pyrrolo[2,3-d]pyrimidine derivative 21 Patented T25005 DRUGINFO D0SR0U Pyrrolo[2,3-d]pyrimidine derivative 22 Patented T25005 DRUGINFO D09IOW Pyrrolo[2,3-d]pyrimidine derivative 23 Patented T25005 DRUGINFO D0CG3V Pyrrolo[2,3-d]pyrimidine derivative 25 Patented T25005 DRUGINFO D0R9HP Pyrrolo[2,3-d]pyrimidine derivative 26 Patented T25005 DRUGINFO D0IX7O Pyrrolo[2,3-d]pyrimidine derivative 27 Patented T25005 DRUGINFO D00GTY Pyrrolo[2,3-d]pyrimidine derivative 28 Patented T25005 DRUGINFO D05UXK Pyrrolo[2,3-d]pyrimidine derivative 29 Patented T25005 DRUGINFO D05YNZ Pyrrolo[2,3-d]pyrimidine derivative 30 Patented T25005 DRUGINFO D0W3BE Pyrrolo[2,3-d]pyrimidine derivative 31 Patented T25005 DRUGINFO D0Q8LH Pyrrolo[2,3-d]pyrimidine derivative 32 Patented T25005 DRUGINFO D0J8UO Pyrrolo[2,3-d]pyrimidine derivative 33 Patented T25005 DRUGINFO D0D4AQ PCI-45292 Preclinical T25005 DRUGINFO D03FUO GDC-0834 Terminated T25005 DRUGINFO D0H3JH CGI-1316 Investigative T25005 DRUGINFO D0MH9X Inositol 1,3,4,5-Tetrakisphosphate Investigative T25005 DRUGINFO D08NTB LFM-A13 Investigative T25005 DRUGINFO D0E7VO PMID24900538C2c Investigative T25005 DRUGINFO D01RHR PMID24915291C31 Investigative T25005 DRUGINFO D06BJG PMID24915291C38 Investigative T25005 DRUGINFO D0N0LN RN486 Investigative T25005 KEGGPATH hsa04064:NF-kappa B signaling pathway T25005 KEGGPATH hsa04380:Osteoclast differentiation T25005 KEGGPATH hsa04611:Platelet activation T25005 KEGGPATH hsa04662:B cell receptor signaling pathway T25005 KEGGPATH hsa04664:Fc epsilon RI signaling pathway T25005 KEGGPATH hsa05340:Primary immunodeficiency T25005 WIKIPATH WP127:IL-5 Signaling Pathway T25005 WIKIPATH WP1449:Regulation of toll-like receptor signaling pathway T25005 WIKIPATH WP2203:TSLP Signaling Pathway T25005 WIKIPATH WP23:B Cell Receptor Signaling Pathway T25005 WIKIPATH WP2694:DAP12 interactions T25005 WIKIPATH WP2746:Signaling by the B Cell Receptor (BCR) T25005 WIKIPATH WP2761:MyD88:Mal cascade initiated on plasma membrane T25005 WIKIPATH WP304:Kit receptor signaling pathway T25005 WHIZPATH PW000453:Fc Epsilon Receptor I Signaling in Mast Cells T25005 REACPATH R-HSA-166058:MyD88:Mal cascade initiated on plasma membrane T25005 REACPATH R-HSA-2029482:Regulation of actin dynamics for phagocytic cup formation T25005 REACPATH R-HSA-2424491:DAP12 signaling T25005 REACPATH R-HSA-2871809:FCERI mediated Ca+2 mobilization T25005 REACPATH R-HSA-5602498:MyD88 deficiency (TLR2/4) T25005 REACPATH R-HSA-5603041:IRAK4 deficiency (TLR2/4) T25005 REACPATH R-HSA-5663213:RHO GTPases Activate WASPs and WAVEs T25005 REACPATH R-HSA-983695:Antigen activates B Cell Receptor (BCR) leading to generation of second messengers T25005 INTEPATH bcr_5pathway:BCR signaling pathway T25005 INTEPATH epopathway:EPO signaling pathway T25005 INTEPATH faspathway:FAS (CD95) signaling pathway T25005 INTEPATH fcer1pathway:Fc-epsilon receptor I signaling in mast cells T25005 INTEPATH pi3kcipathway:Class I PI3K signaling events T25005 PANTPATH P00010:B cell activation T01318 TARGETID T01318 T01318 FORMERID TTDS00059 T01318 UNIPROID PYRD_PLAF7 T01318 TARGNAME Plasmodium Dihydroorotate dehydrogenase (Malaria DHOdehase) T01318 GENENAME Malaria DHOdehase T01318 TARGTYPE Successful target T01318 SYNONYMS PFF0160c; Mitochondrially bound dihydroorotate-ubiqui oxidoreductase; Dihydroorotate oxidase of Plasmodium falciparum; Dihydroorotate dehydrogenase of Plasmodium falciparum; DHOdehase of Plasmodium falciparum; DHODase; DHODH of Plasmodium falciparum; DHOD T01318 FUNCTION Catalyzes the conversion of dihydroorotate to orotate with quinone as electron acceptor. T01318 PDBSTRUC 6GJG; 6E0B; 5TBO; 5FI8; 5DEL T01318 BIOCLASS CH-CH donor oxidoreductase T01318 ECNUMBER EC 1.3.5.2 T01318 SEQUENCE MISKLKPQFMFLPKKHILSYCRKDVLNLFEQKFYYTSKRKESNNMKNESLLRLINYNRYYNKIDSNNYYNGGKILSNDRQYIYSPLCEYKKKINDISSYVSVPFKINIRNLGTSNFVNNKKDVLDNDYIYENIKKEKSKHKKIIFLLFVSLFGLYGFFESYNPEFFLYDIFLKFCLKYIDGEICHDLFLLLGKYNILPYDTSNDSIYACTNIKHLDFINPFGVAAGFDKNGVCIDSILKLGFSFIEIGTITPRGQTGNAKPRIFRDVESRSIINSCGFNNMGCDKVTENLILFRKRQEEDKLLSKHIVGVSIGKNKDTVNIVDDLKYCINKIGRYADYIAINVSSPNTPGLRDNQEAGKLKNIILSVKEEIDNLEKNNIMNDESTYNEDNKIVEKKNNFNKNNSHMMKDAKDNFLWFNTTKKKPLVFVKLAPDLNQEQKKEIADVLLETNIDGMIISNTTTQINDIKSFENKKGGVSGAKLKDISTKFICEMYNYTNKQIPIIASGGIFSGLDALEKIEAGASVCQLYSCLVFNGMKSAVQIKRELNHLLYQRGYYNLKEAIGRKHSKS T01318 DRUGINFO D0S3WH Artemisinin Approved T01318 DRUGINFO D06ZEE Atovaquone Approved T01318 DRUGINFO D08ROP Leflunomide Approved T01318 DRUGINFO D07QFP Teriflunomide Approved T01318 DRUGINFO D0C0NH Avastin+/-Tarceva Phase 3 T01318 DRUGINFO D0DQ6Z 1,4-Naphthoquinone Investigative T01318 DRUGINFO D0S8AC 1-hydroxy-2-dodecyl-4(1H)quinolone Investigative T01318 DRUGINFO D04HZA 2-(2-bromo-2-naphthamido)benzoic acid Investigative T01318 DRUGINFO D05SXU 2-(2-naphthamido)benzoic acid Investigative T01318 DRUGINFO D03QKF 2-(3-(3,5-dichlorophenyl)ureido)benzoic acid Investigative T01318 DRUGINFO D0R1GF 2-[(biphenyl-4-carbonyl)-amino]-benzoic acid Investigative T01318 DRUGINFO D08LMT 3,6,9,12,15-PENTAOXATRICOSAN-1-OL Investigative T01318 DRUGINFO D00YPH 3-hydroxy-2-phenylquinoline-4-carboxylic acid Investigative T01318 DRUGINFO D0C1LW 5,8-hydroxy-naphthoquinone Investigative T01318 DRUGINFO D0E2WX 5-Fluoro orotate Investigative T01318 DRUGINFO D0YN5P 8-aminoquinolines Investigative T01318 DRUGINFO D0F2ME Acetate Ion Investigative T01318 DRUGINFO D04LBT Antimycin A Investigative T01318 DRUGINFO D00LCE Antiproliferative Agent A771726 Investigative T01318 DRUGINFO D02UVH B-Octylglucoside Investigative T01318 DRUGINFO D07NYQ Cinchoninic acid Investigative T01318 DRUGINFO D0WV5R Cyanide Investigative T01318 DRUGINFO D0S8YD Decylamine-N,N-Dimethyl-N-Oxide Investigative T01318 DRUGINFO D00CQT Dichloroallyl lawsone Investigative T01318 DRUGINFO D02YDM Dichloroally-lawsone Investigative T01318 DRUGINFO D04FYN Diethyl 2-((biphenyl-3-ylamino)methylene)malonate Investigative T01318 DRUGINFO D0AZ4T Dihydroorotate Investigative T01318 DRUGINFO D07PUS DSM1 Investigative T01318 DRUGINFO D09WBQ DSM2 Investigative T01318 DRUGINFO D05YJP Ethyl 3-(biphenyl-3-ylamino)-2-cyanoacrylate Investigative T01318 DRUGINFO D0HQ1I GNF-PF-85 Investigative T01318 DRUGINFO D0V8EH Isoxazol Investigative T01318 DRUGINFO D0C7PY Lauryl Dimethylamine-N-Oxide Investigative T01318 DRUGINFO D09EAO LY214352 Investigative T01318 DRUGINFO D0C1NU N-(3,5-dichlorophenyl)-2-methyl-3-nitrobenzamide Investigative T01318 DRUGINFO D01NWQ N-(4-bromo-2-methylphenyl)-2-naphthamide Investigative T01318 DRUGINFO D06IPT N-(Biphenyl-4-yl)-2-cyano-3-hydroxybut-2-enamide Investigative T01318 DRUGINFO D07TKG NSC 665564 Investigative T01318 DRUGINFO D0B1TS Orotate Investigative T01318 DRUGINFO D0S7BK Orotic acid Investigative T01318 DRUGINFO D0P0IE Plumbagin Investigative T01318 DRUGINFO D0X4NX Polyporic acid Investigative T01318 DRUGINFO D0B1SW Redoxal Investigative T01318 DRUGINFO D0H6QL Salicylhydroxamic acid Investigative T01318 DRUGINFO D02TJY Triazine Investigative T01318 DRUGINFO D0YQ2A Undecylamine-n,n-dimethyl-n-oxide Investigative T01318 KEGGPATH hsa00240:Pyrimidine metabolism T01318 KEGGPATH hsa01100:Metabolic pathways T01318 WIKIPATH WP1851:Metabolism of nucleotides T01318 WHIZPATH PW000160:Pyrimidine Metabolism T01318 REACPATH R-HSA-500753:Pyrimidine biosynthesis T68547 TARGETID T68547 T68547 FORMERID TTDS00095 T68547 UNIPROID HDAC1_HUMAN T68547 TARGNAME Histone deacetylase 1 (HDAC1) T68547 GENENAME HDAC1 T68547 TARGTYPE Successful target T68547 SYNONYMS RPD3L1; HD1 T68547 FUNCTION Gives a tag for epigenetic repression and plays an important role in transcriptional regulation, cell cycle progression and developmental events. Histone deacetylases act via the formation of large multiprotein complexes. Deacetylates SP proteins, SP1 and SP3, and regulates their function. Component of the BRG1-RB1-HDAC1 complex, which negatively regulates the CREST-mediated transcription in resting neurons. Upon calcium stimulation, HDAC1 is released from the complex and CREBBP is recruited, which facilitates transcriptional activation. Deacetylates TSHZ3 and regulates its transcriptional repressor activity. Deacetylates 'Lys-310' in RELA and thereby inhibits the transcriptional activity of NF-kappa-B. Deacetylates NR1D2 and abrogates the effect of KAT5-mediated relieving of NR1D2 transcription repression activity. Component of a RCOR/GFI/KDM1A/HDAC complex that suppresses, via histone deacetylase (HDAC) recruitment, a number of genes implicated in multilineage blood cell development. Involved in CIART-mediated transcriptional repression of the circadian transcriptional activator: CLOCK-ARNTL/BMAL1 heterodimer. Required for the transcriptional repression of circadian target genes, such as PER1, mediated by the large PER complex or CRY1 through histone deacetylation. Responsible for the deacetylation of lysine residues on the N-terminal part of the core histones (H2A, H2B, H3 and H4). T68547 PDBSTRUC 5ICN; 4BKX; 1TYI T68547 BIOCLASS Carbon-nitrogen hydrolase T68547 ECNUMBER EC 3.5.1.98 T68547 SEQUENCE MAQTQGTRRKVCYYYDGDVGNYYYGQGHPMKPHRIRMTHNLLLNYGLYRKMEIYRPHKANAEEMTKYHSDDYIKFLRSIRPDNMSEYSKQMQRFNVGEDCPVFDGLFEFCQLSTGGSVASAVKLNKQQTDIAVNWAGGLHHAKKSEASGFCYVNDIVLAILELLKYHQRVLYIDIDIHHGDGVEEAFYTTDRVMTVSFHKYGEYFPGTGDLRDIGAGKGKYYAVNYPLRDGIDDESYEAIFKPVMSKVMEMFQPSAVVLQCGSDSLSGDRLGCFNLTIKGHAKCVEFVKSFNLPMLMLGGGGYTIRNVARCWTYETAVALDTEIPNELPYNDYFEYFGPDFKLHISPSNMTNQNTNEYLEKIKQRLFENLRMLPHAPGVQMQAIPEDAIPEESGDEDEDDPDKRISICSSDKRIACEEEFSDSEEEGEGGRKNSSNFKKAKRVKTEDEKEKDPEEKKEVTEEEKTKEEKPEAKGVKEEVKLA T68547 DRUGINFO D0E3SH Panobinostat Approved T68547 DRUGINFO D0L7LC Romidepsin Approved T68547 DRUGINFO D0E7PQ Vorinostat Approved T68547 DRUGINFO D00SQN HBI-8000 Registered T68547 DRUGINFO D0GH3Q ITF2357 Phase 3 T68547 DRUGINFO D0B3FV NVP-LAQ824 Phase 3 T68547 DRUGINFO D0M8FD SNDX-275 Phase 3 T68547 DRUGINFO D00FHR MGCD-0103 Phase 2 T68547 DRUGINFO D0B7CH Phenylbutyrate Phase 2 T68547 DRUGINFO D01UXJ Resminostat Phase 2 T68547 DRUGINFO D0VE1W SB-623 Phase 2 T68547 DRUGINFO D0I7IB Sodium butyrate Phase 2 T68547 DRUGINFO D06TKI CHR-3996 Phase 1/2 T68547 DRUGINFO D00SSZ OBP-801 Phase 1 T68547 DRUGINFO D0GE5B RG-2833 Phase 1 T68547 DRUGINFO D07FPY SB-639 Phase 1 T68547 DRUGINFO D0S7NE Diaryl amine derivative 2 Patented T68547 DRUGINFO D0KA3X Diaryl amine derivative 3 Patented T68547 DRUGINFO D0QR1Z Isosteric imidazolyl pyrimidine derivative 1 Patented T68547 DRUGINFO D00XWZ PMID28092474-Compound-32a Patented T68547 DRUGINFO D04VQE PMID28092474-Compound-32b Patented T68547 DRUGINFO D0DH7R PMID28092474-Compound-32c Patented T68547 DRUGINFO D0N1RX PMID28092474-Compound-32d Patented T68547 DRUGINFO D0M7XL PMID28092474-Compound-32e Patented T68547 DRUGINFO D0S3ZB PMID28092474-Compound-32f Patented T68547 DRUGINFO D03EUD PMID28092474-Compound-32g Patented T68547 DRUGINFO D0EU5A PMID28092474-Compound-32h Patented T68547 DRUGINFO D0SK9K PMID28092474-Compound-32i Patented T68547 DRUGINFO D01LCZ PMID28092474-Compound-32j Patented T68547 DRUGINFO D0QF0Y PMID28092474-Compound-32k Patented T68547 DRUGINFO D0W1AX PMID28092474-Compound-32l Patented T68547 DRUGINFO D0MQ2D PMID28092474-Compound-32m Patented T68547 DRUGINFO D0O6SJ PMID28092474-Compound-32n Patented T68547 DRUGINFO D06IIL PMID28092474-Compound-32o Patented T68547 DRUGINFO D0MR7U PMID28092474-Compound-32p Patented T68547 DRUGINFO D0TH3L PMID28092474-Compound-32q Patented T68547 DRUGINFO D0ET4U PMID28092474-Compound-32r Patented T68547 DRUGINFO D0YC2M PMID28092474-Compound-32s Patented T68547 DRUGINFO D0CX1Y PMID28092474-Compound-32t Patented T68547 DRUGINFO D00GLJ PMID28092474-Compound-32u Patented T68547 DRUGINFO D08ZJZ PMID28092474-Compound-32v Patented T68547 DRUGINFO D04KQU PMID28092474-Compound-32x Patented T68547 DRUGINFO D0HM6Y PMID28092474-Compound-32y Patented T68547 DRUGINFO D02YDG PMID28092474-Compound-32z Patented T68547 DRUGINFO D00LLN PMID28092474-Compound-33a Patented T68547 DRUGINFO D04MVN PMID28092474-Compound-33b Patented T68547 DRUGINFO D0L3CU PMID28092474-Compound-33c Patented T68547 DRUGINFO D00ACL PMID28092474-Compound-33d Patented T68547 DRUGINFO D0CH4M PMID28092474-Compound-33e Patented T68547 DRUGINFO D0K2UF PMID28092474-Compound-33f Patented T68547 DRUGINFO D08GBR PMID28092474-Compound-33g Patented T68547 DRUGINFO D0JN0A PMID28092474-Compound-33h Patented T68547 DRUGINFO D0E5CO PMID28092474-Compound-33i Patented T68547 DRUGINFO D08GQL PMID28092474-Compound-33j Patented T68547 DRUGINFO D0Q9XK PMID28092474-Compound-33k Patented T68547 DRUGINFO D0SF8N PMID28092474-Compound-33l Patented T68547 DRUGINFO D08XLK PMID28092474-Compound-33m Patented T68547 DRUGINFO D0RD7T PMID28092474-Compound-33o Patented T68547 DRUGINFO D08SNJ PMID28092474-Compound-33p Patented T68547 DRUGINFO D0QN8W PMID28092474-Compound-34a Patented T68547 DRUGINFO D0BY1R PMID28092474-Compound-34b Patented T68547 DRUGINFO D04AMI PMID28092474-Compound-34c Patented T68547 DRUGINFO D0EH2K PMID29671355-Compound-11 Patented T68547 DRUGINFO D0ZG5X PMID29671355-Compound-13 Patented T68547 DRUGINFO D0TN6E PMID29671355-Compound-18 Patented T68547 DRUGINFO D0LV6K PMID29671355-Compound-19 Patented T68547 DRUGINFO D0LP1K PMID29671355-Compound-21 Patented T68547 DRUGINFO D0QX3G PMID29671355-Compound-22 Patented T68547 DRUGINFO D00HXJ PMID29671355-Compound-23 Patented T68547 DRUGINFO D09PVH PMID29671355-Compound-24 Patented T68547 DRUGINFO D0RA0D PMID29671355-Compound-25 Patented T68547 DRUGINFO D0R3RJ PMID29671355-Compound-26 Patented T68547 DRUGINFO D0V5IQ PMID29671355-Compound-27 Patented T68547 DRUGINFO D0Z7QI PMID29671355-Compound-28 Patented T68547 DRUGINFO D0DI9S PMID29671355-Compound-31 Patented T68547 DRUGINFO D0JR9L PMID29671355-Compound-38a Patented T68547 DRUGINFO D0YD7B PMID29671355-Compound-38b Patented T68547 DRUGINFO D0L7HG PMID29671355-Compound-39 Patented T68547 DRUGINFO D0YT8O PMID29671355-Compound-42 Patented T68547 DRUGINFO D0BP8I PMID29671355-Compound-43 Patented T68547 DRUGINFO D0N2DK PMID29671355-Compound-44 Patented T68547 DRUGINFO D0OU0J PMID29671355-Compound-55 Patented T68547 DRUGINFO D0CH8Q PMID29671355-Compound-56 Patented T68547 DRUGINFO D0UD9R PMID29671355-Compound-57 Patented T68547 DRUGINFO D0C9NX PMID29671355-Compound-59 Patented T68547 DRUGINFO D0JB4S PMID29671355-Compound-61 Patented T68547 DRUGINFO D07WAT PMID29671355-Compound-62 Patented T68547 DRUGINFO D0F3TB PMID29671355-Compound-65a Patented T68547 DRUGINFO D0M0RE PMID29671355-Compound-67 Patented T68547 DRUGINFO D0T7OQ PMID29671355-Compound-73 Patented T68547 DRUGINFO D0LN1T PMID29671355-Compound-8 Patented T68547 DRUGINFO D0Q1QY PMID29671355-Compound-9 Patented T68547 DRUGINFO D0MP2U AN-9 Discontinued in Phase 2 T68547 DRUGINFO D0W9NH Tacedinaline Discontinued in Phase 2 T68547 DRUGINFO D0N3SH Pyroxamide Discontinued in Phase 1 T68547 DRUGINFO D0L5DZ 4SC-202 Preclinical T68547 DRUGINFO D0UC6H Chlamydocin Preclinical T68547 DRUGINFO D0W8JE Depudecin Preclinical T68547 DRUGINFO D06RQU HC-Toxin Preclinical T68547 DRUGINFO D03SZR M-carboxycinnamic acid bishydroxamide Preclinical T68547 DRUGINFO D0J8OC Scriptaid Preclinical T68547 DRUGINFO D0UL5X SK-7041 Preclinical T68547 DRUGINFO D0DO5U SK-7068 Preclinical T68547 DRUGINFO D03YVR Oxamflatin Terminated T68547 DRUGINFO D0KE3I (E)-8-Biphenyl-4-yl-1-oxazol-2-yl-oct-7-en-1-one Investigative T68547 DRUGINFO D06BKA 1,1,1-Trifluoro-8-(4-phenoxy-phenoxy)-octan-2-one Investigative T68547 DRUGINFO D04ETX 1,1,1-Trifluoro-8-phenoxy-octan-2-one Investigative T68547 DRUGINFO D0H1FZ 2-(methylsulfonylthio)ethyl 2-propylpentanoate Investigative T68547 DRUGINFO D02VVU 4-Benzenesulfonylamino-N-hydroxy-benzamide Investigative T68547 DRUGINFO D09ZNU 4-Benzoylamino-N-hydroxy-benzamide Investigative T68547 DRUGINFO D05LLX 4-Butyrylamino-N-hydroxy-benzamide Investigative T68547 DRUGINFO D0A5LS 4-Chloro-N-(5-hydroxycarbamoyl-pentyl)-benzamide Investigative T68547 DRUGINFO D06XNP 4-Dimethylamino-N-(6-mercapto-hexyl)-benzamide Investigative T68547 DRUGINFO D04NSP 4-Hydroxy-N-(5-hydroxycarbamoyl-pentyl)-benzamide Investigative T68547 DRUGINFO D02NWS 4-Phenylbutyrohydroxamic acid Investigative T68547 DRUGINFO D03FOD 4-tert-butyl-N-hydroxybenzamide Investigative T68547 DRUGINFO D0V2ZO 5-(4-Chloro-phenyl)-pentanoic acid hydroxyamide Investigative T68547 DRUGINFO D06IQB 5-(4-hydroxyphenyl)-3H-1,2-dithiole-3-thione Investigative T68547 DRUGINFO D0D2KE 5-Mercapto-pentanoic acid phenylamide Investigative T68547 DRUGINFO D02MQM 6-(2-Bromo-acetylamino)-hexanoic acid phenylamide Investigative T68547 DRUGINFO D00GBB 6-(3-Benzoyl-ureido)-hexanoic acid hydroxyamide Investigative T68547 DRUGINFO D06FAK 6-(9H-carbazol-9-yl)-N-hydroxyhexanamide Investigative T68547 DRUGINFO D00ZSD 6-benzenesulfinylhexanoic acid hydroxamide Investigative T68547 DRUGINFO D05AHZ 6-benzenesulfonylhexanoic acid hydroxamide Investigative T68547 DRUGINFO D0B3ZM 6-Mercapto-hexanoic acid phenylamide Investigative T68547 DRUGINFO D09YBN 6-Phenoxy-hexane-1-thiol Investigative T68547 DRUGINFO D0S9JF 6-phenylsulfanylhexanoic acid hydroxamide Investigative T68547 DRUGINFO D0G0OF 7-(1H-indol-5-yloxy)-N-hydroxyheptanamide Investigative T68547 DRUGINFO D0T0BE 7-(3-Benzoyl-ureido)-heptanoic acid hydroxyamide Investigative T68547 DRUGINFO D07HUH 7-(4-(dimethylamino)phenoxy)-N-hydroxyheptanamide Investigative T68547 DRUGINFO D0B2ZJ 7-(Biphenyl-3-yloxy)-1-oxazol-2-yl-heptan-1-one Investigative T68547 DRUGINFO D0Z3BM 7-(Biphenyl-4-yloxy)-1,1,1-trifluoro-heptan-2-one Investigative T68547 DRUGINFO D02WZK 7-(Biphenyl-4-yloxy)-1-oxazol-2-yl-heptan-1-one Investigative T68547 DRUGINFO D04LLD 7-(Biphenyl-4-yloxy)-heptanoic acid hydroxyamide Investigative T68547 DRUGINFO D05VFP 7-(Naphthalen-2-yloxy)-1-oxazol-2-yl-heptan-1-one Investigative T68547 DRUGINFO D01RJY 7-Biphenyl-4-yl-heptanoic acid hydroxyamide Investigative T68547 DRUGINFO D0Z5KX 7-Mercapto-heptanoic acid benzothiazol-2-ylamide Investigative T68547 DRUGINFO D05XAN 7-Mercapto-heptanoic acid biphenyl-3-ylamide Investigative T68547 DRUGINFO D01XWZ 7-Mercapto-heptanoic acid biphenyl-4-ylamide Investigative T68547 DRUGINFO D00SEE 7-Mercapto-heptanoic acid phenylamide Investigative T68547 DRUGINFO D07FJU 7-Mercapto-heptanoic acid pyridin-3-ylamide Investigative T68547 DRUGINFO D0T4IY 7-Mercapto-heptanoic acid quinolin-3-ylamide Investigative T68547 DRUGINFO D02HVH 7-mercapto-N-(4-phenylthiazol-2-yl)heptanamide Investigative T68547 DRUGINFO D05ZGM 7-Phenoxy-heptanoic acid hydroxyamide Investigative T68547 DRUGINFO D03ZUZ 8-(3-Benzoyl-ureido)-octanoic acid hydroxyamide Investigative T68547 DRUGINFO D0GJ1E 8-(4-bromophenyl)-N-hydroxy-8-oxooctanamide Investigative T68547 DRUGINFO D0NL6C 8-(Biphenyl-3-yloxy)-1,1,1-trifluoro-octan-2-one Investigative T68547 DRUGINFO D0A6CB 8-(biphenyl-4-yl)-N-hydroxy-8-oxooctanamide Investigative T68547 DRUGINFO D0AX7B 8-(Biphenyl-4-yloxy)-1,1,1-trifluoro-octan-2-one Investigative T68547 DRUGINFO D03XXI 8-(Biphenyl-4-yloxy)-2-oxo-octanoic acid Investigative T68547 DRUGINFO D0XZ9Q 8-Mercapto-octanoic acid phenylamide Investigative T68547 DRUGINFO D0RU1X 8-Oxo-8-phenyl-octanoic acid Investigative T68547 DRUGINFO D0S0WK 8-Oxo-8-phenyl-octanoic acid hydroxyamide Investigative T68547 DRUGINFO D0H9DS 8-Phenyl-octanoic acid hydroxyamide Investigative T68547 DRUGINFO D05FEJ 9-(Biphenyl-4-yloxy)-1,1,1-trifluoro-nonan-2-one Investigative T68547 DRUGINFO D00KFF 9,9,9-Trifluoro-8-oxo-nonanoic acid phenylamide Investigative T68547 DRUGINFO D0Q8QA ADS-100380 Investigative T68547 DRUGINFO D0M0QJ ADS-102550 Investigative T68547 DRUGINFO D0P9CQ Azithromycinarylalkylhydroxamic Acid Investigative T68547 DRUGINFO D06ONC Azithromycin-N-benzyltriazolyldecahydroxamic Acid Investigative T68547 DRUGINFO D0I5XM Azithromycin-N-benzyltriazolylhexahydroxamic Acid Investigative T68547 DRUGINFO D0H3RO Azithromycin-N-benzyltriazolylnonahydroxamic Acid Investigative T68547 DRUGINFO D0D7KH Azithromycin-N-benzyltriazolyloctahydroxamic Acid Investigative T68547 DRUGINFO D0M1ZI AZUMAMIDE B Investigative T68547 DRUGINFO D0Q9PO AZUMAMIDE C Investigative T68547 DRUGINFO D0E9DD AZUMAMIDE E Investigative T68547 DRUGINFO D02NVY Cyclo(-L-Am7(S2Py)-A2in-L-Ala-D-Pro-) Investigative T68547 DRUGINFO D0R3XO Cyclo(-L-Am7(S2Py)-Aib-L-Ala-D-Pro-) Investigative T68547 DRUGINFO D0N5RV Cyclo(-L-Am7(S2Py)-Aib-L-Ala-D-Tic-) Investigative T68547 DRUGINFO D0X4QC Cyclo(-L-Am7(S2Py)-Aib-L-Ph4-D-Pro-) Investigative T68547 DRUGINFO D03PRG Cyclo(-L-Am7(S2Py)-Aib-L-Ph5-D-Pro-) Investigative T68547 DRUGINFO D0Z6MI Cyclo(-L-Am7(S2Py)-Aib-L-Phe-D-Pro-) Investigative T68547 DRUGINFO D0G1EX Cyclo(-L-Am7(S2Py)-Aib-L-Phg-D-Pro-) Investigative T68547 DRUGINFO D0E8UH Cyclo(-L-Am7(S2Py)-Aib-L-Ser(Bzl)-D-Pro-) Investigative T68547 DRUGINFO D0U0EZ Cyclo(-L-Am7(S2Py)-Aib-L-Ser-D-Pro-) Investigative T68547 DRUGINFO D04CDZ Cyclo(-L-Am7(S2Py)-D-2MePhe-L-Ala-D-Pro-) Investigative T68547 DRUGINFO D02NAF Cyclo(-L-Am7(S2Py)-D-A1in-L-Ala-D-Pro-) Investigative T68547 DRUGINFO D0Z6HR Cyclo(-L-Am7(S2Py)-L-2MePhe-L-Ala-D-Pro-) Investigative T68547 DRUGINFO D00XTC Cyclo(-L-Am7(S2Py)-L-A1in-L-Ala-D-Pro-) Investigative T68547 DRUGINFO D0C0VP Cyclostellettamine derivative Investigative T68547 DRUGINFO D06THS Desclasinose Azithromycinarylalkyl Hydroxamate Investigative T68547 DRUGINFO D0B1YM Gymnochrome E Investigative T68547 DRUGINFO D0Z8PX LARGAZOLE Investigative T68547 DRUGINFO D01AMS N-(2,3-Dimethylphenyl)-N'-hydroxyoctanediamide Investigative T68547 DRUGINFO D05GRZ N-(2,4-Dimethylphenyl)-N'-hydroxyoctanediamide Investigative T68547 DRUGINFO D0B8RC N-(2,5-Dimethylphenyl)-N'-hydroxyoctanediamide Investigative T68547 DRUGINFO D0SQ1F N-(2,6-Dimethylphenyl)-N'-hydroxyoctanediamide Investigative T68547 DRUGINFO D0Q2GM N-(2-amino-5-(thiophen-2-yl)phenyl)nicotinamide Investigative T68547 DRUGINFO D0P1RQ N-(2-aminophenyl)-4-(chroman-3-ylmethyl)benzamide Investigative T68547 DRUGINFO D0YO6M N-(2-aminophenyl)-4-methoxybenzamide Investigative T68547 DRUGINFO D04UVL N-(2-aminophenyl)nicotinamide Investigative T68547 DRUGINFO D01FYB N-(2-aminophenyl)quinoxaline-6-carboxamide Investigative T68547 DRUGINFO D01ZMJ N-(2-Ethylphenyl)-N'-hydroxyoctanediamide Investigative T68547 DRUGINFO D0F0KS N-(2-Mercapto-ethyl)-N'-phenyl-oxalamide Investigative T68547 DRUGINFO D01MFV N-(2-Mercapto-ethyl)-N'-phenyl-succinamide Investigative T68547 DRUGINFO D0L5KP N-(3,4-Dimethylphenyl)-N'-hydroxyoctanediamide Investigative T68547 DRUGINFO D08TIJ N-(3,5-Dimethylphenyl)-N'-hydroxyoctanediamide Investigative T68547 DRUGINFO D0J3CY N-(3-Ethylphenyl)-N'-hydroxyoctanediamide Investigative T68547 DRUGINFO D0M9LJ N-(4-aminobiphenyl-3-yl)nicotinamide Investigative T68547 DRUGINFO D08ICY N-(4-Ethylphenyl)-N'-hydroxyoctanediamide Investigative T68547 DRUGINFO D0E0TA N-(4-hydroxybiphenyl-3-yl)benzamide Investigative T68547 DRUGINFO D0C2KD N-(5-Hydroxycarbamoyl-pentyl)-4-nitro-benzamide Investigative T68547 DRUGINFO D0YY9M N-(6-Hydroxycarbamoyl-hexyl)-benzamide Investigative T68547 DRUGINFO D04HSS N-(6-Mercapto-hexyl)-benzamide Investigative T68547 DRUGINFO D00LSZ N,8-dihydroxy-8-(naphthalen-2-yl)octanamide Investigative T68547 DRUGINFO D08XMS N1-(biphenyl-3-yl)-N8-hydroxyoctanediamide Investigative T68547 DRUGINFO D04DOL N1-(biphenyl-4-yl)-N8-hydroxyoctanediamide Investigative T68547 DRUGINFO D0YP4F N1-hydroxy-N8-(4-phenylthiazol-2-yl)octanediamide Investigative T68547 DRUGINFO D0Q5DI nexturastat A Investigative T68547 DRUGINFO D0PP3Q N-hydroxy-2,2'-bithiophene-5-carboxamide Investigative T68547 DRUGINFO D04ZDI N-Hydroxy-4-((R)-2-phenyl-butyrylamino)-benzamide Investigative T68547 DRUGINFO D0QO0L N-Hydroxy-4-((S)-2-phenyl-butyrylamino)-benzamide Investigative T68547 DRUGINFO D06VBN N-Hydroxy-4-(2-phenyl-butyrylamino)-benzamide Investigative T68547 DRUGINFO D0R4BS N-Hydroxy-4-(3-phenyl-propionylamino)-benzamide Investigative T68547 DRUGINFO D0S7WQ N-Hydroxy-4-(4-phenyl-butyrylamino)-benzamide Investigative T68547 DRUGINFO D0R5VG N-Hydroxy-4-(5-phenyl-pentanoylamino)-benzamide Investigative T68547 DRUGINFO D0Z7YS N-Hydroxy-4-(pentanoylamino-methyl)-benzamide Investigative T68547 DRUGINFO D02UTC N-Hydroxy-4-(phenylacetylamino-methyl)-benzamide Investigative T68547 DRUGINFO D01XXN N-Hydroxy-4-phenylacetylamino-benzamide Investigative T68547 DRUGINFO D05PYF N-hydroxy-5-(pyridin-2-yl)thiophene-2-carboxamide Investigative T68547 DRUGINFO D00PLM N-hydroxy-5-(pyridin-3-yl)thiophene-2-carboxamide Investigative T68547 DRUGINFO D0A7IF N-hydroxy-5-(pyridin-4-yl)thiophene-2-carboxamide Investigative T68547 DRUGINFO D06NVX N-hydroxy-5-phenylthiophene-2-carboxamide Investigative T68547 DRUGINFO D0L4ML N-hydroxy-6-oxo-6-phenylhexanamide Investigative T68547 DRUGINFO D0K8MF N-hydroxy-7-(4-methoxyphenyl)-7-oxoheptanamide Investigative T68547 DRUGINFO D03FFI N-hydroxy-7-(naphthalen-2-yl)-7-oxoheptanamide Investigative T68547 DRUGINFO D03OYL N-hydroxy-7-(naphthalen-2-yloxy)heptanamide Investigative T68547 DRUGINFO D0QX6R N-hydroxy-7-oxo-7-phenylheptanamide Investigative T68547 DRUGINFO D0KM7H N-hydroxy-8-(2-methoxyphenyl)-8-oxooctanamide Investigative T68547 DRUGINFO D0O7UF N-hydroxy-8-(4-methoxyphenyl)-8-oxooctanamide Investigative T68547 DRUGINFO D04XPZ N-hydroxy-8-(naphthalen-2-yl)non-8-enamide Investigative T68547 DRUGINFO D0CJ7L N-hydroxy-8-(naphthalen-2-yl)oct-7-enamide Investigative T68547 DRUGINFO D0L5WI N-hydroxy-8-(naphthalen-2-yl)octanamide Investigative T68547 DRUGINFO D00RGD N-hydroxy-8-oxo-8-(pyridin-3-yl)octanamide Investigative T68547 DRUGINFO D0Z2VP N-hydroxy-9-oxo-9-phenylnonanamide Investigative T68547 DRUGINFO D0D3XC N-hydroxybenzo[b]thiophene-2-carboxamide Investigative T68547 DRUGINFO D0Q2CC N-Hydroxy-N'-(2-methylphenyl)octanediamide Investigative T68547 DRUGINFO D0H7QA N-Hydroxy-N'-(3-methylphenyl)octanediamide Investigative T68547 DRUGINFO D0L6YF N-Hydroxy-N'-(4-methoxyphenyl)octanediamide Investigative T68547 DRUGINFO D00HFS N-Hydroxy-N'-(4-methylphenyl)octanediamide Investigative T68547 DRUGINFO D01EDB NSC-746457 Investigative T68547 DRUGINFO D07YZZ Octanedioic acid bis-hydroxyamide Investigative T68547 DRUGINFO D0E8KR Octanedioic acid hydroxyamide pyridin-2-ylamide Investigative T68547 DRUGINFO D04GGW Octanedioic acid hydroxyamide pyridin-4-ylamide Investigative T68547 DRUGINFO D0N0TS PSAMMAPLIN A Investigative T68547 DRUGINFO D0U3MB SK-683 Investigative T68547 DRUGINFO D0N9AK ST-2986 Investigative T68547 DRUGINFO D0T0SK ST-2987 Investigative T68547 DRUGINFO D01YBR ST-3050 Investigative T68547 DRUGINFO D05GVY Thioacetic acid S-(6-phenylcarbamoyl-hexyl) ester Investigative T68547 KEGGPATH hsa04110:Cell cycle T68547 KEGGPATH hsa04330:Notch signaling pathway T68547 KEGGPATH hsa04919:Thyroid hormone signaling pathway T68547 KEGGPATH hsa05016:Huntington's disease T68547 KEGGPATH hsa05031:Amphetamine addiction T68547 KEGGPATH hsa05034:Alcoholism T68547 KEGGPATH hsa05169:Epstein-Barr virus infection T68547 KEGGPATH hsa05200:Pathways in cancer T68547 KEGGPATH hsa05202:Transcriptional misregulation in cancer T68547 KEGGPATH hsa05203:Viral carcinogenesis T68547 KEGGPATH hsa05206:MicroRNAs in cancer T68547 KEGGPATH hsa05220:Chronic myeloid leukemia T68547 WIKIPATH WP138:Androgen receptor signaling pathway T68547 WIKIPATH WP179:Cell Cycle T68547 WIKIPATH WP1815:Factors involved in megakaryocyte development and platelet production T68547 WIKIPATH WP1858:Mitotic G1-G1/S phases T68547 WIKIPATH WP1905:RNA Polymerase I, RNA Polymerase III, and Mitochondrial Transcription T68547 WIKIPATH WP1976:Signalling by NGF T68547 WIKIPATH WP1984:Integrated Breast Cancer Pathway T68547 WIKIPATH WP2036:TWEAK Signaling Pathway T68547 WIKIPATH WP2064:Neural Crest Differentiation T68547 WIKIPATH WP2446:Retinoblastoma (RB) in Cancer T68547 WIKIPATH WP268:Notch Signaling Pathway T68547 WIKIPATH WP2755:Transcriptional activity of SMAD2/SMAD3:SMAD4 heterotrimer T68547 WIKIPATH WP2864:Apoptosis-related network due to altered Notch3 in ovarian cancer T68547 WIKIPATH WP364:IL-6 signaling pathway T68547 WIKIPATH WP366:TGF beta Signaling Pathway T68547 WIKIPATH WP61:Notch Signaling Pathway T68547 WIKIPATH WP706:SIDS Susceptibility Pathways T68547 REACPATH R-HSA-1538133:G0 and Early G1 T68547 REACPATH R-HSA-193670:p75NTR negatively regulates cell cycle via SC1 T68547 REACPATH R-HSA-201722:Formation of the beta-catenin:TCF transactivating complex T68547 REACPATH R-HSA-2122947:NOTCH1 Intracellular Domain Regulates Transcription T68547 REACPATH R-HSA-2173796:SMAD2/SMAD3:SMAD4 heterotrimer regulates transcription T68547 REACPATH R-HSA-2644606:Constitutive Signaling by NOTCH1 PEST Domain Mutants T68547 REACPATH R-HSA-2894862:Constitutive Signaling by NOTCH1 HD+PEST Domain Mutants T68547 REACPATH R-HSA-3214815:HDACs deacetylate histones T68547 REACPATH R-HSA-3769402:Deactivation of the beta-catenin transactivating complex T68547 REACPATH R-HSA-427413:NoRC negatively regulates rRNA expression T68547 REACPATH R-HSA-73762:RNA Polymerase I Transcription Initiation T68547 REACPATH R-HSA-983231:Factors involved in megakaryocyte development and platelet production T68547 NET_PATH NetPath_11:TCR Signaling Pathway T68547 INTEPATH ar_tf_pathway:Regulation of Androgen receptor activity T68547 INTEPATH betacatenin_nuc_pathway:Regulation of nuclear beta catenin signaling and target gene transcription T68547 INTEPATH e2f_pathway:E2F transcription factor network T68547 INTEPATH era_genomic_pathway:Validated nuclear estrogen receptor alpha network T68547 INTEPATH hdac_classi_pathway:Signaling events mediated by HDAC Class I T68547 INTEPATH hedgehog_glipathway:Hedgehog signaling events mediated by Gli proteins T68547 INTEPATH hes_heypathway:Notch-mediated HES/HEY network T68547 INTEPATH il3_pathway:IL3-mediated signaling events T68547 INTEPATH myc_represspathway:Validated targets of C-MYC transcriptional repression T68547 INTEPATH notch_pathway:Notch signaling pathway T68547 INTEPATH ps1pathway:Presenilin action in Notch and Wnt signaling T68547 INTEPATH ranbp2pathway:Sumoylation by RanBP2 regulates transcriptional repression T68547 INTEPATH rb_1pathway:Regulation of retinoblastoma protein T68547 INTEPATH reg_gr_pathway:Glucocorticoid receptor regulatory network T68547 INTEPATH retinoic_acid_pathway:Retinoic acid receptors-mediated signaling T68547 INTEPATH smad2_3nuclearpathway:Regulation of nuclear SMAD2/3 signaling T68547 INTEPATH telomerasepathway:Regulation of Telomerase T68547 PANTPATH P00057:Wnt signaling pathway T68547 PANTPATH P00059:p53 pathway T93344 TARGETID T93344 T93344 FORMERID TTDS00302 T93344 UNIPROID ERG1_HUMAN T93344 TARGNAME Squalene monooxygenase (SQLE) T93344 GENENAME SQLE T93344 TARGTYPE Successful target T93344 SYNONYMS Squalene epoxidase; SQLE; SE; Oxidosqaulene cyclase T93344 FUNCTION Catalyzes the first oxygenation step in sterol biosynthesis and is suggested to be one of the rate-limiting enzymes in this pathway. T93344 PDBSTRUC 6C6R; 6C6P; 6C6N T93344 BIOCLASS Paired donor oxygen oxidoreductase T93344 ECNUMBER EC 1.14.14.17 T93344 SEQUENCE MWTFLGIATFTYFYKKFGDFITLANREVLLCVLVFLSLGLVLSYRCRHRNGGLLGRQQSGSQFALFSDILSGLPFIGFFWAKSPPESENKEQLEARRRRKGTNISETSLIGTAACTSTSSQNDPEVIIVGAGVLGSALAAVLSRDGRKVTVIERDLKEPDRIVGEFLQPGGYHVLKDLGLGDTVEGLDAQVVNGYMIHDQESKSEVQIPYPLSENNQVQSGRAFHHGRFIMSLRKAAMAEPNAKFIEGVVLQLLEEDDVVMGVQYKDKETGDIKELHAPLTVVADGLFSKFRKSLVSNKVSVSSHFVGFLMKNAPQFKANHAELILANPSPVLIYQISSSETRVLVDIRGEMPRNLREYMVEKIYPQIPDHLKEPFLEATDNSHLRSMPASFLPPSSVKKRGVLLLGDAYNMRHPLTGGGMTVAFKDIKLWRKLLKGIPDLYDDAAIFEAKKSFYWARKTSHSFVVNILAQALYELFSATDDSLHQLRKACFLYFKLGGECVAGPVGLLSVLSPNPLVLIGHFFAVAIYAVYFCFKSEPWITKPRALLSSGAVLYKACSVIFPLIYSEMKYMVH T93344 DRUGINFO D00HPK Naftifine Approved T93344 DRUGINFO D02NTO Tolnaftate Approved T93344 DRUGINFO D0U2BH Epigallocatechin gallate Phase 3 T93344 DRUGINFO D04DMO FR-194738 Terminated T93344 DRUGINFO D0I3XW NB-598 Terminated T93344 DRUGINFO D06MUZ SDZ-87-469 Terminated T93344 DRUGINFO D0F9KV 1(beta)-O-galloylpedunculagin Investigative T93344 DRUGINFO D00QDR 1,2,3,4,6-penta-O-galloyl-beta-D-glucose Investigative T93344 DRUGINFO D07WLU 1,2,6-tri-O-galloyl-beta-D-glucose Investigative T93344 DRUGINFO D0F9RE Allylamines Investigative T93344 DRUGINFO D0Z9YK Chebulinic acid Investigative T93344 DRUGINFO D03SPJ CORILAGIN Investigative T93344 DRUGINFO D0A1CM ELLAGIC ACID Investigative T93344 DRUGINFO D06CPD ETHYLGALLATE Investigative T93344 DRUGINFO D0K2XJ EUGENIIN Investigative T93344 DRUGINFO D0G3SL FUROSIN Investigative T93344 DRUGINFO D0C6QS GERANIIN Investigative T93344 DRUGINFO D0L1XR Green tea Investigative T93344 DRUGINFO D05UWZ Mallotinic acid Investigative T93344 DRUGINFO D0QN6H Mallotusinic acid Investigative T93344 DRUGINFO D01VEP N-cetylgallate Investigative T93344 DRUGINFO D0VS1V N-dodecylgallate Investigative T93344 DRUGINFO D02ZSX OCTYL_GALLATE Investigative T93344 DRUGINFO D0Z2TG Pedunculagin Investigative T93344 DRUGINFO D06YCQ Procyanidin B-2 3,3'-di-O-gallate Investigative T93344 DRUGINFO D0J1QQ Sanguiin H-6 Investigative T93344 DRUGINFO D0A1QJ Tellurium Investigative T93344 DRUGINFO D0T0XY THEASINENSIN A Investigative T93344 DRUGINFO D0F3KP Thiocarbamate Investigative T93344 DRUGINFO D0Z9PB Trisnorsqualene alcohol Investigative T93344 DRUGINFO D0J1DW Trisnorsqualene cyclopropylamine Investigative T93344 DRUGINFO D03RKP Trisnorsqualene difluoromethylidene Investigative T93344 KEGGPATH sce00100:Steroid biosynthesis T93344 KEGGPATH sce00909:Sesquiterpenoid and triterpenoid biosynthesis T93344 KEGGPATH sce01100:Metabolic pathways T93344 KEGGPATH sce01110:Biosynthesis of secondary metabolites T93344 KEGGPATH sce01130:Biosynthesis of antibiotics T93344 WHIZPATH PW000050:Steroid Biosynthesis T93344 REACPATH R-HSA-191273:Cholesterol biosynthesis T93344 REACPATH R-HSA-2426168:Activation of gene expression by SREBF (SREBP) T92057 TARGETID T92057 T92057 FORMERID TTDC00114 T92057 UNIPROID ERBB4_HUMAN T92057 TARGNAME Erbb4 tyrosine kinase receptor (Erbb-4) T92057 GENENAME ERBB4 T92057 TARGTYPE Successful target T92057 SYNONYMS Tyrosine kinase-type cell surface receptor HER4; Receptor tyrosine-protein kinase erbB-4; Proto-oncogene-like protein c-ErbB-4; P180erbB4; HER4 T92057 FUNCTION Required for normal cardiac muscle differentiation during embryonic development, and for postnatal cardiomyocyte proliferation. Required for normal development of the embryonic central nervous system, especially for normal neural crest cell migration and normal axon guidance. Required for mammary gland differentiation, induction of milk proteins and lactation. Acts as cell-surface receptor for the neuregulins NRG1, NRG2, NRG3 and NRG4 and the EGF family members BTC, EREG and HBEGF. Ligand binding triggers receptor dimerization and autophosphorylation at specific tyrosine residues that then serve as binding sites for scaffold proteins and effectors. Ligand specificity and signaling is modulated by alternative splicing, proteolytic processing, and by the formation of heterodimers with other ERBB family members, thereby creating multiple combinations of intracellular phosphotyrosines that trigger ligand- and context-specific cellular responses. Mediates phosphorylation of SHC1 and activation of the MAP kinases MAPK1/ERK2 and MAPK3/ERK1. Isoform JM-A CYT-1 and isoform JM-B CYT-1 phosphorylate PIK3R1, leading to the activation of phosphatidylinositol 3-kinase and AKT1 and protect cells against apoptosis. Isoform JM-A CYT-1 and isoform JM-B CYT-1 mediate reorganization of the actin cytoskeleton and promote cell migration in response to NRG1. Isoform JM-A CYT-2 and isoform JM-B CYT-2 lack the phosphotyrosine that mediates interaction with PIK3R1, and hence do not phosphorylate PIK3R1, do not protect cells against apoptosis, and do not promote reorganization of the actin cytoskeleton and cell migration. Proteolytic processing of isoform JM-A CYT-1 and isoform JM-A CYT-2 gives rise to the corresponding soluble intracellular domains (4ICD) that translocate to the nucleus, promote nuclear import of STAT5A, activation of STAT5A, mammary epithelium differentiation, cell proliferation and activation of gene expression. The ERBB4 soluble intracellular domains (4ICD) colocalize with STAT5A at the CSN2 promoter to regulate transcription of milk proteins during lactation. The ERBB4 soluble intracellular domains can also translocate to mitochondria and promote apoptosis. Tyrosine-protein kinase that plays an essential role as cell surface receptor for neuregulins and EGF family members and regulates development of the heart, the central nervous system and the mammary gland, gene transcription, cell proliferation, differentiation, migration and apoptosis. T92057 PDBSTRUC 3U9U; 3U7U; 3U2P; 3BCE; 3BBW T92057 BIOCLASS Kinase T92057 ECNUMBER EC 2.7.10.1 T92057 SEQUENCE MKPATGLWVWVSLLVAAGTVQPSDSQSVCAGTENKLSSLSDLEQQYRALRKYYENCEVVMGNLEITSIEHNRDLSFLRSVREVTGYVLVALNQFRYLPLENLRIIRGTKLYEDRYALAIFLNYRKDGNFGLQELGLKNLTEILNGGVYVDQNKFLCYADTIHWQDIVRNPWPSNLTLVSTNGSSGCGRCHKSCTGRCWGPTENHCQTLTRTVCAEQCDGRCYGPYVSDCCHRECAGGCSGPKDTDCFACMNFNDSGACVTQCPQTFVYNPTTFQLEHNFNAKYTYGAFCVKKCPHNFVVDSSSCVRACPSSKMEVEENGIKMCKPCTDICPKACDGIGTGSLMSAQTVDSSNIDKFINCTKINGNLIFLVTGIHGDPYNAIEAIDPEKLNVFRTVREITGFLNIQSWPPNMTDFSVFSNLVTIGGRVLYSGLSLLILKQQGITSLQFQSLKEISAGNIYITDNSNLCYYHTINWTTLFSTINQRIVIRDNRKAENCTAEGMVCNHLCSSDGCWGPGPDQCLSCRRFSRGRICIESCNLYDGEFREFENGSICVECDPQCEKMEDGLLTCHGPGPDNCTKCSHFKDGPNCVEKCPDGLQGANSFIFKYADPDRECHPCHPNCTQGCNGPTSHDCIYYPWTGHSTLPQHARTPLIAAGVIGGLFILVIVGLTFAVYVRRKSIKKKRALRRFLETELVEPLTPSGTAPNQAQLRILKETELKRVKVLGSGAFGTVYKGIWVPEGETVKIPVAIKILNETTGPKANVEFMDEALIMASMDHPHLVRLLGVCLSPTIQLVTQLMPHGCLLEYVHEHKDNIGSQLLLNWCVQIAKGMMYLEERRLVHRDLAARNVLVKSPNHVKITDFGLARLLEGDEKEYNADGGKMPIKWMALECIHYRKFTHQSDVWSYGVTIWELMTFGGKPYDGIPTREIPDLLEKGERLPQPPICTIDVYMVMVKCWMIDADSRPKFKELAAEFSRMARDPQRYLVIQGDDRMKLPSPNDSKFFQNLLDEEDLEDMMDAEEYLVPQAFNIPPPIYTSRARIDSNRSEIGHSPPPAYTPMSGNQFVYRDGGFAAEQGVSVPYRAPTSTIPEAPVAQGATAEIFDDSCCNGTLRKPVAPHVQEDSSTQRYSADPTVFAPERSPRGELDEEGYMTPMRDKPKQEYLNPVEENPFVSRRKNGDLQALDNPEYHNASNGPPKAEDEYVNEPLYLNTFANTLGKAEYLKNNILSMPEKAKKAFDNPDYWNHSLPPRSTLQHPDYLQEYSTKYFYKQNGRIRPIVAENPEYLSEFSLKPGTVLPPPPYRHRNTVV T92057 DRUGINFO D06XXH Dacomitinib Approved T92057 DRUGINFO D0OC4O RG7388 Phase 3 T92057 DRUGINFO D0YB3W CI-1033 Phase 2 T92057 DRUGINFO D0Z7IW JI-101 Phase 2 T92057 DRUGINFO D0U3XL JNJ-26483327 Phase 1 T92057 DRUGINFO D05FFT HDS-029 Investigative T92057 DRUGINFO D06BJG PMID24915291C38 Investigative T92057 KEGGPATH hsa04012:ErbB signaling pathway T92057 KEGGPATH hsa04020:Calcium signaling pathway T92057 KEGGPATH hsa04144:Endocytosis T92057 KEGGPATH hsa05205:Proteoglycans in cancer T92057 WIKIPATH WP3297:EV release from cardiac cells and their functional effects T92057 WIKIPATH WP673:ErbB Signaling Pathway T92057 PANTPATH P00004:Alzheimer disease-presenilin pathway T92057 PANTPATH P00012:Cadherin signaling pathway T92057 PANTPATH P00018:EGF receptor signaling pathway T67849 TARGETID T67849 T67849 FORMERID TTDR00930 T67849 UNIPROID PK3CD_HUMAN T67849 TARGNAME PI3-kinase delta (PIK3CD) T67849 GENENAME PIK3CD T67849 TARGTYPE Successful target T67849 SYNONYMS PtdIns-3-kinase subunit p110-delta; PtdIns-3-kinase subunit delta; Phosphoinositide 3-kinase delta; Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit, delta isoform; Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform; Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit delta; PI3Kdelta; PI3K-delta; PI3-kinase subunit delta; PI3-kinase p110 subunit delta; P110delta T67849 FUNCTION Phosphoinositide-3-kinase (PI3K) that phosphorylates PtdIns(4,5)P2 (Phosphatidylinositol 4,5-bisphosphate) to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3). PIP3 plays a key role by recruiting PH domain-containing proteins to the membrane, including AKT1 and PDPK1, activating signaling cascades involved in cell growth, survival, proliferation, motility and morphology. Mediates immune responses. Plays a role in B-cell development, proliferation, migration, and function. Required for B-cell receptor (BCR) signaling. Mediates B-cell proliferation response to anti-IgM, anti-CD40 and IL4 stimulation. Promotes cytokine production in response to TLR4 and TLR9. Required for antibody class switch mediated by TLR9. Involved in the antigen presentation function of B-cells. Involved in B-cell chemotaxis in response to CXCL13 and sphingosine 1-phosphate (S1P). Required for proliferation, signaling and cytokine production of naive, effector and memory T-cells. Required for T-cell receptor (TCR) signaling. Mediates TCR signaling events at the immune synapse. Activation by TCR leads to antigen-dependent memory T-cell migration and retention to antigenic tissues. Together with PIK3CG participates in T-cell development. Contributes to T-helper cell expansion and differentiation. Required for T-cell migration mediated by homing receptors SELL/CD62L, CCR7 and S1PR1 and antigen dependent recruitment of T-cells. Together with PIK3CG is involved in natural killer (NK) cell development and migration towards the sites of inflammation. Participates in NK cell receptor activation. Have a role in NK cell maturation and cytokine production. Together with PIK3CG is involved in neutrophil chemotaxis and extravasation. Together with PIK3CG participates in neutrophil respiratory burst. Have important roles in mast-cell development and mast cell mediated allergic response. Involved in stem cell factor (SCF)-mediated proliferation, adhesion and migration. Required for allergen-IgE-induced degranulation and cytokine release. The lipid kinase activity is required for its biological function. Isoform 2 may be involved in stabilizing total RAS levels, resulting in increased ERK phosphorylation and increased PI3K activity. T67849 PDBSTRUC 6G6W; 5VLR; 5UBT; 5T8F; 5M6U T67849 BIOCLASS Kinase T67849 ECNUMBER EC 2.7.1.153 T67849 SEQUENCE MPPGVDCPMEFWTKEENQSVVVDFLLPTGVYLNFPVSRNANLSTIKQLLWHRAQYEPLFHMLSGPEAYVFTCINQTAEQQELEDEQRRLCDVQPFLPVLRLVAREGDRVKKLINSQISLLIGKGLHEFDSLCDPEVNDFRAKMCQFCEEAAARRQQLGWEAWLQYSFPLQLEPSAQTWGPGTLRLPNRALLVNVKFEGSEESFTFQVSTKDVPLALMACALRKKATVFRQPLVEQPEDYTLQVNGRHEYLYGSYPLCQFQYICSCLHSGLTPHLTMVHSSSILAMRDEQSNPAPQVQKPRAKPPPIPAKKPSSVSLWSLEQPFRIELIQGSKVNADERMKLVVQAGLFHGNEMLCKTVSSSEVSVCSEPVWKQRLEFDINICDLPRMARLCFALYAVIEKAKKARSTKKKSKKADCPIAWANLMLFDYKDQLKTGERCLYMWPSVPDEKGELLNPTGTVRSNPNTDSAAALLICLPEVAPHPVYYPALEKILELGRHSECVHVTEEEQLQLREILERRGSGELYEHEKDLVWKLRHEVQEHFPEALARLLLVTKWNKHEDVAQMLYLLCSWPELPVLSALELLDFSFPDCHVGSFAIKSLRKLTDDELFQYLLQLVQVLKYESYLDCELTKFLLDRALANRKIGHFLFWHLRSEMHVPSVALRFGLILEAYCRGSTHHMKVLMKQGEALSKLKALNDFVKLSSQKTPKPQTKELMHLCMRQEAYLEALSHLQSPLDPSTLLAEVCVEQCTFMDSKMKPLWIMYSNEEAGSGGSVGIIFKNGDDLRQDMLTLQMIQLMDVLWKQEGLDLRMTPYGCLPTGDRTGLIEVVLRSDTIANIQLNKSNMAATAAFNKDALLNWLKSKNPGEALDRAIEEFTLSCAGYCVATYVLGIGDRHSDNIMIRESGQLFHIDFGHFLGNFKTKFGINRERVPFILTYDFVHVIQQGKTNNSEKFERFRGYCERAYTILRRHGLLFLHLFALMRAAGLPELSCSKDIQYLKDSLALGKTEEEALKHFRVKFNEALRESWKTKVNWLAHNVSKDNRQ T67849 DRUGINFO D0S5LD BAY 80-6946 Approved T67849 DRUGINFO D0J5VR Idelalisib Approved T67849 DRUGINFO D0RU0O IPI-145 Approved T67849 DRUGINFO D0O8SJ Umbralisib Approved T67849 DRUGINFO D01QSO Buparlisib Phase 3 T67849 DRUGINFO D07RHP INCB50465 Phase 2 T67849 DRUGINFO DGO2C1 Leniolisib Phase 2 T67849 DRUGINFO DP1SE6 Parsaclisib Phase 2 T67849 DRUGINFO D0LG7X RP6530 Phase 2 T67849 DRUGINFO D07CWH INCB40093 Phase 1/2 T67849 DRUGINFO D05CBJ PA-799 Phase 1/2 T67849 DRUGINFO D03FOP AMG 319 Phase 1 T67849 DRUGINFO DA02DE BGB-10188 Phase 1 T67849 DRUGINFO D03IJO GS-9820 Phase 1 T67849 DRUGINFO D0U5PT GS-9901 Phase 1 T67849 DRUGINFO DDE3Z4 HMPL-689 Phase 1 T67849 DRUGINFO D08WLY ME-401 Phase 1 T67849 DRUGINFO D00GTY Pyrrolo[2,3-d]pyrimidine derivative 28 Patented T67849 DRUGINFO D08TAB XL-499 Preclinical T67849 DRUGINFO D0P1JI Wortmannin Terminated T67849 DRUGINFO D0W1ST Ethyl 1-[(1H-benzimidazol-2(3H)one-5-yl)sulfonyl]-1H-pyrrole-2-carboxylate Investigative T67849 DRUGINFO DOR1I0 ETP-46321 Investigative T67849 DRUGINFO D00ZIK IC87114 Investigative T67849 DRUGINFO D0O2HL IC980033 Investigative T67849 DRUGINFO D07APP LY-292223 Investigative T67849 KEGGPATH hsa00562:Inositol phosphate metabolism T67849 KEGGPATH hsa04012:ErbB signaling pathway T67849 KEGGPATH hsa04014:Ras signaling pathway T67849 KEGGPATH hsa04015:Rap1 signaling pathway T67849 KEGGPATH hsa04022:cGMP-PKG signaling pathway T67849 KEGGPATH hsa04024:cAMP signaling pathway T67849 KEGGPATH hsa04062:Chemokine signaling pathway T67849 KEGGPATH hsa04066:HIF-1 signaling pathway T67849 KEGGPATH hsa04068:FoxO signaling pathway T67849 KEGGPATH hsa04070:Phosphatidylinositol signaling system T67849 KEGGPATH hsa04071:Sphingolipid signaling pathway T67849 KEGGPATH hsa04150:mTOR signaling pathway T67849 KEGGPATH hsa04151:PI3K-Akt signaling pathway T67849 KEGGPATH hsa04152:AMPK signaling pathway T67849 KEGGPATH hsa04210:Apoptosis T67849 KEGGPATH hsa04261:Adrenergic signaling in cardiomyocytes T67849 KEGGPATH hsa04370:VEGF signaling pathway T67849 KEGGPATH hsa04380:Osteoclast differentiation T67849 KEGGPATH hsa04510:Focal adhesion T67849 KEGGPATH hsa04550:Signaling pathways regulating pluripotency of stem cells T67849 KEGGPATH hsa04611:Platelet activation T67849 KEGGPATH hsa04620:Toll-like receptor signaling pathway T67849 KEGGPATH hsa04630:Jak-STAT signaling pathway T67849 KEGGPATH hsa04650:Natural killer cell mediated cytotoxicity T67849 KEGGPATH hsa04660:T cell receptor signaling pathway T67849 KEGGPATH hsa04662:B cell receptor signaling pathway T67849 KEGGPATH hsa04664:Fc epsilon RI signaling pathway T67849 KEGGPATH hsa04666:Fc gamma R-mediated phagocytosis T67849 KEGGPATH hsa04668:TNF signaling pathway T67849 KEGGPATH hsa04670:Leukocyte transendothelial migration T67849 KEGGPATH hsa04722:Neurotrophin signaling pathway T67849 KEGGPATH hsa04725:Cholinergic synapse T67849 KEGGPATH hsa04750:Inflammatory mediator regulation of TRP channels T67849 KEGGPATH hsa04810:Regulation of actin cytoskeleton T67849 KEGGPATH hsa04910:Insulin signaling pathway T67849 KEGGPATH hsa04914:Progesterone-mediated oocyte maturation T67849 KEGGPATH hsa04915:Estrogen signaling pathway T67849 KEGGPATH hsa04917:Prolactin signaling pathway T67849 KEGGPATH hsa04919:Thyroid hormone signaling pathway T67849 KEGGPATH hsa04921:Oxytocin signaling pathway T67849 KEGGPATH hsa04923:Regulation of lipolysis in adipocytes T67849 KEGGPATH hsa04930:Type II diabetes mellitus T67849 KEGGPATH hsa04932:Non-alcoholic fatty liver disease (NAFLD) T67849 KEGGPATH hsa04960:Aldosterone-regulated sodium reabsorption T67849 KEGGPATH hsa04973:Carbohydrate digestion and absorption T67849 KEGGPATH hsa05100:Bacterial invasion of epithelial cells T67849 KEGGPATH hsa05142:Chagas disease (American trypanosomiasis) T67849 KEGGPATH hsa05145:Toxoplasmosis T67849 KEGGPATH hsa05146:Amoebiasis T67849 KEGGPATH hsa05160:Hepatitis C T67849 KEGGPATH hsa05161:Hepatitis B T67849 KEGGPATH hsa05162:Measles T67849 KEGGPATH hsa05164:Influenza A T67849 KEGGPATH hsa05166:HTLV-I infection T67849 KEGGPATH hsa05169:Epstein-Barr virus infection T67849 KEGGPATH hsa05200:Pathways in cancer T67849 KEGGPATH hsa05203:Viral carcinogenesis T67849 KEGGPATH hsa05205:Proteoglycans in cancer T67849 KEGGPATH hsa05210:Colorectal cancer T67849 KEGGPATH hsa05211:Renal cell carcinoma T67849 KEGGPATH hsa05212:Pancreatic cancer T67849 KEGGPATH hsa05213:Endometrial cancer T67849 KEGGPATH hsa05214:Glioma T67849 KEGGPATH hsa05215:Prostate cancer T67849 KEGGPATH hsa05218:Melanoma T67849 KEGGPATH hsa05220:Chronic myeloid leukemia T67849 KEGGPATH hsa05221:Acute myeloid leukemia T67849 KEGGPATH hsa05222:Small cell lung cancer T67849 KEGGPATH hsa05223:Non-small cell lung cancer T67849 KEGGPATH hsa05230:Central carbon metabolism in cancer T67849 KEGGPATH hsa05231:Choline metabolism in cancer T67849 WIKIPATH WP1403:AMPK Signaling T67849 WIKIPATH WP1449:Regulation of toll-like receptor signaling pathway T67849 WIKIPATH WP1544:MicroRNAs in cardiomyocyte hypertrophy T67849 WIKIPATH WP1840:Interleukin-3, 5 and GM-CSF signaling T67849 WIKIPATH WP2261:Signaling Pathways in Glioblastoma T67849 WIKIPATH WP2643:Nanoparticle-mediated activation of receptor signaling T67849 WIKIPATH WP2653:PIP3 activates AKT signaling T67849 WIKIPATH WP2732:Interleukin-2 signaling T67849 WIKIPATH WP2746:Signaling by the B Cell Receptor (BCR) T67849 WIKIPATH WP2747:PI Metabolism T67849 WIKIPATH WP286:IL-3 Signaling Pathway T67849 WIKIPATH WP306:Focal Adhesion T67849 WIKIPATH WP395:IL-4 Signaling Pathway T67849 WIKIPATH WP481:Insulin Signaling T67849 WIKIPATH WP51:Regulation of Actin Cytoskeleton T67849 WIKIPATH WP524:G13 Signaling Pathway T67849 WIKIPATH WP585:Interferon type I signaling pathways T67849 WIKIPATH WP710:DNA Damage Response (only ATM dependent) T67849 WIKIPATH WP75:Toll-like receptor signaling pathway T67849 WHIZPATH PW000168:Phosphatidylinositol Phosphate Metabolism T67849 REACPATH R-HSA-114604:GPVI-mediated activation cascade T67849 REACPATH R-HSA-1257604:PIP3 activates AKT signaling T67849 REACPATH R-HSA-2219530:Constitutive Signaling by Aberrant PI3K in Cancer T67849 REACPATH R-HSA-392451:G beta:gamma signalling through PI3Kgamma T67849 REACPATH R-HSA-512988:Interleukin-3, 5 and GM-CSF signaling T67849 REACPATH R-HSA-912526:Interleukin receptor SHC signaling T67849 REACPATH R-HSA-912631:Regulation of signaling by CBL T67849 REACPATH R-HSA-983695:Antigen activates B Cell Receptor (BCR) leading to generation of second messengers T67849 NET_PATH NetPath_25:FSH Signaling Pathway T67849 INTEPATH cxcr3pathway:CXCR3-mediated signaling events T67849 INTEPATH cxcr4_pathway:CXCR4-mediated signaling events T67849 INTEPATH erbb1_downstream_pathway:ErbB1 downstream signaling T67849 INTEPATH erbb1_internalization_pathway:Internalization of ErbB1 T67849 INTEPATH erbb1_receptor_proximal_pathway:EGF receptor (ErbB1) signaling pathway T67849 INTEPATH erbb2erbb3pathway:ErbB2/ErbB3 signaling events T67849 INTEPATH erbb4_pathway:ErbB4 signaling events T67849 INTEPATH faspathway:FAS (CD95) signaling pathway T67849 INTEPATH nephrin_neph1_pathway:Nephrin/Neph1 signaling in the kidney podocyte T67849 INTEPATH pdgfrbpathway:PDGFR-beta signaling pathway T67849 INTEPATH pi3kcipathway:Class I PI3K signaling events T67849 INTEPATH tcptp_pathway:Signaling events mediated by TCPTP T67849 INTEPATH trail_pathway:TRAIL signaling pathway T67849 PANTPATH P00005:Angiogenesis T67849 PANTPATH P00006:Apoptosis signaling pathway T67849 PANTPATH P00009:Axon guidance mediated by netrin T67849 PANTPATH P00010:B cell activation T67849 PANTPATH P00018:EGF receptor signaling pathway T67849 PANTPATH P00019:Endothelin signaling pathway T67849 PANTPATH P00021:FGF signaling pathway T67849 PANTPATH P00030:Hypoxia response via HIF activation T67849 PANTPATH P00031:Inflammation mediated by chemokine and cytokine signaling pathway T67849 PANTPATH P00033:Insulin/IGF pathway-protein kinase B signaling cascade T67849 PANTPATH P00034:Integrin signalling pathway T67849 PANTPATH P00047:PDGF signaling pathway T67849 PANTPATH P00053:T cell activation T67849 PANTPATH P00056:VEGF signaling pathway T67849 PANTPATH P00059:p53 pathway T67849 PANTPATH P04393:Ras Pathway T67849 PANTPATH P04398:p53 pathway feedback loops 2 T67849 BIOCPATH PWY-6352:3-phosphoinositide biosynthesis T67849 BIOCPATH PWY-6371:Superpathway of inositol phosphate compounds T10897 TARGETID T10897 T10897 FORMERID TTDS00516 T10897 UNIPROID ACOD_HUMAN T10897 TARGNAME Acyl-CoA desaturase (SCD) T10897 GENENAME SCD T10897 TARGTYPE Successful target T10897 SYNONYMS hSCD1; Stearoyl-coenzyme A (Delta9) desaturase; Stearoyl-CoA desaturase; Membrane-bound 9 desaturase; Fatty acid desaturase; DesA3; Des A3; Delta-9-stearoyl desaturase; Delta-9 desaturase; Delta(9)-desaturase; 9 stearoyl-desaturase T10897 FUNCTION Catalyzes the insertion of a cis double bond at the delta-9 position into fatty acyl-CoA substrates including palmitoyl-CoA and stearoyl-CoA. Gives rise to a mixture of 16:1 and 18:1 unsaturated fatty acids. Plays an important role in lipid biosynthesis. Plays an important role in regulating the expression of genes that are involved in lipogenesis and in regulating mitochondrial fatty acid oxidation. Plays an important role in body energy homeostasis. Contributes to the biosynthesis of membrane phospholipids, cholesterol esters and triglycerides. Stearyl-CoA desaturase that utilizes O(2) and electrons from reduced cytochrome b5 to introduce the first double bond into saturated fatty acyl-CoA substrates. T10897 PDBSTRUC 4ZYO T10897 BIOCLASS Paired donor oxygen oxidoreductase T10897 ECNUMBER EC 1.14.19.1 T10897 SEQUENCE MPAHLLQDDISSSYTTTTTITAPPSRVLQNGGDKLETMPLYLEDDIRPDIKDDIYDPTYKDKEGPSPKVEYVWRNIILMSLLHLGALYGITLIPTCKFYTWLWGVFYYFVSALGITAGAHRLWSHRSYKARLPLRLFLIIANTMAFQNDVYEWARDHRAHHKFSETHADPHNSRRGFFFSHVGWLLVRKHPAVKEKGSTLDLSDLEAEKLVMFQRRYYKPGLLMMCFILPTLVPWYFWGETFQNSVFVATFLRYAVVLNATWLVNSAAHLFGYRPYDKNISPRENILVSLGAVGEGFHNYHHSFPYDYSASEYRWHINFTTFFIDCMAALGLAYDRKKVSKAAILARIKRTGDGNYKSG T10897 DRUGINFO D0I8CA Isoxyl Approved T10897 DRUGINFO D09PVO Aramchol Phase 2/3 T10897 DRUGINFO D0S0RS MK-8245 Phase 2 T10897 DRUGINFO D0N1QW 2-(4-benzoylpiperazin-1-yl)thiazole-5-carboxamide Investigative T10897 DRUGINFO D0O7DP CVT-12012 Investigative T10897 DRUGINFO D0D9QN ISIS 147919 Investigative T10897 DRUGINFO D0O3TT MF-152 Investigative T10897 DRUGINFO D00GQC Sterculic acid Investigative T10897 KEGGPATH mtc01100:Metabolic pathways T16987 TARGETID T16987 T16987 FORMERID TTDR00212 T16987 UNIPROID CAH12_HUMAN T16987 TARGNAME Carbonic anhydrase XII (CA-XII) T16987 GENENAME CA12 T16987 TARGTYPE Successful target T16987 SYNONYMS Tumor antigen HOM-RCC-3.1.3; Carbonic anhydrase 12; Carbonate dehydratase XII T16987 FUNCTION Reversible hydration of carbon dioxide. T16987 PDBSTRUC 6G7A; 6G5L; 5MSB; 5MSA; 5LLP T16987 BIOCLASS Alpha-carbonic anhydrase T16987 ECNUMBER EC 4.2.1.1 T16987 SEQUENCE MPRRSLHAAAVLLLVILKEQPSSPAPVNGSKWTYFGPDGENSWSKKYPSCGGLLQSPIDLHSDILQYDASLTPLEFQGYNLSANKQFLLTNNGHSVKLNLPSDMHIQGLQSRYSATQLHLHWGNPNDPHGSEHTVSGQHFAAELHIVHYNSDLYPDASTASNKSEGLAVLAVLIEMGSFNPSYDKIFSHLQHVKYKGQEAFVPGFNIEELLPERTAEYYRYRGSLTTPPCNPTVLWTVFRNPVQISQEQLLALETALYCTHMDDPSPREMINNFRQVQKFDERLVYTSFSQVQVCTAAGLSLGIILSLALAGILGICIVVVVSIWLFRRKSIKKGDNKGVIYKPATKMETEAHA T16987 DRUGINFO D07HBX Salicyclic acid Approved T16987 DRUGINFO D0K1QD Sulfamylon Approved T16987 DRUGINFO D07SDQ Curcumin Phase 3 T16987 DRUGINFO D0A8JP PARABEN Phase 3 T16987 DRUGINFO D0L6HN PHENOL Phase 2/3 T16987 DRUGINFO D0Y6OA Coumate Phase 2 T16987 DRUGINFO D03SLR FERULIC ACID Patented T16987 DRUGINFO D05RAB 1,4-Dihydro-1-methyl-4-oxo-3-pyridinesulfonamide Investigative T16987 DRUGINFO D04SNH 1-Benzyl-1,4-dihydro-4-oxo-3-pyridinesulfonamide Investigative T16987 DRUGINFO D0RK7J 2,2,2-Trifluoro-N-(4-sulfamoyl-phenyl)-acetamide Investigative T16987 DRUGINFO D03DAM 2,2-Dimethyl-N-(4-sulfamoyl-phenyl)-propionamide Investigative T16987 DRUGINFO D0LC0F 2,3-dihydro-1H-indene-5-sulfonamide Investigative T16987 DRUGINFO D0M3PO 2,4-Disulfamyltrifluoromethylaniline Investigative T16987 DRUGINFO D09TES 2-acetamido-2,3-dihydro-1H-indene-5-sulfonic acid Investigative T16987 DRUGINFO D07CYN 2-amino-2,3-dihydro-1H-indene-5-sulfonamide Investigative T16987 DRUGINFO D0OI1H 2-Amino-benzenesulfonamide Investigative T16987 DRUGINFO D0C4QB 2-Amino-indan-5-sulfonic acid Investigative T16987 DRUGINFO D0G0FJ 2-hydrazinylbenzenesulfonamide Investigative T16987 DRUGINFO D0H3NS 2-oxo-2H-chromene-3-carboxylic acid Investigative T16987 DRUGINFO D0D6UR 2-oxo-2H-thiochromene-3-carboxylic acid Investigative T16987 DRUGINFO D0H4CF 3-((4-aminophenyl)diazenyl)benzenesulfonamide Investigative T16987 DRUGINFO D0C7WG 3-((4-hydroxyphenyl)diazenyl)benzenesulfonamide Investigative T16987 DRUGINFO D06ZMH 3-(3-Phenyl-ureido)-benzenesulfonamide Investigative T16987 DRUGINFO D0BD0K 3-(4'-Hydroxyphenyl)diazenylbenzenesulfonamide Investigative T16987 DRUGINFO D0J2AE 3-Amino-benzenesulfonamide Investigative T16987 DRUGINFO D04HRS 4-((4-hydroxyphenyl)diazenyl)benzenesulfonamide Investigative T16987 DRUGINFO D04NSN 4-(2-AMINOETHYL)BENZENESULFONAMIDE Investigative T16987 DRUGINFO D04VLI 4-(2-Hydroxy-ethyl)-benzenesulfonamide Investigative T16987 DRUGINFO D05ETN 4-(2-Methyl-8-quinolinoxy)-3-pyridinesulfonamide Investigative T16987 DRUGINFO D02BMV 4-(2-Propynylthio)pyridine-3-sulfonamide Investigative T16987 DRUGINFO D05EBZ 4-(4-Cyanophenoxy)-3-pyridinesulfonamide Investigative T16987 DRUGINFO D08JCC 4-(4-Fluorophenoxy)-3-pyridinesulfonamide Investigative T16987 DRUGINFO D00RDE 4-(4'-N-Methylphenyl)diazenylbenzenesulfonamide Investigative T16987 DRUGINFO D0R4KQ 4-(5-Methyl-2-pirazolino)-3-pyridinesulfonamide Investigative T16987 DRUGINFO D09TKG 4-(Allylamino)-3-pyridinesulfonamide Investigative T16987 DRUGINFO D0V5OW 4-(Carbamolymethylthio)pyridine-3-sulfonamide Investigative T16987 DRUGINFO D01OTW 4-(Cyanomethylthio)pyridine-3-sulfonamide Investigative T16987 DRUGINFO D05XZM 4-(hydroxymethyl)benzenesulfonamide Investigative T16987 DRUGINFO D0Q5VB 4-(Methylhydrazino)-3-pyridinesulfonamide Investigative T16987 DRUGINFO D0M7VN 4-(N-Methyl-hydrazino)-benzenesulfonamide Investigative T16987 DRUGINFO D02NQK 4-(N-Oxide-2-pyridylthio)pyridine-3-sulfonamide Investigative T16987 DRUGINFO D05JAJ 4-(Quinolinoxy)-3-pyridinesulfonamide Investigative T16987 DRUGINFO D03KRB 4,4'-thiodipyridine-3-sulfonamide Investigative T16987 DRUGINFO D09LUD 4-[2-(3-Phenyl-ureido)-ethyl]-benzenesulfonamide Investigative T16987 DRUGINFO D0P6AM 4-Amino-3-bromo-benzenesulfonamide Investigative T16987 DRUGINFO D0YU8J 4-Amino-3-chloro-benzenesulfonamide Investigative T16987 DRUGINFO D04CVC 4-Amino-3-fluoro-benzenesulfonamide Investigative T16987 DRUGINFO D01STY 4-Amino-3-iodo-benzenesulfonamide Investigative T16987 DRUGINFO D0YD9F 4-Benzenesulfonylamino-benzenesulfonamide Investigative T16987 DRUGINFO D06IOI 4-Benzythiopyridine-3-sulfonamide Investigative T16987 DRUGINFO D00IUB 4-CYANOPHENOL Investigative T16987 DRUGINFO D04VSP 4-Ethoxy-3-pyridinesulfonamide Investigative T16987 DRUGINFO D0UM1I 4-Hydrazino-3-pyridinesulfonamide Investigative T16987 DRUGINFO D0NN3Q 4-Hydrazino-benzenesulfonamide Investigative T16987 DRUGINFO D00NUK 4-Methanesulfonylamino-benzenesulfonamide Investigative T16987 DRUGINFO D00IKQ 4-Methoxy-3-pyridinesulfonamide Investigative T16987 DRUGINFO D07AGM 4-Methylamino-benzenesulfonamide Investigative T16987 DRUGINFO D0J7GU 4-Methylthiopyridine-3-sulfonamide Investigative T16987 DRUGINFO D0N1AW 6-(aminomethyl)-2H-chromen-2-one Investigative T16987 DRUGINFO D0L5TZ 6-(hydroxymethyl)-2H-chromen-2-one Investigative T16987 DRUGINFO D0Q2LL 6-Hydroxy-benzothiazole-2-sulfonic acid amide Investigative T16987 DRUGINFO D00XJA 6-methoxy-2-oxo-2H-chromene-3-carboxylic acid Investigative T16987 DRUGINFO D0G3BI 6-methyl-2-oxo-2H-chromene-3-carboxylic acid Investigative T16987 DRUGINFO D00RNZ 7-(benzyloxy)-2H-chromen-2-one Investigative T16987 DRUGINFO D0LU4S 7-butoxy-2H-chromen-2-one Investigative T16987 DRUGINFO D0RB0D 7-methoxy-2-oxo-2H-chromene-4-carboxylic acid Investigative T16987 DRUGINFO D05QUG 7-phenethoxy-2H-chromen-2-one Investigative T16987 DRUGINFO D0OT5L 7-propoxy-2H-chromen-2-one Investigative T16987 DRUGINFO D06DYP 8-methoxy-2-oxo-2H-chromene-3-carboxylic acid Investigative T16987 DRUGINFO D04POB ACETYLSULFANILAMIDE Investigative T16987 DRUGINFO D0E8CC BENZOLAMIDE Investigative T16987 DRUGINFO D09PWX Carzenide Investigative T16987 DRUGINFO D0V7AA CATECHIN Investigative T16987 DRUGINFO D07QJJ CATECHOL Investigative T16987 DRUGINFO D0VD7H CL-5343 Investigative T16987 DRUGINFO D03ZMQ COUMARIN Investigative T16987 DRUGINFO D00YEF Decane-1,10-diyl disulfamate Investigative T16987 DRUGINFO D09WSJ Decyl sulfamate Investigative T16987 DRUGINFO D0A1CM ELLAGIC ACID Investigative T16987 DRUGINFO D05VSK ETHOXYCOUMARIN Investigative T16987 DRUGINFO D07TAJ Ethyl 7-methoxy-2-oxo-2H-chromene-3-carboxylate Investigative T16987 DRUGINFO D0Y3TZ GALLICACID Investigative T16987 DRUGINFO D0U4BB HERNIARIN Investigative T16987 DRUGINFO D09JPC Hexane-1,6-diamine Investigative T16987 DRUGINFO D0M4EV N-(4-cyanophenyl)sulfamide Investigative T16987 DRUGINFO D0KB6T N-(4-Sulfamoyl-phenyl)-benzamide Investigative T16987 DRUGINFO D0K3LN N-(4-Sulfamoyl-phenyl)-butyramide Investigative T16987 DRUGINFO D0T2YZ N-(4-Sulfamoyl-phenyl)-isobutyramide Investigative T16987 DRUGINFO D0N8LR N-(4-Sulfamoyl-phenyl)-propionamide Investigative T16987 DRUGINFO D0PA5L N-(pentafluorophenyl)sulfamide Investigative T16987 DRUGINFO D09WVV N1-(2-aminoethyl)ethane-1,2-diamine Investigative T16987 DRUGINFO D0X5HL N1-(naphthalen-1-yl)ethane-1,2-diamine Investigative T16987 DRUGINFO D09CXX N-hydroxysulfamide Investigative T16987 DRUGINFO D01XFH N-propynyl amidebenzenesulphonide Investigative T16987 DRUGINFO D0D4OV Octane-1,8-diyl disulfamate Investigative T16987 DRUGINFO D05TLB Octyl sulfamate Investigative T16987 DRUGINFO D0AU0M P-Coumaric Acid Investigative T16987 DRUGINFO D02QGI Pentane-1,5-diamine Investigative T16987 DRUGINFO D0Q0XO Pentanoic acid (4-sulfamoyl-phenyl)-amide Investigative T16987 DRUGINFO D00IAE Prop-2-ynyl 4-sulfamoylbenzoate Investigative T16987 DRUGINFO D0ZC3W P-toluenesulfonamide Investigative T16987 DRUGINFO D02DBP RESORCINOL Investigative T16987 DRUGINFO D0A0YX SACCHARIN Investigative T16987 DRUGINFO D0M9IQ Sodium N-methylphenylaminomethanesulfonate Investigative T16987 DRUGINFO D07UCQ Sodium phenylaminomethanesulfonate Investigative T16987 DRUGINFO D0Q7DJ Syringic Acid Investigative T16987 DRUGINFO D0I0RT Thioureido sulfonamide Investigative T16987 KEGGPATH hsa00910:Nitrogen metabolism T16987 WIKIPATH WP2002:miR-targeted genes in epithelium - TarBase T16987 WIKIPATH WP2003:miR-targeted genes in leukocytes - TarBase T16987 WIKIPATH WP2005:miR-targeted genes in muscle cell - TarBase T16987 WIKIPATH WP2770:Reversible Hydration of Carbon Dioxide T16987 REACPATH R-HSA-1475029:Reversible hydration of carbon dioxide T16987 NET_PATH NetPath_7:TGF_beta_Receptor Signaling Pathway T19433 TARGETID T19433 T19433 FORMERID TTDS00192 T19433 UNIPROID HPGDS_HUMAN T19433 TARGNAME Glutathione-dependent PGD synthase (HPGDS) T19433 GENENAME HPGDS T19433 TARGTYPE Successful target T19433 SYNONYMS HPGDS; Glutathione-S-transferase; GST class-alpha T19433 FUNCTION Bifunctional enzyme which catalyzes both the conversion of PGH2 to PGD2, a prostaglandin involved in smooth muscle contraction/relaxation and a potent inhibitor of platelet aggregation, and the conjugation of glutathione with a widerange of aryl halides and organic isothiocyanates. Also exhibits low glutathione-peroxidase activity towards cumene hydroperoxide. T19433 PDBSTRUC 6N4E; 5YX1; 5YWX; 5YWE; 5AIX T19433 BIOCLASS Intramolecular oxidoreductases T19433 ECNUMBER EC 5.3.99.2 T19433 SEQUENCE MPNYKLTYFNMRGRAEIIRYIFAYLDIQYEDHRIEQADWPEIKSTLPFGKIPILEVDGLTLHQSLAIARYLTKNTDLAGNTEMEQCHVDAIVDTLDDFMSCFPWAEKKQDVKEQMFNELLTYNAPHLMQDLDTYLGGREWLIGNSVTWADFYWEICSTTLLVFKPDLLDNHPRLVTLRKKVQAIPAVANWIKRRPQTKL T19433 DRUGINFO D0L9ZR Praziquantel Approved T19433 DRUGINFO D02AOD HF-0220 Phase 2 T19433 DRUGINFO D06GJP Cibacron blue Investigative T19433 DRUGINFO D06EWG Formic Acid Investigative T19433 DRUGINFO D0PI1C HQL-79 Investigative T19433 DRUGINFO D0AF3A Protoporphyrin IX Investigative T19433 DRUGINFO D08IXW S-hexylglutathione Investigative T19433 KEGGPATH hsa00590:Arachidonic acid metabolism T19433 KEGGPATH hsa01100:Metabolic pathways T19433 WIKIPATH WP2377:Integrated Pancreatic Cancer Pathway T19433 WIKIPATH WP2586:Aryl Hydrocarbon Receptor T19433 WIKIPATH WP2650:Arachidonic acid metabolism T19433 BIOCPATH PWY66-374:C20 prostanoid biosynthesis T94033 TARGETID T94033 T94033 FORMERID TTDS00202 T94033 UNIPROID THRB_HUMAN T94033 TARGNAME Coagulation factor IIa (F2) T94033 GENENAME F2 T94033 TARGTYPE Successful target T94033 SYNONYMS Prothrombin; Coagulation factor II T94033 FUNCTION Thrombin, which cleaves bonds after Arg and Lys, converts fibrinogen to fibrin and activates factors V, VII, VIII, XIII, and, in complex with thrombomodulin, protein C. Functions in blood homeostasis, inflammation and wound healing. T94033 PDBSTRUC 8KME; 7KME; 6EO9; 6EO8; 6EO7 T94033 BIOCLASS Peptidase T94033 ECNUMBER EC 3.4.21.5 T94033 SEQUENCE MAHVRGLQLPGCLALAALCSLVHSQHVFLAPQQARSLLQRVRRANTFLEEVRKGNLERECVEETCSYEEAFEALESSTATDVFWAKYTACETARTPRDKLAACLEGNCAEGLGTNYRGHVNITRSGIECQLWRSRYPHKPEINSTTHPGADLQENFCRNPDSSTTGPWCYTTDPTVRRQECSIPVCGQDQVTVAMTPRSEGSSVNLSPPLEQCVPDRGQQYQGRLAVTTHGLPCLAWASAQAKALSKHQDFNSAVQLVENFCRNPDGDEEGVWCYVAGKPGDFGYCDLNYCEEAVEEETGDGLDEDSDRAIEGRTATSEYQTFFNPRTFGSGEADCGLRPLFEKKSLEDKTERELLESYIDGRIVEGSDAEIGMSPWQVMLFRKSPQELLCGASLISDRWVLTAAHCLLYPPWDKNFTENDLLVRIGKHSRTRYERNIEKISMLEKIYIHPRYNWRENLDRDIALMKLKKPVAFSDYIHPVCLPDRETAASLLQAGYKGRVTGWGNLKETWTANVGKGQPSVLQVVNLPIVERPVCKDSTRIRITDNMFCAGYKPDEGKRGDACEGDSGGPFVMKSPFNNRWYQMGIVSWGEGCDRDGKYGFYTHVFRLKKWIQKVIDQFGE T94033 DRUGINFO D09WKB Anisindione Approved T94033 DRUGINFO D07UWV Argatroban Approved T94033 DRUGINFO D0AW9T ATryn antithrombin Approved T94033 DRUGINFO D09HVL Bivalirudin Approved T94033 DRUGINFO D0M7JT Dabigatran Approved T94033 DRUGINFO D03LWO Desirudin Recombinant Approved T94033 DRUGINFO D07KFG Human prothrombin complex concentrate Approved T94033 DRUGINFO D09LPN Lepirudin Approved T94033 DRUGINFO D06JGH Pyridoxal Phosphate Approved T94033 DRUGINFO D0B5LF Ximelegatran Approved T94033 DRUGINFO D0F3SZ Hirudin Phase 4 T94033 DRUGINFO D01MUU MELAGATRAN Phase 3 T94033 DRUGINFO D0VL4V SR-123781A Phase 2/3 T94033 DRUGINFO D09DFB EFEGATRAN SULFATE HYDRATE Phase 2 T94033 DRUGINFO D0UK1L EP-217609 Phase 2 T94033 DRUGINFO D0I7MX LB-30870 Phase 2 T94033 DRUGINFO D0H9RN NU-172 Phase 2 T94033 DRUGINFO D0N6EA Odiparcil Phase 2 T94033 DRUGINFO D0K8FI Pegmusirudin Phase 2 T94033 DRUGINFO D0GG5I Recombinant RGD-hirudin Phase 2 T94033 DRUGINFO D0PX0N TF0023 Phase 2 T94033 DRUGINFO D0K4FP AZD-8165 Phase 1 T94033 DRUGINFO D05HAD DP-4088 Phase 1 T94033 DRUGINFO D0G6UQ EP-42675 Phase 1 T94033 DRUGINFO D00LOB RWJ-671818 Phase 1 T94033 DRUGINFO D0L2XU Solulin Phase 1 T94033 DRUGINFO D02UIC SSR-128428 Phase 1 T94033 DRUGINFO D0JQ7Y Ximelagatran Withdrawn from market T94033 DRUGINFO D0B1KK AZD0837 Discontinued in Phase 2 T94033 DRUGINFO D0B9EH Dermolastin Discontinued in Phase 2 T94033 DRUGINFO D0H4UJ INOGATRAN Discontinued in Phase 2 T94033 DRUGINFO D0Q3WN Napsagatran Discontinued in Phase 2 T94033 DRUGINFO D06DUO SSR-182289 Discontinued in Phase 2 T94033 DRUGINFO D07MZC Vasoflux Discontinued in Phase 2 T94033 DRUGINFO D0W5XT ARC-183 Discontinued in Phase 1 T94033 DRUGINFO D01IBO BCX-1470 Discontinued in Phase 1 T94033 DRUGINFO D05KTK CJC-1004 Discontinued in Phase 1 T94033 DRUGINFO D02MHE CVS-1123 Discontinued in Phase 1 T94033 DRUGINFO D05MXK GW-473178 Discontinued in Phase 1 T94033 DRUGINFO D09CKF Licostinel Discontinued in Phase 1 T94033 DRUGINFO D0UF5I MPC-0920 Discontinued in Phase 1 T94033 DRUGINFO D0H2ZQ S-18326 Discontinued in Phase 1 T94033 DRUGINFO D0G0XN UK-156406 Discontinued in Phase 1 T94033 DRUGINFO D06ALB BCH-2763 Terminated T94033 DRUGINFO D0G7YZ BMS-189664 Terminated T94033 DRUGINFO D0J6VU CVS-995 Terminated T94033 DRUGINFO D0Y5EX DuP 714 Terminated T94033 DRUGINFO D02QTV Efegatran Terminated T94033 DRUGINFO D0S6XJ GS-522 Terminated T94033 DRUGINFO D0WL1C Hementin Terminated T94033 DRUGINFO D05WYW L-373890 Terminated T94033 DRUGINFO D0L6UZ L-374,087 Terminated T94033 DRUGINFO D0S2JG LB30057 Terminated T94033 DRUGINFO D0SF5F Org-34092 Terminated T94033 DRUGINFO D0RP8F PPACK Terminated T94033 DRUGINFO D02ZWG SR-80027A Terminated T94033 DRUGINFO D0X1OY (3,4-dichlorophenyl)(1H-pyrazol-1-yl)methanone Investigative T94033 DRUGINFO D08WQJ (3-nitro-1H-pyrazol-1-yl)(phenyl)methanone Investigative T94033 DRUGINFO D08OCS (3-nitro-1H-pyrazol-1-yl)(p-tolyl)methanone Investigative T94033 DRUGINFO D05ZIP (4-bromo-1H-pyrazol-1-yl)(p-tolyl)methanone Investigative T94033 DRUGINFO D00WFQ (4-nitro-1H-pyrazol-1-yl)(o-tolyl)methanone Investigative T94033 DRUGINFO D06LPR (4-nitro-1H-pyrazol-1-yl)(phenyl)methanone Investigative T94033 DRUGINFO D0E1NH 1-(HYDROXYMETHYLENEAMINO)-8-HYDROXY-OCTANE Investigative T94033 DRUGINFO D00QDR 1,2,3,4,6-penta-O-galloyl-beta-D-glucose Investigative T94033 DRUGINFO D0IU5E 1-benzoyl-N-phenyl-1H-pyrazole-3-carboxamide Investigative T94033 DRUGINFO D08OLP 2-(2-Hydroxy-phenyl)-1H-indole-5-carboxamidine Investigative T94033 DRUGINFO D0N0PI 2-NAPHTHALENESULFONIC ACID Investigative T94033 DRUGINFO D0SP2I 2-nas-phe(3-am)-4-(2-guanidinoethyl)piperidine Investigative T94033 DRUGINFO D0P3OH 3-chlorophenyl 2-oxo-2H-chromene-3-carboxylate Investigative T94033 DRUGINFO D0N1HV 4-(2,5-DIAMINO-5-HYDROXY-PENTYL)-PHENOL Investigative T94033 DRUGINFO D0CT8A 4-(3,4-Diethoxy-benzylamino)-benzamidine Investigative T94033 DRUGINFO D02XPB 4-(4-Benzyloxy-3-methoxy-benzylamino)-benzamidine Investigative T94033 DRUGINFO D09CVG 4-[3-(4-CHLOROPHENYL)-1H-PYRAZOL-5-YL]PIPERIDINE Investigative T94033 DRUGINFO D0G6RI 4-hydroxyphenylpyruvic acid Investigative T94033 DRUGINFO D05MJU 4-iodobenzo[b]thiophene 2-carboxamidine Investigative T94033 DRUGINFO D0D9NT 4-TERT-BUTYLBENZENESULFONIC ACID Investigative T94033 DRUGINFO D07HWB 5-desgalloylstachyurin Investigative T94033 DRUGINFO D06KCW 6-(2-HYDROXY-CYCLOPENTYL)-7-OXO-HEPTANAMIDINE Investigative T94033 DRUGINFO D09QZJ AC-(D)PHE-PRO-BOROHOMOLYS-OH Investigative T94033 DRUGINFO D0E9ON AC-(D)PHE-PRO-BOROHOMOORNITHINE-OH Investigative T94033 DRUGINFO D0R4AV AC-(D)PHE-PRO-BOROLYS-OH Investigative T94033 DRUGINFO D0T5WR Bbs-Arg-(D-Pip)-Gly-(EQKLISEEDL)-Gly-Hir Investigative T94033 DRUGINFO D0KQ1K Bbs-Arg-(D-Pip)-Gly-(SPH(pY)EKVS)-Gly-Hir Investigative T94033 DRUGINFO D0P0LG Bbs-Arg-(D-Pip)-Gly-(SPHYEKVS)-Gly-Hir Investigative T94033 DRUGINFO D07BJZ Bbs-Arg-(D-Pip)-Gly-S-(GS)11-Gly-Hir Investigative T94033 DRUGINFO D09HFC Bbs-Arg-(D-Pip)-Gly-S-(GS)13-Gly-Hir Investigative T94033 DRUGINFO D0CV4F Bbs-Arg-(D-Pip)-Gly-S-(GS)1-Gly-Hir Investigative T94033 DRUGINFO D01ARY Bbs-Arg-(D-Pip)-Gly-S-(GS)3-Gly-Hir Investigative T94033 DRUGINFO D07BMA Bbs-Arg-(D-Pip)-Gly-S-(GS)5-Gly-Hir Investigative T94033 DRUGINFO D04VYT Bbs-Arg-(D-Pip)-Gly-S-(GS)7-Gly-Hir Investigative T94033 DRUGINFO D0WF2C Bbs-Arg-(D-Pip)-Gly-S-(GS)9-Gly-Hir Investigative T94033 DRUGINFO D07NYX BENZOTHIAZOLE Investigative T94033 DRUGINFO D0N0YX Beta-(2-Naphthyl)-Alanine Investigative T94033 DRUGINFO D03LGM Beta-phenyl-D-phenylalanyl-N-propyl-L-prolinamide Investigative T94033 DRUGINFO D0J1QT BMS-344577 Investigative T94033 DRUGINFO D0JU9N BMS-740808 Investigative T94033 DRUGINFO D0I6DO bufrudin Investigative T94033 DRUGINFO D0I1UF CASUARIIN Investigative T94033 DRUGINFO D01NEZ CHLORODYSINOSIN A Investigative T94033 DRUGINFO D0X0IF COCHINCHINENENE B Investigative T94033 DRUGINFO D0U4HG COCHINCHINENIN B Investigative T94033 DRUGINFO D0K7YL CRA_8696 Investigative T94033 DRUGINFO D0Y8QU CVS-1578 Investigative T94033 DRUGINFO D0D8AK Cyclotheonamide E Investigative T94033 DRUGINFO D0M1AC Cyclotheonamide E4 Investigative T94033 DRUGINFO D0CF3B Cyclotheonamide E5 Investigative T94033 DRUGINFO D0H8OB Desirudine Investigative T94033 DRUGINFO D0P1JQ D-leucyl-N-(3-chlorobenzyl)-L-prolinamide Investigative T94033 DRUGINFO D05BMA D-leucyl-N-(4-carbamimidoylbenzyl)-L-prolinamide Investigative T94033 DRUGINFO D0O1DU D-phenylalanyl-N-(3-chlorobenzyl)-L-prolinamide Investigative T94033 DRUGINFO D07YNF D-phenylalanyl-N-(3-fluorobenzyl)-L-prolinamide Investigative T94033 DRUGINFO D0K3JC D-phenylalanyl-N-(3-methylbenzyl)-L-prolinamide Investigative T94033 DRUGINFO D08EUH D-phenylalanyl-N-benzyl-L-prolinamide Investigative T94033 DRUGINFO D0M4VZ D-Pro-Phe-Arg chloromethyl ketone Investigative T94033 DRUGINFO D0V7RD DYSINOSIN A Investigative T94033 DRUGINFO D06YJX Enoxaprin Investigative T94033 DRUGINFO D06UUK Gamma-Carboxy-Glutamic Acid Investigative T94033 DRUGINFO D07IBU GR-133686 Investigative T94033 DRUGINFO D08YGD Haempatch Investigative T94033 DRUGINFO D02KKL Hemi-Babim Investigative T94033 DRUGINFO D04CQG Heparin-Cantithrombin III Investigative T94033 DRUGINFO D0I0NY L-370,518 Investigative T94033 DRUGINFO D02NHS L-375378 Investigative T94033 DRUGINFO D0QQ4Z LB30812 Investigative T94033 DRUGINFO D03MYL Lysophosphotidylserine Investigative T94033 DRUGINFO D0RQ2T Macrocyclic tripeptide motif Investigative T94033 DRUGINFO D08MEC Melogatran Investigative T94033 DRUGINFO D0I8WD Methyl L-phenylalaninate Investigative T94033 DRUGINFO D01RTU METHYL-PHE-PRO-AMINO-CYCLOHEXYLGLYCINE Investigative T94033 DRUGINFO D05NRZ N4-(N,N-diphenylcarbamoyl)-aminoguanidine Investigative T94033 DRUGINFO D0H5WV OSCILLARIN Investigative T94033 DRUGINFO D0Z2TG Pedunculagin Investigative T94033 DRUGINFO D0ON2Z RAZAXABAN Investigative T94033 DRUGINFO D09OBJ RWJ-50353 Investigative T94033 DRUGINFO D01WDB S-2238 Investigative T94033 DRUGINFO D0W5AW SC-79407 Investigative T94033 DRUGINFO D0F4VK TB-101 Investigative T94033 DRUGINFO D03KFJ TB-102 Investigative T94033 DRUGINFO D0E6SO Tellimagrandin II Investigative T94033 DRUGINFO D05RFC Tumor vascular thrombogen Investigative T94033 DRUGINFO D04PPE VE-04051645 Investigative T94033 DRUGINFO D07QPA Vitamin K Investigative T94033 KEGGPATH hsa04080:Neuroactive ligand-receptor interaction T94033 KEGGPATH hsa04610:Complement and coagulation cascades T94033 KEGGPATH hsa04810:Regulation of actin cytoskeleton T94033 WIKIPATH WP15:Selenium Micronutrient Network T94033 WIKIPATH WP1533:Vitamin B12 Metabolism T94033 WIKIPATH WP176:Folate Metabolism T94033 WIKIPATH WP1794:Cell surface interactions at the vascular wall T94033 WIKIPATH WP1818:Formation of Fibrin Clot (Clotting Cascade) T94033 WIKIPATH WP1824:GPCR downstream signaling T94033 WIKIPATH WP1825:GPCR ligand binding T94033 WIKIPATH WP1884:Platelet Aggregation (Plug Formation) T94033 WIKIPATH WP1929:Thrombin signalling through proteinase activated receptors (PARs) T94033 WIKIPATH WP2664:Gastrin-CREB signalling pathway via PKC and MAPK T94033 WIKIPATH WP272:Blood Clotting Cascade T94033 WIKIPATH WP2762:PTM: gamma carboxylation, hypusine formation and arylsulfatase activation T94033 WIKIPATH WP2799:Regulation of Insulin-like Growth Factor (IGF) Transport and Uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs) T94033 WIKIPATH WP2865:IL1 and megakaryotyces in obesity T94033 WIKIPATH WP51:Regulation of Actin Cytoskeleton T94033 WIKIPATH WP558:Complement and Coagulation Cascades T94033 WHIZPATH PW000047:Vitamin K Metabolism T94033 WHIZPATH PW000562:Coagulation T94033 REACPATH R-HSA-140837:Intrinsic Pathway of Fibrin Clot Formation T94033 REACPATH R-HSA-140875:Common Pathway of Fibrin Clot Formation T94033 REACPATH R-HSA-159740:Gamma-carboxylation of protein precursors T94033 REACPATH R-HSA-159763:Transport of gamma-carboxylated protein precursors from the endoplasmic reticulum to the Golgi apparatus T94033 REACPATH R-HSA-159782:Removal of aminoterminal propeptides from gamma-carboxylated proteins T94033 REACPATH R-HSA-202733:Cell surface interactions at the vascular wall T94033 REACPATH R-HSA-375276:Peptide ligand-binding receptors T94033 REACPATH R-HSA-381426:Regulation of Insulin-like Growth Factor (IGF) transport and uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs) T94033 REACPATH R-HSA-416476:G alpha (q) signalling events T94033 REACPATH R-HSA-456926:Thrombin signalling through proteinase activated receptors (PARs) T94033 NET_PATH NetPath_11:TCR Signaling Pathway T94033 INTEPATH angiopoietinreceptor_pathway:Angiopoietin receptor Tie2-mediated signaling T94033 INTEPATH hnf3bpathway:FOXA2 and FOXA3 transcription factor networks T94033 INTEPATH syndecan_4_pathway:Syndecan-4-mediated signaling events T94033 INTEPATH thrombin_par1_pathway:PAR1-mediated thrombin signaling events T94033 INTEPATH thrombin_par4_pathway:PAR4-mediated thrombin signaling events T94033 INTEPATH thrombin_pathway:Thrombin/protease-activated receptor (PAR) pathway T94033 PANTPATH P00011:Blood coagulation T83369 TARGETID T83369 T83369 FORMERID TTDC00078 T83369 UNIPROID FA9_HUMAN T83369 TARGNAME Coagulation factor IX (F9) T83369 GENENAME F9 T83369 TARGTYPE Successful target T83369 SYNONYMS Plasma thromboplastin component; PTC protein; Factor IX; Christmas factor T83369 FUNCTION Factor IX is a vitamin K-dependent plasma protein that participates in the intrinsic pathway of blood coagulation by converting factor X to its active form in the presence of Ca(2+) ions, phospholipids, and factor VIIIa. T83369 PDBSTRUC 6MV4; 5VYG; 5TNT; 5TNO; 5JBC T83369 BIOCLASS Peptidase T83369 ECNUMBER EC 3.4.21.22 T83369 SEQUENCE MQRVNMIMAESPGLITICLLGYLLSAECTVFLDHENANKILNRPKRYNSGKLEEFVQGNLERECMEEKCSFEEAREVFENTERTTEFWKQYVDGDQCESNPCLNGGSCKDDINSYECWCPFGFEGKNCELDVTCNIKNGRCEQFCKNSADNKVVCSCTEGYRLAENQKSCEPAVPFPCGRVSVSQTSKLTRAETVFPDVDYVNSTEAETILDNITQSTQSFNDFTRVVGGEDAKPGQFPWQVVLNGKVDAFCGGSIVNEKWIVTAAHCVETGVKITVVAGEHNIEETEHTEQKRNVIRIIPHHNYNAAINKYNHDIALLELDEPLVLNSYVTPICIADKEYTNIFLKFGSGYVSGWGRVFHKGRSALVLQYLRVPLVDRATCLRSTKFTIYNNMFCAGFHEGGRDSCQGDSGGPHVTEVEGTSFLTGIISWGEECAMKGKYGIYTKVSRYVNWIKEKTKLT T83369 DRUGINFO D09XTN Emicizumab Approved T83369 DRUGINFO D0P8QN Recombinant Factor IX Approved T83369 DRUGINFO DBHO19 AMT-061 Phase 3 T83369 DRUGINFO D04AYZ CSL-654 Phase 3 T83369 DRUGINFO DN87BL Fidanacogene elaparvovec Phase 3 T83369 DRUGINFO D08YTF RG6013 Phase 3 T83369 DRUGINFO D0VT1S TTP889 Phase 2 T83369 DRUGINFO D0A9PW AMT-060 Phase 1/2 T83369 DRUGINFO DH40QT SB-FIX Phase 1/2 T83369 DRUGINFO D00TXL AAV2-hFIX16 Phase 1 T83369 DRUGINFO D05RBH N9-GP Phase 1 T83369 DRUGINFO D03MCV RB-006 Discontinued in Phase 3 T83369 DRUGINFO D03PJP Trenonacog alfa Discontinued in Phase 3 T83369 DRUGINFO D07JQO SB 249417 Discontinued in Phase 1 T83369 DRUGINFO D0K9KS Draculin Terminated T83369 DRUGINFO D0Z2PJ 4-Benzyloxybenzo[b]thiophene-2-carboxamidine Investigative T83369 DRUGINFO D05MJU 4-iodobenzo[b]thiophene 2-carboxamidine Investigative T83369 DRUGINFO D0EK9T 4-Phenyl-benzo[b]thiophene-2-carboxamidine Investigative T83369 DRUGINFO D0Y4KJ 5-Benzyloxy-benzo[b]thiophene-2-carboxamidine Investigative T83369 DRUGINFO D0LX0D 6-Benzyloxybenzo[b]thiophene-2-carboxamidine Investigative T83369 DRUGINFO D0Z2UT BNP-FIX Investigative T83369 DRUGINFO D09PDK F-9TG Investigative T83369 DRUGINFO D06IGE Factor IX-XTEN Investigative T83369 DRUGINFO D06UUK Gamma-Carboxy-Glutamic Acid Investigative T83369 DRUGINFO D0YX8X MG-1104 Investigative T83369 DRUGINFO D0Q4XG MOD-3012 Investigative T83369 DRUGINFO D0G4LX PMID20121197C57 Investigative T83369 DRUGINFO D0ON2Z RAZAXABAN Investigative T83369 KEGGPATH hsa04610:Complement and coagulation cascades T83369 WIKIPATH WP1818:Formation of Fibrin Clot (Clotting Cascade) T83369 WIKIPATH WP272:Blood Clotting Cascade T83369 WIKIPATH WP2762:PTM: gamma carboxylation, hypusine formation and arylsulfatase activation T83369 WIKIPATH WP558:Complement and Coagulation Cascades T83369 WHIZPATH PW000562:Coagulation T83369 REACPATH R-HSA-140834:Extrinsic Pathway of Fibrin Clot Formation T83369 REACPATH R-HSA-140837:Intrinsic Pathway of Fibrin Clot Formation T83369 REACPATH R-HSA-159740:Gamma-carboxylation of protein precursors T83369 REACPATH R-HSA-159763:Transport of gamma-carboxylated protein precursors from the endoplasmic reticulum to the Golgi apparatus T83369 REACPATH R-HSA-159782:Removal of aminoterminal propeptides from gamma-carboxylated proteins T83369 PANTPATH P00011:Blood coagulation T84631 TARGETID T84631 T84631 FORMERID TTDS00203 T84631 UNIPROID FA10_HUMAN T84631 TARGNAME Coagulation factor Xa (F10) T84631 GENENAME F10 T84631 TARGTYPE Successful target T84631 SYNONYMS Fxa; Factor Xa; F10; Activated coagulation factor X T84631 FUNCTION Factor Xa is avitamin K-dependent glycoprotein that converts prothrombin to thrombin in the presence of factor Va, calcium and phospholipid during blood clotting. T84631 PDBSTRUC 6RK9; 5VOF; 5VOE; 5K0H; 5JZU T84631 BIOCLASS Peptidase T84631 ECNUMBER EC 3.4.21.6 T84631 SEQUENCE MGRPLHLVLLSASLAGLLLLGESLFIRREQANNILARVTRANSFLEEMKKGHLERECMEETCSYEEAREVFEDSDKTNEFWNKYKDGDQCETSPCQNQGKCKDGLGEYTCTCLEGFEGKNCELFTRKLCSLDNGDCDQFCHEEQNSVVCSCARGYTLADNGKACIPTGPYPCGKQTLERRKRSVAQATSSSGEAPDSITWKPYDAADLDPTENPFDLLDFNQTQPERGDNNLTRIVGGQECKDGECPWQALLINEENEGFCGGTILSEFYILTAAHCLYQAKRFKVRVGDRNTEQEEGGEAVHEVEVVIKHNRFTKETYDFDIAVLRLKTPITFRMNVAPACLPERDWAESTLMTQKTGIVSGFGRTHEKGRQSTRLKMLEVPYVDRNSCKLSSSFIITQNMFCAGYDTKQEDACQGDSGGPHVTRFKDTYFVTGIVSWGEGCARKGKYGIYTKVTAFLKWIDRSMKTRGLPKAKSHAPEVITSSPLK T84631 DRUGINFO D0I5HF Apixaban Approved T84631 DRUGINFO D0J0BU BETRIXABAN Approved T84631 DRUGINFO D0U7HJ Certoparin sodium Approved T84631 DRUGINFO D0Q5KL Coagulation Factor IX Approved T84631 DRUGINFO D0P3SY Danaparoid Approved T84631 DRUGINFO D0C3BS DU-176b Approved T84631 DRUGINFO D09XTN Emicizumab Approved T84631 DRUGINFO D0NE9T Fondaparinux sodium Approved T84631 DRUGINFO D08PSU Lmw heparin Approved T84631 DRUGINFO D0N2BX Nadroparin calcium Approved T84631 DRUGINFO D0KG3R Rivaroxaban Approved T84631 DRUGINFO D07JEW Human coagulation factor X BLA submitted T84631 DRUGINFO D01MUU MELAGATRAN Phase 3 T84631 DRUGINFO D00ITC PRT4445 Phase 3 T84631 DRUGINFO D0P2RO SSR-126517E Phase 3 T84631 DRUGINFO D0VL4V SR-123781A Phase 2/3 T84631 DRUGINFO D01FFG Antistasin Phase 2 T84631 DRUGINFO D0UK1L EP-217609 Phase 2 T84631 DRUGINFO D0ID3W GW-813893 Phase 2 T84631 DRUGINFO D07BRZ LY-517717 Phase 2 T84631 DRUGINFO D00ZPT BI-11634 Phase 1 T84631 DRUGINFO D0X2NN BIBT986 Phase 1 T84631 DRUGINFO D0G6UQ EP-42675 Phase 1 T84631 DRUGINFO D00RGF GCC-4401 Phase 1 T84631 DRUGINFO D08UUD R-1663 Phase 1 T84631 DRUGINFO D02UIC SSR-128428 Phase 1 T84631 DRUGINFO D07OGZ Darexaban maleate Discontinued in Phase 3 T84631 DRUGINFO D0CY3A Idraparinux Discontinued in Phase 3 T84631 DRUGINFO D0E2MJ Otamixaban Discontinued in Phase 3 T84631 DRUGINFO D09TGX Valspodar Discontinued in Phase 3 T84631 DRUGINFO D0L9YS Octopamine Discontinued in Phase 2a T84631 DRUGINFO D0V2OS DX-9065 Discontinued in Phase 2 T84631 DRUGINFO D0JH6W DX-9065a Discontinued in Phase 2 T84631 DRUGINFO D0T4UL PD-348292 Discontinued in Phase 2 T84631 DRUGINFO D0G5GJ R-68151 Discontinued in Phase 2 T84631 DRUGINFO D0D5RH TAK-442 Discontinued in Phase 2 T84631 DRUGINFO D0L4PM AVE-3247 Discontinued in Phase 1 T84631 DRUGINFO D03QJN DPC 423 Discontinued in Phase 1 T84631 DRUGINFO D00CIF EMD-503982 Discontinued in Phase 1 T84631 DRUGINFO D0N8JP JTV-803 Discontinued in Phase 1 T84631 DRUGINFO D0G6UP YM-75466 Discontinued in Phase 1 T84631 DRUGINFO D0PG5J ZD-4927 Discontinued in Phase 1 T84631 DRUGINFO D0K5WM CS-3030 Preclinical T84631 DRUGINFO D0X1ZV Trimidox Preclinical T84631 DRUGINFO D0K9KS Draculin Terminated T84631 DRUGINFO D0Q1JW Hirufaxin Terminated T84631 DRUGINFO D0J9UI YM60828 Terminated T84631 DRUGINFO D00QDR 1,2,3,4,6-penta-O-galloyl-beta-D-glucose Investigative T84631 DRUGINFO D0P3OH 3-chlorophenyl 2-oxo-2H-chromene-3-carboxylate Investigative T84631 DRUGINFO D02XPB 4-(4-Benzyloxy-3-methoxy-benzylamino)-benzamidine Investigative T84631 DRUGINFO D07HWB 5-desgalloylstachyurin Investigative T84631 DRUGINFO D0Z8VP Beta-Hydroxy Aspartic Acid Investigative T84631 DRUGINFO D06HOI BMS-269223 Investigative T84631 DRUGINFO D0J1QT BMS-344577 Investigative T84631 DRUGINFO D0JU9N BMS-740808 Investigative T84631 DRUGINFO D0I1UF CASUARIIN Investigative T84631 DRUGINFO D0R5KV CI-1031 Investigative T84631 DRUGINFO D0M4VZ D-Pro-Phe-Arg chloromethyl ketone Investigative T84631 DRUGINFO D09TXU DT-831j Investigative T84631 DRUGINFO D0Q2VA EP-37 Investigative T84631 DRUGINFO D06UUK Gamma-Carboxy-Glutamic Acid Investigative T84631 DRUGINFO D0QR3J GC-2107 Investigative T84631 DRUGINFO D09KKU Lefaxin Investigative T84631 DRUGINFO D0I8WY M55113 Investigative T84631 DRUGINFO D0ES5A Molecule 11 Investigative T84631 DRUGINFO D0Z2TG Pedunculagin Investigative T84631 DRUGINFO D0FV9Y PhSO2-Gly-(Me-Gly)-Arg-(2-thiazole) Investigative T84631 DRUGINFO D0SP5Q PRT-064445 Investigative T84631 DRUGINFO D0ON2Z RAZAXABAN Investigative T84631 DRUGINFO D0K7NJ Recombinant coagulation factors Investigative T84631 DRUGINFO D08CEU Recombinant Factor X Investigative T84631 DRUGINFO D06BPU SC-83157 Investigative T84631 DRUGINFO D01AUI SF303 Investigative T84631 DRUGINFO D00MZS SK509 Investigative T84631 DRUGINFO D0Z9TY SK549 Investigative T84631 DRUGINFO D04QZF SK554 Investigative T84631 DRUGINFO D03QAQ SN429 Investigative T84631 DRUGINFO D0E6SO Tellimagrandin II Investigative T84631 DRUGINFO D07NYR YM-96765 Investigative T84631 DRUGINFO D0R9CH ZK-810388 Investigative T84631 DRUGINFO D02AVL ZK-813039 Investigative T84631 DRUGINFO D02PAU ZK-814048 Investigative T84631 KEGGPATH hsa04610:Complement and coagulation cascades T84631 WIKIPATH WP1818:Formation of Fibrin Clot (Clotting Cascade) T84631 WIKIPATH WP272:Blood Clotting Cascade T84631 WIKIPATH WP2762:PTM: gamma carboxylation, hypusine formation and arylsulfatase activation T84631 WIKIPATH WP2806:Human Complement System T84631 WIKIPATH WP558:Complement and Coagulation Cascades T84631 WHIZPATH PW000562:Coagulation T84631 REACPATH R-HSA-140834:Extrinsic Pathway of Fibrin Clot Formation T84631 REACPATH R-HSA-140837:Intrinsic Pathway of Fibrin Clot Formation T84631 REACPATH R-HSA-140875:Common Pathway of Fibrin Clot Formation T84631 REACPATH R-HSA-159740:Gamma-carboxylation of protein precursors T84631 REACPATH R-HSA-159763:Transport of gamma-carboxylated protein precursors from the endoplasmic reticulum to the Golgi apparatus T84631 REACPATH R-HSA-159782:Removal of aminoterminal propeptides from gamma-carboxylated proteins T84631 INTEPATH integrin2_pathway:Beta2 integrin cell surface interactions T84631 PANTPATH P00011:Blood coagulation T89034 TARGETID T89034 T89034 FORMERID TTDS00392 T89034 UNIPROID PLMN_HUMAN T89034 TARGNAME Plasminogen (PLG) T89034 GENENAME PLG T89034 TARGTYPE Successful target T89034 SYNONYMS Plasmin T89034 FUNCTION In ovulation, weakens the walls of the Graafian follicle. It activates the urokinase-type plasminogen activator, collagenases and several complement zymogens, such as C1 and C5. Cleavage of fibronectin and laminin leads to cell detachment and apoptosis. Also cleaves fibrin, thrombospondin and von Willebrand factor. Its role in tissue remodeling and tumor invasion may be modulated by CSPG4. Binds to cells. Plasmin dissolves the fibrin of blood clots and acts as a proteolytic factor in a variety of other processes including embryonic development, tissue remodeling, tumor invasion, and inflammation. T89034 PDBSTRUC 6D40; 6D3Z; 6D3Y; 6D3X; 5UGG T89034 BIOCLASS Peptidase T89034 ECNUMBER EC 3.4.21.7 T89034 SEQUENCE MEHKEVVLLLLLFLKSGQGEPLDDYVNTQGASLFSVTKKQLGAGSIEECAAKCEEDEEFTCRAFQYHSKEQQCVIMAENRKSSIIIRMRDVVLFEKKVYLSECKTGNGKNYRGTMSKTKNGITCQKWSSTSPHRPRFSPATHPSEGLEENYCRNPDNDPQGPWCYTTDPEKRYDYCDILECEEECMHCSGENYDGKISKTMSGLECQAWDSQSPHAHGYIPSKFPNKNLKKNYCRNPDRELRPWCFTTDPNKRWELCDIPRCTTPPPSSGPTYQCLKGTGENYRGNVAVTVSGHTCQHWSAQTPHTHNRTPENFPCKNLDENYCRNPDGKRAPWCHTTNSQVRWEYCKIPSCDSSPVSTEQLAPTAPPELTPVVQDCYHGDGQSYRGTSSTTTTGKKCQSWSSMTPHRHQKTPENYPNAGLTMNYCRNPDADKGPWCFTTDPSVRWEYCNLKKCSGTEASVVAPPPVVLLPDVETPSEEDCMFGNGKGYRGKRATTVTGTPCQDWAAQEPHRHSIFTPETNPRAGLEKNYCRNPDGDVGGPWCYTTNPRKLYDYCDVPQCAAPSFDCGKPQVEPKKCPGRVVGGCVAHPHSWPWQVSLRTRFGMHFCGGTLISPEWVLTAAHCLEKSPRPSSYKVILGAHQEVNLEPHVQEIEVSRLFLEPTRKDIALLKLSSPAVITDKVIPACLPSPNYVVADRTECFITGWGETQGTFGAGLLKEAQLPVIENKVCNRYEFLNGRVQSTELCAGHLAGGTDSCQGDSGGPLVCFEKDKYILQGVTSWGLGCARPNKPGVYVRVSRFVTWIEGVMRNN T89034 DRUGINFO D07BQE Alteplase Approved T89034 DRUGINFO D0FD0H Aminocaproic Acid Approved T89034 DRUGINFO D0K4DI Anistreplase Approved T89034 DRUGINFO D03HYQ Ranolazine Approved T89034 DRUGINFO D0T1UJ Reteplase Approved T89034 DRUGINFO D04URO Streptokinase Approved T89034 DRUGINFO D0FX8A Tenecteplase Approved T89034 DRUGINFO D05HXX Tranexamic Acid Approved T89034 DRUGINFO D0TC4R Desmoteplase Phase 3 T89034 DRUGINFO D01MUU MELAGATRAN Phase 3 T89034 DRUGINFO D0S4YT Plasminogen Phase 2/3 T89034 DRUGINFO D0RD0Y RetinoStat Phase 2 T89034 DRUGINFO D09IOF Troplasminogen alfa Phase 2 T89034 DRUGINFO D0PK7J bis-triazole derivative 10 Clinical trial T89034 DRUGINFO D0A9HM 1-(2-Oxo-2-p-tolyl-ethyl)-1H-indole-2,3-dione Investigative T89034 DRUGINFO D0VP6M 1-(3,3-Dimethyl-2-oxo-butyl)-1H-indole-2,3-dione Investigative T89034 DRUGINFO D0K4PK 1-guanidino-7-isoquinolinesulphonamide Investigative T89034 DRUGINFO D00PEJ 1-guanidino-N-phenyl-7-isoquinolinesulphonamide Investigative T89034 DRUGINFO D08OLP 2-(2-Hydroxy-phenyl)-1H-indole-5-carboxamidine Investigative T89034 DRUGINFO D0V2MR Bicine Investigative T89034 DRUGINFO D0Y5IQ Grassystatin a Investigative T89034 DRUGINFO D0LJ7R M5 Investigative T89034 DRUGINFO D01JUI N-(4-Chloro-7-p-tolyl-isoquinolin-1-yl)-guanidine Investigative T89034 DRUGINFO D04DYA SMTP-0 Investigative T89034 DRUGINFO D0ND8N Textilinin Investigative T89034 DRUGINFO D0M9XH XP-21510 Investigative T89034 KEGGPATH hsa04080:Neuroactive ligand-receptor interaction T89034 KEGGPATH hsa04610:Complement and coagulation cascades T89034 KEGGPATH hsa05150:Staphylococcus aureus infection T89034 KEGGPATH hsa05164:Influenza A T89034 WIKIPATH WP15:Selenium Micronutrient Network T89034 WIKIPATH WP1533:Vitamin B12 Metabolism T89034 WIKIPATH WP176:Folate Metabolism T89034 WIKIPATH WP1802:Dissolution of Fibrin Clot T89034 WIKIPATH WP272:Blood Clotting Cascade T89034 WIKIPATH WP2769:Activation of Matrix Metalloproteinases T89034 WIKIPATH WP2799:Regulation of Insulin-like Growth Factor (IGF) Transport and Uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs) T89034 WIKIPATH WP2806:Human Complement System T89034 WIKIPATH WP558:Complement and Coagulation Cascades T89034 WHIZPATH PW000562:Coagulation T89034 REACPATH R-HSA-114608:Platelet degranulation T89034 REACPATH R-HSA-1474228:Degradation of the extracellular matrix T89034 REACPATH R-HSA-1592389:Activation of Matrix Metalloproteinases T89034 REACPATH R-HSA-381426:Regulation of Insulin-like Growth Factor (IGF) transport and uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs) T89034 REACPATH R-HSA-75205:Dissolution of Fibrin Clot T89034 INTEPATH amb2_neutrophils_pathway:amb2 Integrin signaling T89034 INTEPATH angiopoietinreceptor_pathway:Angiopoietin receptor Tie2-mediated signaling T89034 INTEPATH p75ntrpathway:p75(NTR)-mediated signaling T89034 INTEPATH syndecan_4_pathway:Syndecan-4-mediated signaling events T89034 INTEPATH upa_upar_pathway:Urokinase-type plasminogen activator (uPA) and uPAR-mediated signaling T89034 PANTPATH P00011:Blood coagulation T89034 PANTPATH P00050:Plasminogen activating cascade T17758 TARGETID T17758 T17758 FORMERID TTDC00312 T17758 UNIPROID UROK_HUMAN T17758 TARGNAME Urokinase-type plasminogen activator (PLAU) T17758 GENENAME PLAU T17758 TARGTYPE Successful target T17758 SYNONYMS UPA; U-plasminogen activator T17758 FUNCTION Specifically cleaves the zymogen plasminogen to form the active enzyme plasmin. T17758 PDBSTRUC 6NMB; 5ZC5; 5ZAJ; 5ZAH; 5ZAG T17758 BIOCLASS Peptidase T17758 ECNUMBER EC 3.4.21.73 T17758 SEQUENCE MRALLARLLLCVLVVSDSKGSNELHQVPSNCDCLNGGTCVSNKYFSNIHWCNCPKKFGGQHCEIDKSKTCYEGNGHFYRGKASTDTMGRPCLPWNSATVLQQTYHAHRSDALQLGLGKHNYCRNPDNRRRPWCYVQVGLKPLVQECMVHDCADGKKPSSPPEELKFQCGQKTLRPRFKIIGGEFTTIENQPWFAAIYRRHRGGSVTYVCGGSLISPCWVISATHCFIDYPKKEDYIVYLGRSRLNSNTQGEMKFEVENLILHKDYSADTLAHHNDIALLKIRSKEGRCAQPSRTIQTICLPSMYNDPQFGTSCEITGFGKENSTDYLYPEQLKMTVVKLISHRECQQPHYYGSEVTTKMLCAADPQWKTDSCQGDSGGPLVCSLQGRMTLTGIVSWGRGCALKDKPGVYTRVSHFLPWIRSHTKEENGLAL T17758 DRUGINFO D03VNX Pro-urokinase Approved T17758 DRUGINFO D0E8UO Urokinase Approved T17758 DRUGINFO D03ZJE PAI-1 Phase 4 T17758 DRUGINFO D0G6ZG Amediplase Phase 3 T17758 DRUGINFO D0G5UW Saruplase Phase 2 T17758 DRUGINFO D03KGH Upamostat Phase 2 T17758 DRUGINFO D01HHJ HTU-PA Phase 1/2 T17758 DRUGINFO D00EPS PMID18163548C4 Clinical trial T17758 DRUGINFO D0G0YZ UK-356202 Clinical trial T17758 DRUGINFO D0D3VA PAI-2 Discontinued in Phase 2 T17758 DRUGINFO D08INO WX-UK1 Discontinued in Phase 1/2 T17758 DRUGINFO D0K1PR B-428 Terminated T17758 DRUGINFO D03NLL (2R)-1-(2,6-dimethylphenoxy)propan-2-amine Investigative T17758 DRUGINFO D0X1OY (3,4-dichlorophenyl)(1H-pyrazol-1-yl)methanone Investigative T17758 DRUGINFO D08OCS (3-nitro-1H-pyrazol-1-yl)(p-tolyl)methanone Investigative T17758 DRUGINFO D05ZIP (4-bromo-1H-pyrazol-1-yl)(p-tolyl)methanone Investigative T17758 DRUGINFO D0F6EZ (4-guanidino-benzyl)-carbamic acid benzyl ester Investigative T17758 DRUGINFO D00WFQ (4-nitro-1H-pyrazol-1-yl)(o-tolyl)methanone Investigative T17758 DRUGINFO D06LPR (4-nitro-1H-pyrazol-1-yl)(phenyl)methanone Investigative T17758 DRUGINFO D0ZM9M 1-[4-(2-oxo-2-phenylethyl)phenyl]guanidine Investigative T17758 DRUGINFO D0IU5E 1-benzoyl-N-phenyl-1H-pyrazole-3-carboxamide Investigative T17758 DRUGINFO D0K4PK 1-guanidino-7-isoquinolinesulphonamide Investigative T17758 DRUGINFO D00PEJ 1-guanidino-N-phenyl-7-isoquinolinesulphonamide Investigative T17758 DRUGINFO D08OLP 2-(2-Hydroxy-phenyl)-1H-indole-5-carboxamidine Investigative T17758 DRUGINFO D09KKF 2-Amino-5-Hydroxy-Benzimidazole Investigative T17758 DRUGINFO D0SP2I 2-nas-phe(3-am)-4-(2-guanidinoethyl)piperidine Investigative T17758 DRUGINFO D06CJP 4-chloro-1-guanidino-7-isoquinolinesulphonamide Investigative T17758 DRUGINFO D05MJU 4-iodobenzo[b]thiophene 2-carboxamidine Investigative T17758 DRUGINFO D02AKP 4-methoxy-N'-(2-phenylacetyl)benzohydrazide Investigative T17758 DRUGINFO D02XJW 5-Methylsulfanyl-thiophene-2-carboxamidine Investigative T17758 DRUGINFO D0A8WP 6-(N-Phenylcarbamyl)-2-Naphthalenecarboxamidine Investigative T17758 DRUGINFO D05ABK ATF-HI-8 Investigative T17758 DRUGINFO D03BWQ ATN-658 Investigative T17758 DRUGINFO D05DNW B-623 Investigative T17758 DRUGINFO D07SFI Benzamidine Investigative T17758 DRUGINFO D01LCS CRA_10655 Investigative T17758 DRUGINFO D0K7YL CRA_8696 Investigative T17758 DRUGINFO D0G6XS Fucose Investigative T17758 DRUGINFO D0EV6B N-(1-Adamantyl)-N'-(4-Guanidinobenzyl)Urea Investigative T17758 DRUGINFO D0D1TX Recombinant human pro-urokinase Investigative T17758 DRUGINFO D0B1AK Thieno[2,3-B]Pyridine-2-Carboxamidine Investigative T17758 DRUGINFO D00LDI UPA-targeted oncolytic Sendai virus Investigative T17758 KEGGPATH hsa04064:NF-kappa B signaling pathway T17758 KEGGPATH hsa04610:Complement and coagulation cascades T17758 KEGGPATH hsa05202:Transcriptional misregulation in cancer T17758 KEGGPATH hsa05205:Proteoglycans in cancer T17758 KEGGPATH hsa05206:MicroRNAs in cancer T17758 WIKIPATH WP1434:Osteopontin Signaling T17758 WIKIPATH WP1802:Dissolution of Fibrin Clot T17758 WIKIPATH WP272:Blood Clotting Cascade T17758 WIKIPATH WP399:Wnt Signaling Pathway and Pluripotency T17758 WIKIPATH WP428:Wnt Signaling Pathway T17758 WIKIPATH WP474:Endochondral Ossification T17758 WIKIPATH WP558:Complement and Coagulation Cascades T17758 WIKIPATH WP615:Senescence and Autophagy in Cancer T17758 WIKIPATH WP710:DNA Damage Response (only ATM dependent) T17758 REACPATH R-HSA-75205:Dissolution of Fibrin Clot T17758 NET_PATH NetPath_14:IL2 Signaling Pathway T17758 NET_PATH NetPath_4:EGFR1 Signaling Pathway T17758 INTEPATH amb2_neutrophils_pathway:amb2 Integrin signaling T17758 INTEPATH ap1_pathway:AP-1 transcription factor network T17758 INTEPATH atf2_pathway:ATF-2 transcription factor network T17758 INTEPATH avb3_opn_pathway:Osteopontin-mediated events T17758 INTEPATH e2f_pathway:E2F transcription factor network T17758 INTEPATH fgf_pathway:FGF signaling pathway T17758 INTEPATH fra_pathway:Validated transcriptional targets of AP1 family members Fra1 and Fra2 T17758 INTEPATH integrin1_pathway:Beta1 integrin cell surface interactions T17758 INTEPATH integrin2_pathway:Beta2 integrin cell surface interactions T17758 INTEPATH integrin3_pathway:Beta3 integrin cell surface interactions T17758 INTEPATH integrin5_pathway:Beta5 beta6 beta7 and beta8 integrin cell surface interactions T17758 INTEPATH upa_upar_pathway:Urokinase-type plasminogen activator (uPA) and uPAR-mediated signaling T17758 PANTPATH P00011:Blood coagulation T17758 PANTPATH P00050:Plasminogen activating cascade T17758 PANTPATH P06959:CCKR signaling map ST T61622 TARGETID T61622 T61622 FORMERID TTDS00451 T61622 UNIPROID RENI_HUMAN T61622 TARGNAME Angiotensinogenase renin (REN) T61622 GENENAME REN T61622 TARGTYPE Successful target T61622 SYNONYMS Renin; Angiotensinogenase T61622 FUNCTION Renin is a highly specific endopeptidase, whose only knownfunction is to generate angiotensin I from angiotensinogen in the plasma, initiating a cascade of reactions that produce an elevation of blood pressure and increased sodium retention by the kidney. T61622 PDBSTRUC 6I3F; 5VRP; 5VPM; 5V8V; 5TMK T61622 BIOCLASS Peptidase T61622 ECNUMBER EC 3.4.23.15 T61622 SEQUENCE MDGWRRMPRWGLLLLLWGSCTFGLPTDTTTFKRIFLKRMPSIRESLKERGVDMARLGPEWSQPMKRLTLGNTTSSVILTNYMDTQYYGEIGIGTPPQTFKVVFDTGSSNVWVPSSKCSRLYTACVYHKLFDASDSSSYKHNGTELTLRYSTGTVSGFLSQDIITVGGITVTQMFGEVTEMPALPFMLAEFDGVVGMGFIEQAIGRVTPIFDNIISQGVLKEDVFSFYYNRDSENSQSLGGQIVLGGSDPQHYEGNFHYINLIKTGVWQIQMKGVSVGSSTLLCEDGCLALVDTGASYISGSTSSIEKLMEALGAKKRLFDYVVKCNEGPTLPDISFHLGGKEYTLTSADYVFQESYSSKKLCTLAIHAMDIPPPTGPTWALGATFIRKFYTEFDRRNNRIGFALAR T61622 DRUGINFO D03SVX Aliskiren Approved T61622 DRUGINFO D0C2EP Remikiren Approved T61622 DRUGINFO D0V3UN CP-80794 Phase 2 T61622 DRUGINFO D07JXN SPP-600 Phase 2 T61622 DRUGINFO D0H8WZ SR-43845 Phase 2 T61622 DRUGINFO D0A5SA TAK-272 Phase 2 T61622 DRUGINFO D03XHS ACT-178882 Phase 1 T61622 DRUGINFO D0U7OS CARD-024 Phase 1 T61622 DRUGINFO D01QSG VTP-27999 Phase 1 T61622 DRUGINFO D09ELW Enalkiren Discontinued in Phase 2 T61622 DRUGINFO D01SGM FK-906 Discontinued in Phase 2 T61622 DRUGINFO D0J5GT ZANKIREN Discontinued in Phase 2 T61622 DRUGINFO D0V4LG RS-8891 Discontinued in Phase 1 T61622 DRUGINFO D0L4VZ SPP-1148 Discontinued in Phase 1 T61622 DRUGINFO D02KEY SPP-676 Discontinued in Phase 1 T61622 DRUGINFO D0K1AF A-74273 Terminated T61622 DRUGINFO D08IDQ BILA-2157BS Terminated T61622 DRUGINFO D02KBO Ciprokiren Terminated T61622 DRUGINFO D05FTY ES-1005 Terminated T61622 DRUGINFO D01EZY JTP-2724 Terminated T61622 DRUGINFO D00MIF JTP-4761 Terminated T61622 DRUGINFO D0V5XL KRI-1314 Terminated T61622 DRUGINFO D06ZKG SC-56525 Terminated T61622 DRUGINFO D0M7HO SQ-33800 Terminated T61622 DRUGINFO D04DZP (H-261)Boc-His-Pro-Phe-His-Leu(OH)-Val-Ile-His-OH Investigative T61622 DRUGINFO D06OBP 1-Hydroxy-2-Amino-3-Cyclohexylpropane Investigative T61622 DRUGINFO D0V4EK 1-Hydroxy-3-Methylbutane Investigative T61622 DRUGINFO D0A9BK 1-Methyl-2-Oxy-5,5-Dimethyl Pyrrolidine Investigative T61622 DRUGINFO D09RQD 2-Cyclopropylmethylenepropanal Investigative T61622 DRUGINFO D02MBW 2-Methyl-3-(2-Aminothiazolo)Propanal Investigative T61622 DRUGINFO D09QXR 3-Phenyl-1,2-Propandiol Investigative T61622 DRUGINFO D0P7NP CP-305202 Investigative T61622 DRUGINFO D0E1KX Dimethylformamide Investigative T61622 DRUGINFO D0TD2F ES-6864 Investigative T61622 DRUGINFO D0K0OY Glu-Trp-Pro-Arg-Pro-Gln-Ile-Pro-Pro Investigative T61622 DRUGINFO D00FHV Iva-His-Pro-Phe-His-ACHPA-Leu-Phe-NH2 Investigative T61622 DRUGINFO D0G9DJ Iva-His-Pro-Phe-His-AHPPA-Leu-Phe-NH2 Investigative T61622 DRUGINFO D09PZT Iva-His-Pro-Phe-His-Sta-Leu-Phe-NH2 Investigative T61622 DRUGINFO D0Q8VT JT-2724 Investigative T61622 DRUGINFO D02MME N-Methyl-N-(Methylbenzyl)Formamide Investigative T61622 DRUGINFO D0J6QC PP1-Pro-Phe-N-MeHis-LVA-Ile-Amp-(O) Investigative T61622 DRUGINFO D0VI7P PP2-Pro-Phe-N-MeHis-LVA-Ile-Amp-(O) Investigative T61622 DRUGINFO D08BRJ Pro-His-Pro-His-Leu-Phe-Val-Tyr Investigative T61622 DRUGINFO D01FJQ Pro-His-Pro-His-Phe-Phe-Val-Tyr Investigative T61622 DRUGINFO D0Q3IE Pro-His-Pro-His-Phe-Phe-Val-Tyr-Lys Investigative T61622 DRUGINFO D0KH9Z Pro-His-Pro-Phe-His-Leu(CH2NH)Val-Ile-His-Lys Investigative T61622 DRUGINFO D0E5QB Ro-65-7219 Investigative T61622 DRUGINFO D04QIA Ro-66-1168 Investigative T61622 DRUGINFO D06JQM SPP-800 Investigative T61622 DRUGINFO D0A3LJ Sul-Pro-Phe-N-MeHis-LVA-Ile-Amp Investigative T61622 DRUGINFO D04GXL Sul-Pro-Phe-N-MeHis-LVA-Ile-Amp-(O) Investigative T61622 KEGGPATH hsa04614:Renin-angiotensin system T61622 WIKIPATH WP2729:Metabolism of Angiotensinogen to Angiotensins T61622 WIKIPATH WP554:ACE Inhibitor Pathway T61622 WHIZPATH PW000563:Angiotensin Metabolism T61622 REACPATH R-HSA-2022377:Metabolism of Angiotensinogen to Angiotensins T56915 TARGETID T56915 T56915 FORMERID TTDS00320 T56915 UNIPROID POL_HV1B1 T56915 TARGNAME Human immunodeficiency virus Protease (HIV PR) T56915 GENENAME HIV PR T56915 TARGTYPE Successful target T56915 SYNONYMS HIV Retropepsin; HIV PR T56915 FUNCTION Gag-Pol polyprotein: Mediates, with Gag polyprotein, the essential events in virion assembly, including binding the plasma membrane, making the protein-protein interactions necessary to create spherical particles, recruiting the viral Env proteins, and packaging the genomic RNA via direct interactions with the RNA packaging sequence (Psi). Gag-Pol polyprotein may regulate its own translation, by the binding genomic RNA in the 5'-UTR. At low concentration, the polyprotein would promote translation, whereas at high concentration, the polyprotein would encapsidate genomic RNA and then shut off translation. T56915 PDBSTRUC 6OE3; 6HAK; 6ELI; 6DUH; 6DUG T56915 BIOCLASS Peptidase T56915 ECNUMBER EC 3.4.23.16 T56915 SEQUENCE PQITLWQRPLVTIKIGGQLKEALLDTGADDTVLEEMSLPGRWKPKMIGGIGGFIKVRQYDQILIEICGHKAIGTVLVGPTPVNIIGRNLLTQIGCTLNF T56915 DRUGINFO D0A0OO Amprenavir Approved T56915 DRUGINFO D07IQS Atazanavir Approved T56915 DRUGINFO D03IGH Darunavir Approved T56915 DRUGINFO D0F5MT Fosamprenavir Approved T56915 DRUGINFO D0V7CF Indinavir Approved T56915 DRUGINFO D0ZU9R Ritonavir Approved T56915 DRUGINFO D0WI3T Saquinavir Approved T56915 DRUGINFO D0EV6T Tipranavir Approved T56915 DRUGINFO D06KJQ BI 201335 Phase 3 T56915 DRUGINFO D07OHT ABT-450 Phase 2 T56915 DRUGINFO D07ZAH ACH-1625 Phase 2 T56915 DRUGINFO D04MCY BMS 650032 Phase 2 T56915 DRUGINFO D0R9MN Danoprevir Phase 2 T56915 DRUGINFO D0Y3JI DG-17 Phase 2 T56915 DRUGINFO D05TKB GS-9256 Phase 2 T56915 DRUGINFO D0W9JM KNI-272 Phase 2 T56915 DRUGINFO D07SMH MK-5172 Phase 2 T56915 DRUGINFO D01ZNQ TMC-310911 Phase 2 T56915 DRUGINFO D01RXW Vaniprevir Phase 2 T56915 DRUGINFO D0W6LW BIT225 Phase 1 T56915 DRUGINFO D04CJN CTP-298 Phase 1 T56915 DRUGINFO D08FYH PF-04776548 Phase 1 T56915 DRUGINFO D09QKI PPL-100 Phase 1 T56915 DRUGINFO D02MMP VX-500 Phase 1 T56915 DRUGINFO D07MPJ A-75925 Discontinued in Phase 2 T56915 DRUGINFO D07FJM BRECANAVIR Discontinued in Phase 2 T56915 DRUGINFO D0J9AK MK-944a Discontinued in Phase 2 T56915 DRUGINFO D0E4FG Mozenavir Discontinued in Phase 2 T56915 DRUGINFO D05UMD R-87366 Discontinued in Phase 2 T56915 DRUGINFO D04GWY Telinavir Discontinued in Phase 2 T56915 DRUGINFO D09HEV GS-9005 Discontinued in Phase 1/2 T56915 DRUGINFO D0U7WN A-80987 Discontinued in Phase 1 T56915 DRUGINFO D01KIS CGP-53437 Discontinued in Phase 1 T56915 DRUGINFO D0U8AR DMP-851 Discontinued in Phase 1 T56915 DRUGINFO D0N3ZY DPC-681 Discontinued in Phase 1 T56915 DRUGINFO D07JJC DPC-684 Discontinued in Phase 1 T56915 DRUGINFO D0X8AU KNI-764 Discontinued in Phase 1 T56915 DRUGINFO D0R5AU LASINAVIR Discontinued in Phase 1 T56915 DRUGINFO D08JTU R-944 Discontinued in Phase 1 T56915 DRUGINFO D03MIP SPI-256 Discontinued in Phase 1 T56915 DRUGINFO D06KPW U-103017 Discontinued in Phase 1 T56915 DRUGINFO D09CAC U-96988 Discontinued in Phase 1 T56915 DRUGINFO D0PB4P XM-323 Discontinued in Phase 1 T56915 DRUGINFO D0GM4S AG-1284 Terminated T56915 DRUGINFO D07PIA AG-1350 Terminated T56915 DRUGINFO D05UMO BAY-793 Terminated T56915 DRUGINFO D00XRK BMS-182193 Terminated T56915 DRUGINFO D01RCC BMS-186318 Terminated T56915 DRUGINFO D06FMY CGP-70726 Terminated T56915 DRUGINFO D0V8PN Droxinavir hydrochloride Terminated T56915 DRUGINFO D02TGW GE-20372A Terminated T56915 DRUGINFO D0R3JE GS-2992 Terminated T56915 DRUGINFO D05GQL KNI-102 Terminated T56915 DRUGINFO D0T4OE Palinavir Terminated T56915 DRUGINFO D0P6DF PD-153103 Terminated T56915 DRUGINFO D0QH0R SB-206343 Terminated T56915 DRUGINFO D07PSP U-75875 Terminated T56915 DRUGINFO D0G6HC JG-365 Investigative T56915 DRUGINFO D0B0XX KH-164 Investigative T31595 TARGETID T31595 T31595 FORMERID TTDS00174 T31595 UNIPROID NRAM_I33A0 T31595 TARGNAME Influenza Neuraminidase (Influ NA) T31595 GENENAME Influ NA T31595 TARGTYPE Successful target T31595 SYNONYMS STNA; NEU1; NANase; N-acylneuraminate glycohydrolase; Influ Sialidase T31595 FUNCTION Unlike other strains, A/WSN/33 neuraminidase binds and activates plasminogen into plasmin in the vicinity of HA so that activated plasmin cleaves HA rendering the virus infectious. T31595 BIOCLASS Glycosylase T31595 ECNUMBER EC 3.2.1.18 T31595 SEQUENCE MNPNQKIITIGSICMVVGIISLILQIGNIISIWISHSIQTGNQNHTGICNQGIITYNVVAGQDSTSVILTGNSSLCPIRGWAIHSKDNGIRIGSKGDVFVIREPFISCSHLECRTFFLTQGALLNDKHSNGTVKDRSPYRALMSCPVGEAPSPYNSRFESVAWSASACHDGMGWLTIGISGPDNGAVAVLKYNGIITETIKSWRKKILRTQESECTCVNGSCFTIMTDGPSNGLASYKIFKIEKGKVTKSIELNAPNSHYEECSCYPDTGKVMCVCRDNWHGSNRPWVSFDQNLDYQIGYICSGVFGDNPRPKDGPGSCGPVSADGANGVKGFSYRYGNGVWIGRTKSDSSRHGFEMIWDPNGWTETDSRFSVRQDVVAMTDRSGYSGSFVQHPELTGLDCMRPCFWVELIRGRPEEETIWTSGSIISFCGVNSDTVDWSWPDGAELPFTIDK T31595 DRUGINFO D0O5NK Oseltamivir Approved T31595 DRUGINFO D0P2IW Peramivir Approved T31595 DRUGINFO D00NPP Zanamivir Approved T31595 DRUGINFO D04VSM CS-8958 Phase 3 T31595 DRUGINFO D03ZKM UX-001 Phase 3 T31595 DRUGINFO D0YO7Y DAS-181 Phase 2 T31595 DRUGINFO D0XJ0P BCX-140 Terminated T31595 DRUGINFO D0Q3ZN GS-3435 Terminated T31595 DRUGINFO D0IH6W (E,E)-1,7-Diphenyl-4,6-heptadien-3-one Investigative T31595 DRUGINFO D0D9NX (E,E)-5-Hydroxy-1,7-diphenyl-4,6-heptadien-3-one Investigative T31595 DRUGINFO D03XVT (S)-1,7-Diphenyl-6(E)-hepten-3-ol Investigative T31595 DRUGINFO D0D8WQ 2,4-Deoxy-4-Guanidino-5-N-Acetyl-Neuraminic Acid Investigative T31595 DRUGINFO D06BSN 2-Deoxy-2,3-Dehydro-N-Acetyl-Neuraminic Acid Investigative T31595 DRUGINFO D0F8CH 4-(Acetylamino)-3-Amino Benzoic Acid Investigative T31595 DRUGINFO D0Q8HV 4-(ACETYLAMINO)-3-HYDROXY-5-NITROBENZOIC ACID Investigative T31595 DRUGINFO D08UEU 4-(ACETYLAMINO)-5-AMINO-3-HYDROXYBENZOIC ACID Investigative T31595 DRUGINFO D0C4GE 4-Amino-2-Deoxy-2,3-Dehydro-N-Neuraminic Acid Investigative T31595 DRUGINFO D01FEA 8-DEOXYGARTANIN Investigative T31595 DRUGINFO D0P3BL A-192558 Investigative T31595 DRUGINFO D06LUX A-315675 Investigative T31595 DRUGINFO D07LUR Alpha-D-Mannose Investigative T31595 DRUGINFO D00RIX APIGENIN Investigative T31595 DRUGINFO D0PE5T BCX-1827 Investigative T31595 DRUGINFO D0I1BA BCX-1898 Investigative T31595 DRUGINFO D0R6YP BCX-1923 Investigative T31595 DRUGINFO D0SD9H Beta-D-Mannose Investigative T31595 DRUGINFO D05FLL CALOPOCARPIN Investigative T31595 DRUGINFO D00PAS Cristacarpin Investigative T31595 DRUGINFO D02HYW CUDRATRICUSXANTHONE Investigative T31595 DRUGINFO D0UR7U Cudratricusxanthone F Investigative T31595 DRUGINFO D0I6EH Cudraxanthone D Investigative T31595 DRUGINFO D0A2OH Cudraxanthone L Investigative T31595 DRUGINFO D05KWF Cudraxanthone M Investigative T31595 DRUGINFO D05BUX Cyclopentane amide derivatives 1 Investigative T31595 DRUGINFO D09YOY Cyclopentane amide derivatives 2 Investigative T31595 DRUGINFO D0B1NY Cyclopentane amide derivatives 3 Investigative T31595 DRUGINFO D0W0BO Cyclopentane amide derivatives 4 Investigative T31595 DRUGINFO D0G5PT DEMETHYLMEDICARPIN Investigative T31595 DRUGINFO D0P5MJ ERYSTAGALLIN A Investigative T31595 DRUGINFO D0UD1U Erysubin D Investigative T31595 DRUGINFO D0M7ZZ Erysubin E Investigative T31595 DRUGINFO D00PZM Erythribyssin D Investigative T31595 DRUGINFO D0E8VD Erythribyssin L Investigative T31595 DRUGINFO D02QCC Erythribyssin M Investigative T31595 DRUGINFO D01FQZ Erythribyssin O Investigative T31595 DRUGINFO D02NRI Eryvarin D Investigative T31595 DRUGINFO D00LEQ FANA Investigative T31595 DRUGINFO D0G6XS Fucose Investigative T31595 DRUGINFO D05IWY Gamma-mangostin Investigative T31595 DRUGINFO D05YJR GARCINONE D Investigative T31595 DRUGINFO D0O8EB GARTANIN Investigative T31595 DRUGINFO D0Z7EL GOSSYPETIN Investigative T31595 DRUGINFO D06IDO GS4071 Investigative T31595 DRUGINFO D09YVT HERBACETIN Investigative T31595 DRUGINFO D05GSS ISONEORAUTENOL Investigative T31595 DRUGINFO D0G3TK KAEMPFEROL Investigative T31595 DRUGINFO D0UK4O KATSUMADAIN A Investigative T31595 DRUGINFO D0K8XC Lactose Investigative T31595 DRUGINFO D0U8AU MACLURAXANTHONE Investigative T31595 DRUGINFO D04UYB MANGIFERIN Investigative T31595 DRUGINFO D01WTQ MANGOSTANIN Investigative T31595 DRUGINFO D0G5MS MANGOSTANOL Investigative T31595 DRUGINFO D0J7YV MANGOSTENONE F Investigative T31595 DRUGINFO D0MA3M MANGOSTENONE G Investigative T31595 DRUGINFO D06PRC MANGOSTIN Investigative T31595 DRUGINFO D01EJH NEORAUTENOL Investigative T31595 DRUGINFO D08WQM O-Sialic Acid Investigative T31595 DRUGINFO D07TDM PHASEOLIN Investigative T31595 DRUGINFO D0A9CZ PHASEOLLIDIN Investigative T31595 DRUGINFO D0I0WF RHODIOLININ Investigative T31595 DRUGINFO D0K6FM SMEATHXANTHONE A Investigative T31595 KEGGPATH stm00511:Other glycan degradation T31479 TARGETID T31479 T31479 FORMERID TTDS00065 T31479 UNIPROID PA21B_HUMAN T31479 TARGNAME Phospholipase A2 (PLA2G1B) T31479 GENENAME PLA2G1B T31479 TARGTYPE Successful target T31479 SYNONYMS Secreted phospholipase A(2); Phosphatidylcholine 2-acylhydrolase 1B; PLA2G1B; Group IB phospholipase A2 T31479 FUNCTION PA2 catalyzes the calcium-dependent hydrolysis of the 2- acyl groups in 3-sn-phosphoglycerides, this releases glycerophospholipids and arachidonic acid that serve as the precursors of signal molecules. T31479 PDBSTRUC 3ELO; 1YSK T31479 BIOCLASS Carboxylic ester hydrolase T31479 ECNUMBER EC 3.1.1.4 T31479 SEQUENCE MKLLVLAVLLTVAAADSGISPRAVWQFRKMIKCVIPGSDPFLEYNNYGCYCGLGGSGTPVDELDKCCQTHDNCYDQAKKLDSCKFLLDNPYTHTYSYSCSGSAITCSSKNKECEAFICNCDRNAAICFSKAPYNKAHKNLDTKKYCQS T31479 DRUGINFO D0OR2L Cholic Acid Approved T31479 DRUGINFO D0FL5V Clobetasol Approved T31479 DRUGINFO D00GOS Clocortolone Approved T31479 DRUGINFO D0G7KJ Diflorasone Approved T31479 DRUGINFO D00FGR Miltefosine Approved T31479 DRUGINFO D0C0KP AllerB Phase 2b T31479 DRUGINFO D00XQO MANOALIDE Phase 2 T31479 DRUGINFO D03VYZ MRX-4 Phase 2 T31479 DRUGINFO D07RKO MRX-6 Phase 2 T31479 DRUGINFO D07LUJ URSOLIC ACID Phase 2 T31479 DRUGINFO D05GZD Rilapladib Phase 1 T31479 DRUGINFO D0L5UO Darapladib Discontinued in Phase 3 T31479 DRUGINFO D08VGT BMY-30129 Discontinued in Phase 2 T31479 DRUGINFO D03RNX EPC-K1 Discontinued in Phase 2 T31479 DRUGINFO D0D3KY SC-106 Discontinued in Phase 2 T31479 DRUGINFO D0MF3C WAY-123641 Discontinued in Phase 2 T31479 DRUGINFO D08YFD PF-05212372 Discontinued in Phase 1 T31479 DRUGINFO D09NBM SB-435495 Discontinued in Phase 1 T31479 DRUGINFO D07OGR YM-26734 Terminated T31479 DRUGINFO D06GOK 2-Methyl-2,4-Pentanediol Investigative T31479 DRUGINFO D0H1JX 3,9-dihydroxy-2,10-diprenylpterocap-6a-ene Investigative T31479 DRUGINFO D05SQA 4'-hydroxy-6,3',5'-triprenylisoflavonone Investigative T31479 DRUGINFO D0L3IQ ABYSSINONE V Investigative T31479 DRUGINFO D0F2ME Acetate Ion Investigative T31479 DRUGINFO D0HZ3Q AGN-190383 Investigative T31479 DRUGINFO D07LUR Alpha-D-Mannose Investigative T31479 DRUGINFO D0P0DA BM-162115 Investigative T31479 DRUGINFO D0T3CM BOLINAQUINONE Investigative T31479 DRUGINFO D02IVU CACOSPONGIONOLIDE Investigative T31479 DRUGINFO D0B9VV CACOSPONGIONOLIDE B Investigative T31479 DRUGINFO D03BAB Cacospongionolide E Investigative T31479 DRUGINFO D0V4NV folipastatin Investigative T31479 DRUGINFO D02FVV HELENAQUINONE Investigative T31479 DRUGINFO D0H2RZ Heptanoic Acid Investigative T31479 DRUGINFO D0O0ZU Hexane-1,6-Diol Investigative T31479 DRUGINFO D0YD6H Hyrtiosulawesine Investigative T31479 DRUGINFO D0SS5D Lpc-Ether Investigative T31479 DRUGINFO D0TN4X LY178002 Investigative T31479 DRUGINFO D00XNF LY256548 Investigative T31479 DRUGINFO D0O2DQ Mepacrine Investigative T31479 DRUGINFO D0G4CI methylglyoxal Investigative T31479 DRUGINFO D06YGT N-Tridecanoic Acid Investigative T31479 DRUGINFO D07IRQ P-Anisic Acid Investigative T31479 DRUGINFO D05DUX Petrosaspongiolide M Investigative T31479 DRUGINFO D02COQ Petrosaspongiolide P Investigative T31479 DRUGINFO D06PLG SB-203347 Investigative T31479 DRUGINFO D03IDX WA-8242-A1 Investigative T31479 KEGGPATH hsa00564:Glycerophospholipid metabolism T31479 KEGGPATH hsa00565:Ether lipid metabolism T31479 KEGGPATH hsa00590:Arachidonic acid metabolism T31479 KEGGPATH hsa00591:Linoleic acid metabolism T31479 KEGGPATH hsa00592:alpha-Linolenic acid metabolism T31479 KEGGPATH hsa01100:Metabolic pathways T31479 KEGGPATH hsa04014:Ras signaling pathway T31479 KEGGPATH hsa04270:Vascular smooth muscle contraction T31479 KEGGPATH hsa04972:Pancreatic secretion T31479 KEGGPATH hsa04975:Fat digestion and absorption T31479 WIKIPATH WP2740:Glycerophospholipid biosynthesis T31479 REACPATH R-HSA-1482788:Acyl chain remodelling of PC T31479 REACPATH R-HSA-1482839:Acyl chain remodelling of PE T31479 REACPATH R-HSA-1482922:Acyl chain remodelling of PI T31479 INTEPATH fcer1pathway:Fc-epsilon receptor I signaling in mast cells T31479 BIOCPATH LIPASYN-PWY:Phospholipases T40016 TARGETID T40016 T40016 FORMERID TTDS00283 T40016 UNIPROID GCR_HUMAN T40016 TARGNAME Glucocorticoid receptor (NR3C1) T40016 GENENAME NR3C1 T40016 TARGTYPE Successful target T40016 SYNONYMS Nuclear receptor subfamily 3 group C member 1; GRL; GR T40016 FUNCTION Receptor for glucocorticoids (GC). Has a dual mode of action: as a transcription factor that binds to glucocorticoid response elements (GRE), both for nuclear and mitochondrial DNA, and as a modulator of other transcription factors. Affects inflammatory responses, cellular proliferation and differentiation in target tissues. Involved in chromatin remodeling. Plays a role in rapid mRNA degradation by binding to the 5' UTR of target mRNAs and interacting with PNRC2 in a ligand-dependent manner which recruits the RNA helicase UPF1 and the mRNA-decapping enzyme DCP1A, leading to RNA decay. Could act as a coactivator for STAT5-dependent transcription upon growth hormone (GH) stimulation and could reveal an essential role of hepatic GR in the control of body growth (By similarity). T40016 PDBSTRUC 6EL9; 6EL7; 6EL6; 6DXK; 6CFN T40016 BIOCLASS Nuclear hormone receptor T40016 SEQUENCE MDSKESLTPGREENPSSVLAQERGDVMDFYKTLRGGATVKVSASSPSLAVASQSDSKQRRLLVDFPKGSVSNAQQPDLSKAVSLSMGLYMGETETKVMGNDLGFPQQGQISLSSGETDLKLLEESIANLNRSTSVPENPKSSASTAVSAAPTEKEFPKTHSDVSSEQQHLKGQTGTNGGNVKLYTTDQSTFDILQDLEFSSGSPGKETNESPWRSDLLIDENCLLSPLAGEDDSFLLEGNSNEDCKPLILPDTKPKIKDNGDLVLSSPSNVTLPQVKTEKEDFIELCTPGVIKQEKLGTVYCQASFPGANIIGNKMSAISVHGVSTSGGQMYHYDMNTASLSQQQDQKPIFNVIPPIPVGSENWNRCQGSGDDNLTSLGTLNFPGRTVFSNGYSSPSMRPDVSSPPSSSSTATTGPPPKLCLVCSDEASGCHYGVLTCGSCKVFFKRAVEGQHNYLCAGRNDCIIDKIRRKNCPACRYRKCLQAGMNLEARKTKKKIKGIQQATTGVSQETSENPGNKTIVPATLPQLTPTLVSLLEVIEPEVLYAGYDSSVPDSTWRIMTTLNMLGGRQVIAAVKWAKAIPGFRNLHLDDQMTLLQYSWMFLMAFALGWRSYRQSSANLLCFAPDLIINEQRMTLPCMYDQCKHMLYVSSELHRLQVSYEEYLCMKTLLLLSSVPKDGLKSQELFDEIRMTYIKELGKAIVKREGNSSQNWQRFYQLTKLLDSMHEVVENLLNYCFQTFLDKTMSIEFPEMLAEIITNQIPKYSNGNIKKLLFHQK T40016 DRUGINFO D0CW1P Betamethasone Approved T40016 DRUGINFO D06CWH Betamethasone Benzoate Approved T40016 DRUGINFO D03SXE Betamethasone Valerate Approved T40016 DRUGINFO D0Y7IU Budesonide Approved T40016 DRUGINFO D09WYX Deflazacort Approved T40016 DRUGINFO D0IT2G Dexamethasone Approved T40016 DRUGINFO D0NA8U Dexamethasone sodium phosphate Approved T40016 DRUGINFO D0FM2P Flunisolide Approved T40016 DRUGINFO D02QJH Fluocinolone Acetonide Approved T40016 DRUGINFO D0P0HT Fluorometholone Approved T40016 DRUGINFO D0LC6K Fluticasone Approved T40016 DRUGINFO D0Y7JU GW685698X Approved T40016 DRUGINFO D05RXI Hydrocortamate Approved T40016 DRUGINFO D0KR5B Hydrocortisone Approved T40016 DRUGINFO D0I5DS Meprednisone Approved T40016 DRUGINFO D08PIQ Methylprednisolone Approved T40016 DRUGINFO D0Z4EI Mifepristone Approved T40016 DRUGINFO D03HYX Mometasone Approved T40016 DRUGINFO D0D1SG Prednisolone Approved T40016 DRUGINFO D0IL7L Prednisone Approved T40016 DRUGINFO D03BLF Triamcinolone Approved T40016 DRUGINFO D03WNG CORT-125134 Phase 3 T40016 DRUGINFO D00TPW FST-201 Phase 3 T40016 DRUGINFO D01IUS Mapracorat Phase 3 T40016 DRUGINFO D0L3HU BAY 86-5044 Phase 2 T40016 DRUGINFO D0I1DZ DE-110 Phase 2 T40016 DRUGINFO D0OR8W ETIPREDNOL DICLOACETATE Phase 2 T40016 DRUGINFO D0M8VL GW-870086-X Phase 2 T40016 DRUGINFO D06XSB GW-870086-X Phase 2 T40016 DRUGINFO D01HYQ IONIS-GCCRRX Phase 2 T40016 DRUGINFO D05RXW LAS-41002 Phase 2 T40016 DRUGINFO D0E2WF ORG 34517/34850 Phase 2 T40016 DRUGINFO D05MDJ ORG-34517 Phase 2 T40016 DRUGINFO D0T5TU TPI-1020 Phase 2 T40016 DRUGINFO D0J6UV IBI-20089 Phase 1 T40016 DRUGINFO D0OS8C NCX-1015 Phase 1 T40016 DRUGINFO D09UFV AZD-5423 Discontinued in Phase 2 T40016 DRUGINFO D01NUG GSK870086 Discontinued in Phase 2 T40016 DRUGINFO D03RCP NM-135 Discontinued in Phase 2 T40016 DRUGINFO D0G2CQ WC-3027 Discontinued in Phase 2 T40016 DRUGINFO D03CHE PF-251802 Discontinued in Phase 1 T40016 DRUGINFO D0I7EX Org-34116 Terminated T40016 DRUGINFO D02UVH B-Octylglucoside Investigative T40016 DRUGINFO D0O0ZU Hexane-1,6-Diol Investigative T40016 KEGGPATH hsa04080:Neuroactive ligand-receptor interaction T40016 WIKIPATH WP170:Nuclear Receptors T40016 WIKIPATH WP1797:Circadian Clock T40016 WIKIPATH WP236:Adipogenesis T40016 WIKIPATH WP2840:Hair Follicle Development: Cytodifferentiation (Part 3 of 3) T40016 WIKIPATH WP2853:Endoderm Differentiation T40016 WIKIPATH WP2882:Nuclear Receptors Meta-Pathway T40016 WIKIPATH WP706:SIDS Susceptibility Pathways T40016 WIKIPATH WP734:Serotonin Receptor 4/6/7 and NR3C Signaling T40016 REACPATH R-HSA-1368108:BMAL1:CLOCK,NPAS2 activates circadian gene expression T40016 NET_PATH NetPath_11:TCR Signaling Pathway T40016 NET_PATH NetPath_14:IL2 Signaling Pathway T40016 INTEPATH ap1_pathway:AP-1 transcription factor network T40016 INTEPATH ar_tf_pathway:Regulation of Androgen receptor activity T40016 INTEPATH hdac_classii_pathway:Signaling events mediated by HDAC Class II T40016 INTEPATH hnf3bpathway:FOXA2 and FOXA3 transcription factor networks T40016 INTEPATH reg_gr_pathway:Glucocorticoid receptor regulatory network T40016 INTEPATH smad2_3nuclearpathway:Regulation of nuclear SMAD2/3 signaling T30081 TARGETID T30081 T30081 FORMERID TTDR00500 T30081 UNIPROID KITH_HUMAN T30081 TARGNAME Thymidine kinase 1 (TK1) T30081 GENENAME TK1 T30081 TARGTYPE Successful target T30081 SYNONYMS Thymidine kinase, cytosolic T30081 FUNCTION cytosol, identical protein binding, thymidine kinase activity, zinc ion binding, DNA metabolic process, nucleobase-containing compound metabolic process, protein homotetramerization, pyrimidine nucleoside salvage, thymidine metabolic process T30081 PDBSTRUC 2WVJ; 2ORV; 1XBT; 1W4R T30081 BIOCLASS Kinase T30081 ECNUMBER EC 2.7.1.21 T30081 SEQUENCE MSCINLPTVLPGSPSKTRGQIQVILGPMFSGKSTELMRRVRRFQIAQYKCLVIKYAKDTRYSSSFCTHDRNTMEALPACLLRDVAQEALGVAVIGIDEGQFFPDIVEFCEAMANAGKTVIVAALDGTFQRKPFGAILNLVPLAESVVKLTAVCMECFREAAYTKRLGTEKEVEVIGGADKYHSVCRLCYFKKASGQPAGPDNKENCPVPGKPGEAVAARKLFAPQQILQCSPAN T30081 DRUGINFO D0RX7Z DEOXYCYTIDINE Approved T30081 DRUGINFO D07BYK Penciclovir Approved T30081 DRUGINFO D08AMJ TK-DLI Preregistration T30081 DRUGINFO D04QPD FV-100 Phase 3 T30081 DRUGINFO D0X4NF Radiosensitizer gene therapy Phase 3 T30081 DRUGINFO D0Z9LP RP101 Phase 2/3 T30081 DRUGINFO D05RRA HQK-1004 Phase 2 T30081 DRUGINFO D02KBE Ad-OC-hsvTK/valacyclovir Phase 1 T30081 DRUGINFO D05GZD Rilapladib Phase 1 T30081 DRUGINFO D0FY1W Thymidine kinase-expressing adenovirus and ganciclovir suicide gene therapy Phase 1 T30081 DRUGINFO D0W8RX Sitimagene ceradenovec Discontinued in Phase 3 T30081 DRUGINFO D07OOW (South)-Methanocarba-Thymidine Investigative T30081 DRUGINFO D0I6UV 1-[(Z)-4-(triphenylmethoxy)-2-butenyl]thymine Investigative T30081 DRUGINFO D07GKK 1-[2-(2-triphenylmethoxyethoxy)ethyl]thymine Investigative T30081 DRUGINFO D00KWL 1-[5-(triphenylmethoxy)pentyl]thymine Investigative T30081 DRUGINFO D02CCD 1-[6-(triphenylmethoxy)hexyl]thymine Investigative T30081 DRUGINFO D0W8AD 1-[7-(triphenylmethoxy)heptyl]thymine Investigative T30081 DRUGINFO D09WYY 2'-deoxythymidine triphosphate Investigative T30081 DRUGINFO D00CVB 2'-Deoxyuridine Investigative T30081 DRUGINFO D0S4SQ 2-phenylamino-9-(4-hydroxy-butyl)-6-oxopurine Investigative T30081 DRUGINFO D0O7GD 3'-(1,2,3-Triazol-1-yl)-3'-deoxy-beta-D-thymidine Investigative T30081 DRUGINFO D01CUJ 3-(2-propyn-1-yl)thymidine Investigative T30081 DRUGINFO D0ST5A 5-Bromothienyldeoxyuridine Investigative T30081 DRUGINFO D04GXW 5-Iodo-2'-Deoxyuridine-5'-Monophosphate Investigative T30081 DRUGINFO D0C7YS 5-propyl-2'-deoxyuridine Investigative T30081 DRUGINFO D08AOD 6-(Dihydroxy-Isobutyl)-Thymine Investigative T30081 DRUGINFO D00CEO 6-Hydroxypropylthymine Investigative T30081 DRUGINFO D0G5VO 9-(4-Hydroxybutyl)-N2-Phenylguanine Investigative T30081 DRUGINFO D0X1HX 9-Hydroxypropyladenine, R-Isomer Investigative T30081 DRUGINFO D0R0EI 9-Hydroxypropyladenine, S-Isomer Investigative T30081 DRUGINFO D0PC2Y BVDU-MP Investigative T30081 DRUGINFO D01GLG Deoxythymidine Investigative T30081 DRUGINFO D0Y4MD Edoxudine Investigative T30081 DRUGINFO D01VKE ITdU Investigative T30081 DRUGINFO D0D7FB L-5-(bromovinyl)deoxyuridine Investigative T30081 DRUGINFO D0HO0W L-5-iodo-2'-deoxyuridine Investigative T30081 DRUGINFO D0YJ5W N2-(3-trifluoromethylphenyl)guanine Investigative T30081 DRUGINFO D04BBF P1-(5'-Adenosyl)P5-(5'-Thymidyl)Pentaphosphate Investigative T30081 DRUGINFO D0ZH0I Thymidine-5'-Phosphate Investigative T89041 TARGETID T89041 T89041 FORMERID TTDS00241 T89041 UNIPROID CP17A_HUMAN T89041 TARGNAME Steroid 17-alpha-monooxygenase (S17AH) T89041 GENENAME CYP17A1 T89041 TARGTYPE Successful target T89041 SYNONYMS Steroid 17-alpha-hydroxylase/17,20 lyase; P450c17; P450-C17; P450 17; CYPXVII; CYP17A1; CYP 17; 17 alpha-Hydroxylase/C17-20-lyase T89041 FUNCTION Conversion of pregnenolone and progesterone to their 17- alpha-hydroxylated products and subsequently to dehydroepiandrosterone (DHEA) and androstenedione. Catalyzes both the 17-alpha-hydroxylation and the 17,20-lyase reaction. Involved in sexual development during fetal life and at puberty. T89041 PDBSTRUC 6CIZ; 6CIR; 6CHI; 5UYS; 5IRV T89041 BIOCLASS Paired donor oxygen oxidoreductase T89041 ECNUMBER EC 1.14.14.19 T89041 SEQUENCE MWELVALLLLTLAYLFWPKRRCPGAKYPKSLLSLPLVGSLPFLPRHGHMHNNFFKLQKKYGPIYSVRMGTKTTVIVGHHQLAKEVLIKKGKDFSGRPQMATLDIASNNRKGIAFADSGAHWQLHRRLAMATFALFKDGDQKLEKIICQEISTLCDMLATHNGQSIDISFPVFVAVTNVISLICFNTSYKNGDPELNVIQNYNEGIIDNLSKDSLVDLVPWLKIFPNKTLEKLKSHVKIRNDLLNKILENYKEKFRSDSITNMLDTLMQAKMNSDNGNAGPDQDSELLSDNHILTTIGDIFGAGVETTTSVVKWTLAFLLHNPQVKKKLYEEIDQNVGFSRTPTISDRNRLLLLEATIREVLRLRPVAPMLIPHKANVDSSIGEFAVDKGTEVIINLWALHHNEKEWHQPDQFMPERFLNPAGTQLISPSVSYLPFGAGPRSCIGEILARQELFLIMAWLLQRFDLEVPDDGQLPSLEGIPKVVFLIDSFKVKIKVRQAWREAQAEGST T89041 DRUGINFO D02STN ABIRATERONE Approved T89041 DRUGINFO D06CNP Abiraterone acetate Approved T89041 DRUGINFO D0X3OI TAK-700 Phase 3 T89041 DRUGINFO D0Q9KR Seviteronel Phase 2 T89041 DRUGINFO D05RVA CFG920 Phase 1/2 T89041 DRUGINFO D01ARU DST-2970 Phase 1 T89041 DRUGINFO D00ZME 1-((9H-Fluoren-2-yl)ethyl)-1H-imidazole Investigative T89041 DRUGINFO D0MM7G 1-((9H-Fluoren-2-yl)methyl)-1H-imidazole Investigative T89041 DRUGINFO D0X1DV 1-(1-(4'-Ethylbiphenyl-4-yl)propyl)-1H-imidazole Investigative T89041 DRUGINFO D00IUN 1-(1-(4-thiophen-3-ylphenyl)ethyl)-1H-imidazole Investigative T89041 DRUGINFO D0B9XL 1-(1-(4-thiophen-3-yl-phenyl)propyl)-1Himidazole Investigative T89041 DRUGINFO D0RI7T 1-(1-(Biphenyl-4-yl)allyl)-1H-imidazole Investigative T89041 DRUGINFO D05LXA 1-(1-Biphenyl-4-yl-2-methyl-propyl)-1H-imidazole Investigative T89041 DRUGINFO D0M8JE 1-(1-Biphenyl-4-yl-2-phenyl-ethyl)-1H-imidazole Investigative T89041 DRUGINFO D0RD3C 1-(1-Biphenyl-4-yl-3-methyl-butyl)-1H-imidazole Investigative T89041 DRUGINFO D0SU0Y 1-(1-Biphenyl-4-yl-butyl)-1H-imidazole Investigative T89041 DRUGINFO D08YCD 1-(1-Biphenyl-4-yl-ethyl)-1H-imidazole Investigative T89041 DRUGINFO D0Q1LG 1-(1-Biphenyl-4-yl-pentyl)-1H-imidazole Investigative T89041 DRUGINFO D09GEH 1-(1-Biphenyl-4-yl-propyl)-1H-imidazole Investigative T89041 DRUGINFO D00GIK 1-(3-(4-chlorophenyl)propyl)-1H-imidazole Investigative T89041 DRUGINFO D0D0DR 1-(3-(4-fluorophenyl)propyl)-1H-imidazole Investigative T89041 DRUGINFO D0AL3G 1-(3,4-dichlorobenzyl)-1H-imidazole Investigative T89041 DRUGINFO D0X4XX 1-(3,4-difluorobenzyl)-1H-imidazole Investigative T89041 DRUGINFO D08OHU 1-(3,5-bis(trifluoromethyl)benzyl)-1H-imidazole Investigative T89041 DRUGINFO D00GIW 1-(3,5-dibromobenzyl)-1H-imidazole Investigative T89041 DRUGINFO D07ORY 1-(3,5-dichlorobenzyl)-1H-imidazole Investigative T89041 DRUGINFO D02HTG 1-(3,5-difluorobenzyl)-1H-imidazole Investigative T89041 DRUGINFO D09TTR 1-(3-phenylpropyl)-1H-imidazole Investigative T89041 DRUGINFO D03VRC 1-(4-Bromobenzyl)-1H-imidazole Investigative T89041 DRUGINFO D0P8PG 1-(4-bromophenethyl)-1H-imidazole Investigative T89041 DRUGINFO D01JZO 1-(4-chlorobenzyl)-1H-imidazole Investigative T89041 DRUGINFO D0T3BL 1-(4-chlorophenethyl)-1H-imidazole Investigative T89041 DRUGINFO D05QPR 1-(4-fluorobenzyl)-1H-imidazole Investigative T89041 DRUGINFO D0U6QM 1-(4-iodobenzyl)-1H-imidazole Investigative T89041 DRUGINFO D0N5GZ 1-(4-methyl-benzyl)-1H-imidazole Investigative T89041 DRUGINFO D0S0EP 1-(4-nitrobenzyl)-1H-imidazole Investigative T89041 DRUGINFO D0L6HY 1-(Bis-biphenyl-4-yl-methyl)-1H-imidazole Investigative T89041 DRUGINFO D06FHE 1-Ethyl-5-(imidazol-1-yl-phenyl-methyl)-1H-indole Investigative T89041 DRUGINFO D07CTI 1-Imidazol-1-ylmethyl-4-nitro-xanthen-9-one Investigative T89041 DRUGINFO D01SZX 1-Imidazol-1-ylmethylxanthen-9-one Investigative T89041 DRUGINFO D0U5GF 2-(1-Imidazol-1-yl-ethyl)-9H-carbazole Investigative T89041 DRUGINFO D05VLU 2,3,4,5-Tetrafluoro-6-pentafluorophenylazo-phenol Investigative T89041 DRUGINFO D07ZNR 2,3,5,6-Tetrafluoro-4-pentafluorophenylazo-phenol Investigative T89041 DRUGINFO D04ISG 3-(1-Chloro-7-methoxy-naphthalen-2-yl)-pyridine Investigative T89041 DRUGINFO D0MA9G 3-(1-ethyl-3,4-dihydronaphthalen-2-yl)-pyridine Investigative T89041 DRUGINFO D0K5KG 3-(1-methyl-3,4-dihydronaphthalen-2-yl)-pyridine Investigative T89041 DRUGINFO D0R0TE 3-(6-Ethoxy-naphthalen-2-yl)-pyridine Investigative T89041 DRUGINFO D0NX0M 3-(6-methoxy-3,4-dihydronaphthalen-2-yl)pyridine Investigative T89041 DRUGINFO D0N1PQ 3-(6-methoxynaphthalen-2-yl)pyridine Investigative T89041 DRUGINFO D06AKB 3-[(4'-Hydroxybiphenyl-4-yl)methyl]pyridine Investigative T89041 DRUGINFO D0L1JF 3-[4-Fluoro-indan-(1Z)-ylidenemethyl]-pyridine Investigative T89041 DRUGINFO D0J4VA 3-fluoro-4'-(1-(pyridin-4-yl)propyl)biphenyl-4-ol Investigative T89041 DRUGINFO D0Q0BK 3-Fluoro-4'-(pyridin-4-ylmethyl)biphenyl-4-ol Investigative T89041 DRUGINFO D09HEA 4-((1H-imidazol-1-yl)methyl)benzonitrile Investigative T89041 DRUGINFO D0QW7W 4-((1H-imidazol-1-yl)methyl)phenol Investigative T89041 DRUGINFO D09VQZ 4-((3',4'-Difluorobiphenyl-4-yl)methyl)pyridine Investigative T89041 DRUGINFO D0U6JI 4'-(1-(pyridin-4-yl)propyl)biphenyl-3-ol Investigative T89041 DRUGINFO D00YHD 4'-(2-methyl-1-(pyridin-4-yl)propyl)biphenyl-3-ol Investigative T89041 DRUGINFO D0LJ9D 4-(4-(thiophen-2-yl)benzyl)pyridine Investigative T89041 DRUGINFO D0Z3GX 4-(4-(thiophen-3-yl)benzyl)pyridine Investigative T89041 DRUGINFO D00DSE 4-(4'-Fluoro-biphenyl-4-ylmethyl)pyridine Investigative T89041 DRUGINFO D02BXS 4'-(Pyridin-4-ylmethyl)biphenyl-3,4-diamine Investigative T89041 DRUGINFO D01REI 4'-(Pyridin-4-ylmethyl)biphenyl-3,4-diol Investigative T89041 DRUGINFO D0WN9P 4'-(Pyridin-4-ylmethyl)biphenyl-3-amine Investigative T89041 DRUGINFO D0Y5KX 4'-(Pyridin-4-ylmethyl)biphenyl-4-amine Investigative T89041 DRUGINFO D0P5CT 4'-(Pyridin-4-ylmethyl)biphenyl-4-carboxamide Investigative T89041 DRUGINFO D0I1YH 4-[(3'-Hydroxybiphenyl-4-yl)methyl]pyridine Investigative T89041 DRUGINFO D03EXD 4-[(4'-Hydroxybiphenyl-4-yl)methyl]pyridine Investigative T89041 DRUGINFO D0T1CH 4-[1-(4'-Methoxybiphenyl-4-yl)propyl]pyridine Investigative T89041 DRUGINFO D05PKT 4-[4-(6-methoxynaphthalen-2-yl)benzyl]pyridine Investigative T89041 DRUGINFO D09VPA 4-[5-Bromo-indan-(1E)-ylidenemethyl]-pyridine Investigative T89041 DRUGINFO D0D9FR 4-[5-Bromo-indan-(1Z)-ylidenemethyl]-pyridine Investigative T89041 DRUGINFO D0YD9J 4-[5-Chloro-indan-(1E)-ylidenemethyl]-pyridine Investigative T89041 DRUGINFO D0F5YU 4-[5-Chloro-indan-(1Z)-ylidenemethyl]-pyridine Investigative T89041 DRUGINFO D03MKT 4-[5-Fluoro-indan-(1E)-ylidenemethyl]-pyridine Investigative T89041 DRUGINFO D09HOE 4-[5-Fluoro-indan-(1Z)-ylidenemethyl]-pyridine Investigative T89041 DRUGINFO D07IQG 4-Bromo-1-imidazol-1-ylmethyl-xanthen-9-one Investigative T89041 DRUGINFO D02CSU 4-Indan-(1Z)-ylidenemethyl-pyridine Investigative T89041 DRUGINFO D04CFP 5-[4-(Pyridin-4-ylmethyl)phenyl]-1H-indole Investigative T89041 DRUGINFO D06HFV 5-[5-Fluoro-indan-(1E)-ylidenemethyl]-pyrimidine Investigative T89041 DRUGINFO D0LC7Z 6-(3-(pyridin-4-yl)phenyl)naphthalen-2-ol Investigative T89041 DRUGINFO D0N1GH 6-(pyridin-3-yl)-2-naphthonitrile Investigative T89041 DRUGINFO D07VGT 6-[4-(Pyridin-4-ylmethyl)phenyl]naphthalen-2-ol Investigative T89041 DRUGINFO D0E8DX 6-Pyridin-3-yl-3,4-dihydroquinoline-2(1H)-thione Investigative T89041 DRUGINFO D02ALK 6-Pyridin-3-yl-naphthalen-2-ol Investigative T89041 DRUGINFO D09GJI 7-(1-(1H-imidazol-1-yl)ethyl)-9H-fluoren-2-ol Investigative T89041 DRUGINFO D0M1YW ANG-3407 Investigative T89041 DRUGINFO D0GJ7J ISOCONAZOLE Investigative T89041 DRUGINFO D0E0ZS N-(4'-Isonicotinoylbiphenyl-3-yl)acetamide Investigative T89041 DRUGINFO D02ZQK N-3-(4-bromophenyl)propyl imidazole Investigative T89041 DRUGINFO D0N7CQ Rac-4'-(1-Imidazol-1-yl-propyl)-biphenyl-3,4-diol Investigative T89041 DRUGINFO D04SHY Rac-4'-(1-Imidazol-1-yl-propyl)-biphenyl-3,5-diol Investigative T89041 DRUGINFO D0Q1FX Rac-4'-(1-Imidazol-1-yl-propyl)-biphenyl-3-ol Investigative T89041 DRUGINFO D0SM4F Rac-4'-(1-Imidazol-1-yl-propyl)-biphenyl-4-ol Investigative T89041 DRUGINFO D03EDD VN/107-1 Investigative T89041 KEGGPATH hsa00140:Steroid hormone biosynthesis T89041 KEGGPATH hsa01100:Metabolic pathways T89041 KEGGPATH hsa04913:Ovarian steroidogenesis T89041 KEGGPATH hsa04917:Prolactin signaling pathway T89041 WIKIPATH WP1879:Phase 1 - Functionalization of compounds T89041 WIKIPATH WP2263:Prostate Cancer T89041 WIKIPATH WP237:Glucocorticoid & Mineralcorticoid Metabolism T89041 WIKIPATH WP2749:Metabolism of steroid hormones and vitamin D T89041 WIKIPATH WP43:Oxidation by Cytochrome P450 T89041 WIKIPATH WP496:Steroid Biosynthesis T89041 WIKIPATH WP702:Metapathway biotransformation T89041 WHIZPATH PW000045:Androgen and Estrogen Metabolism T89041 WHIZPATH PW000141:Steroidogenesis T89041 REACPATH R-HSA-193048:Androgen biosynthesis T89041 REACPATH R-HSA-194002:Glucocorticoid biosynthesis T89041 REACPATH R-HSA-211976:Endogenous sterols T89041 BIOCPATH PWY66-378:Androgen biosynthesis T89041 BIOCPATH PWY66-381:Glucocorticoid biosynthesis T89041 BIOCPATH PWY-7305:Superpathway of steroid hormone biosynthesis T47107 TARGETID T47107 T47107 FORMERID TTDC00015 T47107 UNIPROID KPCG_HUMAN T47107 TARGNAME Protein kinase C gamma (PRKCG) T47107 GENENAME PRKCG T47107 TARGTYPE Successful target T47107 SYNONYMS PRKCG; PKCG; PKC-gamma T47107 FUNCTION Calcium-activated, phospholipid-and diacylglycerol (DAG)-dependent serine/threonine-protein kinase that plays diverse roles in neuronal cells and eye tissues, such as regulation of the neuronal receptors GRIA4/GLUR4 and GRIN1/NMDAR1, modulation of receptors and neuronal functions related to sensitivity to opiates, pain and alcohol, mediation of synaptic function and cell survival after ischemia, and inhibition of gap junction activity after oxidative stress. Binds and phosphorylates GRIA4/GLUR4 glutamate receptor and regulates its function by increasing plasma membrane-associated GRIA4 expression. In primary cerebellar neurons treated with the agonist 3,5-dihyidroxyphenylglycine, functions downstream of the metabotropic glutamate receptor GRM5/MGLUR5 and phosphorylates GRIN1/NMDAR1 receptor which plays a key role in synaptic plasticity, synaptogenesis, excitotoxicity, memory acquisition and learning. May be involved in the regulation of hippocampal long-term potentiation (LTP), but may be not necessary for the process of synaptic plasticity. May be involved in desensitization of mu-type opioid receptor-mediated G-protein activation in the spinal cord, and may be critical for the development and/or maintenance ofmorphine-induced reinforcing effects in the limbic forebrain. May modulate the functionality of mu-type-opioid receptors by participating in a signaling pathway which leads to the phosphorylation anddegradation of opioid receptors. May also contributes to chronic morphine-induced changes in nociceptive processing. Plays a role in neuropathic pain mechanisms and contributes to the maintenance of the allodynia pain produced by peripheral inflammation. Plays an important role in initial sensitivity and tolerance to ethanol, by mediating the behavioral effects of ethanol as well as the effects of this drug on the GABA(A) receptors. During and after cerebral ischemia modulate neurotransmission and cell survival in synaptic membranes, and is involved in insulin-induced inhibition of necrosis, an important mechanism for minimizing ischemic injury. Required for the elimination of multiple climbing fibers during innervation of Purkinje cells in developing cerebellum. Is activated in lens epithelial cells upon hydrogen peroxide treatment, and phosphorylates connexin-43 (GJA1/CX43), resulting in disassembly of GJA1 gap junction plaques and inhibition of gap junction activity which could provide a protective effect against oxidative stress. Phosphorylates p53/TP53 and promotes p53/TP53-dependent apoptosis in response to DNA damage. Involved in the phase resetting of the cerebral cortex circadian clock during temporally restricted feeding. Stabilizes the core clock component ARNTL/BMAL1 by interfering with its ubiquitination, thus suppressing its degradation, resultingin phase resetting of the cerebral cortex clock. T47107 PDBSTRUC 2UZP; 2.00E+73 T47107 BIOCLASS Kinase T47107 ECNUMBER EC 2.7.11.13 T47107 SEQUENCE MAGLGPGVGDSEGGPRPLFCRKGALRQKVVHEVKSHKFTARFFKQPTFCSHCTDFIWGIGKQGLQCQVCSFVVHRRCHEFVTFECPGAGKGPQTDDPRNKHKFRLHSYSSPTFCDHCGSLLYGLVHQGMKCSCCEMNVHRRCVRSVPSLCGVDHTERRGRLQLEIRAPTADEIHVTVGEARNLIPMDPNGLSDPYVKLKLIPDPRNLTKQKTRTVKATLNPVWNETFVFNLKPGDVERRLSVEVWDWDRTSRNDFMGAMSFGVSELLKAPVDGWYKLLNQEEGEYYNVPVADADNCSLLQKFEACNYPLELYERVRMGPSSSPIPSPSPSPTDPKRCFFGASPGRLHISDFSFLMVLGKGSFGKVMLAERRGSDELYAIKILKKDVIVQDDDVDCTLVEKRVLALGGRGPGGRPHFLTQLHSTFQTPDRLYFVMEYVTGGDLMYHIQQLGKFKEPHAAFYAAEIAIGLFFLHNQGIIYRDLKLDNVMLDAEGHIKITDFGMCKENVFPGTTTRTFCGTPDYIAPEIIAYQPYGKSVDWWSFGVLLYEMLAGQPPFDGEDEEELFQAIMEQTVTYPKSLSREAVAICKGFLTKHPGKRLGSGPDGEPTIRAHGFFRWIDWERLERLEIPPPFRPRPCGRSGENFDKFFTRAAPALTPPDRLVLASIDQADFQGFTYVNPDFVHPDARSPTSPVPVPVM T47107 DRUGINFO D07NVU Midostaurin Approved T47107 DRUGINFO D0R2TM BALANOL Terminated T47107 DRUGINFO D0X0HN LY-317644 Terminated T47107 DRUGINFO D0R5ZR RO-320432 Terminated T47107 DRUGINFO D0L1YA (-)-Cercosporamide Investigative T47107 DRUGINFO D00TWA [2,2':5',2'']Terthiophen-4-yl-methanol Investigative T47107 DRUGINFO D05LRV [2,2':5',2'']Terthiophene-4,5''-dicarbaldehyde Investigative T47107 DRUGINFO D0D3MR [2,2':5',2'']Terthiophene-4-carbaldehyde Investigative T47107 DRUGINFO D02QME 2-(4-Hydroxy-phenyl)-3,3-diphenyl-acrylonitrile Investigative T47107 DRUGINFO D0S9UK 2,3,3-Triphenyl-acrylonitrile Investigative T47107 DRUGINFO D09XIE 3-(4-Hydroxy-phenyl)-2,3-diphenyl-acrylonitrile Investigative T47107 DRUGINFO D0EK0G 3-(4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione Investigative T47107 DRUGINFO D06AOY 3-(indole-3-yl)-4-phenyl-1H-pyrrole-2,5-dione Investigative T47107 DRUGINFO D0T0UH 3,3-Bis-(4-hydroxy-phenyl)-2-phenyl-acrylonitrile Investigative T47107 DRUGINFO D0A8MN 3,3-Bis-(4-methoxy-phenyl)-2-phenyl-acrylonitrile Investigative T47107 DRUGINFO D00NYT 3,4-di-(4-methoxyphenyl)-1H-pyrrole-2,5-dione Investigative T47107 DRUGINFO D0C3WY 3,4-diphenyl-1H-pyrrole-2,5-dione Investigative T47107 DRUGINFO D02PUV 4-[1-(4-hydroxyphenyl)-3-methyl-1-butenyl]phenol Investigative T47107 DRUGINFO D0Q3GQ 4-cycloheptyliden(4-hydroxyphenyl)methylphenol Investigative T47107 DRUGINFO D0V9SW 4-cyclohexyliden(4-hydroxyphenyl)methylphenol Investigative T47107 DRUGINFO D04OHM 4-cyclopentyliden(4-hydroxyphenyl)methylphenol Investigative T47107 DRUGINFO D04AXH 8-Octyl-benzolactam-V9 Investigative T47107 DRUGINFO D0TO6S Bisindolylmaleimide-I Investigative T47107 DRUGINFO D06TLL Go 6983 Investigative T47107 DRUGINFO D06ZCX LY-326449 Investigative T47107 DRUGINFO D08GFG Monoctanoin component C Investigative T47107 DRUGINFO D04JNZ PROSTRATIN Investigative T47107 DRUGINFO D0L8HO RO-316233 Investigative T47107 DRUGINFO D09TSC Ro-32-0557 Investigative T47107 KEGGPATH hsa04010:MAPK signaling pathway T47107 KEGGPATH hsa04012:ErbB signaling pathway T47107 KEGGPATH hsa04014:Ras signaling pathway T47107 KEGGPATH hsa04015:Rap1 signaling pathway T47107 KEGGPATH hsa04020:Calcium signaling pathway T47107 KEGGPATH hsa04066:HIF-1 signaling pathway T47107 KEGGPATH hsa04070:Phosphatidylinositol signaling system T47107 KEGGPATH hsa04071:Sphingolipid signaling pathway T47107 KEGGPATH hsa04150:mTOR signaling pathway T47107 KEGGPATH hsa04270:Vascular smooth muscle contraction T47107 KEGGPATH hsa04310:Wnt signaling pathway T47107 KEGGPATH hsa04370:VEGF signaling pathway T47107 KEGGPATH hsa04510:Focal adhesion T47107 KEGGPATH hsa04530:Tight junction T47107 KEGGPATH hsa04540:Gap junction T47107 KEGGPATH hsa04650:Natural killer cell mediated cytotoxicity T47107 KEGGPATH hsa04666:Fc gamma R-mediated phagocytosis T47107 KEGGPATH hsa04670:Leukocyte transendothelial migration T47107 KEGGPATH hsa04713:Circadian entrainment T47107 KEGGPATH hsa04720:Long-term potentiation T47107 KEGGPATH hsa04723:Retrograde endocannabinoid signaling T47107 KEGGPATH hsa04724:Glutamatergic synapse T47107 KEGGPATH hsa04725:Cholinergic synapse T47107 KEGGPATH hsa04726:Serotonergic synapse T47107 KEGGPATH hsa04727:GABAergic synapse T47107 KEGGPATH hsa04728:Dopaminergic synapse T47107 KEGGPATH hsa04730:Long-term depression T47107 KEGGPATH hsa04750:Inflammatory mediator regulation of TRP channels T47107 KEGGPATH hsa04911:Insulin secretion T47107 KEGGPATH hsa04916:Melanogenesis T47107 KEGGPATH hsa04918:Thyroid hormone synthesis T47107 KEGGPATH hsa04919:Thyroid hormone signaling pathway T47107 KEGGPATH hsa04921:Oxytocin signaling pathway T47107 KEGGPATH hsa04960:Aldosterone-regulated sodium reabsorption T47107 KEGGPATH hsa04961:Endocrine and other factor-regulated calcium reabsorption T47107 KEGGPATH hsa04970:Salivary secretion T47107 KEGGPATH hsa04971:Gastric acid secretion T47107 KEGGPATH hsa04972:Pancreatic secretion T47107 KEGGPATH hsa05031:Amphetamine addiction T47107 KEGGPATH hsa05032:Morphine addiction T47107 KEGGPATH hsa05110:Vibrio cholerae infection T47107 KEGGPATH hsa05143:African trypanosomiasis T47107 KEGGPATH hsa05146:Amoebiasis T47107 KEGGPATH hsa05161:Hepatitis B T47107 KEGGPATH hsa05200:Pathways in cancer T47107 KEGGPATH hsa05205:Proteoglycans in cancer T47107 KEGGPATH hsa05206:MicroRNAs in cancer T47107 KEGGPATH hsa05214:Glioma T47107 KEGGPATH hsa05223:Non-small cell lung cancer T47107 KEGGPATH hsa05231:Choline metabolism in cancer T47107 WIKIPATH WP1903:Response to elevated platelet cytosolic Ca2+ T47107 WIKIPATH WP1978:Opioid Signalling T47107 WIKIPATH WP2012:miRs in Muscle Cell Differentiation T47107 WIKIPATH WP2261:Signaling Pathways in Glioblastoma T47107 WIKIPATH WP2688:DAG and IP3 signaling T47107 WIKIPATH WP289:Myometrial Relaxation and Contraction Pathways T47107 WIKIPATH WP35:G Protein Signaling Pathways T47107 WIKIPATH WP363:Wnt Signaling Pathway Netpath T47107 WIKIPATH WP382:MAPK Signaling Pathway T47107 WIKIPATH WP399:Wnt Signaling Pathway and Pluripotency T47107 WIKIPATH WP428:Wnt Signaling Pathway T47107 WIKIPATH WP536:Calcium Regulation in the Cardiac Cell T47107 REACPATH R-HSA-111933:Calmodulin induced events T47107 REACPATH R-HSA-114516:Disinhibition of SNARE formation T47107 REACPATH R-HSA-416993:Trafficking of GluR2-containing AMPA receptors T47107 REACPATH R-HSA-418597:G alpha (z) signalling events T47107 REACPATH R-HSA-5099900:WNT5A-dependent internalization of FZD4 T47107 REACPATH R-HSA-76005:Response to elevated platelet cytosolic Ca2+ T47107 INTEPATH endothelinpathway:Endothelins T47107 INTEPATH il8cxcr1_pathway:IL8- and CXCR1-mediated signaling events T47107 INTEPATH il8cxcr2_pathway:IL8- and CXCR2-mediated signaling events T47107 INTEPATH nfat_3pathway:Role of Calcineurin-dependent NFAT signaling in lymphocytes T47107 INTEPATH retinoic_acid_pathway:Retinoic acid receptors-mediated signaling T47107 INTEPATH thrombin_par1_pathway:PAR1-mediated thrombin signaling events T47107 INTEPATH txa2pathway:Thromboxane A2 receptor signaling T47107 PANTPATH P00002:Alpha adrenergic receptor signaling pathway T47107 PANTPATH P00003:Alzheimer disease-amyloid secretase pathway T47107 PANTPATH P00005:Angiogenesis T47107 PANTPATH P00006:Apoptosis signaling pathway T47107 PANTPATH P00018:EGF receptor signaling pathway T47107 PANTPATH P00019:Endothelin signaling pathway T47107 PANTPATH P00021:FGF signaling pathway T47107 PANTPATH P00027:Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway T47107 PANTPATH P00042:Muscarinic acetylcholine receptor 1 and 3 signaling pathway T47107 PANTPATH P00056:VEGF signaling pathway T47107 PANTPATH P00057:Wnt signaling pathway T47107 PANTPATH P04374:5HT2 type receptor mediated signaling pathway T47107 PANTPATH P04385:Histamine H1 receptor mediated signaling pathway T47107 PANTPATH P04391:Oxytocin receptor mediated signaling pathway T47107 PANTPATH P04394:Thyrotropin-releasing hormone receptor signaling pathway T17980 TARGETID T17980 T17980 FORMERID TTDS00406 T17980 UNIPROID FYN_HUMAN T17980 TARGNAME Fyn tyrosine protein kinase (FYN) T17980 GENENAME FYN T17980 TARGTYPE Successful target T17980 SYNONYMS Tyrosine-protein kinase Fyn; Src-like kinase; SLK; Proto-oncogene tyrosine-protein kinase Fyn; Proto-oncogene c-Fyn; Proto-oncogene Syn; Fyn p59-Fyn; Fyn Protooncogene Syn T17980 FUNCTION Inactive FYN is phosphorylated on its C-terminal tail within the catalytic domain. Following activation by PKA, the protein subsequently associates with PTK2/FAK1, allowing PTK2/FAK1 phosphorylation, activation and targeting to focal adhesions. Involved in the regulation of cell adhesion and motility through phosphorylation of CTNNB1 (beta-catenin) and CTNND1 (delta-catenin). Regulates cytoskeletal remodeling by phosphorylating several proteins including the actin regulator WAS and the microtubule-associated proteins MAP2 and MAPT. Promotes cell survival by phosphorylating AGAP2/PIKE-A and preventing its apoptotic cleavage. Participates in signal transduction pathways that regulate the integrity of the glomerular slit diaphragm (an essential part of the glomerular filter of the kidney) by phosphorylating several slit diaphragm components including NPHS1, KIRREL1 and TRPC6. Plays a role in neural processes by phosphorylating DPYSL2, a multifunctional adapter protein within the central nervous system, ARHGAP32, a regulator for Rho family GTPases implicated in various neural functions, and SNCA, a small pre-synaptic protein. Participates in the downstream signaling pathways that lead to T-cell differentiation and proliferation following T-cell receptor (TCR) stimulation. Phosphorylates PTK2B/PYK2 in response to T-cell receptor activation. Also participates in negative feedback regulation of TCR signaling through phosphorylation of PAG1, thereby promoting interaction between PAG1 and CSK and recruitment of CSK to lipid rafts. CSK maintains LCK and FYN in an inactive form. Promotes CD28-induced phosphorylation of VAV1. Non-receptor tyrosine-protein kinase that plays a role in many biological processes including regulation of cell growth and survival, cell adhesion, integrin-mediated signaling, cytoskeletal remodeling, cell motility, immune response and axon guidance. T17980 PDBSTRUC 6IPZ; 6IPY; 6EDF; 4ZNX; 4U1P T17980 BIOCLASS Kinase T17980 ECNUMBER EC 2.7.10.2 T17980 SEQUENCE MGCVQCKDKEATKLTEERDGSLNQSSGYRYGTDPTPQHYPSFGVTSIPNYNNFHAAGGQGLTVFGGVNSSSHTGTLRTRGGTGVTLFVALYDYEARTEDDLSFHKGEKFQILNSSEGDWWEARSLTTGETGYIPSNYVAPVDSIQAEEWYFGKLGRKDAERQLLSFGNPRGTFLIRESETTKGAYSLSIRDWDDMKGDHVKHYKIRKLDNGGYYITTRAQFETLQQLVQHYSERAAGLCCRLVVPCHKGMPRLTDLSVKTKDVWEIPRESLQLIKRLGNGQFGEVWMGTWNGNTKVAIKTLKPGTMSPESFLEEAQIMKKLKHDKLVQLYAVVSEEPIYIVTEYMNKGSLLDFLKDGEGRALKLPNLVDMAAQVAAGMAYIERMNYIHRDLRSANILVGNGLICKIADFGLARLIEDNEYTARQGAKFPIKWTAPEAALYGRFTIKSDVWSFGILLTELVTKGRVPYPGMNNREVLEQVERGYRMPCPQDCPISLHELMIHCWKKDPEERPTFEYLQSFLEDYFTATEPQYQPGENL T17980 DRUGINFO D0E6XR Dasatinib Approved T17980 DRUGINFO D0U3XL JNJ-26483327 Phase 1 T17980 DRUGINFO D0OD8N 1-Methoxy-2-[2-(2-Methoxy-Ethoxy]-Ethane Investigative T17980 DRUGINFO D09QBA CEP-5104 Investigative T17980 DRUGINFO D07IHM CEP-6331 Investigative T17980 DRUGINFO D0YZ7H JNJ-10198409 Investigative T17980 DRUGINFO D08RZB PMID15546730C2 Investigative T17980 DRUGINFO D09XIL Ro-4396686 Investigative T17980 KEGGPATH hsa04071:Sphingolipid signaling pathway T17980 KEGGPATH hsa04360:Axon guidance T17980 KEGGPATH hsa04380:Osteoclast differentiation T17980 KEGGPATH hsa04510:Focal adhesion T17980 KEGGPATH hsa04520:Adherens junction T17980 KEGGPATH hsa04611:Platelet activation T17980 KEGGPATH hsa04650:Natural killer cell mediated cytotoxicity T17980 KEGGPATH hsa04660:T cell receptor signaling pathway T17980 KEGGPATH hsa04664:Fc epsilon RI signaling pathway T17980 KEGGPATH hsa04725:Cholinergic synapse T17980 KEGGPATH hsa05020:Prion diseases T17980 KEGGPATH hsa05130:Pathogenic Escherichia coli infection T17980 KEGGPATH hsa05162:Measles T17980 KEGGPATH hsa05416:Viral myocarditis T17980 WIKIPATH WP1794:Cell surface interactions at the vascular wall T17980 WIKIPATH WP1799:Costimulation by the CD28 family T17980 WIKIPATH WP1826:GPVI-mediated activation cascade T17980 WIKIPATH WP185:Integrin-mediated Cell Adhesion T17980 WIKIPATH WP1866:NCAM signaling for neurite out-growth T17980 WIKIPATH WP1867:Nephrin interactions T17980 WIKIPATH WP1868:Netrin-1 signaling T17980 WIKIPATH WP1883:Platelet Adhesion to exposed collagen T17980 WIKIPATH WP1907:Semaphorin interactions T17980 WIKIPATH WP2034:Leptin signaling pathway T17980 WIKIPATH WP205:IL-7 Signaling Pathway T17980 WIKIPATH WP2203:TSLP Signaling Pathway T17980 WIKIPATH WP2272:Pathogenic Escherichia coli infection T17980 WIKIPATH WP23:B Cell Receptor Signaling Pathway T17980 WIKIPATH WP2332:Interleukin-11 Signaling Pathway T17980 WIKIPATH WP2380:BDNF signaling pathway T17980 WIKIPATH WP2572:Primary Focal Segmental Glomerulosclerosis FSGS T17980 WIKIPATH WP2583:T-Cell Receptor and Co-stimulatory Signaling T17980 WIKIPATH WP2653:PIP3 activates AKT signaling T17980 WIKIPATH WP2684:Host Interactions of HIV factors T17980 WIKIPATH WP2694:DAP12 interactions T17980 WIKIPATH WP2713:Signaling by SCF-KIT T17980 WIKIPATH WP2746:Signaling by the B Cell Receptor (BCR) T17980 WIKIPATH WP2759:Fc epsilon receptor (FCERI) signaling T17980 WIKIPATH WP2858:Ectoderm Differentiation T17980 WIKIPATH WP286:IL-3 Signaling Pathway T17980 WIKIPATH WP304:Kit receptor signaling pathway T17980 WIKIPATH WP49:IL-2 Signaling Pathway T17980 WIKIPATH WP585:Interferon type I signaling pathways T17980 WIKIPATH WP69:TCR Signaling Pathway T17980 WHIZPATH PW000453:Fc Epsilon Receptor I Signaling in Mast Cells T17980 REACPATH R-HSA-114604:GPVI-mediated activation cascade T17980 REACPATH R-HSA-1257604:PIP3 activates AKT signaling T17980 REACPATH R-HSA-1433559:Regulation of KIT signaling T17980 REACPATH R-HSA-202733:Cell surface interactions at the vascular wall T17980 REACPATH R-HSA-2029481:FCGR activation T17980 REACPATH R-HSA-210990:PECAM1 interactions T17980 REACPATH R-HSA-2219530:Constitutive Signaling by Aberrant PI3K in Cancer T17980 REACPATH R-HSA-2424491:DAP12 signaling T17980 REACPATH R-HSA-2682334:EPH-Ephrin signaling T17980 REACPATH R-HSA-2730905:Role of LAT2/NTAL/LAB on calcium mobilization T17980 REACPATH R-HSA-373753:Nephrin interactions T17980 REACPATH R-HSA-375165:NCAM signaling for neurite out-growth T17980 REACPATH R-HSA-389356:CD28 co-stimulation T17980 REACPATH R-HSA-389357:CD28 dependent PI3K/Akt signaling T17980 REACPATH R-HSA-389359:CD28 dependent Vav1 pathway T17980 REACPATH R-HSA-389513:CTLA4 inhibitory signaling T17980 REACPATH R-HSA-3928662:EPHB-mediated forward signaling T17980 REACPATH R-HSA-3928663:EPHA-mediated growth cone collapse T17980 REACPATH R-HSA-3928665:EPH-ephrin mediated repulsion of cells T17980 REACPATH R-HSA-399956:CRMPs in Sema3A signaling T17980 REACPATH R-HSA-418885:DCC mediated attractive signaling T17980 REACPATH R-HSA-418886:Netrin mediated repulsion signals T17980 REACPATH R-HSA-4420097:VEGFA-VEGFR2 Pathway T17980 REACPATH R-HSA-5621480:Dectin-2 family T17980 REACPATH R-HSA-5621575:CD209 (DC-SIGN) signaling T17980 REACPATH R-HSA-5673001:RAF/MAP kinase cascade T17980 REACPATH R-HSA-75892:Platelet Adhesion to exposed collagen T17980 REACPATH R-HSA-912631:Regulation of signaling by CBL T17980 REACPATH R-HSA-983695:Antigen activates B Cell Receptor (BCR) leading to generation of second messengers T17980 NET_PATH NetPath_14:IL2 Signaling Pathway T17980 NET_PATH NetPath_23:TSH Signaling Pathway T17980 NET_PATH NetPath_7:TGF_beta_Receptor Signaling Pathway T17980 INTEPATH ajdiss_2pathway:Posttranslational regulation of adherens junction stability and dissassembly T17980 INTEPATH alphasynuclein_pathway:Alpha-synuclein signaling T17980 INTEPATH amb2_neutrophils_pathway:amb2 Integrin signaling T17980 INTEPATH angiopoietinreceptor_pathway:Angiopoietin receptor Tie2-mediated signaling T17980 INTEPATH cd8tcrpathway:TCR signaling in naïve CD8+ T cells T17980 INTEPATH cxcr4_pathway:CXCR4-mediated signaling events T17980 INTEPATH ecadherin_keratinocyte_pathway:E-cadherin signaling in keratinocytes T17980 INTEPATH epha_fwdpathway:EPHA forward signaling T17980 INTEPATH ephrinarevpathway:Ephrin A reverse signaling T17980 INTEPATH ephrinbrevpathway:Ephrin B reverse signaling T17980 INTEPATH erbb4_pathway:ErbB4 signaling events T17980 INTEPATH fak_pathway:Signaling events mediated by focal adhesion kinase T17980 INTEPATH fcer1pathway:Fc-epsilon receptor I signaling in mast cells T17980 INTEPATH glypican_1pathway:Glypican 1 network T17980 INTEPATH il2_1pathway:IL2-mediated signaling events T17980 INTEPATH nephrin_neph1_pathway:Nephrin/Neph1 signaling in the kidney podocyte T17980 INTEPATH netrin_pathway:Netrin-mediated signaling events T17980 INTEPATH p38alphabetapathway:Regulation of p38-alpha and p38-beta T17980 INTEPATH pdgfrbpathway:PDGFR-beta signaling pathway T17980 INTEPATH pi3kcipathway:Class I PI3K signaling events T17980 INTEPATH ptp1bpathway:Signaling events mediated by PTP1B T17980 INTEPATH reelinpathway:Reelin signaling pathway T17980 INTEPATH syndecan_3_pathway:Syndecan-3-mediated signaling events T17980 INTEPATH tcr_pathway:TCR signaling in naïve CD4+ T cells T17980 INTEPATH txa2pathway:Thromboxane A2 receptor signaling T17980 INTEPATH vegfr1_2_pathway:Signaling events mediated by VEGFR1 and VEGFR2 T17980 PANTPATH P00007:Axon guidance mediated by semaphorins T17980 PANTPATH P00012:Cadherin signaling pathway T17980 PANTPATH P00034:Integrin signalling pathway T17980 PANTPATH P00049:Parkinson disease T27602 TARGETID T27602 T27602 FORMERID TTDS00282 T27602 UNIPROID TRY1_HUMAN T27602 TARGNAME Cationic trypsinogen (PRSS1) T27602 GENENAME PRSS1 T27602 TARGTYPE Successful target T27602 SYNONYMS Trypsin-1; Trypsin I; TRYP1; TRY1; TRP1; Serine protease 1; Beta-trypsin T27602 FUNCTION Has activity against the synthetic substrates Boc-Phe-Ser-Arg-Mec, Boc-Leu-Thr-Arg-Mec, Boc-Gln-Ala-Arg-Mec and Boc-Val-Pro-Arg-Mec. The single-chain form is more active than the two-chain form against all of these substrates. T27602 PDBSTRUC 4WXV; 4WWY; 2RA3; 1TRN; 1FXY T27602 BIOCLASS Peptidase T27602 ECNUMBER EC 3.4.21.4 T27602 SEQUENCE MNPLLILTFVAAALAAPFDDDDKIVGGYNCEENSVPYQVSLNSGYHFCGGSLINEQWVVSAGHCYKSRIQVRLGEHNIEVLEGNEQFINAAKIIRHPQYDRKTLNNDIMLIKLSSRAVINARVSTISLPTAPPATGTKCLISGWGNTASSGADYPDELQCLDAPVLSQAKCEASYPGKITSNMFCVGFLEGGKDSCQGDSGGPVVCNGQLQGVVSWGDGCAQKNKPGVYTKVYNYVKWIKNTIAANS T27602 DRUGINFO D0SH3I Bortezomib Approved T27602 DRUGINFO D01MUU MELAGATRAN Phase 3 T27602 DRUGINFO D0DF1R Ulinastatin Phase 3 T27602 DRUGINFO D04TEF Alpha-1 antitrypsin Phase 2 T27602 DRUGINFO D0B9EH Dermolastin Discontinued in Phase 2 T27602 DRUGINFO D05QMJ RWJ-56423 Discontinued in Phase 1 T27602 DRUGINFO D0GR2H BMY-44621 Terminated T27602 DRUGINFO D0CV7T Patamostat Terminated T27602 DRUGINFO D09TNA 1-(3-Amino-benzyl)-1H-indole-5-carboxamidine Investigative T27602 DRUGINFO D0EH1F 1-(3-Nitro-benzyl)-1H-indole-5-carboxamidine Investigative T27602 DRUGINFO D0F2YC 1,3-Dibenzyl-[1,3]diazetidine-2,4-dione Investigative T27602 DRUGINFO D05ICF 1,3-Di-p-tolyl-[1,3]diazetidine-2,4-dione Investigative T27602 DRUGINFO D0M2PE 1-Benzyl-1H-indole-5-carboxamidine Investigative T27602 DRUGINFO D08OLP 2-(2-Hydroxy-phenyl)-1H-indole-5-carboxamidine Investigative T27602 DRUGINFO D0J2SM 2-(2-Iodo-phenyl)-benzo[d][1,3]oxazin-4-one Investigative T27602 DRUGINFO D0Z7YI 2-Propionyl-1H-indole-6-carboxamidine Investigative T27602 DRUGINFO D0CT8A 4-(3,4-Diethoxy-benzylamino)-benzamidine Investigative T27602 DRUGINFO D02XPB 4-(4-Benzyloxy-3-methoxy-benzylamino)-benzamidine Investigative T27602 DRUGINFO D08OCL 4-(5-Nitro-indol-1-ylmethyl)-benzamidine Investigative T27602 DRUGINFO D0N1PW 4-Indol-1-ylmethyl-benzamidine Investigative T27602 DRUGINFO D00POF 6-Styryl-naphthalene-2-carboxamidine Investigative T27602 DRUGINFO D0S4MQ 8-Bromo-6-styryl-naphthalene-2-carboxamidine Investigative T27602 DRUGINFO D0K0GU 8-Furan-3-yl-6-styryl-naphthalene-2-carboxamidine Investigative T27602 DRUGINFO D05ABK ATF-HI-8 Investigative T27602 DRUGINFO D07SFI Benzamidine Investigative T27602 DRUGINFO D0O0GT CVS-2139 Investigative T27602 DRUGINFO D0C1TS CVS-2359 Investigative T27602 DRUGINFO D07IBU GR-133686 Investigative T27602 DRUGINFO D0Y5IQ Grassystatin a Investigative T27602 DRUGINFO D0JR9V JBP-1 Investigative T27602 DRUGINFO D02NHS L-375378 Investigative T27602 DRUGINFO D0RQ2T Macrocyclic tripeptide motif Investigative T27602 DRUGINFO D0M1LO Piperidine-1-carboxamidine Investigative T27602 DRUGINFO D0F9YV PMID3514912C9 Investigative T27602 DRUGINFO D08SMN POP-1 Investigative T27602 DRUGINFO D08SKX recAAT, PPL Therapeutics/Bayer Investigative T27602 DRUGINFO D09OBJ RWJ-50353 Investigative T27602 DRUGINFO D03ZUM Tert-butyloxy carbonyl-D-Phe-pro-Arg-H Investigative T27602 KEGGPATH hsa04080:Neuroactive ligand-receptor interaction T27602 KEGGPATH hsa04972:Pancreatic secretion T27602 KEGGPATH hsa04974:Protein digestion and absorption T27602 KEGGPATH hsa05164:Influenza A T27602 WIKIPATH WP2769:Activation of Matrix Metalloproteinases T27602 REACPATH R-HSA-1592389:Activation of Matrix Metalloproteinases T27602 REACPATH R-HSA-196741:Cobalamin (Cbl, vitamin B12) transport and metabolism T18477 TARGETID T18477 T18477 FORMERID TTDC00018 T18477 UNIPROID HS90A_HUMAN T18477 TARGNAME Heat shock protein 90 alpha (HSP90A) T18477 GENENAME HSP90AA1 T18477 TARGTYPE Successful target T18477 SYNONYMS Renal carcinoma antigen NY-REN-38; Lipopolysaccharide-associated protein 2; LPS-associated protein 2; LAP-2; Heat shock protein HSP 90-alpha; Heat shock 86 kDa; HSPCA; HSPC1; HSP90A; HSP86; HSP 86 T18477 FUNCTION Undergoes a functional cycle that is linked to its ATPase activity which is essential for its chaperone activity. This cycle probably induces conformational changes in the client proteins, thereby causing their activation. Interacts dynamically with various co-chaperones that modulate its substrate recognition, ATPase cycle and chaperone function. Engages with a range of client protein classes via its interaction with various co-chaperone proteins or complexes, that act as adapters, simultaneously able to interact with the specific client and the central chaperone itself. Recruitment of ATP and co-chaperone followed by client protein forms a functional chaperone. After the completion of the chaperoning process, properly folded client protein and co-chaperone leave HSP90 in an ADP-bound partially open conformation and finally, ADP is released from HSP90 which acquires an open conformation for the next cycle. Apart from its chaperone activity, it also plays a role in the regulation of the transcription machinery. HSP90 and its co-chaperones modulate transcription at least at three different levels. In the first place, they alter the steady-state levels of certain transcription factors in response to various physiological cues(). Second, they modulate the activity of certain epigenetic modifiers, such as histone deacetylases or DNA methyl transferases, and thereby respond to the change in the environment. Third, they participate in the eviction of histones from the promoter region of certain genes and thereby turn on gene expression. Binds bacterial lipopolysaccharide (LPS) and mediates LPS-induced inflammatory response, including TNF secretion by monocytes. Antagonizes STUB1-mediated inhibition of TGF-beta signaling via inhibition of STUB1-mediated SMAD3 ubiquitination and degradation. Molecular chaperone that promotes the maturation, structural maintenance and proper regulation of specific target proteins involved for instance in cell cycle control and signal transduction. T18477 PDBSTRUC 6GR5; 6GR4; 6GR3; 6GR1; 6GQU T18477 BIOCLASS Heat shock protein T18477 SEQUENCE MPEETQTQDQPMEEEEVETFAFQAEIAQLMSLIINTFYSNKEIFLRELISNSSDALDKIRYESLTDPSKLDSGKELHINLIPNKQDRTLTIVDTGIGMTKADLINNLGTIAKSGTKAFMEALQAGADISMIGQFGVGFYSAYLVAEKVTVITKHNDDEQYAWESSAGGSFTVRTDTGEPMGRGTKVILHLKEDQTEYLEERRIKEIVKKHSQFIGYPITLFVEKERDKEVSDDEAEEKEDKEEEKEKEEKESEDKPEIEDVGSDEEEEKKDGDKKKKKKIKEKYIDQEELNKTKPIWTRNPDDITNEEYGEFYKSLTNDWEDHLAVKHFSVEGQLEFRALLFVPRRAPFDLFENRKKKNNIKLYVRRVFIMDNCEELIPEYLNFIRGVVDSEDLPLNISREMLQQSKILKVIRKNLVKKCLELFTELAEDKENYKKFYEQFSKNIKLGIHEDSQNRKKLSELLRYYTSASGDEMVSLKDYCTRMKENQKHIYYITGETKDQVANSAFVERLRKHGLEVIYMIEPIDEYCVQQLKEFEGKTLVSVTKEGLELPEDEEEKKKQEEKKTKFENLCKIMKDILEKKVEKVVVSNRLVTSPCCIVTSTYGWTANMERIMKAQALRDNSTMGYMAAKKHLEINPDHSIIETLRQKAEADKNDKSVKDLVILLYETALLSSGFSLEDPQTHANRIYRMIKLGLGIDEDDPTADDTSAAVTEEMPPLEGDDDTSRMEEVD T18477 DRUGINFO D0G5UB Amlexanox Approved T18477 DRUGINFO D06NSS Cromoglicate Approved T18477 DRUGINFO D05HWN BIIB-021 Phase 2 T18477 DRUGINFO D0Y9PZ Efungumab Phase 2 T18477 DRUGINFO D08PYO KW-2478 Phase 2 T18477 DRUGINFO D05BYA NVP-AUY922 Phase 2 T18477 DRUGINFO D0SC2J Tanespimycin Phase 2 T18477 DRUGINFO D09XGB VER 50589 Phase 2 T18477 DRUGINFO D07MPL SNX-5422 Phase 1/2 T18477 DRUGINFO D03LRU Alvespimycin hydrochloride Phase 1 T18477 DRUGINFO D06YSP AT13387 Phase 1 T18477 DRUGINFO D0H3VK BIIB 028 Phase 1 T18477 DRUGINFO D02TTL Debio 0932 Phase 1 T18477 DRUGINFO D02PGP PU3 Phase 1 T18477 DRUGINFO D0V9MT PU-AD Phase 1 T18477 DRUGINFO D0ME2T RTA-901 Phase 1 T18477 DRUGINFO D03IKZ HBP-347 Discontinued in Phase 3 T18477 DRUGINFO D03PKI Geldanamycin Discontinued in Phase 2 T18477 DRUGINFO D0BM6S IPI-493 Discontinued in Phase 1 T18477 DRUGINFO D00OCB CCT-018159 Preclinical T18477 DRUGINFO D0X5YU KOS-2484 Preclinical T18477 DRUGINFO D0KC7K EC-154 Terminated T18477 DRUGINFO D05RTH 17-desmethoxy-17-aminogeldanamycin Investigative T18477 DRUGINFO D0K4RN 2-(1H-pyrrol-1-ylcarbonyl)benzene-1,3,5-triol Investigative T18477 DRUGINFO D06GOK 2-Methyl-2,4-Pentanediol Investigative T18477 DRUGINFO D08CZD 4-(2-methoxyethoxy)-6-methylpyrimidin-2-amine Investigative T18477 DRUGINFO D0D3BP 6-(3-BROMO-2-NAPHTHYL)-1,3,5-TRIAZINE-2,4-DIAMINE Investigative T18477 DRUGINFO D00PMS 8-BENZO[1,3]DIOXOL-,5-YLMETHYL-9-BUTYL-9H- Investigative T18477 DRUGINFO D01GGU 9-Butyl-8-(3-Methoxybenzyl)-9h-Purin-6-Amine Investigative T18477 DRUGINFO D05UTX 9-Butyl-8-(4-Methoxybenzyl)-9h-Purin-6-Amine Investigative T18477 DRUGINFO D0H6OS Geldanamycin-estradiol hybrid Investigative T18477 DRUGINFO D07WDQ GNF-PF-67 Investigative T18477 DRUGINFO D02IIL KOSN1559 Investigative T18477 DRUGINFO D0H0KA Macbecin Investigative T18477 DRUGINFO D0D5KQ PU24S Investigative T18477 DRUGINFO D0ZA6G Radicicol Investigative T18477 DRUGINFO D0M2TY RHEIN Investigative T18477 DRUGINFO D0K0TJ SNX-2112 Investigative T18477 DRUGINFO D0T4MS VER-49009 Investigative T18477 DRUGINFO D05GKC ZEARALANONE Investigative T18477 KEGGPATH hsa04141:Protein processing in endoplasmic reticulum T18477 KEGGPATH hsa04151:PI3K-Akt signaling pathway T18477 KEGGPATH hsa04612:Antigen processing and presentation T18477 KEGGPATH hsa04621:NOD-like receptor signaling pathway T18477 KEGGPATH hsa04914:Progesterone-mediated oocyte maturation T18477 KEGGPATH hsa04915:Estrogen signaling pathway T18477 KEGGPATH hsa05200:Pathways in cancer T18477 KEGGPATH hsa05215:Prostate cancer T18477 WIKIPATH WP1433:NOD pathway T18477 WIKIPATH WP1850:Metabolism of nitric oxide T18477 WIKIPATH WP1859:Mitotic G2-G2/M phases T18477 WIKIPATH WP1907:Semaphorin interactions T18477 WIKIPATH WP1910:Signaling by EGFR T18477 WIKIPATH WP2100:Arylhydrocarbon receptor (AhR) signaling pathway T18477 WIKIPATH WP231:TNF alpha Signaling Pathway T18477 WIKIPATH WP2355:Corticotropin-releasing hormone T18477 WIKIPATH WP2586:Aryl Hydrocarbon Receptor T18477 WIKIPATH WP262:EBV LMP1 signaling T18477 WIKIPATH WP2683:Influenza Life Cycle T18477 WIKIPATH WP2719:Fcgamma receptor (FCGR) dependent phagocytosis T18477 WIKIPATH WP2780:Signaling by ERBB2 T18477 WIKIPATH WP2784:Binding and Uptake of Ligands by Scavenger Receptors T18477 WIKIPATH WP2873:Aryl Hydrocarbon Receptor Pathway T18477 WIKIPATH WP2882:Nuclear Receptors Meta-Pathway T18477 WIKIPATH WP2884:NRF2 pathway T18477 REACPATH R-HSA-1236382:Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants T18477 REACPATH R-HSA-1474151:Tetrahydrobiopterin (BH4) synthesis, recycling, salvage and regulation T18477 REACPATH R-HSA-2029482:Regulation of actin dynamics for phagocytic cup formation T18477 REACPATH R-HSA-203615:eNOS activation T18477 REACPATH R-HSA-2565942:Regulation of PLK1 Activity at G2/M Transition T18477 REACPATH R-HSA-3371568:Attenuation phase T18477 REACPATH R-HSA-3371571:HSF1-dependent transactivation T18477 REACPATH R-HSA-380259:Loss of Nlp from mitotic centrosomes T18477 REACPATH R-HSA-380270:Recruitment of mitotic centrosome proteins and complexes T18477 REACPATH R-HSA-380284:Loss of proteins required for interphase microtubule organization?from the centrosome T18477 REACPATH R-HSA-3928663:EPHA-mediated growth cone collapse T18477 REACPATH R-HSA-4420097:VEGFA-VEGFR2 Pathway T18477 REACPATH R-HSA-5218920:VEGFR2 mediated vascular permeability T18477 REACPATH R-HSA-5620912:Anchoring of the basal body to the plasma membrane T18477 REACPATH R-HSA-5637810:Constitutive Signaling by EGFRvIII T18477 NET_PATH NetPath_11:TCR Signaling Pathway T18477 NET_PATH NetPath_14:IL2 Signaling Pathway T18477 INTEPATH ar_tf_pathway:Regulation of Androgen receptor activity T18477 INTEPATH avb3_integrin_pathway:Integrins in angiogenesis T18477 INTEPATH erbb_network_pathway:ErbB receptor signaling network T18477 INTEPATH hdac_classii_pathway:Signaling events mediated by HDAC Class II T18477 INTEPATH hif1apathway:Hypoxic and oxygen homeostasis regulation of HIF-1-alpha T18477 INTEPATH il2_pi3kpathway:IL2 signaling events mediated by PI3K T18477 INTEPATH ilk_pathway:Integrin-linked kinase signaling T18477 INTEPATH lkb1_pathway:LKB1 signaling events T18477 INTEPATH myc_activpathway:Validated targets of C-MYC transcriptional activation T18477 INTEPATH pi3kciaktpathway:Class I PI3K signaling events mediated by Akt T18477 INTEPATH pi3kcipathway:Class I PI3K signaling events T18477 INTEPATH reg_gr_pathway:Glucocorticoid receptor regulatory network T18477 INTEPATH telomerasepathway:Regulation of Telomerase T18477 INTEPATH vegfr1_2_pathway:Signaling events mediated by VEGFR1 and VEGFR2 T18477 INTEPATH vegfr1_pathway:VEGFR1 specific signals T48069 TARGETID T48069 T48069 FORMERID TTDS00269 T48069 UNIPROID IGF1R_HUMAN T48069 TARGNAME Insulin-like growth factor I receptor (IGF1R) T48069 GENENAME IGF1R T48069 TARGTYPE Successful target T48069 SYNONYMS Type 1 insulin-like growth factor receptor; Insulin-like growth factor 1 receptor; IGF-IR; IGF-I receptor; IGF-1R; IGF-1 receptor; CD221 antigen; CD221 T48069 FUNCTION Binds IGF1 with high affinity and IGF2 and insulin (INS) with a lower affinity. The activated IGF1R is involved in cell growth and survival control. IGF1R is crucial for tumor transformation and survival of malignant cell. Ligand binding activates the receptor kinase, leading to receptor autophosphorylation, and tyrosines phosphorylation of multiple substrates, that function as signaling adapter proteins including, the insulin-receptor substrates (IRS1/2), Shc and 14-3-3 proteins. Phosphorylation of IRSs proteins lead to the activation of two main signaling pathways: the PI3K-AKT/PKB pathway and the Ras-MAPK pathway. The result of activating the MAPK pathway is increased cellular proliferation, whereas activating the PI3K pathway inhibits apoptosis and stimulates protein synthesis. Phosphorylated IRS1 can activate the 85 kDa regulatory subunit of PI3K (PIK3R1), leading to activation of several downstream substrates, including protein AKT/PKB. AKT phosphorylation, in turn, enhances protein synthesis through mTOR activation and triggers the antiapoptotic effects of IGFIR through phosphorylation and inactivation of BAD. In parallel to PI3K-driven signaling, recruitment of Grb2/SOS by phosphorylated IRS1 or Shc leads to recruitment of Ras and activation of the ras-MAPK pathway. In addition to these two main signaling pathways IGF1R signals also through the Janus kinase/signal transducer and activator of transcription pathway (JAK/STAT). Phosphorylation of JAK proteins can lead to phosphorylation/activation of signal transducers and activators of transcription (STAT) proteins. In particular activation of STAT3, may be essential for the transforming activity of IGF1R. The JAK/STAT pathway activates gene transcription and may be responsible for the transforming activity. JNK kinases can also be activated by the IGF1R. IGF1 exerts inhibiting activities on JNK activation via phosphorylation and inhibition of MAP3K5/ASK1, which is able to directly associate with the IGF1R. Receptor tyrosine kinase which mediates actions of insulin-like growth factor 1 (IGF1). T48069 PDBSTRUC 5U8R; 5U8Q; 5HZN; 5FXS; 5FXR T48069 BIOCLASS Kinase T48069 ECNUMBER EC 2.7.10.1 T48069 SEQUENCE MKSGSGGGSPTSLWGLLFLSAALSLWPTSGEICGPGIDIRNDYQQLKRLENCTVIEGYLHILLISKAEDYRSYRFPKLTVITEYLLLFRVAGLESLGDLFPNLTVIRGWKLFYNYALVIFEMTNLKDIGLYNLRNITRGAIRIEKNADLCYLSTVDWSLILDAVSNNYIVGNKPPKECGDLCPGTMEEKPMCEKTTINNEYNYRCWTTNRCQKMCPSTCGKRACTENNECCHPECLGSCSAPDNDTACVACRHYYYAGVCVPACPPNTYRFEGWRCVDRDFCANILSAESSDSEGFVIHDGECMQECPSGFIRNGSQSMYCIPCEGPCPKVCEEEKKTKTIDSVTSAQMLQGCTIFKGNLLINIRRGNNIASELENFMGLIEVVTGYVKIRHSHALVSLSFLKNLRLILGEEQLEGNYSFYVLDNQNLQQLWDWDHRNLTIKAGKMYFAFNPKLCVSEIYRMEEVTGTKGRQSKGDINTRNNGERASCESDVLHFTSTTTSKNRIIITWHRYRPPDYRDLISFTVYYKEAPFKNVTEYDGQDACGSNSWNMVDVDLPPNKDVEPGILLHGLKPWTQYAVYVKAVTLTMVENDHIRGAKSEILYIRTNASVPSIPLDVLSASNSSSQLIVKWNPPSLPNGNLSYYIVRWQRQPQDGYLYRHNYCSKDKIPIRKYADGTIDIEEVTENPKTEVCGGEKGPCCACPKTEAEKQAEKEEAEYRKVFENFLHNSIFVPRPERKRRDVMQVANTTMSSRSRNTTAADTYNITDPEELETEYPFFESRVDNKERTVISNLRPFTLYRIDIHSCNHEAEKLGCSASNFVFARTMPAEGADDIPGPVTWEPRPENSIFLKWPEPENPNGLILMYEIKYGSQVEDQRECVSRQEYRKYGGAKLNRLNPGNYTARIQATSLSGNGSWTDPVFFYVQAKTGYENFIHLIIALPVAVLLIVGGLVIMLYVFHRKRNNSRLGNGVLYASVNPEYFSAADVYVPDEWEVAREKITMSRELGQGSFGMVYEGVAKGVVKDEPETRVAIKTVNEAASMRERIEFLNEASVMKEFNCHHVVRLLGVVSQGQPTLVIMELMTRGDLKSYLRSLRPEMENNPVLAPPSLSKMIQMAGEIADGMAYLNANKFVHRDLAARNCMVAEDFTVKIGDFGMTRDIYETDYYRKGGKGLLPVRWMSPESLKDGVFTTYSDVWSFGVVLWEIATLAEQPYQGLSNEQVLRFVMEGGLLDKPDNCPDMLFELMRMCWQYNPKMRPSFLEIISSIKEEMEPGFREVSFYYSEENKLPEPEELDLEPENMESVPLDPSASSSSLPLPDRHSGHKAENGPGPGVLVLRASFDERQPYAHMNGGRKNERALPLPQSSTC T48069 DRUGINFO D0F3JT Mecasermin Approved T48069 DRUGINFO D0N3NZ Somatomedin-1 Approved T48069 DRUGINFO D0EN0W Teprotumumab Approved T48069 DRUGINFO D01GFX OSI-906 Phase 3 T48069 DRUGINFO D06APK Rinfabate Phase 2/3 T48069 DRUGINFO D00AKR AMG 479 Phase 2 T48069 DRUGINFO D01SJS AXL-1717 Phase 2 T48069 DRUGINFO D0E5DP Cixutumumab Phase 2 T48069 DRUGINFO D00BUO MM-141 Phase 2 T48069 DRUGINFO D03BHM R1507 Phase 2 T48069 DRUGINFO D0T5JS TT-100 Phase 2 T48069 DRUGINFO D00VKK VPI-2690B Phase 2 T48069 DRUGINFO D07HPJ AEW-541 Phase 1 T48069 DRUGINFO D0O7QQ BIIB 022 Phase 1 T48069 DRUGINFO D01OYS Cyclolignan picropodophyllin Phase 1 T48069 DRUGINFO D4JYH3 FPI-1434 Phase 1 T48069 DRUGINFO D0L1ZM HF-0299 Phase 1 T48069 DRUGINFO D03WNN RG-7010 Phase 1 T48069 DRUGINFO D00BPE AVE-1642 Discontinued in Phase 2 T48069 DRUGINFO D0M3OR KW-2450 Discontinued in Phase 1/2 T48069 DRUGINFO D0U6KH Figitumumab Discontinued in Phase 1 T48069 DRUGINFO D0LF0O BMS-695735 Preclinical T48069 DRUGINFO D0TI4U EGFR/IGFR tandem adnectin Preclinical T48069 DRUGINFO D0W9KO 4-((1H-indazol-6-ylamino)methyl)benzene-1,2-diol Investigative T48069 DRUGINFO D0L7MM 4-((naphthalen-2-ylamino)methyl)benzene-1,2-diol Investigative T48069 DRUGINFO D07LUR Alpha-D-Mannose Investigative T48069 DRUGINFO D00ICA AMP-PNP Investigative T48069 DRUGINFO D0M4SY BMS-536924 Investigative T48069 DRUGINFO D0G6XS Fucose Investigative T48069 DRUGINFO D0O0RY JB-1 Investigative T48069 DRUGINFO D06NMZ NVP-ADW742 Investigative T48069 KEGGPATH hsa04014:Ras signaling pathway T48069 KEGGPATH hsa04015:Rap1 signaling pathway T48069 KEGGPATH hsa04066:HIF-1 signaling pathway T48069 KEGGPATH hsa04068:FoxO signaling pathway T48069 KEGGPATH hsa04114:Oocyte meiosis T48069 KEGGPATH hsa04144:Endocytosis T48069 KEGGPATH hsa04151:PI3K-Akt signaling pathway T48069 KEGGPATH hsa04152:AMPK signaling pathway T48069 KEGGPATH hsa04510:Focal adhesion T48069 KEGGPATH hsa04520:Adherens junction T48069 KEGGPATH hsa04550:Signaling pathways regulating pluripotency of stem cells T48069 KEGGPATH hsa04730:Long-term depression T48069 KEGGPATH hsa04913:Ovarian steroidogenesis T48069 KEGGPATH hsa04914:Progesterone-mediated oocyte maturation T48069 KEGGPATH hsa05200:Pathways in cancer T48069 KEGGPATH hsa05202:Transcriptional misregulation in cancer T48069 KEGGPATH hsa05205:Proteoglycans in cancer T48069 KEGGPATH hsa05214:Glioma T48069 KEGGPATH hsa05215:Prostate cancer T48069 KEGGPATH hsa05218:Melanoma T48069 WIKIPATH WP1544:MicroRNAs in cardiomyocyte hypertrophy T48069 WIKIPATH WP2032:TSH signaling pathway T48069 WIKIPATH WP2261:Signaling Pathways in Glioblastoma T48069 WIKIPATH WP254:Apoptosis T48069 WIKIPATH WP2677:Signaling by Type 1 Insulin-like Growth Factor 1 Receptor (IGF1R) T48069 WIKIPATH WP306:Focal Adhesion T48069 WIKIPATH WP474:Endochondral Ossification T48069 WIKIPATH WP481:Insulin Signaling T48069 WIKIPATH WP615:Senescence and Autophagy in Cancer T48069 REACPATH R-HSA-2428928:IRS-related events triggered by IGF1R T48069 REACPATH R-HSA-2428933:SHC-related events triggered by IGF1R T48069 INTEPATH ajdiss_2pathway:Posttranslational regulation of adherens junction stability and dissassembly T48069 INTEPATH avb3_integrin_pathway:Integrins in angiogenesis T48069 INTEPATH ecadherin_stabilization_pathway:Stabilization and expansion of the E-cadherin adherens junction T48069 INTEPATH er_nongenomic_pathway:Plasma membrane estrogen receptor signaling T48069 INTEPATH igf1_pathway:IGF1 pathway T48069 INTEPATH shp2_pathway:SHP2 signaling T48069 PANTPATH P00032:Insulin/IGF pathway-mitogen activated protein kinase kinase/MAP kinase cascade T48069 PANTPATH P00033:Insulin/IGF pathway-protein kinase B signaling cascade T25258 TARGETID T25258 T25258 FORMERID TTDR00007 T25258 UNIPROID MDR1_HUMAN T25258 TARGNAME Multidrug resistance protein 1 (ABCB1) T25258 GENENAME ABCB1 T25258 TARGTYPE Successful target T25258 SYNONYMS PGY1; P-glycoprotein 1; MDR1; CD243 antigen; CD243; ATP-binding cassette sub-family B member 1 T25258 FUNCTION Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells. T25258 PDBSTRUC 6QEX; 6FN4; 6FN1; 6C0V T25258 BIOCLASS ABC transporter T25258 ECNUMBER EC 7.6.2.2 T25258 SEQUENCE MDLEGDRNGGAKKKNFFKLNNKSEKDKKEKKPTVSVFSMFRYSNWLDKLYMVVGTLAAIIHGAGLPLMMLVFGEMTDIFANAGNLEDLMSNITNRSDINDTGFFMNLEEDMTRYAYYYSGIGAGVLVAAYIQVSFWCLAAGRQIHKIRKQFFHAIMRQEIGWFDVHDVGELNTRLTDDVSKINEGIGDKIGMFFQSMATFFTGFIVGFTRGWKLTLVILAISPVLGLSAAVWAKILSSFTDKELLAYAKAGAVAEEVLAAIRTVIAFGGQKKELERYNKNLEEAKRIGIKKAITANISIGAAFLLIYASYALAFWYGTTLVLSGEYSIGQVLTVFFSVLIGAFSVGQASPSIEAFANARGAAYEIFKIIDNKPSIDSYSKSGHKPDNIKGNLEFRNVHFSYPSRKEVKILKGLNLKVQSGQTVALVGNSGCGKSTTVQLMQRLYDPTEGMVSVDGQDIRTINVRFLREIIGVVSQEPVLFATTIAENIRYGRENVTMDEIEKAVKEANAYDFIMKLPHKFDTLVGERGAQLSGGQKQRIAIARALVRNPKILLLDEATSALDTESEAVVQVALDKARKGRTTIVIAHRLSTVRNADVIAGFDDGVIVEKGNHDELMKEKGIYFKLVTMQTAGNEVELENAADESKSEIDALEMSSNDSRSSLIRKRSTRRSVRGSQAQDRKLSTKEALDESIPPVSFWRIMKLNLTEWPYFVVGVFCAIINGGLQPAFAIIFSKIIGVFTRIDDPETKRQNSNLFSLLFLALGIISFITFFLQGFTFGKAGEILTKRLRYMVFRSMLRQDVSWFDDPKNTTGALTTRLANDAAQVKGAIGSRLAVITQNIANLGTGIIISFIYGWQLTLLLLAIVPIIAIAGVVEMKMLSGQALKDKKELEGSGKIATEAIENFRTVVSLTQEQKFEHMYAQSLQVPYRNSLRKAHIFGITFSFTQAMMYFSYAGCFRFGAYLVAHKLMSFEDVLLVFSAVVFGAMAVGQVSSFAPDYAKAKISAAHIIMIIEKTPLIDSYSTEGLMPNTLEGNVTFGEVVFNYPTRPDIPVLQGLSLEVKKGQTLALVGSSGCGKSTVVQLLERFYDPLAGKVLLDGKEIKRLNVQWLRAHLGIVSQEPILFDCSIAENIAYGDNSRVVSQEEIVRAAKEANIHAFIESLPNKYSTKVGDKGTQLSGGQKQRIAIARALVRQPHILLLDEATSALDTESEKVVQEALDKAREGRTCIVIAHRLSTIQNADLIVVFQNGRVKEHGTHQQLLAQKGIYFSMVSVQAGTKRQ T25258 DRUGINFO D06XVF CBT-1 Phase 3 T25258 DRUGINFO D09LSY EDP-322 Phase 1 T25258 DRUGINFO D0GS2W W-198 Phase 1 T25258 DRUGINFO D06DCL LY335979 Discontinued in Phase 3 T25258 DRUGINFO D02VJY Biricodar Discontinued in Phase 2 T25258 DRUGINFO D04RLX Tariquidar Discontinued in Phase 2 T25258 DRUGINFO D09FGX ELACRIDAR Discontinued in Phase 1 T25258 DRUGINFO D0SR4G ONT-093 Discontinued in Phase 1 T25258 DRUGINFO D03PLP [1,1':2',1'']-terphenyl-4,3'',5''-triol Investigative T25258 DRUGINFO D0AW4W 4,3'',5''-trimethoxy-[1,1':2',1'']-terphenyl Investigative T25258 DRUGINFO D05XGZ 6-(3,5-dimethoxy-phenyl)-naphthalen-2-ol Investigative T25258 DRUGINFO D0O9NE TRISMETHOXYRESVERATROL Investigative T25258 DRUGINFO D04GYT XR-9456 Investigative T25258 DRUGINFO D09HIM XR-9504 Investigative T25258 DRUGINFO D0A4TF XR-9544 Investigative T25258 DRUGINFO D0S8CE XR-9577 Investigative T25258 KEGGPATH hsa02010:ABC transporters T25258 KEGGPATH hsa04976:Bile secretion T25258 KEGGPATH hsa05206:MicroRNAs in cancer T25258 WIKIPATH WP1604:Codeine and Morphine Metabolism T25258 WIKIPATH WP2289:Drug Induction of Bile Acid Pathway T25258 WIKIPATH WP2328:Allograft Rejection T25258 WIKIPATH WP2377:Integrated Pancreatic Cancer Pathway T25258 WIKIPATH WP2489:Multi Drug Resistance Protein 1 (Glycoprotein 1) Regulation T25258 WIKIPATH WP2712:Abacavir transport and metabolism T25258 WIKIPATH WP299:Nuclear Receptors in Lipid Metabolism and Toxicity T25258 REACPATH R-HSA-382556:ABC-family proteins mediated transport T25258 NET_PATH NetPath_11:TCR Signaling Pathway T25258 NET_PATH NetPath_14:IL2 Signaling Pathway T25258 INTEPATH hif1_tfpathway:HIF-1-alpha transcription factor network T40474 TARGETID T40474 T40474 FORMERID TTDC00110 T40474 UNIPROID MET_HUMAN T40474 TARGNAME Proto-oncogene c-Met (MET) T40474 GENENAME MET T40474 TARGTYPE Successful target T40474 SYNONYMS Tyrosine-protein kinase Met; Scatter factor receptor; SF receptor; Met proto-oncogene tyrosine kinase; Hepatocyte growth factor receptor; HGF/SF receptor; HGF-SF receptor; HGF receptor; C-met; C-Met receptor tyrosine kinase T40474 FUNCTION Regulates many physiological processes including proliferation, scattering, morphogenesis and survival. Ligand binding at the cell surface induces autophosphorylation of MET on its intracellular domain that provides docking sites for downstream signaling molecules. Following activation by ligand, interacts with the PI3-kinase subunit PIK3R1, PLCG1, SRC, GRB2, STAT3 or the adapter GAB1. Recruitment of these downstream effectors by MET leads to the activation of several signaling cascades including the RAS-ERK, PI3 kinase-AKT, or PLCgamma-PKC. The RAS-ERK activation is associated with the morphogenetic effects while PI3K/AKT coordinates prosurvival effects. During embryonic development, MET signaling plays a role in gastrulation, development and migration of muscles and neuronal precursors, angiogenesis and kidney formation. In adults, participates in wound healing as well as organ regeneration and tissue remodeling. Promotes also differentiation and proliferation of hematopoietic cells. May regulate cortical bone osteogenesis. Receptor tyrosine kinase that transduces signals from the extracellular matrix into the cytoplasm by binding to hepatocyte growth factor/HGF ligand. T40474 PDBSTRUC 6I04; 6GCU; 5YA5; 5UAF; 5UAD T40474 BIOCLASS Kinase T40474 ECNUMBER EC 2.7.10.1 T40474 SEQUENCE MKAPAVLAPGILVLLFTLVQRSNGECKEALAKSEMNVNMKYQLPNFTAETPIQNVILHEHHIFLGATNYIYVLNEEDLQKVAEYKTGPVLEHPDCFPCQDCSSKANLSGGVWKDNINMALVVDTYYDDQLISCGSVNRGTCQRHVFPHNHTADIQSEVHCIFSPQIEEPSQCPDCVVSALGAKVLSSVKDRFINFFVGNTINSSYFPDHPLHSISVRRLKETKDGFMFLTDQSYIDVLPEFRDSYPIKYVHAFESNNFIYFLTVQRETLDAQTFHTRIIRFCSINSGLHSYMEMPLECILTEKRKKRSTKKEVFNILQAAYVSKPGAQLARQIGASLNDDILFGVFAQSKPDSAEPMDRSAMCAFPIKYVNDFFNKIVNKNNVRCLQHFYGPNHEHCFNRTLLRNSSGCEARRDEYRTEFTTALQRVDLFMGQFSEVLLTSISTFIKGDLTIANLGTSEGRFMQVVVSRSGPSTPHVNFLLDSHPVSPEVIVEHTLNQNGYTLVITGKKITKIPLNGLGCRHFQSCSQCLSAPPFVQCGWCHDKCVRSEECLSGTWTQQICLPAIYKVFPNSAPLEGGTRLTICGWDFGFRRNNKFDLKKTRVLLGNESCTLTLSESTMNTLKCTVGPAMNKHFNMSIIISNGHGTTQYSTFSYVDPVITSISPKYGPMAGGTLLTLTGNYLNSGNSRHISIGGKTCTLKSVSNSILECYTPAQTISTEFAVKLKIDLANRETSIFSYREDPIVYEIHPTKSFISGGSTITGVGKNLNSVSVPRMVINVHEAGRNFTVACQHRSNSEIICCTTPSLQQLNLQLPLKTKAFFMLDGILSKYFDLIYVHNPVFKPFEKPVMISMGNENVLEIKGNDIDPEAVKGEVLKVGNKSCENIHLHSEAVLCTVPNDLLKLNSELNIEWKQAISSTVLGKVIVQPDQNFTGLIAGVVSISTALLLLLGFFLWLKKRKQIKDLGSELVRYDARVHTPHLDRLVSARSVSPTTEMVSNESVDYRATFPEDQFPNSSQNGSCRQVQYPLTDMSPILTSGDSDISSPLLQNTVHIDLSALNPELVQAVQHVVIGPSSLIVHFNEVIGRGHFGCVYHGTLLDNDGKKIHCAVKSLNRITDIGEVSQFLTEGIIMKDFSHPNVLSLLGICLRSEGSPLVVLPYMKHGDLRNFIRNETHNPTVKDLIGFGLQVAKGMKYLASKKFVHRDLAARNCMLDEKFTVKVADFGLARDMYDKEYYSVHNKTGAKLPVKWMALESLQTQKFTTKSDVWSFGVLLWELMTRGAPPYPDVNTFDITVYLLQGRRLLQPEYCPDPLYEVMLKCWHPKAEMRPSFSELVSRISAIFSTFIGEHYVHVNATYVNVKCVAPYPSLLSSEDNADDEVDTRPASFWETS T40474 DRUGINFO D0IQ6P Cabozantinib Approved T40474 DRUGINFO D07OJZ Capmatinib Approved T40474 DRUGINFO D03ZBT Crizotinib Approved T40474 DRUGINFO D0R8QG Tepotinib Approved T40474 DRUGINFO DQ5X1Z Amivantamab Phase 3 T40474 DRUGINFO D0N1YF Beperminogene perplasmid Phase 3 T40474 DRUGINFO D0H9PT RG3638 Phase 3 T40474 DRUGINFO D0LW0T Savolitinib Phase 3 T40474 DRUGINFO D0ZI1F Tivantinib Phase 3 T40474 DRUGINFO D05BLN MGCD516 Phase 2/3 T40474 DRUGINFO D0OK2N AMG 208 Phase 2 T40474 DRUGINFO D0G0BL AMG 337 Phase 2 T40474 DRUGINFO DV3Y7F APL-101 Phase 2 T40474 DRUGINFO D01TBJ CMX-2043 Phase 2 T40474 DRUGINFO D0FE7D Emibetuzumab Phase 2 T40474 DRUGINFO D0R0YW HM-5016504 Phase 2 T40474 DRUGINFO D06EGV LY2801653 Phase 2 T40474 DRUGINFO D03SXS LY-2875358 Phase 2 T40474 DRUGINFO D07ARN SAR-125844 Phase 2 T40474 DRUGINFO D42TUS Telisotuzumab vedotin Phase 2 T40474 DRUGINFO D0D1GF XL880 Phase 2 T40474 DRUGINFO D0A3OE Anti-C-met CAR-T cells Phase 1/2 T40474 DRUGINFO D0O6WV BMS-777607 Phase 1/2 T40474 DRUGINFO D09ZNL ChronSeal Phase 1/2 T40474 DRUGINFO D00DRL MK-2461 Phase 1/2 T40474 DRUGINFO D0B4OK Sym015 Phase 1/2 T40474 DRUGINFO D02EOR ABBV-399 Phase 1 T40474 DRUGINFO D0I2IY ABT-700 Phase 1 T40474 DRUGINFO D0FA6S Altiratinib Phase 1 T40474 DRUGINFO D0D1HI Autologous T Cells Expressing MET scFv CAR Phase 1 T40474 DRUGINFO D95YSW BPI-9016 M Phase 1 T40474 DRUGINFO D04XUJ CBT-101 Phase 1 T40474 DRUGINFO D03GTO C-Met/PD-L1 CAR-T Cell Phase 1 T40474 DRUGINFO D09ETH E-7050 Phase 1 T40474 DRUGINFO D0Y8UV EMD-1204831 Phase 1 T40474 DRUGINFO D0N6VK Hepapoietin Phase 1 T40474 DRUGINFO D0YT8P JNJ-38877605 Phase 1 T40474 DRUGINFO D01IJM LY3164530 Phase 1 T40474 DRUGINFO D05OMT MK-8033 Phase 1 T40474 DRUGINFO D01LCC PF-4217903 Phase 1 T40474 DRUGINFO D01FSX REGN5093 Phase 1 T40474 DRUGINFO D7HZ3T RXDX-106 Phase 1 T40474 DRUGINFO D0ZU5F SGX523 Phase 1 T40474 DRUGINFO D7M8LI TPX-0022 Phase 1 T40474 DRUGINFO DU6H8Z TR1801-ADC Phase 1 T40474 DRUGINFO D1TNJ2 XL092 Phase 1 T40474 DRUGINFO D0NO6E Mteron-F1 Preclinical T40474 DRUGINFO D1AD6L NPS-1034 Preclinical T40474 DRUGINFO D0S1II 1-(2-nitrophenethyl)-1H-pyrrolo[3,2-b]pyridine Investigative T40474 DRUGINFO D0U4JW 1-(phenylsulfonyl)-1H-pyrrolo[3,2-b]pyridine Investigative T40474 DRUGINFO D0N5XG 1-benzyl-1H-pyrrolo[3,2-b]pyridine Investigative T40474 DRUGINFO D0S0GT 3-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine Investigative T40474 DRUGINFO D00FZA ALD-805 Investigative T40474 DRUGINFO D0T1YH ALD-806 Investigative T40474 DRUGINFO D07OXC AM7 Investigative T40474 DRUGINFO D07CFW Anti-cMET mab Investigative T40474 DRUGINFO D03LZK APS-3010 Investigative T40474 DRUGINFO D0NX6F BAY-85-3474 Investigative T40474 DRUGINFO D0M4SY BMS-536924 Investigative T40474 DRUGINFO D0I2PS CMET Avimer polypeptides Investigative T40474 DRUGINFO D0W8GP DP-3590 Investigative T40474 DRUGINFO D0PS7U GE-137 Investigative T40474 DRUGINFO D0Z4RX HuMax-cMet Investigative T40474 DRUGINFO D05GSI LA-480 Investigative T40474 DRUGINFO D0AD6Z mab 224G11 Investigative T40474 DRUGINFO D0G3ZN PF-00614435 Investigative T40474 DRUGINFO D00TBD PHA-665752 Investigative T40474 DRUGINFO D0RO9R PMID21123062C27 Investigative T40474 DRUGINFO D00EMH PMID21967808CR-16 Investigative T40474 DRUGINFO D04CUA PMID24210504C1o Investigative T40474 DRUGINFO D0M0SV PRS-110 Investigative T40474 DRUGINFO D0N6QO RP-1040 Investigative T40474 DRUGINFO D0E1QI SU11274 Investigative T40474 DRUGINFO D0BS6B TP-801 Investigative T40474 KEGGPATH hsa04014:Ras signaling pathway T40474 KEGGPATH hsa04015:Rap1 signaling pathway T40474 KEGGPATH hsa04060:Cytokine-cytokine receptor interaction T40474 KEGGPATH hsa04144:Endocytosis T40474 KEGGPATH hsa04151:PI3K-Akt signaling pathway T40474 KEGGPATH hsa04360:Axon guidance T40474 KEGGPATH hsa04510:Focal adhesion T40474 KEGGPATH hsa04520:Adherens junction T40474 KEGGPATH hsa05100:Bacterial invasion of epithelial cells T40474 KEGGPATH hsa05120:Epithelial cell signaling in Helicobacter pylori infection T40474 KEGGPATH hsa05144:Malaria T40474 KEGGPATH hsa05200:Pathways in cancer T40474 KEGGPATH hsa05202:Transcriptional misregulation in cancer T40474 KEGGPATH hsa05205:Proteoglycans in cancer T40474 KEGGPATH hsa05206:MicroRNAs in cancer T40474 KEGGPATH hsa05211:Renal cell carcinoma T40474 KEGGPATH hsa05218:Melanoma T40474 KEGGPATH hsa05230:Central carbon metabolism in cancer T40474 WIKIPATH WP1907:Semaphorin interactions T40474 WIKIPATH WP2002:miR-targeted genes in epithelium - TarBase T40474 WIKIPATH WP2004:miR-targeted genes in lymphocytes - TarBase T40474 WIKIPATH WP2005:miR-targeted genes in muscle cell - TarBase T40474 WIKIPATH WP2006:miR-targeted genes in squamous cell - TarBase T40474 WIKIPATH WP2261:Signaling Pathways in Glioblastoma T40474 WIKIPATH WP2870:Extracellular vesicle-mediated signaling in recipient cells T40474 WIKIPATH WP306:Focal Adhesion T40474 WIKIPATH WP313:Signaling of Hepatocyte Growth Factor Receptor T40474 WIKIPATH WP366:TGF beta Signaling Pathway T40474 REACPATH R-HSA-416550:Sema4D mediated inhibition of cell attachment and migration T40474 INTEPATH a6b1_a6b4_integrin_pathway:a6b1 and a6b4 Integrin signaling T40474 INTEPATH ajdiss_2pathway:Posttranslational regulation of adherens junction stability and dissassembly T40474 INTEPATH arf6_pathway:Arf6 signaling events T40474 INTEPATH ecadherin_stabilization_pathway:Stabilization and expansion of the E-cadherin adherens junction T40474 INTEPATH fgf_pathway:FGF signaling pathway T40474 INTEPATH met_pathway:Signaling events mediated by Hepatocyte Growth Factor Receptor (c-Met) T40474 INTEPATH p53downstreampathway:Direct p53 effectors T40474 INTEPATH rb_1pathway:Regulation of retinoblastoma protein T40474 INTEPATH syndecan_1_pathway:Syndecan-1-mediated signaling events T40474 INTEPATH tcptp_pathway:Signaling events mediated by TCPTP T43332 TARGETID T43332 T43332 FORMERID TTDR00947 T43332 UNIPROID FA7_HUMAN T43332 TARGNAME Coagulation factor VII (F7) T43332 GENENAME F7 T43332 TARGTYPE Successful target T43332 SYNONYMS Serum prothrombin conversion accelerator; SPCA; Proconvertin; Eptacog alfa T43332 FUNCTION Initiates the extrinsic pathway of blood coagulation. Serine protease that circulates in the blood in a zymogen form. Factor VII is converted to factor VIIa by factor Xa, factor XIIa, factor IXa, or thrombin by minor proteolysis. In the presence of tissue factor and calcium ions, factor VIIa then converts factor X to factor Xa by limited proteolysis. Factor VIIa will also convert factor IX to factor IXa in the presence of tissue factor and calcium. T43332 PDBSTRUC 5U6J; 5TQG; 5TQF; 5TQE; 5PB6 T43332 BIOCLASS Peptidase T43332 ECNUMBER EC 3.4.21.21 T43332 SEQUENCE MVSQALRLLCLLLGLQGCLAAGGVAKASGGETRDMPWKPGPHRVFVTQEEAHGVLHRRRRANAFLEELRPGSLERECKEEQCSFEEAREIFKDAERTKLFWISYSDGDQCASSPCQNGGSCKDQLQSYICFCLPAFEGRNCETHKDDQLICVNENGGCEQYCSDHTGTKRSCRCHEGYSLLADGVSCTPTVEYPCGKIPILEKRNASKPQGRIVGGKVCPKGECPWQVLLLVNGAQLCGGTLINTIWVVSAAHCFDKIKNWRNLIAVLGEHDLSEHDGDEQSRRVAQVIIPSTYVPGTTNHDIALLRLHQPVVLTDHVVPLCLPERTFSERTLAFVRFSLVSGWGQLLDRGATALELMVLNVPRLMTQDCLQQSRKVGDSPNITEYMFCAGYSDGSKDSCKGDSGGPHATHYRGTWYLTGIVSWGQGCATVGHFGVYTRVSQYIEWLQKLMRSEPRPGVLLRAPFP T43332 DRUGINFO D0C9IW Factor viia Approved T43332 DRUGINFO D09SHH BAX-817 Phase 3 T43332 DRUGINFO D00VMA Vatreptacog alfa (activated) Phase 3 T43332 DRUGINFO D0C0CE Activated recombinant FVII-albumin fusion protein Phase 2/3 T43332 DRUGINFO D0HZ2A Recombinant factor VIIa PEGylated liposomal Phase 1/2 T43332 DRUGINFO D0R4YQ CB-813 Phase 1 T43332 DRUGINFO D05GPB Eptacog alfa Phase 1 T43332 DRUGINFO D00EYC F-7TG Phase 1 T43332 DRUGINFO D0J3YX BAY 86-6150 Discontinued in Phase 2/3 T43332 DRUGINFO D0K3LX RNAPc2 Discontinued in Phase 2 T43332 DRUGINFO D0CT8A 4-(3,4-Diethoxy-benzylamino)-benzamidine Investigative T43332 DRUGINFO D02XPB 4-(4-Benzyloxy-3-methoxy-benzylamino)-benzamidine Investigative T43332 DRUGINFO D01NCC Factor-VIIa-XTEN Investigative T43332 DRUGINFO D0G6XS Fucose Investigative T43332 DRUGINFO D02PKV Human recombinant factor VIIa Investigative T43332 DRUGINFO D0R9UQ Long-acting Factor VII conjugate Investigative T43332 DRUGINFO D0O9RV MOD-5023 Investigative T43332 KEGGPATH hsa04610:Complement and coagulation cascades T43332 WIKIPATH WP15:Selenium Micronutrient Network T43332 WIKIPATH WP1533:Vitamin B12 Metabolism T43332 WIKIPATH WP176:Folate Metabolism T43332 WIKIPATH WP1797:Circadian Clock T43332 WIKIPATH WP1818:Formation of Fibrin Clot (Clotting Cascade) T43332 WIKIPATH WP272:Blood Clotting Cascade T43332 WIKIPATH WP2762:PTM: gamma carboxylation, hypusine formation and arylsulfatase activation T43332 WIKIPATH WP558:Complement and Coagulation Cascades T43332 WHIZPATH PW000562:Coagulation T43332 REACPATH R-HSA-1368108:BMAL1:CLOCK,NPAS2 activates circadian gene expression T43332 REACPATH R-HSA-140834:Extrinsic Pathway of Fibrin Clot Formation T43332 REACPATH R-HSA-159740:Gamma-carboxylation of protein precursors T43332 REACPATH R-HSA-159763:Transport of gamma-carboxylated protein precursors from the endoplasmic reticulum to the Golgi apparatus T43332 REACPATH R-HSA-159782:Removal of aminoterminal propeptides from gamma-carboxylated proteins T43332 PANTPATH P00005:Angiogenesis T43332 PANTPATH P00011:Blood coagulation T33489 TARGETID T33489 T33489 FORMERID TTDC00149 T33489 UNIPROID STS_HUMAN T33489 TARGNAME Steryl-sulfatase (STS) T33489 GENENAME STS T33489 TARGTYPE Successful target T33489 SYNONYMS Steryl-sulfate sulfohydrolase; Steroid sulfatase; STS; Estrone sulfatase; Arylsulfatase C; ASC T33489 FUNCTION Conversion of sulfated steroid precursors to estrogens during pregnancy. T33489 PDBSTRUC 1P49 T33489 BIOCLASS Sulfuric ester hydrolase T33489 ECNUMBER EC 3.1.6.2 T33489 SEQUENCE MPLRKMKIPFLLLFFLWEAESHAASRPNIILVMADDLGIGDPGCYGNKTIRTPNIDRLASGGVKLTQHLAASPLCTPSRAAFMTGRYPVRSGMASWSRTGVFLFTASSGGLPTDEITFAKLLKDQGYSTALIGKWHLGMSCHSKTDFCHHPLHHGFNYFYGISLTNLRDCKPGEGSVFTTGFKRLVFLPLQIVGVTLLTLAALNCLGLLHVPLGVFFSLLFLAALILTLFLGFLHYFRPLNCFMMRNYEIIQQPMSYDNLTQRLTVEAAQFIQRNTETPFLLVLSYLHVHTALFSSKDFAGKSQHGVYGDAVEEMDWSVGQILNLLDELRLANDTLIYFTSDQGAHVEEVSSKGEIHGGSNGIYKGGKANNWEGGIRVPGILRWPRVIQAGQKIDEPTSNMDIFPTVAKLAGAPLPEDRIIDGRDLMPLLEGKSQRSDHEFLFHYCNAYLNAVRWHPQNSTSIWKAFFFTPNFNPVGSNGCFATHVCFCFGSYVTHHDPPLLFDISKDPRERNPLTPASEPRFYEILKVMQEAADRHTQTLPEVPDQFSWNNFLWKPWLQLCCPSTGLSCQCDREKQDKRLSR T33489 DRUGINFO D0E6OC Tranilast Approved T33489 DRUGINFO D0Y6OA Coumate Phase 2 T33489 DRUGINFO D0I3RN PGL-2 Phase 2 T33489 DRUGINFO D04ZND PGL-2001 Phase 2 T33489 DRUGINFO D07ZNI STX-140 Phase 2 T33489 DRUGINFO D05NJI STX 64 Phase 1 T33489 DRUGINFO D08BTV 2-(4-cyclohexylthiosemicarbazono)methyl-phenol Investigative T33489 DRUGINFO D0I4LL 2',4'-dicyanobiphenyl-4-yl sulfamate Investigative T33489 DRUGINFO D03XJE 2-Adamantan-2-ylidenemethyl-benzooxazol-6-ol Investigative T33489 DRUGINFO D07GRM 2-Amino-3-Oxo-4-Sulfo-Butyric Acid Investigative T33489 DRUGINFO D0N8VZ 2-ethylestradiol 3,17-O,O-bis-sulfamate Investigative T33489 DRUGINFO D0FH1V 2-methylsulfanylestradiol 3,17-O,O-bis-sulfamate Investigative T33489 DRUGINFO D06IMK 3-(4-cyclohexylthiosemicarbazono)methyl-phenol Investigative T33489 DRUGINFO D0Y9SI 3-(4-hexylthiosemicarbazono)methyl-benzoic acid Investigative T33489 DRUGINFO D04HNO 3-{3-[(aminosulfonyl)oxy]benzoyl}phenyl sulfamate Investigative T33489 DRUGINFO D04YVS 3-{4-[(aminosulfonyl)oxy]benzoyl}phenyl sulfamate Investigative T33489 DRUGINFO D09BUM 4-(4-cyclohexylthiosemicarbazono)methyl-phenol Investigative T33489 DRUGINFO D0AL2D 4-{4-[(aminosulfonyl)oxy]benzoyl}phenyl sulfamate Investigative T33489 DRUGINFO D0P6IO 4-Sulfamoyloxy-benzoic acid butyl ester Investigative T33489 DRUGINFO D05TRN 4-Sulfamoyloxy-benzoic acid cycloheptyl ester Investigative T33489 DRUGINFO D0P9ZV 4-Sulfamoyloxy-benzoic acid cyclohexyl ester Investigative T33489 DRUGINFO D0T5OD 4-Sulfamoyloxy-benzoic acid cyclooctyl ester Investigative T33489 DRUGINFO D0U7PV 4-Sulfamoyloxy-benzoic acid cyclopentyl ester Investigative T33489 DRUGINFO D06YDQ 4-Sulfamoyloxy-benzoic acid heptyl ester Investigative T33489 DRUGINFO D0D1CV 4-Sulfamoyloxy-benzoic acid hexyl ester Investigative T33489 DRUGINFO D06SMY 4-Sulfamoyloxy-benzoic acid nonyl ester Investigative T33489 DRUGINFO D03NUT 4-Sulfamoyloxy-benzoic acid octyl ester Investigative T33489 DRUGINFO D00OZS 4-Sulfamoyloxy-benzoic acid pentyl ester Investigative T33489 DRUGINFO D01ACT 4-Sulfamoyloxy-benzoic acid propyl ester Investigative T33489 DRUGINFO D0W6GB Benzomate Investigative T33489 DRUGINFO D02UVH B-Octylglucoside Investigative T33489 DRUGINFO D0R7QY EMATE Investigative T33489 DRUGINFO D00LFX Estradiol 17-O-sulfamate Investigative T33489 DRUGINFO D0S3RZ Estradiol 3,17-O,O-bis-sulfamate Investigative T33489 DRUGINFO D0G1XC MHL cyclohexylthiosemicarbazone Investigative T33489 DRUGINFO D09ROV Nortropinyl-arylsulfonylurea 3 Investigative T33489 DRUGINFO D00AON Sulfamic acid 2-nonyl-4-oxo-4H-chromen-6-yl ester Investigative T33489 DRUGINFO D06DVJ Sulfamic acid 3-(3-hydroxy-benzoyl)-phenyl ester Investigative T33489 DRUGINFO D02RJA Sulfamic acid 3-(3-methoxy-benzoyl)-phenyl ester Investigative T33489 DRUGINFO D0S5BA Sulfamic acid 3-(4-hydroxy-benzoyl)-phenyl ester Investigative T33489 DRUGINFO D05KKB Sulfamic acid 3-(4-methoxy-benzoyl)-phenyl ester Investigative T33489 DRUGINFO D0G8HD Sulfamic acid 3-benzoyl-phenyl ester Investigative T33489 DRUGINFO D0M2WG Sulfamic acid 4-(2-hydroxy-benzoyl)-phenyl ester Investigative T33489 DRUGINFO D0B1JM Sulfamic acid 4-(2-methoxy-benzoyl)-phenyl ester Investigative T33489 DRUGINFO D06ADL Sulfamic acid 4-(3-methoxy-benzoyl)-phenyl ester Investigative T33489 DRUGINFO D0B2XN Sulfamic acid 4-benzoyl-phenyl ester Investigative T33489 KEGGPATH hsa00140:Steroid hormone biosynthesis T33489 WIKIPATH WP2788:Sphingolipid metabolism T33489 WIKIPATH WP2877:Vitamin D Receptor Pathway T33489 WIKIPATH WP697:Estrogen metabolism T33489 WHIZPATH PW000045:Androgen and Estrogen Metabolism T33489 REACPATH R-HSA-1660662:Glycosphingolipid metabolism T69128 TARGETID T69128 T69128 FORMERID TTDNS00597 T69128 UNIPROID ROS1_HUMAN T69128 TARGNAME Proto-oncogene c-Ros (ROS1) T69128 GENENAME ROS1 T69128 TARGTYPE Successful target T69128 SYNONYMS c-Ros receptor tyrosine kinase; Receptor tyrosine kinase c-ros oncogene 1; ROS; Proto-oncogene tyrosine-protein kinase ROS; Proto-oncogene c-Ros-1; MCF3 T69128 FUNCTION Orphan receptor tyrosine kinase (RTK) that plays a role in epithelial cell differentiation and regionalization of the proximal epididymal epithelium. May activate several downstream signaling pathways related to cell differentiation, proliferation, growth and survival including the PI3 kinase-mTOR signaling pathway. Mediates the phosphorylation of PTPN11, an activator of this pathway. May also phosphorylate and activate the transcription factor STAT3 to control anchorage-independent cell growth. Mediates the phosphorylation and the activation of VAV3, a guanine nucleotide exchange factor regulating cell morphology. May activate other downstream signaling proteins including AKT1, MAPK1, MAPK3, IRS1 and PLCG2. T69128 PDBSTRUC 4UXL; 3ZBF T69128 BIOCLASS Kinase T69128 ECNUMBER EC 2.7.10.1 T69128 SEQUENCE MKNIYCLIPKLVNFATLGCLWISVVQCTVLNSCLKSCVTNLGQQLDLGTPHNLSEPCIQGCHFWNSVDQKNCALKCRESCEVGCSSAEGAYEEEVLENADLPTAPFASSIGSHNMTLRWKSANFSGVKYIIQWKYAQLLGSWTYTKTVSRPSYVVKPLHPFTEYIFRVVWIFTAQLQLYSPPSPSYRTHPHGVPETAPLIRNIESSSPDTVEVSWDPPQFPGGPILGYNLRLISKNQKLDAGTQRTSFQFYSTLPNTIYRFSIAAVNEVGEGPEAESSITTSSSAVQQEEQWLFLSRKTSLRKRSLKHLVDEAHCLRLDAIYHNITGISVDVHQQIVYFSEGTLIWAKKAANMSDVSDLRIFYRGSGLISSISIDWLYQRMYFIMDELVCVCDLENCSNIEEITPPSISAPQKIVADSYNGYVFYLLRDGIYRADLPVPSGRCAEAVRIVESCTLKDFAIKPQAKRIIYFNDTAQVFMSTFLDGSASHLILPRIPFADVKSFACENNDFLVTDGKVIFQQDALSFNEFIVGCDLSHIEEFGFGNLVIFGSSSQLHPLPGRPQELSVLFGSHQALVQWKPPALAIGANVILISDIIELFELGPSAWQNWTYEVKVSTQDPPEVTHIFLNISGTMLNVPELQSAMKYKVSVRASSPKRPGPWSEPSVGTTLVPASEPPFIMAVKEDGLWSKPLNSFGPGEFLSSDIGNVSDMDWYNNSLYYSDTKGDVFVWLLNGTDISENYHLPSIAGAGALAFEWLGHFLYWAGKTYVIQRQSVLTGHTDIVTHVKLLVNDMVVDSVGGYLYWTTLYSVESTRLNGESSLVLQTQPWFSGKKVIALTLDLSDGLLYWLVQDSQCIHLYTAVLRGQSTGDTTITEFAAWSTSEISQNALMYYSGRLFWINGFRIITTQEIGQKTSVSVLEPARFNQFTIIQTSLKPLPGNFSFTPKVIPDSVQESSFRIEGNASSFQILWNGPPAVDWGVVFYSVEFSAHSKFLASEQHSLPVFTVEGLEPYALFNLSVTPYTYWGKGPKTSLSLRAPETVPSAPENPRIFILPSGKCCNKNEVVVEFRWNKPKHENGVLTKFEIFYNISNQSITNKTCEDWIAVNVTPSVMSFQLEGMSPRCFIAFQVRAFTSKGPGPYADVVKSTTSEINPFPHLITLLGNKIVFLDMDQNQVVWTFSAERVISAVCYTADNEMGYYAEGDSLFLLHLHNRSSSELFQDSLVFDITVITIDWISRHLYFALKESQNGMQVFDVDLEHKVKYPREVKIHNRNSTIISFSVYPLLSRLYWTEVSNFGYQMFYYSIISHTLHRILQPTATNQQNKRNQCSCNVTEFELSGAMAIDTSNLEKPLIYFAKAQEIWAMDLEGCQCWRVITVPAMLAGKTLVSLTVDGDLIYWIITAKDSTQIYQAKKGNGAIVSQVKALRSRHILAYSSVMQPFPDKAFLSLASDTVEPTILNATNTSLTIRLPLAKTNLTWYGITSPTPTYLVYYAEVNDRKNSSDLKYRILEFQDSIALIEDLQPFSTYMIQIAVKNYYSDPLEHLPPGKEIWGKTKNGVPEAVQLINTTVRSDTSLIISWRESHKPNGPKESVRYQLAISHLALIPETPLRQSEFPNGRLTLLVTRLSGGNIYVLKVLACHSEEMWCTESHPVTVEMFNTPEKPYSLVPENTSLQFNWKAPLNVNLIRFWVELQKWKYNEFYHVKTSCSQGPAYVCNITNLQPYTSYNVRVVVVYKTGENSTSLPESFKTKAGVPNKPGIPKLLEGSKNSIQWEKAEDNGCRITYYILEIRKSTSNNLQNQNLRWKMTFNGSCSSVCTWKSKNLKGIFQFRVVAANNLGFGEYSGISENIILVGDDFWIPETSFILTIIVGIFLVVTIPLTFVWHRRLKNQKSAKEGVTVLINEDKELAELRGLAAGVGLANACYAIHTLPTQEEIENLPAFPREKLTLRLLLGSGAFGEVYEGTAVDILGVGSGEIKVAVKTLKKGSTDQEKIEFLKEAHLMSKFNHPNILKQLGVCLLNEPQYIILELMEGGDLLTYLRKARMATFYGPLLTLVDLVDLCVDISKGCVYLERMHFIHRDLAARNCLVSVKDYTSPRIVKIGDFGLARDIYKNDYYRKRGEGLLPVRWMAPESLMDGIFTTQSDVWSFGILIWEILTLGHQPYPAHSNLDVLNYVQTGGRLEPPRNCPDDLWNLMTQCWAQEPDQRPTFHRIQDQLQLFRNFFLNSIYKSRDEANNSGVINESFEGEDGDVICLNSDDIMPVALMETKNREGLNYMVLATECGQGEEKSEGPLGSQESESCGLRKEEKEPHADKDFCQEKQVAYCPSGKPEGLNYACLTHSGYGDGSD T69128 DRUGINFO D03ZBT Crizotinib Approved T69128 DRUGINFO D0O0LS Entrectinib Approved T69128 DRUGINFO D0AF6O Lorlatinib Approved T69128 DRUGINFO D2KV8B AB-106 Phase 2 T69128 DRUGINFO D05NFR TPX-0005 Phase 1/2 T69128 DRUGINFO D0N0DU DS-6051 Phase 1 T69128 DRUGINFO D0MX7B Carboxamide derivative 4 Patented T69128 DRUGINFO D0T8XD Imidazo[1,2-b]pyridazine derivative 1 Patented T69128 DRUGINFO D0M8UO Imidazo[1,2-b]pyridazine derivative 2 Patented T69128 DRUGINFO D0N1CF Imidazo[1,2-b]pyridazine derivative 3 Patented T69128 DRUGINFO D0N8YJ PMID28270010-Compound-Figure21-b Patented T69128 DRUGINFO D0K5UF PMID24432909C8e Investigative T69128 WIKIPATH WP2431:Spinal Cord Injury T73475 TARGETID T73475 T73475 FORMERID TTDR00029 T73475 UNIPROID MMP7_HUMAN T73475 TARGNAME Matrix metalloproteinase-7 (MMP-7) T73475 GENENAME MMP7 T73475 TARGTYPE Successful target T73475 SYNONYMS Uterine metalloproteinase; Pump-1 protease; PUMP1; Matrin; Matrilysin; MPSL1 T73475 FUNCTION Activates procollagenase. Degrades casein, gelatins of types I, III, IV, and V, and fibronectin. T73475 PDBSTRUC 5UE5; 5UE2; 2Y6D; 2Y6C; 2MZI T73475 BIOCLASS Peptidase T73475 ECNUMBER EC 3.4.24.23 T73475 SEQUENCE MRLTVLCAVCLLPGSLALPLPQEAGGMSELQWEQAQDYLKRFYLYDSETKNANSLEAKLKEMQKFFGLPITGMLNSRVIEIMQKPRCGVPDVAEYSLFPNSPKWTSKVVTYRIVSYTRDLPHITVDRLVSKALNMWGKEIPLHFRKVVWGTADIMIGFARGAHGDSYPFDGPGNTLAHAFAPGTGLGGDAHFDEDERWTDGSSLGINFLYAATHELGHSLGMGHSSDPNAVMYPTYGNGDPQNFKLSQDDIKGIQKLYGKRSNSRKK T73475 DRUGINFO D00MDP Prinomastat Approved T73475 DRUGINFO D05VZE Marimastat Phase 3 T73475 DRUGINFO D01EUF BMS 275291 Discontinued in Phase 3 T73475 DRUGINFO D08WBF BB-3644 Terminated T73475 DRUGINFO D0Y1XT SC-44463 Terminated T73475 DRUGINFO D08ELY 3-Benzenesulfonyl-heptanoic acid hydroxyamide Investigative T73475 DRUGINFO D0N6CD 3-Cyclohexanesulfonyl-heptanoic acid hydroxyamide Investigative T73475 DRUGINFO D0P8EY Folate gamma-hydroxamic acid Investigative T73475 DRUGINFO D06HSC Folate gamma-L-phenylalaninehydroxamic acid Investigative T73475 DRUGINFO D0ZB6O Folate gamma-L-proline-hydroxamic acid Investigative T73475 DRUGINFO D0W2UK IK-862 Investigative T73475 DRUGINFO D0A4TC MMI270 Investigative T73475 DRUGINFO D07SPC N-hydroxy-2,3-bis(phenylsulfonamido)propanamide Investigative T73475 DRUGINFO D0BI8T RS-39066 Investigative T73475 DRUGINFO D07GEL SL422 Investigative T73475 DRUGINFO D03AMR SR-973 Investigative T73475 KEGGPATH hsa04310:Wnt signaling pathway T73475 WIKIPATH WP129:Matrix Metalloproteinases T73475 WIKIPATH WP2324:AGE/RAGE pathway T73475 WIKIPATH WP2769:Activation of Matrix Metalloproteinases T73475 WIKIPATH WP399:Wnt Signaling Pathway and Pluripotency T73475 REACPATH R-HSA-1442490:Collagen degradation T73475 REACPATH R-HSA-1474228:Degradation of the extracellular matrix T73475 REACPATH R-HSA-1592389:Activation of Matrix Metalloproteinases T73475 REACPATH R-HSA-2022090:Assembly of collagen fibrils and other multimeric structures T73475 NET_PATH NetPath_8:Wnt Signaling Pathway T73475 INTEPATH ajdiss_2pathway:Posttranslational regulation of adherens junction stability and dissassembly T73475 INTEPATH p75ntrpathway:p75(NTR)-mediated signaling T73475 INTEPATH syndecan_1_pathway:Syndecan-1-mediated signaling events T73475 PANTPATH P00004:Alzheimer disease-presenilin pathway T73475 PANTPATH P00057:Wnt signaling pathway T73475 PANTPATH P06959:CCKR signaling map ST T59102 TARGETID T59102 T59102 FORMERID TTDR01217 T59102 UNIPROID PGFRB_HUMAN T59102 TARGNAME Platelet-derived growth factor receptor beta (PDGFRB) T59102 GENENAME PDGFRB T59102 TARGTYPE Successful target T59102 SYNONYMS Platelet-derived growth factor receptor 1; PDGFR1; PDGFR-beta; PDGFR-1; PDGFR; PDGF-R-beta; CD140b antigen; CD140b; CD140 antigen-like family member B; Beta-type platelet-derived growth factor receptor; Beta-PDGFR; Beta platelet-derived growth factor receptor T59102 FUNCTION Plays an essential role in blood vessel development by promoting proliferation, migration and recruitment of pericytes and smooth muscle cells to endothelial cells. Plays a role in the migration of vascular smooth muscle cells and the formation of neointima at vascular injury sites. Required for normal development of the cardiovascular system. Required for normal recruitment of pericytes (mesangial cells) in the kidney glomerulus, and for normal formation of a branched network of capillaries in kidney glomeruli. Promotes rearrangement of the actin cytoskeleton and the formation of membrane ruffles. Binding of its cognate ligands - homodimeric PDGFB, heterodimers formed by PDGFA and PDGFB or homodimeric PDGFD -leads to the activation of several signaling cascades; the response depends on the nature of the bound ligand and is modulated by the formation of heterodimers between PDGFRA and PDGFRB. Phosphorylates PLCG1, PIK3R1, PTPN11, RASA1/GAP, CBL, SHC1 and NCK1. Activation of PLCG1 leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate, mobilization of cytosolic Ca(2+) and the activation of protein kinase C. Phosphorylation of PIK3R1, the regulatory subunit of phosphatidylinositol 3-kinase, leads to the activation of the AKT1 signaling pathway. Phosphorylation of SHC1, or of the C-terminus of PTPN11, creates a binding site for GRB2, resulting in the activation of HRAS, RAF1 and down-stream MAP kinases, including MAPK1/ERK2 and/or MAPK3/ERK1. Promotes phosphorylation and activation of SRC family kinases. Promotes phosphorylation of PDCD6IP/ALIX and STAM. Receptor signaling is down-regulated by protein phosphatases that dephosphorylate the receptor and its down-stream effectors, and by rapid internalization of the activated receptor. Tyrosine-protein kinase that acts as cell-surface receptor for homodimeric PDGFB and PDGFD and for heterodimers formed by PDGFA and PDGFB, and plays an essential role in the regulation of embryonic development, cell proliferation, survival, differentiation, chemotaxis and migration. T59102 PDBSTRUC 3MJG; 2PLE; 2PLD; 2L6W; 2IUI T59102 BIOCLASS Kinase T59102 ECNUMBER EC 2.7.10.1 T59102 SEQUENCE MRLPGAMPALALKGELLLLSLLLLLEPQISQGLVVTPPGPELVLNVSSTFVLTCSGSAPVVWERMSQEPPQEMAKAQDGTFSSVLTLTNLTGLDTGEYFCTHNDSRGLETDERKRLYIFVPDPTVGFLPNDAEELFIFLTEITEITIPCRVTDPQLVVTLHEKKGDVALPVPYDHQRGFSGIFEDRSYICKTTIGDREVDSDAYYVYRLQVSSINVSVNAVQTVVRQGENITLMCIVIGNEVVNFEWTYPRKESGRLVEPVTDFLLDMPYHIRSILHIPSAELEDSGTYTCNVTESVNDHQDEKAINITVVESGYVRLLGEVGTLQFAELHRSRTLQVVFEAYPPPTVLWFKDNRTLGDSSAGEIALSTRNVSETRYVSELTLVRVKVAEAGHYTMRAFHEDAEVQLSFQLQINVPVRVLELSESHPDSGEQTVRCRGRGMPQPNIIWSACRDLKRCPRELPPTLLGNSSEEESQLETNVTYWEEEQEFEVVSTLRLQHVDRPLSVRCTLRNAVGQDTQEVIVVPHSLPFKVVVISAILALVVLTIISLIILIMLWQKKPRYEIRWKVIESVSSDGHEYIYVDPMQLPYDSTWELPRDQLVLGRTLGSGAFGQVVEATAHGLSHSQATMKVAVKMLKSTARSSEKQALMSELKIMSHLGPHLNVVNLLGACTKGGPIYIITEYCRYGDLVDYLHRNKHTFLQHHSDKRRPPSAELYSNALPVGLPLPSHVSLTGESDGGYMDMSKDESVDYVPMLDMKGDVKYADIESSNYMAPYDNYVPSAPERTCRATLINESPVLSYMDLVGFSYQVANGMEFLASKNCVHRDLAARNVLICEGKLVKICDFGLARDIMRDSNYISKGSTFLPLKWMAPESIFNSLYTTLSDVWSFGILLWEIFTLGGTPYPELPMNEQFYNAIKRGYRMAQPAHASDEIYEIMQKCWEEKFEIRPPFSQLVLLLERLLGEGYKKKYQQVDEEFLRSDHPAILRSQARLPGFHGLRSPLDTSSVLYTAVQPNEGDNDYIIPLPDPKPEVADEGPLEGSPSLASSTLNEVNTSSTISCDSPLEPQDEPEPEPQLELQVEPEPELEQLPDSGCPAPRAEAEDSFL T59102 DRUGINFO D0T5QT Becaplermin Approved T59102 DRUGINFO D01PZD Romiplostim Approved T59102 DRUGINFO D0W5HK Sorafenib Approved T59102 DRUGINFO D02WVT E-3810 Phase 3 T59102 DRUGINFO D0Z6MT Famitinib Phase 2 T59102 DRUGINFO D00NSD XL-820 Phase 2 T59102 DRUGINFO D00DRL MK-2461 Phase 1/2 T59102 DRUGINFO D0GB2L SNN-0031 Phase 1/2 T59102 DRUGINFO D0T2ER TAK-593 Phase 1 T59102 DRUGINFO D0D3FB PMID25656651-Compound-21a Patented T59102 DRUGINFO D0XQ5F PMID25656651-Compound-21b Patented T59102 DRUGINFO D0YX2B PMID28460551-Compound-2 Patented T59102 DRUGINFO D0AK1F Pyridine derivative 18 Patented T59102 DRUGINFO D08PAV CDP-860 Discontinued in Phase 2 T59102 DRUGINFO D00QCB SRI-62-834 Discontinued in Phase 2 T59102 DRUGINFO D0KX1E CEP-2563 Discontinued in Phase 1 T59102 DRUGINFO D06GBK AG1295 Terminated T59102 DRUGINFO D03WTT RG-13022 Terminated T59102 DRUGINFO D09OLH (1H-indol-2-yl)(5-methoxy-1H-indol-2-yl)methanone Investigative T59102 DRUGINFO D0G0KQ (1H-indol-2-yl)(5-phenoxy-1H-indol-2-yl)methanone Investigative T59102 DRUGINFO D0D7ZL (1H-indol-2-yl)(6-methoxy-1H-indol-2-yl)methanone Investigative T59102 DRUGINFO D05WTI (2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamine Investigative T59102 DRUGINFO D0H7MF (5-fluoro-1H-indol-2-yl)-(1H-indol-2-yl)methanone Investigative T59102 DRUGINFO D0XS9E (5-hydroxy-1H-indol-2-yl)(1H-indol-2-yl)methanone Investigative T59102 DRUGINFO D0I7QX (benzo[b]furan-2-yl)-(1H-indol-2-yl)methanone Investigative T59102 DRUGINFO D00YCU 1-Phenyl-1H-benzoimidazol-5-ol Investigative T59102 DRUGINFO D01FWD 1-Phenyl-1H-benzoimidazole Investigative T59102 DRUGINFO D0XC6G 2-(1H-indazol-3-yl)-1H-benzo[d]imidazole Investigative T59102 DRUGINFO D07JDY 3-((E)-Styryl)-quinoline Investigative T59102 DRUGINFO D06MCJ 3-(1H-Indol-3-yl)-6,7-dimethoxy-quinoline Investigative T59102 DRUGINFO D0GN3E 3-(1H-Indol-3-yl)-quinoline Investigative T59102 DRUGINFO D0K9ON 3-(2-Cyclohexyl-ethyl)-6,7-dimethoxy-quinoline Investigative T59102 DRUGINFO D0P0RD 3-(3,4-Dichloro-phenyl)-6,7-dimethoxy-quinoline Investigative T59102 DRUGINFO D0AO6T 3-(3,4-Difluoro-phenyl)-6,7-dimethoxy-quinoline Investigative T59102 DRUGINFO D08SUH 3-(3,4-Dimethoxy-phenyl)-6,7-dimethoxy-quinoline Investigative T59102 DRUGINFO D0A6YP 3-(3-Fluoro-phenyl)-6,7-dimethoxy-quinoline Investigative T59102 DRUGINFO D00QPG 3-(4-dimethylamino-benzylidenyl)-2-indolinone Investigative T59102 DRUGINFO D0I0GL 3-(4-Fluoro-phenyl)-6,7-dimethoxy-quinoline Investigative T59102 DRUGINFO D0K3CJ 3-(6,7-Dimethoxy-quinolin-4-yloxy)-phenol Investigative T59102 DRUGINFO D02QBH 3-(6,7-Dimethoxy-quinolin-4-yloxy)-phenylamine Investigative T59102 DRUGINFO D07QMC 3-Benzimidazol-2-ylhydroquinolin-2-one Investigative T59102 DRUGINFO D06VNR 3-Benzyloxy-6,7-dimethoxy-quinoline Investigative T59102 DRUGINFO D08KWL 3-Cyclohexylethynyl-6,7-dimethoxy-quinoline Investigative T59102 DRUGINFO D0KF3N 3-Cyclopent-1-enyl-6,7-dimethoxy-quinoline Investigative T59102 DRUGINFO D00LRC 3-Cyclopentyl-6,7-dimethoxy-quinoline Investigative T59102 DRUGINFO D0IR5I 3-Pyridin-3-yl-quinoline-6,7-diol Investigative T59102 DRUGINFO D0H9TO 3-Pyridin-4-yl-quinolin-7-ol Investigative T59102 DRUGINFO D0Q3DS 3-Pyridin-4-yl-quinoline Investigative T59102 DRUGINFO D0K9VE 3-Pyridin-4-yl-quinoline-5,7-diol Investigative T59102 DRUGINFO D05GBY 3-Thiophen-3-yl-quinoline Investigative T59102 DRUGINFO D0F1RU 4-(2,3-Dimethoxy-phenoxy)-6,7-dimethoxy-quinoline Investigative T59102 DRUGINFO D0YE1X 4-(3,4-Dimethoxy-phenoxy)-6,7-dimethoxy-quinoline Investigative T59102 DRUGINFO D0C2KK 4-(3,5-Dimethoxy-phenoxy)-6,7-dimethoxy-quinoline Investigative T59102 DRUGINFO D03HLH 4-(3-Bromo-phenoxy)-6,7-dimethoxy-quinazoline Investigative T59102 DRUGINFO D05QMN 4-(3-Bromo-phenoxy)-6,7-dimethoxy-quinoline Investigative T59102 DRUGINFO D0Y1CJ 4-(3-Ethoxy-phenoxy)-6,7-dimethoxy-quinoline Investigative T59102 DRUGINFO D03FCU 4-(3-Ethyl-phenoxy)-6,7-dimethoxy-quinoline Investigative T59102 DRUGINFO D03IPZ 4-(3-Fluoro-phenoxy)-6,7-dimethoxy-quinoline Investigative T59102 DRUGINFO D0K2YG 4-(5-Methoxy-benzoimidazol-1-yl)-phenylamine Investigative T59102 DRUGINFO D03MQI 4-(6,7-Dimethoxy-quinolin-3-yl)-benzoic acid Investigative T59102 DRUGINFO D0H4JB 4-(6,7-Dimethoxy-quinolin-3-yl)-phenol Investigative T59102 DRUGINFO D01MUN 4-Benzoimidazol-1-yl-phenylamine Investigative T59102 DRUGINFO D01UYS 5-(6,7-Dimethoxy-quinolin-3-yl)-1H-pyridin-2-one Investigative T59102 DRUGINFO D0SG0G 5,6,7-Trimethoxy-3-pyridin-4-yl-quinoline Investigative T59102 DRUGINFO D0P0WT 5,7-Dimethoxy-3-pyridin-4-yl-quinoline Investigative T59102 DRUGINFO D0RD5S 5,7-Dimethoxy-3-thiophen-3-yl-quinoline Investigative T59102 DRUGINFO D07ZWN 5,7-Dimethyl-3-thiophen-3-yl-quinoline Investigative T59102 DRUGINFO D02XKJ 5-Methoxy-1-phenyl-1H-benzoimidazole Investigative T59102 DRUGINFO D0CF9B 6,7-Dichloro-3-thiophen-3-yl-quinoline Investigative T59102 DRUGINFO D0QT4X 6,7-Difluoro-3-thiophen-3-yl-quinoline Investigative T59102 DRUGINFO D06LLF 6,7-Dimethoxy-3-((E)-styryl)-quinoline Investigative T59102 DRUGINFO D07CFT 6,7-Dimethoxy-3-(3-methoxy-phenyl)-quinoline Investigative T59102 DRUGINFO D0G0KN 6,7-Dimethoxy-3-(4-methoxy-phenyl)-quinoline Investigative T59102 DRUGINFO D08JGS 6,7-Dimethoxy-3-(4-nitro-phenyl)-quinoline Investigative T59102 DRUGINFO D0WW8M 6,7-Dimethoxy-3-phenylethynyl-quinoline Investigative T59102 DRUGINFO D0G6SA 6,7-Dimethoxy-3-phenyl-quinoline Investigative T59102 DRUGINFO D0C1BE 6,7-Dimethoxy-3-p-tolyl-quinoline Investigative T59102 DRUGINFO D00RBV 6,7-Dimethoxy-3-pyridin-3-yl-quinoline Investigative T59102 DRUGINFO D0T9FQ 6,7-Dimethoxy-3-pyridin-4-yl-quinoline Investigative T59102 DRUGINFO D0G0ZQ 6,7-Dimethoxy-3-thiophen-2-yl-quinoline Investigative T59102 DRUGINFO D01XDV 6,7-Dimethoxy-4-(2-methoxy-phenoxy)-quinoline Investigative T59102 DRUGINFO D09QTC 6,7-Dimethoxy-4-(3-methoxy-phenoxy)-quinoline Investigative T59102 DRUGINFO D0ZS3F 6,7-Dimethoxy-4-(3-nitro-phenoxy)-quinoline Investigative T59102 DRUGINFO D0R8BC 6,7-Dimethoxy-4-(4-methoxy-phenoxy)-quinoline Investigative T59102 DRUGINFO D0VJ5W 6,7-Dimethoxy-4-m-tolyloxy-quinoline Investigative T59102 DRUGINFO D0CW1Q 6,7-Dimethoxy-4-phenoxy-quinoline Investigative T59102 DRUGINFO D04PQX 6-Methoxy-3-pyridin-4-yl-quinoline Investigative T59102 DRUGINFO D0W7IN 6-Methoxy-3-thiophen-3-yl-quinoline Investigative T59102 DRUGINFO D0Z4HV 7-Chloro-3-pyridin-4-yl-quinoline Investigative T59102 DRUGINFO D05SNG 7-Fluoro-3-thiophen-3-yl-quinoline Investigative T59102 DRUGINFO D02PZZ 7-Methoxy-3-pyridin-4-yl-quinoline Investigative T59102 DRUGINFO D0V8QI 7-Methoxy-3-thiophen-3-yl-quinoline Investigative T59102 DRUGINFO D0A6AA 7-Thiophen-3-yl-[1,3]dioxolo[4,5-g]quinoline Investigative T59102 DRUGINFO D0U3WQ AGL 2043 Investigative T59102 DRUGINFO D02CUF Benzyl-(6,7-dimethoxy-quinolin-3-yl)-amine Investigative T59102 DRUGINFO D0L0MZ Bis(5-acetoxybenzo[b]furan-2-yl)methanone Investigative T59102 DRUGINFO D07AXL Bis(5-aminobenzo[b]furan-2-yl)methanone Investigative T59102 DRUGINFO D0I3XZ Bis-(5-hydroxy-1H-indol-2-yl)-methanone Investigative T59102 DRUGINFO D02OBA Bis(5-hydroxybenzo[b]furan-2-yl)methanone Investigative T59102 DRUGINFO D09PUW Bis(5-methoxybenzo[b]furan-2-yl)methanone Investigative T59102 DRUGINFO D03VAA Bis(6-hydroxybenzo[b]furan-2-yl)methanone Investigative T59102 DRUGINFO D0Z3DW Bis(benzo[b]furan-2-yl)methanone Investigative T59102 DRUGINFO D0M4SY BMS-536924 Investigative T59102 DRUGINFO D05QBZ CP-673451 Investigative T59102 DRUGINFO D0G5YI Di(1H-indol-2-yl)methanone Investigative T59102 DRUGINFO D0UN9O GTP-14564 Investigative T59102 DRUGINFO D0D5EW HKI-9924129 Investigative T59102 DRUGINFO D0YZ7H JNJ-10198409 Investigative T59102 DRUGINFO D06ZUA Ki-11502 Investigative T59102 DRUGINFO D08BJR Ki-20227 Investigative T59102 DRUGINFO D0P3JW PD-0166326 Investigative T59102 DRUGINFO D0S1KJ PD-0173952 Investigative T59102 DRUGINFO D03NPX PD-0173955 Investigative T59102 DRUGINFO D0GW4Q PD-0173956 Investigative T59102 DRUGINFO D0Z7GH PD-0173958 Investigative T59102 DRUGINFO D0OH3J PD-0179483 Investigative T59102 DRUGINFO D0BW4G PDGF receptor tyrosine kinase inhibitor III Investigative T59102 DRUGINFO D0C2GE PMID22765894C8h Investigative T59102 DRUGINFO D09XIL Ro-4396686 Investigative T59102 DRUGINFO D0W9BF RPR-101511 Investigative T59102 DRUGINFO D0FH3M RPR-108514A Investigative T59102 DRUGINFO D09LPL SU-11652 Investigative T59102 DRUGINFO D0H1OK TG-100435 Investigative T59102 DRUGINFO D00YNJ XB-387 Investigative T59102 KEGGPATH hsa04010:MAPK signaling pathway T59102 KEGGPATH hsa04014:Ras signaling pathway T59102 KEGGPATH hsa04015:Rap1 signaling pathway T59102 KEGGPATH hsa04020:Calcium signaling pathway T59102 KEGGPATH hsa04060:Cytokine-cytokine receptor interaction T59102 KEGGPATH hsa04151:PI3K-Akt signaling pathway T59102 KEGGPATH hsa04510:Focal adhesion T59102 KEGGPATH hsa04540:Gap junction T59102 KEGGPATH hsa04810:Regulation of actin cytoskeleton T59102 KEGGPATH hsa05166:HTLV-I infection T59102 KEGGPATH hsa05200:Pathways in cancer T59102 KEGGPATH hsa05206:MicroRNAs in cancer T59102 KEGGPATH hsa05214:Glioma T59102 KEGGPATH hsa05215:Prostate cancer T59102 KEGGPATH hsa05218:Melanoma T59102 KEGGPATH hsa05230:Central carbon metabolism in cancer T59102 KEGGPATH hsa05231:Choline metabolism in cancer T59102 WIKIPATH WP1916:Signaling by PDGF T59102 WIKIPATH WP2261:Signaling Pathways in Glioblastoma T59102 WIKIPATH WP2526:PDGF Pathway T59102 WIKIPATH WP2653:PIP3 activates AKT signaling T59102 WIKIPATH WP306:Focal Adhesion T59102 WIKIPATH WP322:Osteoblast Signaling T59102 WIKIPATH WP382:MAPK Signaling Pathway T59102 WIKIPATH WP51:Regulation of Actin Cytoskeleton T59102 REACPATH R-HSA-1257604:PIP3 activates AKT signaling T59102 REACPATH R-HSA-2219530:Constitutive Signaling by Aberrant PI3K in Cancer T59102 REACPATH R-HSA-5673001:RAF/MAP kinase cascade T59102 INTEPATH integrin3_pathway:Beta3 integrin cell surface interactions T59102 INTEPATH myc_represspathway:Validated targets of C-MYC transcriptional repression T59102 INTEPATH nectin_pathway:Nectin adhesion pathway T59102 INTEPATH pdgf_pathway:PDGF receptor signaling network T59102 INTEPATH pdgfrbpathway:PDGFR-beta signaling pathway T59102 INTEPATH ptp1bpathway:Signaling events mediated by PTP1B T59102 INTEPATH s1p_s1p1_pathway:S1P1 pathway T59102 INTEPATH s1p_s1p3_pathway:S1P3 pathway T59102 INTEPATH shp2_pathway:SHP2 signaling T59102 INTEPATH tcptp_pathway:Signaling events mediated by TCPTP T59102 INTEPATH upa_upar_pathway:Urokinase-type plasminogen activator (uPA) and uPAR-mediated signaling T59102 PANTPATH P00005:Angiogenesis T59102 PANTPATH P00047:PDGF signaling pathway T76024 TARGETID T76024 T76024 FORMERID TTDC00085 T76024 UNIPROID C1S_HUMAN T76024 TARGNAME Complement C1s component (C1S) T76024 GENENAME C1S T76024 TARGTYPE Successful target T76024 SYNONYMS Complement component 1 subcomponent s; Complement C1s subcomponent; C1-esterase; C1 esterase T76024 FUNCTION C1r activates C1s so that it can, in turn, activate C2 and C4. C1s B chain is a serine protease that combines with C1q and C1r to form C1, the first component of the classical pathway of the complement system. T76024 PDBSTRUC 6F1H; 6F1C; 4LOT; 4LOS; 4LOR T76024 BIOCLASS Peptidase T76024 ECNUMBER EC 3.4.21.42 T76024 SEQUENCE MWCIVLFSLLAWVYAEPTMYGEILSPNYPQAYPSEVEKSWDIEVPEGYGIHLYFTHLDIELSENCAYDSVQIISGDTEEGRLCGQRSSNNPHSPIVEEFQVPYNKLQVIFKSDFSNEERFTGFAAYYVATDINECTDFVDVPCSHFCNNFIGGYFCSCPPEYFLHDDMKNCGVNCSGDVFTALIGEIASPNYPKPYPENSRCEYQIRLEKGFQVVVTLRREDFDVEAADSAGNCLDSLVFVAGDRQFGPYCGHGFPGPLNIETKSNALDIIFQTDLTGQKKGWKLRYHGDPMPCPKEDTPNSVWEPAKAKYVFRDVVQITCLDGFEVVEGRVGATSFYSTCQSNGKWSNSKLKCQPVDCGIPESIENGKVEDPESTLFGSVIRYTCEEPYYYMENGGGGEYHCAGNGSWVNEVLGPELPKCVPVCGVPREPFEEKQRIIGGSDADIKNFPWQVFFDNPWAGGALINEYWVLTAAHVVEGNREPTMYVGSTSVQTSRLAKSKMLTPEHVFIHPGWKLLEVPEGRTNFDNDIALVRLKDPVKMGPTVSPICLPGTSSDYNLMDGDLGLISGWGRTEKRDRAVRLKAARLPVAPLRKCKEVKVEKPTADAEAYVFTPNMICAGGEKGMDSCKGDSGGAFAVQDPNDKTKFYAAGLVSWGPQCGTYGLYTRVKNYVDWIMKTMQENSTPRED T76024 DRUGINFO D0BK4X Cinryze Approved T76024 DRUGINFO DJ0L4K Sutimlimab Phase 3 T76024 DRUGINFO D0OC5T ANX005 Phase 1 T76024 DRUGINFO D06SHZ SHP616 Phase 1 T76024 DRUGINFO D0X1EV TNT009 Phase 1 T76024 DRUGINFO D05TDJ TS01 Phase 1 T76024 DRUGINFO D0G6XS Fucose Investigative T76024 DRUGINFO D0J1CC PMID16460935C28 Investigative T76024 KEGGPATH hsa04610:Complement and coagulation cascades T76024 KEGGPATH hsa05133:Pertussis T76024 KEGGPATH hsa05150:Staphylococcus aureus infection T76024 KEGGPATH hsa05322:Systemic lupus erythematosus T76024 WIKIPATH WP1798:Complement cascade T76024 WIKIPATH WP2806:Human Complement System T76024 WIKIPATH WP545:Complement Activation, Classical Pathway T76024 WIKIPATH WP558:Complement and Coagulation Cascades T76024 NET_PATH NetPath_7:TGF_beta_Receptor Signaling Pathway T06273 TARGETID T06273 T06273 FORMERID TTDS00191 T06273 UNIPROID PARP1_HUMAN T06273 TARGNAME Poly [ADP-ribose] polymerase 1 (PARP1) T06273 GENENAME PARP1 T06273 TARGTYPE Successful target T06273 SYNONYMS Protein poly-ADP-ribosyltransferase PARP1; Poly[ADP-ribose] synthetase-1; Poly[ADP-ribose] synthase 1; Poly(ADP-ribose)polymerase-1; PPOL; PARP-1; NAD(+)Poly [ADP-ribose] polymerase-1 ADP-ribosyltransferase-1; NAD(+) ADP-ribosyltransferase-1; NAD(+) ADP-ribosyltransferase 1; DNA ADP-ribosyltransferase PARP1; ARTD1; ADPRT 1; ADPRT; ADP-ribosyltransferase diphtheria toxin-like 1 T06273 FUNCTION Mainly mediates glutamate and aspartate ADP-ribosylation of target proteins: the ADP-D-ribosyl group of NAD(+) is transferred to the acceptor carboxyl group of glutamate and aspartate residues and further ADP-ribosyl groups are transferred to the 2'-position of the terminal adenosine moiety, building up a polymer with an average chain length of 20-30 units. Mediates the poly(ADP-ribosyl)ation of a number of proteins, including itself, APLF and CHFR. Also mediates serine ADP-ribosylation of target proteins following interaction with HPF1; HPF1 conferring serine specificity. Probably also catalyzes tyrosine ADP-ribosylation of target proteins following interaction with HPF1. Catalyzes the poly-ADP-ribosylation of histones in a HPF1-dependent manner. Involved in the base excision repair (BER) pathway by catalyzing the poly-ADP-ribosylation of a limited number of acceptor proteins involved in chromatin architecture and in DNA metabolism. ADP-ribosylation follows DNA damage and appears as an obligatory step in a detection/signaling pathway leading to the reparation of DNA strand breaks. In addition to base excision repair (BER) pathway, also involved in double-strand breaks (DSBs) repair: together with TIMELESS, accumulates at DNA damage sites and promotes homologous recombination repair by mediating poly-ADP-ribosylation. In addition to proteins, also able to ADP-ribosylate DNA: catalyzes ADP-ribosylation of DNA strand break termini containing terminal phosphates and a 2'-OH group in single- and double-stranded DNA, respectively. Required for PARP9 and DTX3L recruitment to DNA damage sites. PARP1-dependent PARP9-DTX3L-mediated ubiquitination promotes the rapid and specific recruitment of 53BP1/TP53BP1, UIMC1/RAP80, and BRCA1 to DNA damage sites. Acts as a regulator of transcription: positively regulates the transcription of MTUS1 and negatively regulates the transcription of MTUS2/TIP150. With EEF1A1 and TXK, forms a complex that acts as a T-helper 1 (Th1) cell-specific transcription factor and binds the promoter of IFN-gamma to directly regulate its transcription, and is thus involved importantly in Th1 cytokine production. Involved in the synthesis of ATP in the nucleus, together with NMNAT1, PARG and NUDT5. Nuclear ATP generation is required for extensive chromatin remodeling events that are energy-consuming. Poly-ADP-ribosyltransferase that mediates poly-ADP-ribosylation of proteins and plays a key role in DNA repair. T06273 PDBSTRUC 6GHK; 6BHV; 5XSU; 5XST; 5XSR T06273 BIOCLASS Glycosyltransferases T06273 ECNUMBER EC 2.4.2.30 T06273 SEQUENCE MAESSDKLYRVEYAKSGRASCKKCSESIPKDSLRMAIMVQSPMFDGKVPHWYHFSCFWKVGHSIRHPDVEVDGFSELRWDDQQKVKKTAEAGGVTGKGQDGIGSKAEKTLGDFAAEYAKSNRSTCKGCMEKIEKGQVRLSKKMVDPEKPQLGMIDRWYHPGCFVKNREELGFRPEYSASQLKGFSLLATEDKEALKKQLPGVKSEGKRKGDEVDGVDEVAKKKSKKEKDKDSKLEKALKAQNDLIWNIKDELKKVCSTNDLKELLIFNKQQVPSGESAILDRVADGMVFGALLPCEECSGQLVFKSDAYYCTGDVTAWTKCMVKTQTPNRKEWVTPKEFREISYLKKLKVKKQDRIFPPETSASVAATPPPSTASAPAAVNSSASADKPLSNMKILTLGKLSRNKDEVKAMIEKLGGKLTGTANKASLCISTKKEVEKMNKKMEEVKEANIRVVSEDFLQDVSASTKSLQELFLAHILSPWGAEVKAEPVEVVAPRGKSGAALSKKSKGQVKEEGINKSEKRMKLTLKGGAAVDPDSGLEHSAHVLEKGGKVFSATLGLVDIVKGTNSYYKLQLLEDDKENRYWIFRSWGRVGTVIGSNKLEQMPSKEDAIEHFMKLYEEKTGNAWHSKNFTKYPKKFYPLEIDYGQDEEAVKKLTVNPGTKSKLPKPVQDLIKMIFDVESMKKAMVEYEIDLQKMPLGKLSKRQIQAAYSILSEVQQAVSQGSSDSQILDLSNRFYTLIPHDFGMKKPPLLNNADSVQAKVEMLDNLLDIEVAYSLLRGGSDDSSKDPIDVNYEKLKTDIKVVDRDSEEAEIIRKYVKNTHATTHNAYDLEVIDIFKIEREGECQRYKPFKQLHNRRLLWHGSRTTNFAGILSQGLRIAPPEAPVTGYMFGKGIYFADMVSKSANYCHTSQGDPIGLILLGEVALGNMYELKHASHISKLPKGKHSVKGLGKTTPDPSANISLDGVDVPLGTGISSGVNDTSLLYNEYIVYDIAQVNLKYLLKLKFNFKTSLW T06273 DRUGINFO D09LSX KU-0058948 Approved T06273 DRUGINFO D06NVJ Nicotinamide Approved T06273 DRUGINFO D0DN0W Niraparib Tosylate Approved T06273 DRUGINFO D09NTC CC-486 Phase 3 T06273 DRUGINFO D0Z2UW Nicaraven Phase 3 T06273 DRUGINFO D06KZL AG140699 Phase 2 T06273 DRUGINFO D0F5TD PMID27841036-Compound-37 Phase 2 T06273 DRUGINFO DP48WE Stenoparib Phase 2 T06273 DRUGINFO D8TE4F AMXI 5001 Phase 1/2 T06273 DRUGINFO DO0LP3 NMS-03305293 Phase 1 T06273 DRUGINFO D01KFW 3-oxo-2,3-dihydro-1H-indazole-4-carboxamide derivative 1 Patented T06273 DRUGINFO D0M0WS 3-oxo-2,3-dihydro-1H-indazole-4-carboxamide derivative 2 Patented T06273 DRUGINFO D09HUV 3-oxo-2,3-dihydro-1H-indazole-4-carboxamide derivative 3 Patented T06273 DRUGINFO D02QFM 3-oxo-2,3-dihydro-1H-indazole-4-carboxamide derivative 4 Patented T06273 DRUGINFO D09ZIM 3-oxo-2,3-dihydro-1H-indazole-4-carboxamide derivative 5 Patented T06273 DRUGINFO D0TD8R 3-phenyl isoquinolin-1(2H) derivative 1 Patented T06273 DRUGINFO D0G8HX 3-phenyl isoquinolin-1(2H) derivative 2 Patented T06273 DRUGINFO D0O9FC 4-Carboxamido-isoindolinone derivative 1 Patented T06273 DRUGINFO D08YPU 4-Carboxamido-isoindolinone derivative 2 Patented T06273 DRUGINFO D0R0PO 4-Carboxamido-isoindolinone derivative 3 Patented T06273 DRUGINFO D0Z5DI 4-Carboxamido-isoindolinone derivative 4 Patented T06273 DRUGINFO D0GH4V 4-Carboxamido-isoindolinone derivative 5 Patented T06273 DRUGINFO D09WUA 7-azaindole derivative 8 Patented T06273 DRUGINFO D01PYO Benzimidazole carboxamide derivative 1 Patented T06273 DRUGINFO D0P3YA Dihydrodiazepinocarbazolone derivative 1 Patented T06273 DRUGINFO D0B3QI Dihydropyrido phthalazinone derivative 1 Patented T06273 DRUGINFO D0J4GY Dihydropyrido phthalazinone derivative 2 Patented T06273 DRUGINFO D0M9TG Phthalazine derivative 3 Patented T06273 DRUGINFO D05ZBB Phthalazine ketone derivative 1 Patented T06273 DRUGINFO D0B4FV Phthalazine ketone derivative 2 Patented T06273 DRUGINFO D0AN7Z Phthalazine ketone derivative 3 Patented T06273 DRUGINFO D02KMI PMID27841036-Compound-33 Patented T06273 DRUGINFO D0J2SR Quinazolinedione derivative 1 Patented T06273 DRUGINFO D0IX2C Quinazolinedione derivative 2 Patented T06273 DRUGINFO D08KAH Quinazolinedione derivative 3 Patented T06273 DRUGINFO D0Z8IR Tetra-cyclic pyridophthalazinone derivative 1 Patented T06273 DRUGINFO D0MP4W Tetra-hydro-quinoline derivative 1 Patented T06273 DRUGINFO D0E9JI Tricyclic indole compound 13 Patented T06273 DRUGINFO D04ABS CPH-102 Preclinical T06273 DRUGINFO D04WDX PJ34 Preclinical T06273 DRUGINFO D0O3FX NU1025 Terminated T06273 DRUGINFO D04ZQJ (E)-N-(4-Phenylthiazol-2-yl) cinnamamide Investigative T06273 DRUGINFO D09SZG [2(R,S)-2-Sulfanylheptanoyl]-Phe-Ala Investigative T06273 DRUGINFO D0FF4M 1,2,3,4,4a,5-hexahydrophenanthridin-6(10bH)-one Investigative T06273 DRUGINFO D0NU5Z 1,7,8,9-tetrahydro-1,5-diaza-trindene-4,6-dione Investigative T06273 DRUGINFO D0TH7S 2-(2-Chlorophenyl)-2H-indazole-7-carboxamide Investigative T06273 DRUGINFO D0XZ5D 2-(3-Chlorophenyl)-2H-indazole-7-carboxamide Investigative T06273 DRUGINFO D01YIR 2-(3'-Methoxyphenyl) Benzimidazole-4-Carboxamide Investigative T06273 DRUGINFO D0U5WY 2-(3-Piperidin-1-yl-propyl)-3H-quinazolin-4-one Investigative T06273 DRUGINFO D00TUB 2-(4-Amino-phenyl)-8-hydroxy-3H-quinazolin-4-one Investigative T06273 DRUGINFO D0GA0Y 2-(4-Amino-phenyl)-8-methyl-3H-quinazolin-4-one Investigative T06273 DRUGINFO D0WO3P 2-(4-Azido-phenyl)-8-methoxy-3H-quinazolin-4-one Investigative T06273 DRUGINFO D0PT1K 2-(4-Chlorophenyl)-2H-indazole-7-carboxamide Investigative T06273 DRUGINFO D08ZVM 2-(4-Chlorophenyl)-5-Quinoxalinecarboxamide Investigative T06273 DRUGINFO D0Y1MH 2-(4-Hydroxy-phenyl)-8-methyl-3H-quinazolin-4-one Investigative T06273 DRUGINFO D0B2WX 2-(4-Methoxy-phenyl)-8-methyl-3H-quinazolin-4-one Investigative T06273 DRUGINFO D04TDX 2-(4-methoxyphenyl)quinoline-8-carboxamide Investigative T06273 DRUGINFO D05HJG 2,3-dihydro-1H-benzo[de]isoquinolin-1-one Investigative T06273 DRUGINFO D07SRJ 2,8-Dimethyl-3H-quinazolin-4-one Investigative T06273 DRUGINFO D02QZF 2-Benzyl-2H-indazole-7-carboxamide Investigative T06273 DRUGINFO D0Z3PB 2-ethylquinoline-8-carboxamide Investigative T06273 DRUGINFO D07CRG 2H-Isoquinolin-1-one Investigative T06273 DRUGINFO D0S8HZ 2-Methylquinoline-8-carboxamide Investigative T06273 DRUGINFO D0I2AF 2-phenyl-2H-benzo[d][1,2,3]triazole-4-carboxamide Investigative T06273 DRUGINFO D0IX3I 2-phenyl-2H-indazole-7-carboxamide Investigative T06273 DRUGINFO D08OUR 2-phenylpyrazolo-[1,5-a]pyridine-7-carboxamide Investigative T06273 DRUGINFO D0Z9DY 2-phenylquinoline-8-carboxamide Investigative T06273 DRUGINFO D08GMO 3-(4-aminophenyl)quinoxaline-5-carboxamide Investigative T06273 DRUGINFO D0M9TW 3-(4-cyanophenyl)quinoxaline-5-carboxamide Investigative T06273 DRUGINFO D0L1RZ 3-(4-methoxyphenyl)quinoxaline-5-carboxamide Investigative T06273 DRUGINFO D0K2PD 3-aminobenzamide Investigative T06273 DRUGINFO D0EI6X 3-aminobenzo[c][1,5]naphthyridin-6(5H)-one Investigative T06273 DRUGINFO D0K7JT 3-Ethenylquinoline-8-carboxamide Investigative T06273 DRUGINFO D0UF0U 3-Ethylquinoline-8-carboxamide Investigative T06273 DRUGINFO D00OZA 3-Ethynylquinoline-8-carboxamide Investigative T06273 DRUGINFO D05ZTI 3-Hydroxy-benzamide Investigative T06273 DRUGINFO D02MPP 3-Methoxybenzamide Investigative T06273 DRUGINFO D08XPZ 3-Methylquinoline-8-carboxamide Investigative T06273 DRUGINFO D0F8ZI 3-Morpholin-4-ylmethyl-5H-phenanthridin-6-one Investigative T06273 DRUGINFO D0L1NQ 3-Phenylquinoline-8-carboxamide Investigative T06273 DRUGINFO D0T5TT 3-Prop-1-ynylquinoline-8-carboxamide Investigative T06273 DRUGINFO D0GJ8U 4-(4-Morpholin-4-yl-butyl)-2H-phthalazin-1-one Investigative T06273 DRUGINFO D05WYN 4-(5-Morpholin-4-yl-pentyl)-2H-phthalazin-1-one Investigative T06273 DRUGINFO D03JTS 4-amino-1,8-naphthalimide Investigative T06273 DRUGINFO D08QWR 4-benzylphthalazin-1(2H)-one Investigative T06273 DRUGINFO D05GMW 4-methylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione Investigative T06273 DRUGINFO D05RXG 5-amino-3,4-dihydroisoquinolin-1(2H)-one Investigative T06273 DRUGINFO D07WPL 5-aminoisoquinolin-1(2H)-one Investigative T06273 DRUGINFO D01EVX 5-Chloro-2-methyl-3H-quinazolin-4-one Investigative T06273 DRUGINFO D02XLC 5-methylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione Investigative T06273 DRUGINFO D04ATU 8-Amino-6H,11H-indeno[1,2-c]isoquinolin-5-one Investigative T06273 DRUGINFO D0O0GA 8-Fluoro-6H,11H-indeno[1,2-c]isoquinolin-5-one Investigative T06273 DRUGINFO D0G5VD 8-Hydroxy-2-(4-nitro-phenyl)-3H-quinazolin-4-one Investigative T06273 DRUGINFO D0O6WW 8-Hydroxy-2-phenyl-3H-quinazolin-4-one Investigative T06273 DRUGINFO D0OF1I 8-Methoxy-2-(4-nitro-phenyl)-3H-quinazolin-4-one Investigative T06273 DRUGINFO D0T3SY 8-Methoxy-2-methyl-3H-quinazolin-4-one Investigative T06273 DRUGINFO D06NKJ 8-Methoxy-2-phenyl-3H-quinazolin-4-one Investigative T06273 DRUGINFO D07BPT 8-Methyl-2-(4-nitro-phenyl)-3H-quinazolin-4-one Investigative T06273 DRUGINFO D0E5EW 8-Methyl-2-phenyl-3H-quinazolin-4-one Investigative T06273 DRUGINFO D0E0QT 8-Nitro-6H,11H-indeno[1,2-c]isoquinolin-5-one Investigative T06273 DRUGINFO D04UPQ 9-Amino-6H,11H-indeno[1,2-c]isoquinolin-5-one Investigative T06273 DRUGINFO D07BBR 9-Fluoro-6H,11H-indeno[1,2-c]isoquinolin-5-one Investigative T06273 DRUGINFO D0VY5O A-620223 Investigative T06273 DRUGINFO D05XMG AG-014376 Investigative T06273 DRUGINFO D05APM ANG-2684 Investigative T06273 DRUGINFO D02JHW ANG-2864 Investigative T06273 DRUGINFO D0M6WJ Benzo[c][1,5]naphthyridin-6(5H)-one Investigative T06273 DRUGINFO D0R7FS BPI-704001 Investigative T06273 DRUGINFO D01RXM BZ3 Investigative T06273 DRUGINFO D0ZK3L BZ5 Investigative T06273 DRUGINFO D04LDH BZ6 Investigative T06273 DRUGINFO D0JD1O Carba-Nicotinamide-Adenine-Dinucleotide Investigative T06273 DRUGINFO D02GPJ CEP-6800 Investigative T06273 DRUGINFO D0W7XH DR2313 Investigative T06273 DRUGINFO D04AYN EB-47 Investigative T06273 DRUGINFO D0CA2S HYDAMTIQ Investigative T06273 DRUGINFO D08AOV INO-1002 Investigative T06273 DRUGINFO D05SYO KR-33889 Investigative T06273 DRUGINFO D07QPV KU-58684 Investigative T06273 DRUGINFO D04QRM ME0328 Investigative T06273 DRUGINFO D00WMC N-(4-Phenylthiazol-2-yl)isonicotinamide Investigative T06273 DRUGINFO D0E2VC PD-128763 Investigative T06273 DRUGINFO D0R7HU Pyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione Investigative T06273 DRUGINFO D03VNZ Pyrrolo[3,4-e]indole-1,3(2H,6H)-dione Investigative T06273 DRUGINFO D07AGU Quinoline-8-carboxamide Investigative T06273 DRUGINFO D0P4DG S-070 Investigative T06273 DRUGINFO D0EQ1J S-111 Investigative T06273 DRUGINFO D0EW8Y Thieno-phenanthridin-6-one Investigative T06273 DRUGINFO D0E7UW TI3 Investigative T06273 DRUGINFO D0L6LO TI4 Investigative T06273 KEGGPATH hsa03410:Base excision repair T06273 KEGGPATH hsa04064:NF-kappa B signaling pathway T06273 WIKIPATH WP2355:Corticotropin-releasing hormone T06273 WIKIPATH WP2513:Nanoparticle triggered regulated necrosis T06273 WIKIPATH WP2755:Transcriptional activity of SMAD2/SMAD3:SMAD4 heterotrimer T06273 WIKIPATH WP314:FAS pathway and Stress induction of HSP regulation T06273 REACPATH R-HSA-5696400:Dual Incision in GG-NER T06273 INTEPATH caspase_pathway:Caspase Cascade in Apoptosis T06273 INTEPATH hes_heypathway:Notch-mediated HES/HEY network T06273 INTEPATH ilk_pathway:Integrin-linked kinase signaling T06273 PANTPATH P00020:FAS signaling pathway T03691 TARGETID T03691 T03691 FORMERID TTDC00130 T03691 UNIPROID LKHA4_HUMAN T03691 TARGNAME Leukotriene A-4 hydrolase (LTA4H) T03691 GENENAME LTA4H T03691 TARGTYPE Successful target T03691 SYNONYMS Leukotriene A4 hydrolase; Leukotriene A(4)Leukotriene A-4 hydrolase hydrolase; Leukotriene A(4) hydrolase; LTA4; LTA-H; LTA-4hydrolase; LTA-4 hydrolase T03691 FUNCTION Has also aminopeptidase activity. Epoxide hydrolase that catalyzes the final step in the biosynthesis of the proinflammatory mediator leukotriene B4. T03691 PDBSTRUC 6END; 6ENC; 6ENB; 5NIE; 5NID T03691 BIOCLASS Ether bond hydrolase T03691 ECNUMBER EC 3.3.2.6 T03691 SEQUENCE MPEIVDTCSLASPASVCRTKHLHLRCSVDFTRRTLTGTAALTVQSQEDNLRSLVLDTKDLTIEKVVINGQEVKYALGERQSYKGSPMEISLPIALSKNQEIVIEISFETSPKSSALQWLTPEQTSGKEHPYLFSQCQAIHCRAILPCQDTPSVKLTYTAEVSVPKELVALMSAIRDGETPDPEDPSRKIYKFIQKVPIPCYLIALVVGALESRQIGPRTLVWSEKEQVEKSAYEFSETESMLKIAEDLGGPYVWGQYDLLVLPPSFPYGGMENPCLTFVTPTLLAGDKSLSNVIAHEISHSWTGNLVTNKTWDHFWLNEGHTVYLERHICGRLFGEKFRHFNALGGWGELQNSVKTFGETHPFTKLVVDLTDIDPDVAYSSVPYEKGFALLFYLEQLLGGPEIFLGFLKAYVEKFSYKSITTDDWKDFLYSYFKDKVDVLNQVDWNAWLYSPGLPPIKPNYDMTLTNACIALSQRWITAKEDDLNSFNATDLKDLSSHQLNEFLAQTLQRAPLPLGHIKRMQEVYNFNAINNSEIRFRWLRLCIQSKWEDAIPLALKMATEQGRMKFTRPLFKDLAAFDKSHDQAVRTYQEHKASMHPVTAMLVGKDLKVD T03691 DRUGINFO D0RA5Q Bestatin Approved T03691 DRUGINFO D07VNH Acebilustat Phase 1 T03691 DRUGINFO D06XEL DG051 Discontinued in Phase 2 T03691 DRUGINFO D0I4OV (4-(thiophen-2-yl)phenyl)methanamine Investigative T03691 DRUGINFO D0J0WO (4-fluorophenyl)(pyridin-4-yl)methanone Investigative T03691 DRUGINFO D0C1XE (R)-2-((4-benzylphenoxy)methyl)piperidine Investigative T03691 DRUGINFO D00FDS (R)-2-((4-phenoxyphenoxy)methyl)piperidine Investigative T03691 DRUGINFO D06SMN (R)-2-(4-Benzylphenoxymethyl)pyrrolidine Investigative T03691 DRUGINFO D01RVF (R)-N-benzyl-4-(pyrrolidin-2-ylmethoxy)aniline Investigative T03691 DRUGINFO D0H9NZ (R/S)-2-((4-benzylphenoxy)methyl)piperazine Investigative T03691 DRUGINFO D07ZJS (R/S)-2-((4-benzylphenoxy)methyl)piperidine Investigative T03691 DRUGINFO D00TNN (R/S)-2-((4-phenoxyphenoxy)methyl)piperidine Investigative T03691 DRUGINFO D05NXQ (S)-2-((4-phenoxyphenoxy)methyl)piperidine Investigative T03691 DRUGINFO D0R7BT 1-(2,2'-bithiophen-5-yl)methanamine Investigative T03691 DRUGINFO D0V0MH 1-(4-Phenoxyphenyl)piperazine Investigative T03691 DRUGINFO D07LTR 1-(pentyloxy)-4-phenoxybenzene Investigative T03691 DRUGINFO D0P7DF 1-[4-(4-Iodophenoxy)phenyl]piperazine Investigative T03691 DRUGINFO D09BWE 1-[4-(Benzothiazol-2-yloxy)benzyl]piperidin-4-ol Investigative T03691 DRUGINFO D07TVA 1-butoxy-4-phenoxybenzene Investigative T03691 DRUGINFO D0W2OP 2-(4-benzylphenoxy)ethanamine Investigative T03691 DRUGINFO D02AYI 2-(4-phenoxyphenoxy)ethanamine Investigative T03691 DRUGINFO D0PF9Q 2-(4-Piperidin-1-ylmethylphenoxy)benzothiazole Investigative T03691 DRUGINFO D0C8MT 2-(7-(benzyloxy)-1H-indol-3-yl)ethanamine Investigative T03691 DRUGINFO D03GON 2-[4-(2-Azepan-1-ylethoxy)phenoxy]benzooxazole Investigative T03691 DRUGINFO D08UIO 2-[4-(2-Azepan-1-ylethoxy)phenoxy]benzothiazole Investigative T03691 DRUGINFO D09PGC 2-[4-(2-Morpholin-4-ylethoxy)phenoxy]benzooxazole Investigative T03691 DRUGINFO D0Q8LS 2-[4-(2-Piperidin-1-ylethyl)phenoxy]benzothiazole Investigative T03691 DRUGINFO D06RWH 2-Amino-N-[4-(phenylmethoxy)phenyl]-acetamide Investigative T03691 DRUGINFO D09DRF 3-(Benzyloxy)Pyridin-2-Amine Investigative T03691 DRUGINFO D01KOI 4-(2-amino-1,3-thiazol-4-yl)phenol Investigative T03691 DRUGINFO D0I7MC 4-(4-(pentyloxy)phenoxy)phenol Investigative T03691 DRUGINFO D01QWO 4-(4-butoxyphenoxy)phenol Investigative T03691 DRUGINFO D0Y6IV 4-(4-propoxyphenoxy)phenol Investigative T03691 DRUGINFO D0VN8V 4-[2-(4-Benzylphenoxy)ethyl]pyridine Investigative T03691 DRUGINFO D09MDO 4-amino-N-[4-(benzyloxy)phenyl]butanamide Investigative T03691 DRUGINFO D0M2CY 4S-4,5-Diamino-N-(4-phenoxyphenyl)pentanamide Investigative T03691 DRUGINFO D00YCG 5-[2-(1H-pyrrol-1-yl)ethoxy]-1H-indole Investigative T03691 DRUGINFO D00TWK 5-[2-(4-hydroxyphenyl)ethyl]benzene-1,3-diol Investigative T03691 DRUGINFO D0SZ9E 8(S)-amino-2(R)-methyl-7-oxononanoic acid Investigative T03691 DRUGINFO D0F2ME Acetate Ion Investigative T03691 DRUGINFO D00UIN JNJ-10392980 Investigative T03691 DRUGINFO D0G0JC N-(pyridin-3-ylmethyl)aniline Investigative T03691 DRUGINFO D0U1UV N1-[4-(Phenylmethoxy)phenyl]-D-aspartamine Investigative T03691 DRUGINFO D04DRM N1-[4-(Phenylmethoxy)phenyl]-D-glutamine Investigative T03691 DRUGINFO D0LZ3O N1-[4-(Phenylmethoxy)phenyl]-L-aspartamine Investigative T03691 DRUGINFO D0HA1K N1-[4-(Phenylmethoxy)phenyl]-L-glutamine Investigative T03691 DRUGINFO D04ZLZ N4-[4-(Phenylmethoxy)phenyl]-L-aspartamine Investigative T03691 DRUGINFO D09OWF N5-(4-Phenoxyphenyl)-L-glutamine Investigative T03691 DRUGINFO D02TMR N5-[(4-Phenoxy)-3-pyridyl]-L-glutamamide Investigative T03691 DRUGINFO D08WZB N5-[4-(1H-pyrrol-1-yl)phenyl]-L-glutamamide Investigative T03691 DRUGINFO D07KBF N5-[4-(2-methylphenoxy)phenyl]-L-glutamamide Investigative T03691 DRUGINFO D0DI4I N5-[4-(2-Oxo-3-phenylpropoxy)phenyl]-L-glutamine Investigative T03691 DRUGINFO D0N6TC N5-[4-(2-phenylethoxy)phenyl]-L-glutamine Investigative T03691 DRUGINFO D00FCJ N5-[4-(3-methylphenoxy)phenyl]-L-glutamamide Investigative T03691 DRUGINFO D01YJJ N5-[4-(3-Phenylpropoxy)phenyl]-L-glutamine Investigative T03691 DRUGINFO D0B9UW N5-[4-(4-(3-Furyl)phenoxy)phenyl]-L-glutamamide Investigative T03691 DRUGINFO D0G8SW N5-[4-(4-methylphenoxy)phenyl]-L-glutamamide Investigative T03691 DRUGINFO D0Z6DL N5-[4-(N-Phenylamino)phenyl]-L-glutamine Investigative T03691 DRUGINFO D0U1EV N5-[4-(Phenylmethoxy)phenyl]-D-glutamine Investigative T03691 DRUGINFO D04CZF N5-[4-(Phenylmethoxy)phenyl]-L-glutamamide Investigative T03691 DRUGINFO D08TNQ N5-[4-(Phenylmethoxy)phenyl]-L-glutamine Investigative T03691 DRUGINFO D0U2AM N5-[4-Benzylphenyl]-L-glutamamide Investigative T03691 DRUGINFO D0B0DP N6-[4-(4-methylphenoxy)phenyl]-L-homoglutamine Investigative T03691 DRUGINFO D0A2YG N-methyl-1-(2-thiophen-2-ylphenyl)methanamine Investigative T03691 DRUGINFO D03UIF SA-6541 Investigative T03691 KEGGPATH hsa00590:Arachidonic acid metabolism T03691 KEGGPATH hsa01100:Metabolic pathways T03691 WIKIPATH WP167:Eicosanoid Synthesis T03691 WIKIPATH WP2650:Arachidonic acid metabolism T03691 WHIZPATH PW000044:Arachidonic Acid Metabolism T03691 BIOCPATH PWY66-375:Leukotriene biosynthesis T11211 TARGETID T11211 T11211 FORMERID TTDS00367 T11211 UNIPROID ANDR_HUMAN T11211 TARGNAME Androgen receptor (AR) T11211 GENENAME AR T11211 TARGTYPE Successful target T11211 SYNONYMS Testosterone receptor; Nuclear receptor subfamily 3 group C member 4; NR3C4; Dihydrotestosterone receptor; DHTR T11211 FUNCTION Transcription factor activity is modulated by bound coactivator and corepressor proteins like ZBTB7A that recruits NCOR1 and NCOR2 to the androgen response elements/ARE on target genes, negatively regulating androgen receptor signaling and androgen-induced cell proliferation. Transcription activation is also down-regulated by NR0B2. Activated, but not phosphorylated, by HIPK3 and ZIPK/DAPK3. Steroid hormone receptors are ligand-activated transcription factors that regulate eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. T11211 PDBSTRUC 5VO4; 5V8Q; 5T8J; 5T8E; 5JJM T11211 BIOCLASS Nuclear hormone receptor T11211 SEQUENCE MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGLEGESLGCSGSAAAGSSGTLELPSTLSLYKSGALDEAAAYQSRDYYNFPLALAGPPPPPPPPHPHARIKLENPLDYGSAWAAAAAQCRYGDLASLHGAGAAGPGSGSPSAAASSSWHTLFTAEEGQLYGPCGGGGGGGGGGGGGGGGGGGGGGGEAGAVAPYGYTRPPQGLAGQESDFTAPDVWYPGGMVSRVPYPSPTCVKSEMGPWMDSYSGPYGDMRLETARDHVLPIDYYFPPQKTCLICGDEASGCHYGALTCGSCKVFFKRAAEGKQKYLCASRNDCTIDKFRRKNCPSCRLRKCYEAGMTLGARKLKKLGNLKLQEEGEASSTTSPTEETTQKLTVSHIEGYECQPIFLNVLEAIEPGVVCAGHDNNQPDSFAALLSSLNELGERQLVHVVKWAKALPGFRNLHVDDQMAVIQYSWMGLMVFAMGWRSFTNVNSRMLYFAPDLVFNEYRMHKSRMYSQCVRMRHLSQEFGWLQITPQEFLCMKALLLFSIIPVDGLKNQKFFDELRMNYIKELDRIIACKRKNPTSCSRRFYQLTKLLDSVQPIARELHQFTFDLLIKSHMVSVDFPEMMAEIISVQVPKILSGKVKPIYFHTQ T11211 DRUGINFO D0S7LG ARN-509 Approved T11211 DRUGINFO D0V9BD Bicalutamide Approved T11211 DRUGINFO D08TEJ Clascoterone Approved T11211 DRUGINFO D06AEO Cyproterone Approved T11211 DRUGINFO D0DV6D Darolutamide Approved T11211 DRUGINFO D09NNA Dromostanolone Approved T11211 DRUGINFO D0QK5X Enzalutamide Approved T11211 DRUGINFO D0SC8F Ethylestrenol Approved T11211 DRUGINFO D0R7JT Fludrocortisone Approved T11211 DRUGINFO D0B2WJ Flufenamic Acid Approved T11211 DRUGINFO D0L2LS Fluoxymesterone Approved T11211 DRUGINFO D0Y0SW Flutamide Approved T11211 DRUGINFO D0BC2E Hydroxyflutamide Approved T11211 DRUGINFO D00YWP Nandrolone Approved T11211 DRUGINFO D0SN9T Nilutamide Approved T11211 DRUGINFO D0U3GL Oxandrolone Approved T11211 DRUGINFO D0K0EK Prasterone Approved T11211 DRUGINFO D06XMU Testosterone Approved T11211 DRUGINFO D04DJN Dihydrotestosterone Phase 4 T11211 DRUGINFO DE4AO8 HC-1119 Phase 3 T11211 DRUGINFO D04NNJ ZANOTERONE Phase 3 T11211 DRUGINFO D04KYB ASCJ-9 Phase 2 T11211 DRUGINFO DZTX12 ASC-J9 Phase 2 T11211 DRUGINFO D0C9EN AZD5312 Phase 2 T11211 DRUGINFO D0RV6F MK-0773 Phase 2 T11211 DRUGINFO D0G1IV Testogen TDS Phase 2 T11211 DRUGINFO D0U0BU TOK-001 Phase 2 T11211 DRUGINFO D0N7DQ APC-100 Phase 1/2 T11211 DRUGINFO D3ZY1K ARV-110 Phase 1/2 T11211 DRUGINFO DS41PJ ARV-471 Phase 1/2 T11211 DRUGINFO D03CVT ONC1-13B Phase 1/2 T11211 DRUGINFO D08AAV AZD-3514 Phase 1 T11211 DRUGINFO DNY63Z CC-94676 Phase 1 T11211 DRUGINFO D0D3FP Drug 2881078 Phase 1 T11211 DRUGINFO D0C4FS DT-200 Phase 1 T11211 DRUGINFO DY7Q1O EPI-7386 Phase 1 T11211 DRUGINFO D04XWX PS-178990 Phase 1 T11211 DRUGINFO D09ZLZ RAD-140 Phase 1 T11211 DRUGINFO D0N5NC TAS3681 Phase 1 T11211 DRUGINFO D05VNP TESTOSTERONE BUCICLATE Phase 1 T11211 DRUGINFO D09IZX GW-275919 Discontinued in Phase 2 T11211 DRUGINFO D0F7WQ HE-2000 Discontinued in Phase 2 T11211 DRUGINFO D0E3EK NP-619 Discontinued in Phase 2 T11211 DRUGINFO D08NNR Testosterone glucoside Discontinued in Phase 2 T11211 DRUGINFO D03SHP GSK2849466 Discontinued in Phase 1 T11211 DRUGINFO D03KTE LGD2941 Discontinued in Phase 1 T11211 DRUGINFO D05BCA MX-4509 Discontinued in Phase 1 T11211 DRUGINFO D00ABW Opterone Discontinued in Phase 1 T11211 DRUGINFO D0S7UU PF-06260414 Discontinued in Phase 1 T11211 DRUGINFO D0BJ7W GLPG-0492 Preclinical T11211 DRUGINFO D0G6PL LG-2293 Terminated T11211 DRUGINFO D07VUD ZD-3980 Terminated T11211 DRUGINFO D01ETZ [3H]methyltrienolone Investigative T11211 DRUGINFO D06VZE [3H]mibolerone Investigative T11211 DRUGINFO D06BLF 1,2-dibromo-4-(1,2-dibromoethyl)cyclohexane Investigative T11211 DRUGINFO D07TLT 11-methyl-6,11-dihydro-5H-benzo[a]carbazol-9-ol Investigative T11211 DRUGINFO D00QVP 6,11-dihydrothiochromeno[4,3-b]indol-8-ol Investigative T11211 DRUGINFO D0W8AI Andromustine Investigative T11211 DRUGINFO D0D8QN ARN34 Investigative T11211 DRUGINFO D02RZC ASC-JMX2 Investigative T11211 DRUGINFO D0O0II ASC-JMZ1 Investigative T11211 DRUGINFO D09HQH Boldenone Investigative T11211 DRUGINFO D03KYW Calusterone Investigative T11211 DRUGINFO D0W5IF CH-4933468 Investigative T11211 DRUGINFO D0Z3WA Delta1-dihydrotestosterone Investigative T11211 DRUGINFO D04MFW DL-3 Investigative T11211 DRUGINFO D0T1DZ EPI-001 Investigative T11211 DRUGINFO D04QFY GTx-027 Investigative T11211 DRUGINFO D0NH0U HYG-440 Investigative T11211 DRUGINFO D0MM9P OXENDLONE Investigative T11211 DRUGINFO D0A7YH Palodesangren C Investigative T11211 DRUGINFO D0I3LL Palodesangren D Investigative T11211 DRUGINFO D0JI4G Palodesangren E Investigative T11211 DRUGINFO D07KOY RU-59063 Investigative T11211 DRUGINFO D0JC4J SARMs Investigative T11211 DRUGINFO D0C1UP SX-ARPC Investigative T11211 DRUGINFO D09XGK Testetrol Investigative T11211 KEGGPATH hsa04114:Oocyte meiosis T11211 KEGGPATH hsa05200:Pathways in cancer T11211 KEGGPATH hsa05215:Prostate cancer T11211 WIKIPATH WP138:Androgen receptor signaling pathway T11211 WIKIPATH WP170:Nuclear Receptors T11211 WIKIPATH WP1984:Integrated Breast Cancer Pathway T11211 WIKIPATH WP2263:Prostate Cancer T11211 WIKIPATH WP2377:Integrated Pancreatic Cancer Pathway T11211 WIKIPATH WP706:SIDS Susceptibility Pathways T11211 REACPATH R-HSA-383280:Nuclear Receptor transcription pathway T11211 REACPATH R-HSA-5625886:Activated PKN1 stimulates transcription of AR (androgen receptor) regulated genes KLK2 and KLK3 T11211 NET_PATH NetPath_2:AndrogenReceptor Signaling Pathway T11211 NET_PATH NetPath_25:FSH Signaling Pathway T11211 NET_PATH NetPath_4:EGFR1 Signaling Pathway T11211 INTEPATH ar_nongenomic_pathway:Nongenotropic Androgen signaling T11211 INTEPATH ar_pathway:Coregulation of Androgen receptor activity T11211 INTEPATH ar_tf_pathway:Regulation of Androgen receptor activity T11211 INTEPATH betacatenin_nuc_pathway:Regulation of nuclear beta catenin signaling and target gene transcription T11211 INTEPATH hes_heypathway:Notch-mediated HES/HEY network T11211 INTEPATH hnf3apathway:FOXA1 transcription factor network T11211 INTEPATH smad2_3nuclearpathway:Regulation of nuclear SMAD2/3 signaling T63484 TARGETID T63484 T63484 FORMERID TTDR00008 T63484 UNIPROID G6PD_HUMAN T63484 TARGNAME Glucose-6-phosphate dehydrogenase (G6PD) T63484 GENENAME G6PD T63484 TARGTYPE Successful target T63484 SYNONYMS Glucose-6-phosphate 1-dehydrogenase T63484 FUNCTION The main function of this enzyme is to provide reducing power (NADPH) and pentose phosphates for fatty acid and nucleic acid synthesis. Catalyzes the rate-limiting step of the oxidative pentose-phosphate pathway, which represents a route for the dissimilation of carbohydrates besides glycolysis. T63484 PDBSTRUC 6.00E+08; 6.00E+07; 5UKW; 2BHL; 2BH9 T63484 BIOCLASS CH-OH donor oxidoreductase T63484 ECNUMBER EC 1.1.1.49 T63484 SEQUENCE MAEQVALSRTQVCGILREELFQGDAFHQSDTHIFIIMGASGDLAKKKIYPTIWWLFRDGLLPENTFIVGYARSRLTVADIRKQSEPFFKATPEEKLKLEDFFARNSYVAGQYDDAASYQRLNSHMNALHLGSQANRLFYLALPPTVYEAVTKNIHESCMSQIGWNRIIVEKPFGRDLQSSDRLSNHISSLFREDQIYRIDHYLGKEMVQNLMVLRFANRIFGPIWNRDNIACVILTFKEPFGTEGRGGYFDEFGIIRDVMQNHLLQMLCLVAMEKPASTNSDDVRDEKVKVLKCISEVQANNVVLGQYVGNPDGEGEATKGYLDDPTVPRGSTTATFAAVVLYVENERWDGVPFILRCGKALNERKAEVRLQFHDVAGDIFHQQCKRNELVIRVQPNEAVYTKMMTKKPGMFFNPEESELDLTYGNRYKNVKLPDAYERLILDVFCGSQMHFVRSDELREAWRIFTPLLHQIELEKPKPIPYIYGSRGPTEADELMKRVGFQYEGTYKWVNPHKL T63484 DRUGINFO D0K0EK Prasterone Approved T63484 DRUGINFO D0O8FW EPIANDROSTERONE Phase 3 T63484 DRUGINFO D05JCG CBF-BS2 Discontinued in Phase 2 T63484 DRUGINFO D0J2FY 2'-Monophosphoadenosine 5'-Diphosphoribose Investigative T63484 DRUGINFO D01HNP Hydroxyacetic Acid Investigative T63484 DRUGINFO D0FF3D Metazamide Investigative T63484 KEGGPATH hsa00030:Pentose phosphate pathway T63484 KEGGPATH hsa00480:Glutathione metabolism T63484 KEGGPATH hsa01100:Metabolic pathways T63484 KEGGPATH hsa01130:Biosynthesis of antibiotics T63484 KEGGPATH hsa01200:Carbon metabolism T63484 KEGGPATH hsa05230:Central carbon metabolism in cancer T63484 WIKIPATH WP100:Glutathione metabolism T63484 WIKIPATH WP134:Pentose Phosphate Pathway T63484 WIKIPATH WP1848:Metabolism of carbohydrates T63484 WIKIPATH WP1946:Cori Cycle T63484 WIKIPATH WP2002:miR-targeted genes in epithelium - TarBase T63484 WIKIPATH WP2003:miR-targeted genes in leukocytes - TarBase T63484 WIKIPATH WP2004:miR-targeted genes in lymphocytes - TarBase T63484 WIKIPATH WP2005:miR-targeted genes in muscle cell - TarBase T63484 WIKIPATH WP2877:Vitamin D Receptor Pathway T63484 WIKIPATH WP2882:Nuclear Receptors Meta-Pathway T63484 WIKIPATH WP2884:NRF2 pathway T63484 WIKIPATH WP692:Sulfation Biotransformation Reaction T63484 WHIZPATH PW000055:Pentose Phosphate Pathway T63484 WHIZPATH PW000630:Warburg Effect T63484 REACPATH R-HSA-5628897:TP53 Regulates Metabolic Genes T63484 NET_PATH NetPath_7:TGF_beta_Receptor Signaling Pathway T63484 BIOCPATH OXIDATIVEPENT-PWY-1:Pentose phosphate pathway (oxidative branch) T63484 BIOCPATH PENTOSE-P-PWY:Pentose phosphate pathway T34234 TARGETID T34234 T34234 FORMERID TTDS00251 T34234 UNIPROID VDR_HUMAN T34234 TARGNAME Vitamin D3 receptor (VDR) T34234 GENENAME VDR T34234 TARGTYPE Successful target T34234 SYNONYMS Vitamin D(3) receptor; Nuclear vitamin D receptor; Nuclear receptor subfamily 1 group I member 1; NR1I1; 1,25-dihydroxyvitamin D3 receptor T34234 FUNCTION Enters the nucleus upon vitamin D3 binding where it forms heterodimers with the retinoid X receptor/RXR. The VDR-RXR heterodimers bind to specific response elements on DNA and activate the transcription of vitamin D3-responsive target genes. Plays a central role in calcium homeostasis. Nuclear receptor for calcitriol, the active form of vitamin D3 which mediates the action of this vitamin on cells. T34234 PDBSTRUC 5YT2; 5YSY; 5V39; 5GT4; 4ITF T34234 BIOCLASS Nuclear hormone receptor T34234 SEQUENCE MEAMAASTSLPDPGDFDRNVPRICGVCGDRATGFHFNAMTCEGCKGFFRRSMKRKALFTCPFNGDCRITKDNRRHCQACRLKRCVDIGMMKEFILTDEEVQRKREMILKRKEEEALKDSLRPKLSEEQQRIIAILLDAHHKTYDPTYSDFCQFRPPVRVNDGGGSHPSRPNSRHTPSFSGDSSSSCSDHCITSSDMMDSSSFSNLDLSEEDSDDPSVTLELSQLSMLPHLADLVSYSIQKVIGFAKMIPGFRDLTSEDQIVLLKSSAIEVIMLRSNESFTMDDMSWTCGNQDYKYRVSDVTKAGHSLELIEPLIKFQVGLKKLNLHEEEHVLLMAICIVSPDRPGVQDAALIEAIQDRLSNTLQTYIRCRHPPPGSHLLYAKMIQKLADLRSLNEEHSKQYRCLSFQPECSMKLTPLVLEVFGNEIS T34234 DRUGINFO D02VPX Calcidiol Approved T34234 DRUGINFO D01QUS Calcipotriol Approved T34234 DRUGINFO D0T2PL Calcitriol Approved T34234 DRUGINFO D0K5WS Cholecalciferol Approved T34234 DRUGINFO D0G8OC Dihydrotachysterol Approved T34234 DRUGINFO D0G5CF Doxercalciferol Approved T34234 DRUGINFO D06JPB Ergocalciferol Approved T34234 DRUGINFO D01UFN Falecalcitrol Approved T34234 DRUGINFO D0N1TP Paricalcitol Approved T34234 DRUGINFO D0U8CR S-06911 Phase 3 T34234 DRUGINFO D09ZJQ Seocalcitol Phase 3 T34234 DRUGINFO D0R8IE Inecalcitol oral Phase 2 T34234 DRUGINFO D05SOH CTAP-201 Phase 1 T34234 DRUGINFO D00CGH RO-23-7553 Phase 1 T34234 DRUGINFO D0P1KV PMID27454349-Compound-100 Patented T34234 DRUGINFO D0WT4I PMID27454349-Compound-101 Patented T34234 DRUGINFO D0O2HK PMID27454349-Compound-102 Patented T34234 DRUGINFO D0UK7K PMID27454349-Compound-91 Patented T34234 DRUGINFO D0P8CM PMID27454349-Compound-92 Patented T34234 DRUGINFO D09KWM PMID27454349-Compound-93 Patented T34234 DRUGINFO D0WV1W PMID27454349-Compound-94 Patented T34234 DRUGINFO D0JC8M PMID27454349-Compound-95 Patented T34234 DRUGINFO D0UY3J PMID27454349-Compound-96 Patented T34234 DRUGINFO D03ZXP PMID27454349-Compound-97 Patented T34234 DRUGINFO D00SZR PMID27454349-Compound-98 Patented T34234 DRUGINFO D0PJ2C PMID27454349-Compound-99 Patented T34234 DRUGINFO D06SBK Atocalcitol Discontinued in Phase 2 T34234 DRUGINFO D0RF9T Lexacalcitol Discontinued in Phase 2 T34234 DRUGINFO D0I4GI RO-26-9228 Discontinued in Phase 2 T34234 DRUGINFO D07BDY Tisocalcitate Discontinued in Phase 2 T34234 DRUGINFO D08KZR BXL-746 Discontinued in Phase 1 T34234 DRUGINFO D0KK4U CB-1267 Terminated T34234 DRUGINFO D0T9SJ CEP-4186 Terminated T34234 DRUGINFO D0O6WJ Ecalcidene Terminated T34234 DRUGINFO D02EHY 2MD Investigative T34234 DRUGINFO D06RBG 3-keto-lithocholic acid Investigative T34234 DRUGINFO D06DEL calcitriol-26,23-lactone Investigative T34234 DRUGINFO D0K8VA gemini Investigative T34234 DRUGINFO D0X3DK KSP-BCS-1-alpha-CHF2-1624F2-2 Investigative T34234 DRUGINFO D0XZ2P KSP-BCS-1-alpha-CHF2-20-epi-22-oxabishomo-26-OH Investigative T34234 DRUGINFO D07AHG LG190178 Investigative T34234 DRUGINFO D0C7NV MC-1301 Investigative T34234 DRUGINFO D0D6XV TEI-9647 Investigative T34234 DRUGINFO D0X0AM ZK159222 Investigative T34234 KEGGPATH hsa04961:Endocrine and other factor-regulated calcium reabsorption T34234 KEGGPATH hsa04978:Mineral absorption T34234 KEGGPATH hsa05152:Tuberculosis T34234 WIKIPATH WP1531:Vitamin D Metabolism T34234 WIKIPATH WP170:Nuclear Receptors T34234 WIKIPATH WP2289:Drug Induction of Bile Acid Pathway T34234 WIKIPATH WP2877:Vitamin D Receptor Pathway T34234 WIKIPATH WP2882:Nuclear Receptors Meta-Pathway T34234 WIKIPATH WP299:Nuclear Receptors in Lipid Metabolism and Toxicity T34234 WIKIPATH WP34:Ovarian Infertility Genes T34234 REACPATH R-HSA-383280:Nuclear Receptor transcription pathway T34234 NET_PATH NetPath_16:IL4 Signaling Pathway T34234 INTEPATH deltanp63pathway:Validated transcriptional targets of deltaNp63 isoforms T34234 INTEPATH p53downstreampathway:Direct p53 effectors T34234 INTEPATH retinoic_acid_pathway:Retinoic acid receptors-mediated signaling T34234 INTEPATH rxr_vdr_pathway:RXR and RAR heterodimerization with other nuclear receptor T34234 INTEPATH smad2_3nuclearpathway:Regulation of nuclear SMAD2/3 signaling T34234 INTEPATH tap63pathway:Validated transcriptional targets of TAp63 isoforms T34234 PANTPATH P04396:Vitamin D metabolism and pathway T13260 TARGETID T13260 T13260 FORMERID TTDS00252 T13260 UNIPROID CP19A_HUMAN T13260 TARGNAME Aromatase (CYP19A1) T13260 GENENAME CYP19A1 T13260 TARGTYPE Successful target T13260 SYNONYMS P-450AROM; Estrogen synthetase; Estrogen synthase; Cytochrome P450 19A1; Cytochrome P-450AROM; CYPXIX; CYP19; CYAR; ARO1 T13260 FUNCTION Catalyzes the formation of aromatic C18 estrogens from C19 androgens. T13260 PDBSTRUC 5JL9; 5JL7; 5JL6; 5JKW; 5JKV T13260 BIOCLASS Paired donor oxygen oxidoreductase T13260 ECNUMBER EC 1.14.14.14 T13260 SEQUENCE MVLEMLNPIHYNITSIVPEAMPAATMPVLLLTGLFLLVWNYEGTSSIPGPGYCMGIGPLISHGRFLWMGIGSACNYYNRVYGEFMRVWISGEETLIISKSSSMFHIMKHNHYSSRFGSKLGLQCIGMHEKGIIFNNNPELWKTTRPFFMKALSGPGLVRMVTVCAESLKTHLDRLEEVTNESGYVDVLTLLRRVMLDTSNTLFLRIPLDESAIVVKIQGYFDAWQALLIKPDIFFKISWLYKKYEKSVKDLKDAIEVLIAEKRRRISTEEKLEECMDFATELILAEKRGDLTRENVNQCILEMLIAAPDTMSVSLFFMLFLIAKHPNVEEAIIKEIQTVIGERDIKIDDIQKLKVMENFIYESMRYQPVVDLVMRKALEDDVIDGYPVKKGTNIILNIGRMHRLEFFPKPNEFTLENFAKNVPYRYFQPFGFGPRGCAGKYIAMVMMKAILVTLLRRFHVKTLQGQCVESIQKIHDLSLHPDETKNMLEMIFTPRNSDRCLEH T13260 DRUGINFO D0M6DO Aminoglutethimide Approved T13260 DRUGINFO D0W0BF Anastrozole Approved T13260 DRUGINFO D0D2VS Exemestane Approved T13260 DRUGINFO D0ZX1P FADROZOLE Approved T13260 DRUGINFO D0C1WH Letrozole Approved T13260 DRUGINFO D0C7JF Testolactone Approved T13260 DRUGINFO D0B4ES Atamestane + Toremifene Phase 3 T13260 DRUGINFO D08UGX LIAROZOLE Phase 2/3 T13260 DRUGINFO D02XMD BGS-649 Phase 2 T13260 DRUGINFO D0Y6OA Coumate Phase 2 T13260 DRUGINFO D0J8RR Dextromethorphan+quinidine Phase 2 T13260 DRUGINFO D02ABO NARINGENIN Phase 1 T13260 DRUGINFO D0B6PZ FORMESTANE Withdrawn from market T13260 DRUGINFO D04PSL FINROZOLE Discontinued in Phase 2 T13260 DRUGINFO D0U9LL NKS-01 Discontinued in Phase 2 T13260 DRUGINFO D0D3PF VOROZOLE Discontinued in Phase 2 T13260 DRUGINFO D0Y2OG YM-511 Discontinued in Phase 2 T13260 DRUGINFO D0FS9K MINAMESTANE Terminated T13260 DRUGINFO D06JUR Rogletimide Terminated T13260 DRUGINFO D00HVZ (+/-)-7-methoxy-2-(4-methoxyphenyl)chroman-4-one Investigative T13260 DRUGINFO D0A2FO (+/-)-7-methoxy-2-phenylchroman-4-one Investigative T13260 DRUGINFO D09XKH (2S)-5,7,2',4'-tetrahydroxyflavanone Investigative T13260 DRUGINFO D0NH6T (2S)-abyssinone II Investigative T13260 DRUGINFO D09OPA (2S)-euchrenone a7 Investigative T13260 DRUGINFO D0D7GG 1-(1-Benzyl-2-biphenyl-4-yl-ethyl)-1H-imidazole Investigative T13260 DRUGINFO D01IJX 1-(2-(benzo[b]thiophen-4-yl)ethyl)-1H-imidazole Investigative T13260 DRUGINFO D08TKB 1-(2-phenoxybenzyl)-1H-imidazole Investigative T13260 DRUGINFO D0D0DR 1-(3-(4-fluorophenyl)propyl)-1H-imidazole Investigative T13260 DRUGINFO D03KLN 1-(3-Methoxy-naphthalen-2-yl)-1H-imidazole Investigative T13260 DRUGINFO D0XS6T 1-(4-Aminophenyl)-2-(1H-imidazol-1-yl)ethanone Investigative T13260 DRUGINFO D05FFY 1-(4-Cyanobenzyl)-5-methyl-1H-imidazole Investigative T13260 DRUGINFO D0V3MV 1-(4-nitro-2-phenoxybenzyl)-1H-imidazole Investigative T13260 DRUGINFO D0F4WQ 1-(4-Nitro-2-phenylsulfanylbenzyl)-1H-imidazole Investigative T13260 DRUGINFO D0S0OV 1-(7-Methoxy-2-phenyl-chroman-4-yl)-1H-imidazole Investigative T13260 DRUGINFO D07TIJ 1-(9H-fluoren-9-yl)-1H-imidazole Investigative T13260 DRUGINFO D0GL0L 1-(9-phenyl-9H-fluoren-9-yl)-1H-1,2,4-triazole Investigative T13260 DRUGINFO D02SIT 1-(9-Phenyl-9H-fluoren-9-yl)1H-imidazole Investigative T13260 DRUGINFO D0I5PY 1-(biphenyl-3-ylmethyl)-1H-1,2,4-triazole Investigative T13260 DRUGINFO D0P3ND 1-[(7-Fluoronaphth-2-yl)methyl]-1H-imidazole Investigative T13260 DRUGINFO D0C3XU 10-EPI-8-DEOXY-CUMAMBRIN B Investigative T13260 DRUGINFO D04TBB 11BETA,13-DIHYDRO-10-EPI-8-DEOXYCUMAM-BRIN B Investigative T13260 DRUGINFO D07PHV 1-Bromo-4-imidazol-1-ylmethyl-xanthen-9-one Investigative T13260 DRUGINFO D06FHE 1-Ethyl-5-(imidazol-1-yl-phenyl-methyl)-1H-indole Investigative T13260 DRUGINFO D07CTI 1-Imidazol-1-ylmethyl-4-nitro-xanthen-9-one Investigative T13260 DRUGINFO D01SZX 1-Imidazol-1-ylmethylxanthen-9-one Investigative T13260 DRUGINFO D0G6QL 1-Naphthalen-2-yl-1H-imidazole Investigative T13260 DRUGINFO D08UQH 2-(1H-Imidazol-1-yl)-1-(4-nitrophenyl)ethanone Investigative T13260 DRUGINFO D0B8PE 2-(3-hydroxyphenyl)-7-methoxychroman-4-one Investigative T13260 DRUGINFO D0W3LM 2-(4-hydroxyphenyl)-7-methoxychroman-4-one Investigative T13260 DRUGINFO D0K5GG 2,3,4-Trimethoxy-4'-amino-trans-stilbene Investigative T13260 DRUGINFO D0G2JV 2,3,5-Trimethoxy-4'-amino-trans-stilbene Investigative T13260 DRUGINFO D0F4MF 2,3-Dimethoxy-4'-amino-trans-stilbene Investigative T13260 DRUGINFO D0A7PA 2,4-Dimethoxy-3'-amino-trans-stilbene Investigative T13260 DRUGINFO D0I1SI 2,4-Dimethoxy-4'-amino-trans-stilbene Investigative T13260 DRUGINFO D0W7GU 2,5-Dimethoxy-4'-amino-trans-stilbene Investigative T13260 DRUGINFO D0W4IB 2-Imidazol-1-yl-7-methoxy-3-phenyl-chromen-4-one Investigative T13260 DRUGINFO D0AW7Q 2-Imidazol-1-ylmethylxanthen-9-one Investigative T13260 DRUGINFO D08FOJ 2-phenyl-2,3-dihydrobenzo[h]chromen-4-one Investigative T13260 DRUGINFO D07FGX 2-Phenyl-3-pyridin-4-ylmethylene-chroman-4-one Investigative T13260 DRUGINFO D0O0BL 2-Phenyl-4-[1,2,4]triazol-1-yl-chroman-7-ol Investigative T13260 DRUGINFO D04WJN 3-((1H-imidazol-1-yl)methyl)-9H-xanthen-9-one Investigative T13260 DRUGINFO D0MA9G 3-(1-ethyl-3,4-dihydronaphthalen-2-yl)-pyridine Investigative T13260 DRUGINFO D0K5KG 3-(1-methyl-3,4-dihydronaphthalen-2-yl)-pyridine Investigative T13260 DRUGINFO D02XTS 3-(2,2-Diphenyl-vinyl)-pyridine Investigative T13260 DRUGINFO D0I5NW 3-(3,4-dihydronaphthalen-2-yl)pyridine Investigative T13260 DRUGINFO D08HPU 3-(3-methyl-3,4-dihydronaphthalen-2-yl)pyridine Investigative T13260 DRUGINFO D01MPK 3-(4-Amino-phenyl)-1-methyl-pyrrolidine-2,5-dione Investigative T13260 DRUGINFO D0B5MZ 3-(4-Amino-phenyl)-3-butyl-piperidine-2,6-dione Investigative T13260 DRUGINFO D0Z1OI 3-(4-Amino-phenyl)-3-ethyl-pyrrolidine-2,5-dione Investigative T13260 DRUGINFO D0E2RV 3-(4-Amino-phenyl)-3-heptyl-piperidine-2,6-dione Investigative T13260 DRUGINFO D0O1ZM 3-(4-Amino-phenyl)-3-hexyl-piperidine-2,6-dione Investigative T13260 DRUGINFO D05HRP 3-(4-Amino-phenyl)-3-methyl-pyrrolidine-2,5-dione Investigative T13260 DRUGINFO D0A2GB 3-(4-Amino-phenyl)-3-pentyl-piperidine-2,6-dione Investigative T13260 DRUGINFO D0AM2Z 3-(4-Amino-phenyl)-3-propyl-piperidine-2,6-dione Investigative T13260 DRUGINFO D0H1LK 3-(4-Amino-phenyl)-pyrrolidine-2,5-dione Investigative T13260 DRUGINFO D0X1QS 3-(4-methyl-3,4-dihydronaphthalen-2-yl)pyridine Investigative T13260 DRUGINFO D04IBH 3-(5-Bromo-6-methoxy-naphthalen-2-yl)-pyridine Investigative T13260 DRUGINFO D08ZTZ 3-(5-Chloro-6-methoxy-naphthalen-2-yl)-pyridine Investigative T13260 DRUGINFO D0R0TE 3-(6-Ethoxy-naphthalen-2-yl)-pyridine Investigative T13260 DRUGINFO D0NX0M 3-(6-methoxy-3,4-dihydronaphthalen-2-yl)pyridine Investigative T13260 DRUGINFO D0N1PQ 3-(6-methoxynaphthalen-2-yl)pyridine Investigative T13260 DRUGINFO D00BVP 3-(imidazolylmethyl)-4'-methoxyflavone Investigative T13260 DRUGINFO D08EZA 3-(imidazolylmethyl)-4'-nitroflavone Investigative T13260 DRUGINFO D04VRY 3-(imidazolylmethyl)-7-methoxy-4'-nitroflavone Investigative T13260 DRUGINFO D07SOM 3-(imidazolylmethyl)flavone Investigative T13260 DRUGINFO D08FAB 3-(naphthalen-2-yl)pyridine Investigative T13260 DRUGINFO D08KLN 3,4'-(Ethane-1,2-diyl)dibenzenamine Investigative T13260 DRUGINFO D0NB8V 3,4,5-Trimethoxy-3'-amino-trans-stilbene Investigative T13260 DRUGINFO D09MQF 3,4,5-Trimethoxy-4'-amino-trans-stilbene Investigative T13260 DRUGINFO D07JKK 3,4-bis(3,4-dimethoxyphenyl)furan-2(5H)-one Investigative T13260 DRUGINFO D0T0CK 3,4-Dimethoxy-4'-amino-trans-stilbene Investigative T13260 DRUGINFO D0S7VY 3,5-Diacetoxy-4'-amino-trans-stilbene Investigative T13260 DRUGINFO D03FBI 3,5-Diamino-4'-amino-trans-stilbene Investigative T13260 DRUGINFO D0J4VR 3,5-Dihydroxyl-4'-amino-trans-stilbene Investigative T13260 DRUGINFO D0Q8UZ 3,5-Dimethoxy-4'-amino-trans-stilbene Investigative T13260 DRUGINFO D0TM4K 3-[3-Methyl-indan-(1E)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D02BWQ 3-[3-Methyl-indan-(1Z)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D0Y0CT 3-[3-Phenyl-indan-(1E)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D0V3YH 3-[4-Chloro-indan-(1E)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D05MQE 3-[4-Chloro-indan-(1Z)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D04QPK 3-[4-Fluoro-indan-(1E)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D0L1JF 3-[4-Fluoro-indan-(1Z)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D04CLL 3-[4-Methyl-indan-(1E)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D0AH1B 3-[4-Methyl-indan-(1Z)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D08AZK 3-[5-Bromo-indan-(1E)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D0U7RR 3-[5-Bromo-indan-(1Z)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D02NAG 3-[5-Chloro-indan-(1E)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D04ELJ 3-[5-Chloro-indan-(1Z)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D0N9PY 3-[5-Ethoxy-indan-(1E)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D0Q3JZ 3-[5-Ethoxy-indan-(1Z)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D0V8CR 3-[5-Fluoro-indan-(1E)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D0M7FS 3-[5-Fluoro-indan-(1Z)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D09YXV 3-[5-Methoxy-indan-(1E)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D08PNF 3-[5-Methoxy-indan-(1Z)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D00VUO 3-[6-Methoxy-indan-(1E)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D0AY4E 3-[6-Methyl-indan-(1E)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D0Y7RB 3-[6-Methyl-indan-(1Z)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D0YS2F 3-[7-Methoxy-indan-(1E)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D0Q6XB 3-Amino-4'-amino-trans-stilbene Investigative T13260 DRUGINFO D00GCK 3-Fluoren-9-ylidenemethyl-pyridine Investigative T13260 DRUGINFO D0Q0BK 3-Fluoro-4'-(pyridin-4-ylmethyl)biphenyl-4-ol Investigative T13260 DRUGINFO D01SUE 3-Indan-(1E)-ylidenemethyl-pyridine Investigative T13260 DRUGINFO D07PYC 3-Indan-(1Z)-ylidenemethyl-pyridine Investigative T13260 DRUGINFO D07UVN 3-Methoxyl-4'-amino-trans-stilbene Investigative T13260 DRUGINFO D0J8FS 3-Nitro-4'-nitro-trans-stilbene Investigative T13260 DRUGINFO D0M5EW 4-((1H-imidazol-1-yl)methyl)-2H-chromen-2-one Investigative T13260 DRUGINFO D09HEA 4-((1H-imidazol-1-yl)methyl)benzonitrile Investigative T13260 DRUGINFO D0N7QV 4-(1-Imidazol-1-yl-vinyl)-benzonitrile Investigative T13260 DRUGINFO D0U6NJ 4-(2-(1H-imidazol-1-yl)ethoxy)-2H-chromen-2-one Investigative T13260 DRUGINFO D0Z4GR 4-(2,2-Diphenyl-vinyl)-pyridine Investigative T13260 DRUGINFO D04HVL 4-(3,4,5-Trimethoxyphenethyl)aniline Investigative T13260 DRUGINFO D0O6ZM 4-(3,4-Dimethoxyphenethyl)aniline Investigative T13260 DRUGINFO D0WK9Q 4-(3,5-Dimethoxyphenethyl)benzenamine Investigative T13260 DRUGINFO D01REI 4'-(Pyridin-4-ylmethyl)biphenyl-3,4-diol Investigative T13260 DRUGINFO D0WN9P 4'-(Pyridin-4-ylmethyl)biphenyl-3-amine Investigative T13260 DRUGINFO D0I1YH 4-[(3'-Hydroxybiphenyl-4-yl)methyl]pyridine Investigative T13260 DRUGINFO D03EXD 4-[(4'-Hydroxybiphenyl-4-yl)methyl]pyridine Investigative T13260 DRUGINFO D0D9FR 4-[5-Bromo-indan-(1Z)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D0YD9J 4-[5-Chloro-indan-(1E)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D0F5YU 4-[5-Chloro-indan-(1Z)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D03MKT 4-[5-Fluoro-indan-(1E)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D09HOE 4-[5-Fluoro-indan-(1Z)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D09HGK 4-[5-Methoxy-indan-(1E)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D07ZYL 4-[5-Methoxy-indan-(1Z)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D0K3CE 4-[6-Methoxy-indan-(1E)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D0J2WW 4-[6-Methoxy-indan-(1Z)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D0D8GU 4-[6-Methyl-indan-(1E)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D07ZCD 4-[6-Methyl-indan-(1Z)-ylidenemethyl]-pyridine Investigative T13260 DRUGINFO D0M8RO 4-ANDROSTENE-3-17-DIONE Investigative T13260 DRUGINFO D07IQG 4-Bromo-1-imidazol-1-ylmethyl-xanthen-9-one Investigative T13260 DRUGINFO D06WPP 4'-bromo-3-(imidazolylmethyl)-7-methoxyflavone Investigative T13260 DRUGINFO D09ZHX 4'-bromo-3-(imidazolylmethyl)flavone Investigative T13260 DRUGINFO D05PXK 4'-cyano-3-(imidazolylmethyl)-7-methoxyflavone Investigative T13260 DRUGINFO D0CR6B 4'-cyano-3-(imidazolylmethyl)flavone Investigative T13260 DRUGINFO D04IJE 4-Fluoren-9-ylidenemethyl-pyridine Investigative T13260 DRUGINFO D0J3PK 4-Imidazol-1-yl-2-phenyl-chroman-7-ol Investigative T13260 DRUGINFO D0W9ZC 4-Imidazol-1-ylmethyl-1-nitrothioxanthen-9-one Investigative T13260 DRUGINFO D01LOU 4-Imidazol-1-ylmethyl-1-nitro-xanthen-9-one Investigative T13260 DRUGINFO D0HC9U 4-Imidazol-1-ylmethyl-2-nitroxanthen-9-one Investigative T13260 DRUGINFO D0K5JU 4-Imidazol-1-ylmethyl-3-nitroxanthen-9-one Investigative T13260 DRUGINFO D0I2UE 4-Imidazol-1-ylmethylthioxanthen-9-one Investigative T13260 DRUGINFO D0F5AC 4-Imidazol-1-ylmethylxanthen-9-one Investigative T13260 DRUGINFO D05YNW 4-Indan-(1E)-ylidenemethyl-pyridine Investigative T13260 DRUGINFO D02CSU 4-Indan-(1Z)-ylidenemethyl-pyridine Investigative T13260 DRUGINFO D0Y0QI 5-((1H-imidazol-1-yl)methyl)-7,8-dihydroquinoline Investigative T13260 DRUGINFO D0X8UK 5-(2-(1H-imidazol-1-yl)ethyl)quinoline Investigative T13260 DRUGINFO D0E9WX 5-[5-Bromo-indan-(1E)-ylidenemethyl]-1H-imidazole Investigative T13260 DRUGINFO D02XHH 5-[5-Bromo-indan-(1Z)-ylidenemethyl]-1H-imidazole Investigative T13260 DRUGINFO D06HFV 5-[5-Fluoro-indan-(1E)-ylidenemethyl]-pyrimidine Investigative T13260 DRUGINFO D04REX 5-[5-Fluoro-indan-(1Z)-ylidenemethyl]-pyrimidine Investigative T13260 DRUGINFO D0C8EO 5-[5-Methoxy-indan-(1E)-ylidenemethyl]-thiazole Investigative T13260 DRUGINFO D0U6IT 5-[5-Methoxy-indan-(1Z)-ylidenemethyl]-thiazole Investigative T13260 DRUGINFO D0UI8Q 5-Bromo-8-imidazol-1-ylmethyl-chromen-4-one Investigative T13260 DRUGINFO D03TRM 5-Indan-(1E)-ylidenemethyl-1H-imidazole Investigative T13260 DRUGINFO D09QDY 5-Indan-(1Z)-ylidenemethyl-1H-imidazole Investigative T13260 DRUGINFO D0K2DR 5-Pyridin-3-yl-1,3-dihydro-2H-indol-2-one Investigative T13260 DRUGINFO D0G9WP 5-Pyridin-3-yl-2,3-dihydro-1H-inden-1-one Investigative T13260 DRUGINFO D0T2IX 6-((1H-imidazol-1-yl)methyl)-2H-chromene-2-thione Investigative T13260 DRUGINFO D08PKR 6-Imidazol-1-yl-isoquinoline Investigative T13260 DRUGINFO D0OY1J 7-((1H-imidazol-1-yl)methyl)-2H-chromen-2-one Investigative T13260 DRUGINFO D0DJ3R 7-((1H-imidazol-1-yl)methyl)-4H-chromen-4-one Investigative T13260 DRUGINFO D0PU5V 7-((1H-imidazol-1-yl)methyl)isoquinoline Investigative T13260 DRUGINFO D07TUX 7-(2-(1H-imidazol-1-yl)ethoxy)-2H-chromen-2-one Investigative T13260 DRUGINFO D0SY6C 7,4'-Dihydroxyflavone Investigative T13260 DRUGINFO D0L9BT 7-[1,2,4]Triazol-4-ylmethyl-chromen-4-one Investigative T13260 DRUGINFO D0Y0EK 7-hydroxy-2-(3-hydroxyphenyl)chroman-4-one Investigative T13260 DRUGINFO D05ZPO 7-hydroxy-2-phenylchroman-4-one Investigative T13260 DRUGINFO D0V8SM 8-Imidazol-1-ylmethyl-5-nitro-chromen-4-one Investigative T13260 DRUGINFO D0V0DB 9-Hydroxy-7,8-benzoflavone Investigative T13260 DRUGINFO D01OQW ALBANOL A Investigative T13260 DRUGINFO D0I7GE ALPHA-NAPHTHOFLAVONE Investigative T13260 DRUGINFO D0W9PF ANDROSTENEDONE Investigative T13260 DRUGINFO D00RIX APIGENIN Investigative T13260 DRUGINFO D0QL1V Benzyl-biphenyl-4-ylmethyl-imidazol-1-yl-amine Investigative T13260 DRUGINFO D0S9YX biochanin A Investigative T13260 DRUGINFO D0W3LG Broussoflavonol F Investigative T13260 DRUGINFO D0V1UY CGS-18320B Investigative T13260 DRUGINFO D01UYI Chrysin Investigative T13260 DRUGINFO D0U9QB DEHYDROLEUCODIN Investigative T13260 DRUGINFO D0Y8XJ Docosapentaenoic acid Investigative T13260 DRUGINFO D0S0RK flavone Investigative T13260 DRUGINFO D05IWY Gamma-mangostin Investigative T13260 DRUGINFO D05YJR GARCINONE D Investigative T13260 DRUGINFO D0Z7EL GOSSYPETIN Investigative T13260 DRUGINFO D09ZIW Isogemichalcone C Investigative T13260 DRUGINFO D0E5FV ISOLICOFLAVONOL Investigative T13260 DRUGINFO D0K4PY LIQUIRTIGENIN Investigative T13260 DRUGINFO D06HJB LUDARTIN Investigative T13260 DRUGINFO D0M2IB MDL-18962 Investigative T13260 DRUGINFO D0F8IB MONODICTYOCHROMONE B Investigative T13260 DRUGINFO D0U8JC MORACHALCONE A Investigative T13260 DRUGINFO D08IIW MR-16089 Investigative T13260 DRUGINFO D0DO1T MR-20492 Investigative T13260 DRUGINFO D02LTV MR-20494 Investigative T13260 DRUGINFO D0R4WW MR-20496 Investigative T13260 DRUGINFO D00AVS MR-20814 Investigative T13260 DRUGINFO D0C5ZP N-(2-benzyloxy-4-nitrophenyl)methanesulfonamide Investigative T13260 DRUGINFO D0F9MQ N-(2-hexyloxy-4-nitrophenyl)methanesulfonamide Investigative T13260 DRUGINFO D04DZZ N-(2-nonyloxy-4-nitrophenyl)methanesulfonamide Investigative T13260 DRUGINFO D0E3IK N-(2-Propyloxy-4-nitrophenyl)methanesulfonamide Investigative T13260 DRUGINFO D0M0FE N-[2-(4'-Nitrophenyl)ethyl]-imidazole Investigative T13260 DRUGINFO D0R2YN NSC-122427 Investigative T13260 DRUGINFO D00ZPJ NSC-12999 Investigative T13260 DRUGINFO D06AZC NSC-131736 Investigative T13260 DRUGINFO D07PHT NSC-289311 Investigative T13260 DRUGINFO D06GIV NSC-356483 Investigative T13260 DRUGINFO D0S8MJ NSC-356781 Investigative T13260 DRUGINFO D08ARY NSC-368272 Investigative T13260 DRUGINFO D02QSH NSC-368280 Investigative T13260 DRUGINFO D0Y4TE NSC-369087 Investigative T13260 DRUGINFO D0M4CX NSC-613604 Investigative T13260 DRUGINFO D0Y9HD NSC-625409 Investigative T13260 DRUGINFO D0T3ED NSC-666292 Investigative T13260 DRUGINFO D0HR9S NSC-683634 Investigative T13260 DRUGINFO D08AAP NSC-75308 Investigative T13260 DRUGINFO D09MYQ NSC-93358 Investigative T13260 DRUGINFO D01KKU NSC-94258 Investigative T13260 DRUGINFO D0P5ZV NSC-94891 Investigative T13260 DRUGINFO D0Y1EX Org-33201 Investigative T13260 KEGGPATH hsa00140:Steroid hormone biosynthesis T13260 KEGGPATH hsa01100:Metabolic pathways T13260 KEGGPATH hsa04913:Ovarian steroidogenesis T13260 WIKIPATH WP1879:Phase 1 - Functionalization of compounds T13260 WIKIPATH WP1984:Integrated Breast Cancer Pathway T13260 WIKIPATH WP2035:FSH signaling pathway T13260 WIKIPATH WP2749:Metabolism of steroid hormones and vitamin D T13260 WIKIPATH WP34:Ovarian Infertility Genes T13260 WIKIPATH WP43:Oxidation by Cytochrome P450 T13260 WIKIPATH WP465:Tryptophan metabolism T13260 WIKIPATH WP702:Metapathway biotransformation T13260 WHIZPATH PW000045:Androgen and Estrogen Metabolism T13260 REACPATH R-HSA-211976:Endogenous sterols T13260 NET_PATH NetPath_25:FSH Signaling Pathway T13260 PANTPATH P02727:Androgen/estrogene/progesterone biosynthesis T13260 BIOCPATH PWY66-380:Estradiol biosynthesis I T13260 BIOCPATH PWY-7305:Superpathway of steroid hormone biosynthesis T13260 BIOCPATH PWY-7306:Estradiol biosynthesis II T85799 TARGETID T85799 T85799 FORMERID TTDC00165 T85799 UNIPROID CDK4_HUMAN T85799 TARGNAME Cyclin-dependent kinase 4 (CDK4) T85799 GENENAME CDK4 T85799 TARGTYPE Successful target T85799 SYNONYMS PSK-J3; Cell division protein kinase 4 T85799 FUNCTION Phosphorylation of RB1 allows dissociation of the transcription factor E2F from the RB/E2F complexes and the subsequent transcription of E2F target genes which are responsible for the progression through the G(1) phase. Hypophosphorylates RB1 in early G(1) phase. Cyclin D-CDK4 complexes are major integrators of various mitogenenic and antimitogenic signals. Also phosphorylates SMAD3 in a cell-cycle-dependent manner and represses its transcriptional activity. Component of the ternary complex, cyclin D/CDK4/CDKN1B, required for nuclear translocation and activity of the cyclin D-CDK4 complex. Ser/Thr-kinase component of cyclin D-CDK4 (DC) complexes that phosphorylate and inhibit members of the retinoblastoma (RB) protein family including RB1 and regulate the cell-cycle during G(1)/S transition. T85799 PDBSTRUC 5FWP; 5FWM; 5FWL; 5FWK; 3G33 T85799 BIOCLASS Kinase T85799 ECNUMBER EC 2.7.11.22 T85799 SEQUENCE MATSRYEPVAEIGVGAYGTVYKARDPHSGHFVALKSVRVPNGGGGGGGLPISTVREVALLRRLEAFEHPNVVRLMDVCATSRTDREIKVTLVFEHVDQDLRTYLDKAPPPGLPAETIKDLMRQFLRGLDFLHANCIVHRDLKPENILVTSGGTVKLADFGLARIYSYQMALTPVVVTLWYRAPEVLLQSTYATPVDMWSVGCIFAEMFRRKPLFCGNSEADQLGKIFDLIGLPPEDDWPRDVSLPRGAFPPRGPRPVQSVVPEMEESGAQLLLEMLTFNPHKRISAFRALQHSYLHKDEGNPE T85799 DRUGINFO D07ESC Apremilast Approved T85799 DRUGINFO D05SBO LY2835219 Approved T85799 DRUGINFO D00UZR Palbociclib Approved T85799 DRUGINFO D01HVT Ribociclib Succinate Approved T85799 DRUGINFO D0AP9E Trilaciclib Approved T85799 DRUGINFO D08MXP LEE011 Phase 3 T85799 DRUGINFO D0WU1O G1T38 Phase 2 T85799 DRUGINFO D0W8IY P-276 Phase 2 T85799 DRUGINFO D05IRT P276-00 Phase 2 T85799 DRUGINFO D01UMT Ro 31-7453 Phase 2 T85799 DRUGINFO D8ZV2Q FCN-437 Phase 1/2 T85799 DRUGINFO D4IS0G GLR2007 Phase 1/2 T85799 DRUGINFO D0IX4B AG-024322 Phase 1 T85799 DRUGINFO DKCU40 FN-1501 Phase 1 T85799 DRUGINFO D01XZG G1T28-1 Phase 1 T85799 DRUGINFO D0DX4J P1446A-05 Phase 1 T85799 DRUGINFO DZJ3D5 PF-07220060 Phase 1 T85799 DRUGINFO D0P1CV PHA-793887 Phase 1 T85799 DRUGINFO D03DKV RGB-286638 Phase 1 T85799 DRUGINFO D0WT7D Imidazo pyridine derivative 3 Patented T85799 DRUGINFO D0LX6X Indole-based analog 13 Patented T85799 DRUGINFO D0W4MN Isoquinoline 1,3-dione derivative 1 Patented T85799 DRUGINFO D0M5DX Oxazolyl methylthiothiazole derivative 1 Patented T85799 DRUGINFO D03HED Palbociclib/ribociclib analog 1 Patented T85799 DRUGINFO D0X5VI PMID25726713-Compound-47 Patented T85799 DRUGINFO D0WJ3W PMID25726713-Compound-48 Patented T85799 DRUGINFO D07TVO PMID25726713-Compound-49 Patented T85799 DRUGINFO D0Y8JF PMID25726713-Compound-50 Patented T85799 DRUGINFO D0KH7Q PMID25726713-Compound-51 Patented T85799 DRUGINFO D0H4HD PMID25991433-Compound-A1 Patented T85799 DRUGINFO D0FQ6V PMID26161698-Compound-17 Patented T85799 DRUGINFO D04AKA Pyrrolo[2,3-d]pyrimidine derivative 10 Patented T85799 DRUGINFO D08KKC Pyrrolo[2,3-d]pyrimidine derivative 9 Patented T85799 DRUGINFO D0NV9O BAY 10-00394 Discontinued in Phase 2 T85799 DRUGINFO D04FHB R547 Discontinued in Phase 1 T85799 DRUGINFO D00VBT ZK 304709 Discontinued in Phase 1 T85799 DRUGINFO D07ZJC INOC-005 Preclinical T85799 DRUGINFO D0Y6HA CYC-103 Terminated T85799 DRUGINFO D0Z0KD PD-0183812 Terminated T85799 DRUGINFO D0G4JS 1-(1H-Indazol-6-yl)-3-pyridin-2-yl-urea Investigative T85799 DRUGINFO D0M8CO 1-(7-Hydroxy-naphthalen-1-yl)-3-pyridin-2-yl-urea Investigative T85799 DRUGINFO D0X1NW 1-(9-Oxo-9H-fluoren-4-yl)-3-pyridin-2-yl-urea Investigative T85799 DRUGINFO D0W6CE 10-hydroxy-18-methoxybetaenone Investigative T85799 DRUGINFO D0T2VG 1-Pyridin-2-yl-3-quinolin-5-yl-urea Investigative T85799 DRUGINFO D0EK0G 3-(4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione Investigative T85799 DRUGINFO D06AOY 3-(indole-3-yl)-4-phenyl-1H-pyrrole-2,5-dione Investigative T85799 DRUGINFO D00NYT 3,4-di-(4-methoxyphenyl)-1H-pyrrole-2,5-dione Investigative T85799 DRUGINFO D0C3WY 3,4-diphenyl-1H-pyrrole-2,5-dione Investigative T85799 DRUGINFO D0A5RM 4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol Investigative T85799 DRUGINFO D07HPE Cdk4 inhibitor III Investigative T85799 DRUGINFO D09OAH Fascaplysin Investigative T85799 DRUGINFO D0D5HQ K00024 Investigative T85799 DRUGINFO D03VDM N-(2-(1H-Indol-3-yl)ethyl)biphenyl-4-carboxamide Investigative T85799 DRUGINFO D0VD8B NSC-625987 Investigative T85799 DRUGINFO D0Y5RO NU-6102 Investigative T85799 DRUGINFO D04WFN NU6140 Investigative T85799 DRUGINFO D0P6JS PMID18986805C9b Investigative T85799 DRUGINFO D02DLC PYRAZOLOPYRIDAZINE 1 Investigative T85799 DRUGINFO D0O0VP PYRAZOLOPYRIDAZINE 2 Investigative T85799 DRUGINFO D09RYV Ro-0505124 Investigative T85799 KEGGPATH hsa04110:Cell cycle T85799 KEGGPATH hsa04115:p53 signaling pathway T85799 KEGGPATH hsa04151:PI3K-Akt signaling pathway T85799 KEGGPATH hsa04530:Tight junction T85799 KEGGPATH hsa04660:T cell receptor signaling pathway T85799 KEGGPATH hsa05161:Hepatitis B T85799 KEGGPATH hsa05162:Measles T85799 KEGGPATH hsa05166:HTLV-I infection T85799 KEGGPATH hsa05200:Pathways in cancer T85799 KEGGPATH hsa05203:Viral carcinogenesis T85799 KEGGPATH hsa05212:Pancreatic cancer T85799 KEGGPATH hsa05214:Glioma T85799 KEGGPATH hsa05218:Melanoma T85799 KEGGPATH hsa05219:Bladder cancer T85799 KEGGPATH hsa05220:Chronic myeloid leukemia T85799 KEGGPATH hsa05222:Small cell lung cancer T85799 KEGGPATH hsa05223:Non-small cell lung cancer T85799 WIKIPATH WP1530:miRNA Regulation of DNA Damage Response T85799 WIKIPATH WP179:Cell Cycle T85799 WIKIPATH WP1858:Mitotic G1-G1/S phases T85799 WIKIPATH WP1971:Integrated Cancer pathway T85799 WIKIPATH WP1984:Integrated Breast Cancer Pathway T85799 WIKIPATH WP2032:TSH signaling pathway T85799 WIKIPATH WP2261:Signaling Pathways in Glioblastoma T85799 WIKIPATH WP2263:Prostate Cancer T85799 WIKIPATH WP2377:Integrated Pancreatic Cancer Pathway T85799 WIKIPATH WP2431:Spinal Cord Injury T85799 WIKIPATH WP2446:Retinoblastoma (RB) in Cancer T85799 WIKIPATH WP2698:Meiotic Recombination T85799 WIKIPATH WP2751:Transcriptional Regulation of White Adipocyte Differentiation T85799 WIKIPATH WP2772:S Phase T85799 WIKIPATH WP2828:Bladder Cancer T85799 WIKIPATH WP2878:PPAR Alpha Pathway T85799 WIKIPATH WP34:Ovarian Infertility Genes T85799 WIKIPATH WP45:G1 to S cell cycle control T85799 WIKIPATH WP707:DNA Damage Response T85799 REACPATH R-HSA-2559580:Oxidative Stress Induced Senescence T85799 REACPATH R-HSA-2559582:Senescence-Associated Secretory Phenotype (SASP) T85799 REACPATH R-HSA-2559585:Oncogene Induced Senescence T85799 REACPATH R-HSA-3214858:RMTs methylate histone arginines T85799 REACPATH R-HSA-381340:Transcriptional regulation of white adipocyte differentiation T85799 REACPATH R-HSA-69229:Ubiquitin-dependent degradation of Cyclin D1 T85799 REACPATH R-HSA-69231:Cyclin D associated events in G1 T85799 REACPATH R-HSA-912446:Meiotic recombination T85799 NET_PATH NetPath_11:TCR Signaling Pathway T85799 NET_PATH NetPath_21:RANKL Signaling Pathway T85799 NET_PATH NetPath_4:EGFR1 Signaling Pathway T85799 INTEPATH atf2_pathway:ATF-2 transcription factor network T85799 INTEPATH foxm1pathway:FOXM1 transcription factor network T85799 INTEPATH myc_activpathway:Validated targets of C-MYC transcriptional activation T85799 INTEPATH nfat_tfpathway:Calcineurin-regulated NFAT-dependent transcription in lymphocytes T85799 INTEPATH rb_1pathway:Regulation of retinoblastoma protein T85799 INTEPATH smad2_3nuclearpathway:Regulation of nuclear SMAD2/3 signaling T60366 TARGETID T60366 T60366 FORMERID TTDS00313 T60366 UNIPROID DCOR_HUMAN T60366 TARGNAME Ornithine decarboxylase (ODC1) T60366 GENENAME ODC1 T60366 TARGTYPE Successful target T60366 SYNONYMS ODC T60366 FUNCTION Polyamines are essential for cell proliferation and are implicated in cellular processes, ranging from DNA replication to apoptosis. Catalyzes the first and rate-limiting step of polyamine biosynthesis that converts ornithine into putrescine, which is the precursor for the polyamines, spermidine and spermine. T60366 PDBSTRUC 5BWA; 4ZGY; 2OO0; 2ON3; 1D7K T60366 BIOCLASS Carbon-carbon lyase T60366 ECNUMBER EC 4.1.1.17 T60366 SEQUENCE MNNFGNEEFDCHFLDEGFTAKDILDQKINEVSSSDDKDAFYVADLGDILKKHLRWLKALPRVTPFYAVKCNDSKAIVKTLAATGTGFDCASKTEIQLVQSLGVPPERIIYANPCKQVSQIKYAANNGVQMMTFDSEVELMKVARAHPKAKLVLRIATDDSKAVCRLSVKFGATLRTSRLLLERAKELNIDVVGVSFHVGSGCTDPETFVQAISDARCVFDMGAEVGFSMYLLDIGGGFPGSEDVKLKFEEITGVINPALDKYFPSDSGVRIIAEPGRYYVASAFTLAVNIIAKKIVLKEQTGSDDEDESSEQTFMYYVNDGVYGSFNCILYDHAHVKPLLQKRPKPDEKYYSSSIWGPTCDGLDRIVERCDLPEMHVGDWMLFENMGAYTVAAASTFNGFQRPTIYYVMSGPAWQLMQQFQNPDFPPEVEEQDASTLPVSCAWESGMKRHRAACASASINV T60366 DRUGINFO D0X7JR Eflornithine Approved T60366 DRUGINFO D00FMV Putrescine Discontinued in Phase 2 T60366 DRUGINFO D02XYV (2R,5R)-delta-methyl-alpha-acetylenic putrescine Investigative T60366 DRUGINFO D0XR2J 1-Amino-3-(aminoxy)-2-propanol Dihydrochloride Investigative T60366 DRUGINFO D0K6WI 3-(Aminooxy)propan-1-amine hydrochloride Investigative T60366 DRUGINFO D0N4YR 3-methoxy-4-hydroxylonchocarpin Investigative T60366 DRUGINFO D0F3QP 4-hydroxylonchocarpin Investigative T60366 DRUGINFO D08TLJ Alpha-monofluoromethyl-3,4-dehydroornithine Investigative T60366 DRUGINFO D0H2OA Alpha-monofluoromethyl-3,4-dehydroornithine ethyl ester Investigative T60366 DRUGINFO D08CKE Alpha-monofluoromethyl-3,4-dehydroornithine methyl ester Investigative T60366 DRUGINFO D01OHD AMXT-1501 Investigative T60366 DRUGINFO D01IGU APA Investigative T60366 DRUGINFO D03LMM G418 Investigative T60366 DRUGINFO D04ZDD LONCHOCARPUSONE Investigative T60366 DRUGINFO D09AHL N-Pyridoxyl-Glycine-5-Monophosphate Investigative T60366 DRUGINFO D0I5PZ N'-Pyridoxyl-Lysine-5'-Monophosphate Investigative T60366 DRUGINFO D0B8JD Pyridoxine-5'-Phosphate Investigative T60366 DRUGINFO D04FIN ZAPOTIN Investigative T60366 WHIZPATH PW000037:Spermidine and Spermine Biosynthesis T60366 NET_PATH NetPath_11:TCR Signaling Pathway T60366 NET_PATH NetPath_14:IL2 Signaling Pathway T60366 NET_PATH NetPath_7:TGF_beta_Receptor Signaling Pathway T60366 INTEPATH myc_activpathway:Validated targets of C-MYC transcriptional activation T60366 PANTPATH P02758:Ornithine degradation T60366 PANTPATH P06959:CCKR signaling map ST T60366 BIOCPATH PWY-46:Putrescine biosynthesis I T52227 TARGETID T52227 T52227 FORMERID TTDS00301 T52227 UNIPROID TYSY_CANAL T52227 TARGNAME Candida Thymidylate synthase (Candi TMP1) T52227 GENENAME Candi TMP1 T52227 TARGTYPE Successful target T52227 SYNONYMS Tsase of Candida albicans; TS of Candida albicans; TMP1; Human recombinant thymidylate synthase; HrTS T52227 FUNCTION Contributes to thede novo mitochondrial thymidylate biosynthesis pathway. T52227 BIOCLASS Methyltransferase T52227 ECNUMBER EC 2.1.1.45 T52227 SEQUENCE MTVSPNTAEQAYLDLCKRIIDEGEHRPDRTGTGTKSLFAPPQLRFDLSNDTFPLLTTKKVFSKGIIHELLWFVAGSTDAKILSEKGVKIWEGNGSREFLDKLGLTHRREGDLGPVYGFQWRHFGAEYKDCDSDYTGQGFDQLQDVIKKLKTNPYDRRIIMSAWNPPDFAKMALPPCHVFCQFYVNFPTSSPDPNNPKQAKTAKPKLSCLLYQRSCDMGLGVPFNIASYALLTKMIAHVVDMDCGEFIHTLGDAHVYLDHIDALKEQFERIPKQFPKLVIKEERKNEIKSIDDFKFEDFEIVGYEPYPPIKMKMSV T52227 DRUGINFO D00HCQ Capecitabine Approved T52227 DRUGINFO D0O1WX Ciprofloxacin XR Approved T52227 DRUGINFO D0TS1Z Floxuridine Approved T52227 DRUGINFO D0S5WG Flucytosine Approved T52227 DRUGINFO D05LEO Fluorouracil Approved T52227 DRUGINFO D0M3MN Leucovorin/5-fluorouracil Approved T52227 DRUGINFO D0Y4GO Pemetrexed Approved T52227 DRUGINFO D01KKQ Raltitrexed Approved T52227 DRUGINFO D05RHI Trifluridine Approved T52227 DRUGINFO D06WQT Nolatrexed Phase 3 T52227 DRUGINFO D0I9GR Plevitrexed Phase 2 T52227 DRUGINFO D04FYZ Plevitrexed (R)-isomer Phase 2 T52227 DRUGINFO D0Q0UA UFT/leucovorin calcium Phase 2 T52227 DRUGINFO D05CQS NB1011 Phase 1/2 T52227 DRUGINFO D0S9MD DFP-11207 Phase 1 T52227 DRUGINFO D0U2CT EMITEFUR Discontinued in Preregistration T52227 DRUGINFO D0Y4AZ Galocitabine Discontinued in Phase 3 T52227 DRUGINFO D0E8JO FO-152 Discontinued in Phase 2 T52227 DRUGINFO D0B6GJ TT-62 Discontinued in Phase 2 T52227 DRUGINFO D0C4YA AG-331 Discontinued in Phase 1 T52227 DRUGINFO D0L0AU DMPDDF Terminated T52227 DRUGINFO D03BTP Fosfluridine tidoxil Terminated T52227 DRUGINFO D00BNE (6s)-5,6,7,8-Tetrahydrofolate Investigative T52227 DRUGINFO D0G6CU 1,3-propanediphosphonic acid Investigative T52227 DRUGINFO D01GMJ 1,4-Dithiothreitol Investigative T52227 DRUGINFO D0PG5D 10-Propargyl-5,8-Dideazafolic Acid Investigative T52227 DRUGINFO D08STR 2'-5'dideoxyuridine Investigative T52227 DRUGINFO D05HOO 2-bromophenol Investigative T52227 DRUGINFO D06FMH 2'-Deoxycytidine-5'-Monophosphate Investigative T52227 DRUGINFO D0G9XX 2'-Deoxyguanosine-5'-Monophosphate Investigative T52227 DRUGINFO D00CVB 2'-Deoxyuridine Investigative T52227 DRUGINFO D0CZ3C 2'-deoxyuridylic acid Investigative T52227 DRUGINFO D0Q5FV 2-Sulfhydryl-Ethanol Investigative T52227 DRUGINFO D0F2VL 3-Amino-5,6-dihydro-2H-benzo[f]quinazolin-1-one Investigative T52227 DRUGINFO D0UL7N 3-DIPHENOL-6-NITRO-3H-BENZO[DE]ISOCHROMEN-1-ONE Investigative T52227 DRUGINFO D09QPT 3-Methyl-2H-benzo[f]quinazolin-1-one Investigative T52227 DRUGINFO D02MUO 4-CHLORO-3',3''-DIBROMOPHENOL-1,8-NAPHTHALEIN Investigative T52227 DRUGINFO D0A6BH 5,10-Methylene-6-Hydrofolic Acid Investigative T52227 DRUGINFO D0I0OH 5-Fluoro-2'-Deoxyuridine-5'-Monophosphate Investigative T52227 DRUGINFO D0JY6J 6-ETHYL-5-PHENYLPYRIMIDINE-2,4-DIAMINE Investigative T52227 DRUGINFO D04IRR Ly231514 Tetra Glu Investigative T52227 DRUGINFO D0X9QV LY341770 Investigative T52227 DRUGINFO D0XV3B Methionine Sulfoxide Investigative T52227 DRUGINFO D0F1LA N,O-Didansyl-L-Tyrosine Investigative T52227 DRUGINFO D0U0VO N-[Tosyl-D-Prolinyl]Amino-Ethanethiol Investigative T52227 DRUGINFO D0YX9D N-Carboxymethionine Investigative T52227 DRUGINFO D01OVV OVI-117 Investigative T52227 DRUGINFO D0UZ9U PREMETREXED Investigative T52227 DRUGINFO D0P7JE S,S-(2-Hydroxyethyl)Thiocysteine Investigative T52227 DRUGINFO D01FCH Sp-722 Investigative T52227 DRUGINFO D0K7CR Sp-876 Investigative T52227 DRUGINFO D0ZH0I Thymidine-5'-Phosphate Investigative T52227 DRUGINFO D07LML Tosyl-D-Proline Investigative T52227 DRUGINFO D0H9DJ Uridine-5'-Monophosphate Investigative T52227 DRUGINFO D0VZ0I ZD1604 Investigative T52227 KEGGPATH hsa00240:Pyrimidine metabolism T52227 KEGGPATH hsa00670:One carbon pool by folate T52227 KEGGPATH hsa01100:Metabolic pathways T52227 WIKIPATH WP1601:Fluoropyrimidine Activity T52227 WIKIPATH WP1851:Metabolism of nucleotides T52227 WIKIPATH WP2002:miR-targeted genes in epithelium - TarBase T52227 WIKIPATH WP2003:miR-targeted genes in leukocytes - TarBase T52227 WIKIPATH WP2004:miR-targeted genes in lymphocytes - TarBase T52227 WIKIPATH WP2005:miR-targeted genes in muscle cell - TarBase T52227 WIKIPATH WP2377:Integrated Pancreatic Cancer Pathway T52227 WIKIPATH WP241:One Carbon Metabolism T52227 WIKIPATH WP2446:Retinoblastoma (RB) in Cancer T52227 WIKIPATH WP2525:Trans-sulfuration and one carbon metabolism T52227 WHIZPATH PW000160:Pyrimidine Metabolism T52227 REACPATH R-HSA-113510:E2F mediated regulation of DNA replication T52227 REACPATH R-HSA-500753:Pyrimidine biosynthesis T52227 REACPATH R-HSA-69205:G1/S-Specific Transcription T52227 INTEPATH e2f_pathway:E2F transcription factor network T52227 PANTPATH P02739:De novo pyrimidine deoxyribonucleotide biosynthesis T52227 PANTPATH P02743:Formyltetrahydroformate biosynthesis T52227 BIOCPATH PWY66-385:DTMP de novo biosynthesis (mitochondrial) T52227 BIOCPATH PWY-7184:Pyrimidine deoxyribonucleotides de novo biosynthesis T52227 BIOCPATH PWY-7199:Pyrimidine deoxyribonucleosides salvage T52227 BIOCPATH PWY-7200:Superpathway of pyrimidine deoxyribonucleoside salvage T52227 BIOCPATH PWY-7210:Pyrimidine deoxyribonucleotides biosynthesis from CTP T52227 BIOCPATH PWY-7211:Superpathway of pyrimidine deoxyribonucleotides de novo biosynthesis T82577 TARGETID T82577 T82577 FORMERID TTDS00181 T82577 UNIPROID ACE_HUMAN T82577 TARGNAME Angiotensin-converting enzyme (ACE) T82577 GENENAME SLC33A1 T82577 TARGTYPE Successful target T82577 SYNONYMS Kininase II; Dipeptidyl carboxypeptidase I; DCP1; DCP; CD143 antigen; CD143; ACE T82577 FUNCTION Able to inactivate bradykinin, a potent vasodilator. Has also a glycosidase activity which releases GPI-anchored proteins from the membrane by cleaving the mannose linkage in the GPI moiety. Converts angiotensin I to angiotensin II by release of the terminal His-Leu, this results in an increase of the vasoconstrictor activity of angiotensin. T82577 PDBSTRUC 6QS1; 6H5X; 6H5W; 6F9V; 6F9U T82577 BIOCLASS Glycosylase T82577 ECNUMBER EC 3.2.1.- T82577 SEQUENCE MGAASGRRGPGLLLPLPLLLLLPPQPALALDPGLQPGNFSADEAGAQLFAQSYNSSAEQVLFQSVAASWAHDTNITAENARRQEEAALLSQEFAEAWGQKAKELYEPIWQNFTDPQLRRIIGAVRTLGSANLPLAKRQQYNALLSNMSRIYSTAKVCLPNKTATCWSLDPDLTNILASSRSYAMLLFAWEGWHNAAGIPLKPLYEDFTALSNEAYKQDGFTDTGAYWRSWYNSPTFEDDLEHLYQQLEPLYLNLHAFVRRALHRRYGDRYINLRGPIPAHLLGDMWAQSWENIYDMVVPFPDKPNLDVTSTMLQQGWNATHMFRVAEEFFTSLELSPMPPEFWEGSMLEKPADGREVVCHASAWDFYNRKDFRIKQCTRVTMDQLSTVHHEMGHIQYYLQYKDLPVSLRRGANPGFHEAIGDVLALSVSTPEHLHKIGLLDRVTNDTESDINYLLKMALEKIAFLPFGYLVDQWRWGVFSGRTPPSRYNFDWWYLRTKYQGICPPVTRNETHFDAGAKFHVPNVTPYIRYFVSFVLQFQFHEALCKEAGYEGPLHQCDIYRSTKAGAKLRKVLQAGSSRPWQEVLKDMVGLDALDAQPLLKYFQPVTQWLQEQNQQNGEVLGWPEYQWHPPLPDNYPEGIDLVTDEAEASKFVEEYDRTSQVVWNEYAEANWNYNTNITTETSKILLQKNMQIANHTLKYGTQARKFDVNQLQNTTIKRIIKKVQDLERAALPAQELEEYNKILLDMETTYSVATVCHPNGSCLQLEPDLTNVMATSRKYEDLLWAWEGWRDKAGRAILQFYPKYVELINQAARLNGYVDAGDSWRSMYETPSLEQDLERLFQELQPLYLNLHAYVRRALHRHYGAQHINLEGPIPAHLLGNMWAQTWSNIYDLVVPFPSAPSMDTTEAMLKQGWTPRRMFKEADDFFTSLGLLPVPPEFWNKSMLEKPTDGREVVCHASAWDFYNGKDFRIKQCTTVNLEDLVVAHHEMGHIQYFMQYKDLPVALREGANPGFHEAIGDVLALSVSTPKHLHSLNLLSSEGGSDEHDINFLMKMALDKIAFIPFSYLVDQWRWRVFDGSITKENYNQEWWSLRLKYQGLCPPVPRTQGDFDPGAKFHIPSSVPYIRYFVSFIIQFQFHEALCQAAGHTGPLHKCDIYQSKEAGQRLATAMKLGFSRPWPEAMQLITGQPNMSASAMLSYFKPLLDWLRTENELHGEKLGWPQYNWTPNSARSEGPLPDSGRVSFLGLDLDAQQARVGQWLLLFLGIALLVATLGLSQRLFSIRHRSLHRHSHGPQFGSEVELRHS T82577 DRUGINFO D0X5SJ Alacepril Approved T82577 DRUGINFO D0U3EC Benazepril Approved T82577 DRUGINFO D0I0EG Captopril Approved T82577 DRUGINFO D04GKO Cilazapril Approved T82577 DRUGINFO D0G8QW Delapril Approved T82577 DRUGINFO D09HDR Deserpidine Approved T82577 DRUGINFO D00SEB Enalapril Approved T82577 DRUGINFO D0N5HJ Enalaprilat Approved T82577 DRUGINFO D0X8KY Fosinopril Approved T82577 DRUGINFO D0U4UQ Hydrochlorothiazide Approved T82577 DRUGINFO D0S0ES Imidapril Approved T82577 DRUGINFO D07HGR Lisinopril Approved T82577 DRUGINFO D00HDU Moexipril Approved T82577 DRUGINFO D03KYG Perindopril Approved T82577 DRUGINFO D0I7SZ Quinapril Approved T82577 DRUGINFO D01STB Ramipril Approved T82577 DRUGINFO D0G8NJ Rescinnamine Approved T82577 DRUGINFO D05MFG Spirapril Approved T82577 DRUGINFO D02DSZ Temocapril hydrochloride Approved T82577 DRUGINFO D0M5OC Trandolapril Approved T82577 DRUGINFO D04PBH CONTIGOSIDE B Phase 2/3 T82577 DRUGINFO D00ERV Gallopamil Phase 2 T82577 DRUGINFO D0C1AY GW-796406 Phase 1 T82577 DRUGINFO D0K6SM Ilepatril Discontinued in Phase 2/3 T82577 DRUGINFO D05NRI Ceronapril Discontinued in Phase 2 T82577 DRUGINFO D08DWH Idrapril Discontinued in Phase 2 T82577 DRUGINFO D0N5HN M-100240 Discontinued in Phase 2 T82577 DRUGINFO D02JUM METIAPRIL Discontinued in Phase 2 T82577 DRUGINFO D03DRW UTIBAPRIL Discontinued in Phase 2 T82577 DRUGINFO D00FHI Zabiciprilat Discontinued in Phase 2 T82577 DRUGINFO D04MBS BMS-182657 Terminated T82577 DRUGINFO D0KR3X CGS-30440 Terminated T82577 DRUGINFO D05COG DU-1777 Terminated T82577 DRUGINFO D0F9BX GW-660511 Terminated T82577 DRUGINFO D05UQD Omapatrilat Terminated T82577 DRUGINFO D0K9YR SCH-54470 Terminated T82577 DRUGINFO D0I5QZ SQ-26332 Terminated T82577 DRUGINFO D0U7TM [Cyclopentyl-(2-nitro-benzoyl)-amino]-acetic acid Investigative T82577 DRUGINFO D06IEN 2-(Acetylamino)-2-Deoxy-a-D-Glucopyranose Investigative T82577 DRUGINFO D0F2ME Acetate Ion Investigative T82577 DRUGINFO D08BFU ASTRAGALIN Investigative T82577 DRUGINFO D07BNP BRL-36378 Investigative T82577 DRUGINFO D0EW3L BUTEIN Investigative T82577 DRUGINFO D04DHD fasidotrilat Investigative T82577 DRUGINFO D0HC9P Kaempferol-3-O-(2''-O-galloyl)-glucoside Investigative T82577 DRUGINFO D0B8WQ lisinopril-tryptophan Investigative T82577 DRUGINFO D07APP LY-292223 Investigative T82577 DRUGINFO D0R6KV moexiprilat Investigative T82577 DRUGINFO D0K8ED N-Carboxymethyl-N-cyclopentyl-phthalamic acid Investigative T82577 DRUGINFO D09GXF RB-105 Investigative T82577 DRUGINFO D0A1RG RIP Investigative T82577 DRUGINFO D0OZ3S RJM-0035-K002 Investigative T82577 DRUGINFO D02FMN RXP-407 Investigative T82577 KEGGPATH hsa04614:Renin-angiotensin system T82577 KEGGPATH hsa05142:Chagas disease (American trypanosomiasis) T82577 KEGGPATH hsa05410:Hypertrophic cardiomyopathy (HCM) T82577 WIKIPATH WP2729:Metabolism of Angiotensinogen to Angiotensins T82577 WIKIPATH WP554:ACE Inhibitor Pathway T82577 WHIZPATH PW000563:Angiotensin Metabolism T82577 REACPATH R-HSA-2022377:Metabolism of Angiotensinogen to Angiotensins T97587 TARGETID T97587 T97587 FORMERID TTDS00445 T97587 UNIPROID ITA4_HUMAN T97587 TARGNAME Integrin alpha-4 (ITGA4) T97587 GENENAME ITGA4 T97587 TARGTYPE Successful target T97587 SYNONYMS Very late antigen 4; VLA4 subunit alpha; VLA-4 subunit alpha; VLA-4; Integrin alphaIV; Integrin alpha4; Integrin alpha-IV; CD49d; CD49 antigenlike family member D; CD49 antigen-like family member D T97587 FUNCTION Integrins alpha-4/beta-1 (VLA-4) and alpha-4/beta-7 are receptors for fibronectin. They recognize one or more domains within the alternatively spliced CS-1 and CS-5 regions of fibronectin. They are also receptors for VCAM1. Integrin alpha-4/beta-1 recognizes the sequence Q-I-D-S in VCAM1. Integrin alpha-4/beta-7 is also a receptor for MADCAM1. It recognizes the sequence L-D-T in MADCAM1. On activated endothelial cells integrin VLA-4 triggers homotypic aggregation for most VLA-4-positive leukocyte cell lines. It may also participate in cytolytic T-cell interactions with target cells. ITGA4:ITGB1 binds to fractalkine (CX3CL1) and may act as its coreceptor in CX3CR1-dependent fractalkine signaling. ITGA4:ITGB1 binds to PLA2G2A via a site (site 2) which is distinct from the classical ligand-binding site (site 1) and this induces integrin conformational changes and enhanced ligand binding to site 1. T97587 PDBSTRUC 5FPI; 5C7Z; 4HKC; 3V4V; 3V4P T97587 BIOCLASS Integrin T97587 SEQUENCE MAWEARREPGPRRAAVRETVMLLLCLGVPTGRPYNVDTESALLYQGPHNTLFGYSVVLHSHGANRWLLVGAPTANWLANASVINPGAIYRCRIGKNPGQTCEQLQLGSPNGEPCGKTCLEERDNQWLGVTLSRQPGENGSIVTCGHRWKNIFYIKNENKLPTGGCYGVPPDLRTELSKRIAPCYQDYVKKFGENFASCQAGISSFYTKDLIVMGAPGSSYWTGSLFVYNITTNKYKAFLDKQNQVKFGSYLGYSVGAGHFRSQHTTEVVGGAPQHEQIGKAYIFSIDEKELNILHEMKGKKLGSYFGASVCAVDLNADGFSDLLVGAPMQSTIREEGRVFVYINSGSGAVMNAMETNLVGSDKYAARFGESIVNLGDIDNDGFEDVAIGAPQEDDLQGAIYIYNGRADGISSTFSQRIEGLQISKSLSMFGQSISGQIDADNNGYVDVAVGAFRSDSAVLLRTRPVVIVDASLSHPESVNRTKFDCVENGWPSVCIDLTLCFSYKGKEVPGYIVLFYNMSLDVNRKAESPPRFYFSSNGTSDVITGSIQVSSREANCRTHQAFMRKDVRDILTPIQIEAAYHLGPHVISKRSTEEFPPLQPILQQKKEKDIMKKTINFARFCAHENCSADLQVSAKIGFLKPHENKTYLAVGSMKTLMLNVSLFNAGDDAYETTLHVKLPVGLYFIKILELEEKQINCEVTDNSGVVQLDCSIGYIYVDHLSRIDISFLLDVSSLSRAEEDLSITVHATCENEEEMDNLKHSRVTVAIPLKYEVKLTVHGFVNPTSFVYGSNDENEPETCMVEKMNLTFHVINTGNSMAPNVSVEIMVPNSFSPQTDKLFNILDVQTTTGECHFENYQRVCALEQQKSAMQTLKGIVRFLSKTDKRLLYCIKADPHCLNFLCNFGKMESGKEASVHIQLEGRPSILEMDETSALKFEIRATGFPEPNPRVIELNKDENVAHVLLEGLHHQRPKRYFTIVIISSSLLLGLIVLLLISYVMWKAGFFKRQYKSILQEENRRDSWSYINSKSNDD T97587 DRUGINFO D09EBL Antegren Approved T97587 DRUGINFO D0N5ZS Vedolizmab Approved T97587 DRUGINFO D04WQJ AMG-181 Phase 2 T97587 DRUGINFO D0Q5LF BIO-1211 Phase 2 T97587 DRUGINFO D0C9XA GSK683699 Phase 2 T97587 DRUGINFO D05ZWG Senktide Phase 2 T97587 DRUGINFO D01CYT ELND-002 Phase 1 T97587 DRUGINFO D05JPJ ELND-004 Phase 1 T97587 DRUGINFO D0FU1J PTG-100 Phase 1 T97587 DRUGINFO D05SHQ ASP-2002 Investigative T97587 DRUGINFO D00GWR CT301 Investigative T97587 KEGGPATH hsa04151:PI3K-Akt signaling pathway T97587 KEGGPATH hsa04510:Focal adhesion T97587 KEGGPATH hsa04512:ECM-receptor interaction T97587 KEGGPATH hsa04514:Cell adhesion molecules (CAMs) T97587 KEGGPATH hsa04640:Hematopoietic cell lineage T97587 KEGGPATH hsa04670:Leukocyte transendothelial migration T97587 KEGGPATH hsa04672:Intestinal immune network for IgA production T97587 KEGGPATH hsa04810:Regulation of actin cytoskeleton T97587 KEGGPATH hsa05140:Leishmaniasis T97587 KEGGPATH hsa05410:Hypertrophic cardiomyopathy (HCM) T97587 KEGGPATH hsa05412:Arrhythmogenic right ventricular cardiomyopathy (ARVC) T97587 KEGGPATH hsa05414:Dilated cardiomyopathy T97587 WIKIPATH WP1794:Cell surface interactions at the vascular wall T97587 WIKIPATH WP1829:Immunoregulatory interactions between a Lymphoid and a non-Lymphoid cell T97587 WIKIPATH WP1833:Integrin cell surface interactions T97587 WIKIPATH WP185:Integrin-mediated Cell Adhesion T97587 WIKIPATH WP2118:Arrhythmogenic Right Ventricular Cardiomyopathy T97587 WIKIPATH WP306:Focal Adhesion T97587 REACPATH R-HSA-198933:Immunoregulatory interactions between a Lymphoid and a non-Lymphoid cell T97587 REACPATH R-HSA-202733:Cell surface interactions at the vascular wall T97587 REACPATH R-HSA-216083:Integrin cell surface interactions T97587 INTEPATH a4b7_pathway:a4b7 Integrin signaling T97587 INTEPATH arf6_traffickingpathway:Arf6 trafficking events T97587 INTEPATH cxcr4_pathway:CXCR4-mediated signaling events T97587 INTEPATH integrin_a4b1_pathway:Alpha4 beta1 integrin signaling events T97587 INTEPATH integrin_cs_pathway:Integrin family cell surface interactions T97587 INTEPATH integrin1_pathway:Beta1 integrin cell surface interactions T97587 INTEPATH integrin5_pathway:Beta5 beta6 beta7 and beta8 integrin cell surface interactions T97587 INTEPATH lymphangiogenesis_pathway:VEGFR3 signaling in lymphatic endothelium T97587 INTEPATH plexind1_pathway:Plexin-D1 Signaling T97587 PANTPATH P00034:Integrin signalling pathway T84621 TARGETID T84621 T84621 FORMERID TTDS00420 T84621 UNIPROID C11B1_HUMAN T84621 TARGNAME Steroid 11-beta-hydroxylase (CYP11B1) T84621 GENENAME CYP11B1 T84621 TARGTYPE Successful target T84621 SYNONYMS S11BH; P450C11; P-450c11; CYPXIB1; CYP11B1 T84621 FUNCTION Has steroid 11-beta-hydroxylase activity. In addition to this activity, the 18 or 19-hydroxylation of steroids and the aromatization of androstendione to estrone have also been ascribed to cytochrome P450 XIB. T84621 PDBSTRUC 6M7X T84621 BIOCLASS Paired donor oxygen oxidoreductase T84621 ECNUMBER EC 1.14.15.4 T84621 SEQUENCE MALRAKAEVCMAVPWLSLQRAQALGTRAARVPRTVLPFEAMPRRPGNRWLRLLQIWREQGYEDLHLEVHQTFQELGPIFRYDLGGAGMVCVMLPEDVEKLQQVDSLHPHRMSLEPWVAYRQHRGHKCGVFLLNGPEWRFNRLRLNPEVLSPNAVQRFLPMVDAVARDFSQALKKKVLQNARGSLTLDVQPSIFHYTIEASNLALFGERLGLVGHSPSSASLNFLHALEVMFKSTVQLMFMPRSLSRWTSPKVWKEHFEAWDCIFQYGDNCIQKIYQELAFSRPQQYTSIVAELLLNAELSPDAIKANSMELTAGSVDTTVFPLLMTLFELARNPNVQQALRQESLAAAASISEHPQKATTELPLLRAALKETLRLYPVGLFLERVASSDLVLQNYHIPAGTLVRVFLYSLGRNPALFPRPERYNPQRWLDIRGSGRNFYHVPFGFGMRQCLGRRLAEAEMLLLLHHVLKHLQVETLTQEDIKMVYSFILRPSMFPLLTFRAIN T84621 DRUGINFO D0ZX1P FADROZOLE Approved T84621 DRUGINFO D0Q9JT Metyrapone Approved T84621 DRUGINFO D03AJU Osilodrostat Approved T84621 DRUGINFO D08WHC (3-((1H-imidazol-1-yl)methyl)phenyl)methanol Investigative T84621 DRUGINFO D0N8QD (4-((1H-imidazol-1-yl)methyl)phenyl)methanol Investigative T84621 DRUGINFO D0R8NE 1-(2-Phenoxy-ethyl)-1H-imidazole Investigative T84621 DRUGINFO D0N4VI 1-(3,4-dihydronaphthalen-2-yl)-1H-imidazole Investigative T84621 DRUGINFO D07JMO 1-(3-Bromobenzyl)-1H-imidazole Investigative T84621 DRUGINFO D0S4WQ 1-(3-Chlorobenzyl)-1H-imidazole Investigative T84621 DRUGINFO D08HHA 1-(3-Fluorobenzyl)-1H-imidazole Investigative T84621 DRUGINFO D03KLN 1-(3-Methoxy-naphthalen-2-yl)-1H-imidazole Investigative T84621 DRUGINFO D0HL9S 1-(4-Aminobenzyl)-1H-imidazole Investigative T84621 DRUGINFO D03VRC 1-(4-Bromobenzyl)-1H-imidazole Investigative T84621 DRUGINFO D07DQJ 1-(4-Bromobenzyl)-5-phenyl-1H-imidazole Investigative T84621 DRUGINFO D0W8IZ 1-(4-Chlorobenzyl)-5-phenyl-1H-imidazole Investigative T84621 DRUGINFO D0NV7W 1-(4-Cyanobenzyl)-5-(2-fluorophenyl)-1H-imidazole Investigative T84621 DRUGINFO D0I2UH 1-(4-Cyanobenzyl)-5-(2-methylphenyl)-1H-imidazole Investigative T84621 DRUGINFO D00PXF 1-(4-Cyanobenzyl)-5-(3-fluorophenyl)-1H-imidazole Investigative T84621 DRUGINFO D02PSL 1-(4-Cyanobenzyl)-5-(3-methylphenyl)-1H-imidazole Investigative T84621 DRUGINFO D0P1UO 1-(4-Cyanobenzyl)-5-(4-fluorophenyl)-1H-imidazole Investigative T84621 DRUGINFO D0V6QN 1-(4-Cyanobenzyl)-5-(4-methylphenyl)-1H-imidazole Investigative T84621 DRUGINFO D06RSD 1-(4-Cyanobenzyl)-5-(4-pyridyl)-1H-imidazole Investigative T84621 DRUGINFO D0L2QD 1-(4-Cyanobenzyl)-5-bromo-1H-imidazole Investigative T84621 DRUGINFO D07EJK 1-(4-Cyanobenzyl)-5-formyl-1H-imidazole Investigative T84621 DRUGINFO D08ORG 1-(4-Cyanobenzyl)-5-hydroxymethyl-1H-imidazole Investigative T84621 DRUGINFO D05FFY 1-(4-Cyanobenzyl)-5-methyl-1H-imidazole Investigative T84621 DRUGINFO D0Q8KM 1-(4-Cyanobenzyl)-5-phenyl-1H-imidazole Investigative T84621 DRUGINFO D05QPR 1-(4-fluorobenzyl)-1H-imidazole Investigative T84621 DRUGINFO D06NFC 1-(4-Fluorobenzyl)-5-phenyl-1H-imidazole Investigative T84621 DRUGINFO D0T8JU 1-(4-Methoxybenzyl)-5-phenyl-1H-imidazole Investigative T84621 DRUGINFO D0M9VK 1-(6-Methoxy-naphthalen-2-yl)-1H-imidazole Investigative T84621 DRUGINFO D08YGW 1-Benzyl-5-phenyl-1H-imidazole Investigative T84621 DRUGINFO D05VAN 1-Ethyl-3-imidazol-1-ylmethyl-1H-indole Investigative T84621 DRUGINFO D0G6QL 1-Naphthalen-2-yl-1H-imidazole Investigative T84621 DRUGINFO D0Y2AK 1-Phenyl-2-pyridin-3-yl-propan-1-one Investigative T84621 DRUGINFO D0P9JF 2-Methyl-1,2-di-pyridin-3-yl-1-methoxypropane Investigative T84621 DRUGINFO D0HV5D 2-Methyl-1,2-di-pyridin-3-yl-propan-1-one oxime Investigative T84621 DRUGINFO D0G3RD 2-Methyl-1,2-di-pyridin-3-yl-propane Investigative T84621 DRUGINFO D04QWX 2-Methyl-1,2-di-pyridin-3-yl-propylchloride Investigative T84621 DRUGINFO D04MEE 2-Methyl-1,2-di-pyridin-3-yl-propyliodide Investigative T84621 DRUGINFO D07SAF 2-Methyl-1-phenyl-2-pyridin-3-yl-propan-1-ol Investigative T84621 DRUGINFO D08UWI 2-Methyl-1-phenyl-2-pyridin-3-yl-propan-1-one Investigative T84621 DRUGINFO D0C7YL 3-((1H-imidazol-1-yl)methyl)aniline Investigative T84621 DRUGINFO D0V9JS 3-(1,1-Dimethyl-2-phenyl-ethyl)-pyridine Investigative T84621 DRUGINFO D0D7YL 3-(1,2-dihydroacenaphthylen-3-yl)pyridine Investigative T84621 DRUGINFO D04PKP 3-(1,2-dihydroacenaphthylen-5-yl)pyridine Investigative T84621 DRUGINFO D0D8KN 3-(1-Benzyl-1H-imidazol-5-yl)-1-propanol Investigative T84621 DRUGINFO D04ISG 3-(1-Chloro-7-methoxy-naphthalen-2-yl)-pyridine Investigative T84621 DRUGINFO D0MA9G 3-(1-ethyl-3,4-dihydronaphthalen-2-yl)-pyridine Investigative T84621 DRUGINFO D02LWB 3-(1H-inden-2-yl)pyridine Investigative T84621 DRUGINFO D0K5KG 3-(1-methyl-3,4-dihydronaphthalen-2-yl)-pyridine Investigative T84621 DRUGINFO D0I9PA 3-(2,3-Dihydro-1,4-benzodioxin-6-yl)pyridine Investigative T84621 DRUGINFO D02FRA 3-(2-Chloro-1,1-dimethyl-2-phenyl-ethyl)-pyridine Investigative T84621 DRUGINFO D0I5NW 3-(3,4-dihydronaphthalen-2-yl)pyridine Investigative T84621 DRUGINFO D0Q5ZZ 3-(3-Benzyl-6-methoxynaphthalen-2-yl)pyridine Investigative T84621 DRUGINFO D05IXU 3-(3-Benzylnaphthalen-2-yl)pyridine Investigative T84621 DRUGINFO D08HPU 3-(3-methyl-3,4-dihydronaphthalen-2-yl)pyridine Investigative T84621 DRUGINFO D0L4NG 3-(4-ethyl-3,4-dihydronaphthalen-2-yl)pyridine Investigative T84621 DRUGINFO D0X1QS 3-(4-methyl-3,4-dihydronaphthalen-2-yl)pyridine Investigative T84621 DRUGINFO D0VL3R 3-(5,6,7,8-Tetrahydronaphthalen-2-yl)pyridine Investigative T84621 DRUGINFO D04IBH 3-(5-Bromo-6-methoxy-naphthalen-2-yl)-pyridine Investigative T84621 DRUGINFO D08ZTZ 3-(5-Chloro-6-methoxy-naphthalen-2-yl)-pyridine Investigative T84621 DRUGINFO D0D8YE 3-(5-methoxy-1H-inden-2-yl)pyridine Investigative T84621 DRUGINFO D0RJ6S 3-(6-Bromo-naphthalen-2-yl)-pyridine Investigative T84621 DRUGINFO D0R0TE 3-(6-Ethoxy-naphthalen-2-yl)-pyridine Investigative T84621 DRUGINFO D0NX0M 3-(6-methoxy-3,4-dihydronaphthalen-2-yl)pyridine Investigative T84621 DRUGINFO D0S8FV 3-(6-Methoxy-3-methylnaphthalen-2-yl)pyridine Investigative T84621 DRUGINFO D0B2UM 3-(6-Methoxynaphthalen-2-yl)-4-methylpyridine Investigative T84621 DRUGINFO D0Q6BJ 3-(6-Methoxynaphthalen-2-yl)-5-phenylpyridine Investigative T84621 DRUGINFO D02GFK 3-(6-Methoxynaphthalen-2-yl)pyridin-4-amine Investigative T84621 DRUGINFO D0N1PQ 3-(6-methoxynaphthalen-2-yl)pyridine Investigative T84621 DRUGINFO D08FAB 3-(naphthalen-2-yl)pyridine Investigative T84621 DRUGINFO D02UZI 3-[(Z)-2-phenylvinyl]pyridine Investigative T84621 DRUGINFO D0AK9S 3-[1-(4-Bromobenzyl)-1H-imidazol-5-yl]-1-propanol Investigative T84621 DRUGINFO D0PH1G 3-[1-(4-Cyanobenzyl)-1H-imidazol-5-yl]-1-propanol Investigative T84621 DRUGINFO D06JYY 3-[3-(4-Methoxybenzyl)naphthalen-2-yl]pyridine Investigative T84621 DRUGINFO D0V3YH 3-[4-Chloro-indan-(1E)-ylidenemethyl]-pyridine Investigative T84621 DRUGINFO D05MQE 3-[4-Chloro-indan-(1Z)-ylidenemethyl]-pyridine Investigative T84621 DRUGINFO D04QPK 3-[4-Fluoro-indan-(1E)-ylidenemethyl]-pyridine Investigative T84621 DRUGINFO D04CLL 3-[4-Methyl-indan-(1E)-ylidenemethyl]-pyridine Investigative T84621 DRUGINFO D08AZK 3-[5-Bromo-indan-(1E)-ylidenemethyl]-pyridine Investigative T84621 DRUGINFO D0U7RR 3-[5-Bromo-indan-(1Z)-ylidenemethyl]-pyridine Investigative T84621 DRUGINFO D02NAG 3-[5-Chloro-indan-(1E)-ylidenemethyl]-pyridine Investigative T84621 DRUGINFO D04ELJ 3-[5-Chloro-indan-(1Z)-ylidenemethyl]-pyridine Investigative T84621 DRUGINFO D0N9PY 3-[5-Ethoxy-indan-(1E)-ylidenemethyl]-pyridine Investigative T84621 DRUGINFO D0Q3JZ 3-[5-Ethoxy-indan-(1Z)-ylidenemethyl]-pyridine Investigative T84621 DRUGINFO D0V8CR 3-[5-Fluoro-indan-(1E)-ylidenemethyl]-pyridine Investigative T84621 DRUGINFO D0M7FS 3-[5-Fluoro-indan-(1Z)-ylidenemethyl]-pyridine Investigative T84621 DRUGINFO D09YXV 3-[5-Methoxy-indan-(1E)-ylidenemethyl]-pyridine Investigative T84621 DRUGINFO D08PNF 3-[5-Methoxy-indan-(1Z)-ylidenemethyl]-pyridine Investigative T84621 DRUGINFO D0YS2F 3-[7-Methoxy-indan-(1E)-ylidenemethyl]-pyridine Investigative T84621 DRUGINFO D0Y3AV 3-Ethoxy-5-(6-methoxynaphthalen-2-yl)pyridine Investigative T84621 DRUGINFO D0Q0BK 3-Fluoro-4'-(pyridin-4-ylmethyl)biphenyl-4-ol Investigative T84621 DRUGINFO D00RRV 3-Imidazol-1-ylmethyl-1H-indole Investigative T84621 DRUGINFO D01CGR 3-Imidazol-1-ylmethyl-2-isopropyl-1H-indole Investigative T84621 DRUGINFO D07JCO 3-Imidazol-1-yl-quinoline Investigative T84621 DRUGINFO D01SUE 3-Indan-(1E)-ylidenemethyl-pyridine Investigative T84621 DRUGINFO D07PYC 3-Indan-(1Z)-ylidenemethyl-pyridine Investigative T84621 DRUGINFO D0X4LQ 3-MeSO2-DDE Investigative T84621 DRUGINFO D08IDC 3-methoxy-5-(6-methoxynaphthalen-2-yl)pyridine Investigative T84621 DRUGINFO D00DUJ 3-Phenanthren-9-yl-pyridine Investigative T84621 DRUGINFO D09HEA 4-((1H-imidazol-1-yl)methyl)benzonitrile Investigative T84621 DRUGINFO D09VQZ 4-((3',4'-Difluorobiphenyl-4-yl)methyl)pyridine Investigative T84621 DRUGINFO D0Y1YZ 4-(2-Imidazol-1-yl-ethoxy)-benzamide Investigative T84621 DRUGINFO D0LJ9D 4-(4-(thiophen-2-yl)benzyl)pyridine Investigative T84621 DRUGINFO D0Z3GX 4-(4-(thiophen-3-yl)benzyl)pyridine Investigative T84621 DRUGINFO D00DSE 4-(4'-Fluoro-biphenyl-4-ylmethyl)pyridine Investigative T84621 DRUGINFO D0C6US 4-(6-methoxy-3,4-dihydronaphthalen-2-yl)pyridine Investigative T84621 DRUGINFO D0S4KP 4-(6-Methoxy-3-methylnaphthalen-2-yl)isoquinoline Investigative T84621 DRUGINFO D06CWR 4-(6-Methoxynaphthalen-2-yl)isoquinoline Investigative T84621 DRUGINFO D02BXS 4'-(Pyridin-4-ylmethyl)biphenyl-3,4-diamine Investigative T84621 DRUGINFO D01REI 4'-(Pyridin-4-ylmethyl)biphenyl-3,4-diol Investigative T84621 DRUGINFO D0WN9P 4'-(Pyridin-4-ylmethyl)biphenyl-3-amine Investigative T84621 DRUGINFO D0Y5KX 4'-(Pyridin-4-ylmethyl)biphenyl-4-amine Investigative T84621 DRUGINFO D0I1YH 4-[(3'-Hydroxybiphenyl-4-yl)methyl]pyridine Investigative T84621 DRUGINFO D03EXD 4-[(4'-Hydroxybiphenyl-4-yl)methyl]pyridine Investigative T84621 DRUGINFO D09VPA 4-[5-Bromo-indan-(1E)-ylidenemethyl]-pyridine Investigative T84621 DRUGINFO D0D9FR 4-[5-Bromo-indan-(1Z)-ylidenemethyl]-pyridine Investigative T84621 DRUGINFO D0YD9J 4-[5-Chloro-indan-(1E)-ylidenemethyl]-pyridine Investigative T84621 DRUGINFO D0F5YU 4-[5-Chloro-indan-(1Z)-ylidenemethyl]-pyridine Investigative T84621 DRUGINFO D03MKT 4-[5-Fluoro-indan-(1E)-ylidenemethyl]-pyridine Investigative T84621 DRUGINFO D09HOE 4-[5-Fluoro-indan-(1Z)-ylidenemethyl]-pyridine Investigative T84621 DRUGINFO D02CSU 4-Indan-(1Z)-ylidenemethyl-pyridine Investigative T84621 DRUGINFO D02JUJ 5-(6-Methoxynaphthalen-2-yl)pyridin-3-ol Investigative T84621 DRUGINFO D04CFP 5-[4-(Pyridin-4-ylmethyl)phenyl]-1H-indole Investigative T84621 DRUGINFO D0E9WX 5-[5-Bromo-indan-(1E)-ylidenemethyl]-1H-imidazole Investigative T84621 DRUGINFO D02XHH 5-[5-Bromo-indan-(1Z)-ylidenemethyl]-1H-imidazole Investigative T84621 DRUGINFO D06HFV 5-[5-Fluoro-indan-(1E)-ylidenemethyl]-pyrimidine Investigative T84621 DRUGINFO D03TRM 5-Indan-(1E)-ylidenemethyl-1H-imidazole Investigative T84621 DRUGINFO D09QDY 5-Indan-(1Z)-ylidenemethyl-1H-imidazole Investigative T84621 DRUGINFO D07NAH 5-Naphthalen-2-yl-1H-imidazole Investigative T84621 DRUGINFO D0L8KL 5-Naphthalen-2-yl-oxazole Investigative T84621 DRUGINFO D0K2DR 5-Pyridin-3-yl-1,3-dihydro-2H-indol-2-one Investigative T84621 DRUGINFO D0G9WP 5-Pyridin-3-yl-2,3-dihydro-1H-inden-1-one Investigative T84621 DRUGINFO D0Q3CX 6-(4-Methylpyridin-3-yl)-2-naphthonitrile Investigative T84621 DRUGINFO D0N1GH 6-(pyridin-3-yl)-2-naphthonitrile Investigative T84621 DRUGINFO D07VGT 6-[4-(Pyridin-4-ylmethyl)phenyl]naphthalen-2-ol Investigative T84621 DRUGINFO D03YHZ 6-Isoquinolin-4-yl-3,4-dihydroquinolin-2(1H)-one Investigative T84621 DRUGINFO D02ZQM 6-Pyridin-3-yl-1,2,3,4-tetrahydronaphthalen-2-ol Investigative T84621 DRUGINFO D09CPC 6-Pyridin-3-yl-3,4-dihydro-1H-quinolin-2-one Investigative T84621 DRUGINFO D07WLT 6-Pyridin-3-yl-3,4-dihydronaphthalen-2(1H)-one Investigative T84621 DRUGINFO D0E8DX 6-Pyridin-3-yl-3,4-dihydroquinoline-2(1H)-thione Investigative T84621 DRUGINFO D02ALK 6-Pyridin-3-yl-naphthalen-2-ol Investigative T84621 DRUGINFO D09GJI 7-(1-(1H-imidazol-1-yl)ethyl)-9H-fluoren-2-ol Investigative T84621 DRUGINFO D0O7TC 7-Pyridin-3-yl-2H-1,4-benzothiazin-3(4H)-one Investigative T84621 DRUGINFO D0X0IH BENZYLIMIDAZOLE Investigative T84621 DRUGINFO D03CWL Methyl 3-(1-Benzyl-1H-imidazol-5-yl)-propanoate Investigative T84621 DRUGINFO D0WW4F METYRAPOL Investigative T84621 DRUGINFO D0E0ZS N-(4'-Isonicotinoylbiphenyl-3-yl)acetamide Investigative T84621 DRUGINFO D0JE1I R-fadrozole Investigative T84621 DRUGINFO D0I0NP SL125 Investigative T84621 KEGGPATH hsa00140:Steroid hormone biosynthesis T84621 KEGGPATH hsa01100:Metabolic pathways T84621 WIKIPATH WP2355:Corticotropin-releasing hormone T84621 WIKIPATH WP2749:Metabolism of steroid hormones and vitamin D T84621 WIKIPATH WP43:Oxidation by Cytochrome P450 T84621 WIKIPATH WP702:Metapathway biotransformation T84621 WHIZPATH PW000141:Steroidogenesis T84621 REACPATH R-HSA-194002:Glucocorticoid biosynthesis T84621 REACPATH R-HSA-211976:Endogenous sterols T84621 BIOCPATH PWY66-381:Glucocorticoid biosynthesis T84621 BIOCPATH PWY66-382:Mineralocorticoid biosynthesis T84621 BIOCPATH PWY-7305:Superpathway of steroid hormone biosynthesis T55922 TARGETID T55922 T55922 FORMERID TTDR00414 T55922 UNIPROID DCAM_HUMAN T55922 TARGNAME S-adenosylmethionine decarboxylase proenzyme (AMD1) T55922 GENENAME AMD1 T55922 TARGTYPE Successful target T55922 SYNONYMS SamDC; S-adenosylmethioninedecarboxylase; AdoMetDC; AMD T55922 FUNCTION Promotes maintenance and self-renewal of embryonic stem cells, by maintaining spermine levels. Essential for biosynthesis of the polyamines spermidine and spermine. T55922 PDBSTRUC 3H0W; 3H0V; 3EPB; 3EPA; 3EP9 T55922 BIOCLASS Carbon-carbon lyase T55922 ECNUMBER EC 4.1.1.50 T55922 SEQUENCE MEAAHFFEGTEKLLEVWFSRQQPDANQGSGDLRTIPRSEWDILLKDVQCSIISVTKTDKQEAYVLSESSMFVSKRRFILKTCGTTLLLKALVPLLKLARDYSGFDSIQSFFYSRKNFMKPSHQGYPHRNFQEEIEFLNAIFPNGAAYCMGRMNSDCWYLYTLDFPESRVISQPDQTLEILMSELDPAVMDQFYMKDGVTAKDVTRESGIRDLIPGSVIDATMFNPCGYSMNGMKSDGTYWTIHITPEPEFSYVSFETNLSQTSYDDLIRKVVEVFKPGKFVTTLFVNQSSKCRTVLASPQKIEGFKRLDCQSAMFNDYNFVFTSFAKKQQQQQS T55922 DRUGINFO D03ZFN Tromethamine Approved T55922 DRUGINFO D0E2WF ORG 34517/34850 Phase 2 T55922 DRUGINFO D00FMV Putrescine Discontinued in Phase 2 T55922 DRUGINFO D0S6VX CGP-40215A Terminated T55922 DRUGINFO D05FFR MGBG Terminated T55922 DRUGINFO D0P5YR [(2-aminooxyethyl)methylamino]-5'-deoxyadenosine Investigative T55922 DRUGINFO D0Y7YL 5'-([(Z)-4-amino-2-butenyl]methylamino)-5'-deoxyadenosine Investigative T55922 DRUGINFO D0YM6B 5'-Deoxy-5'-(N,N-dimethylamino)-8-methyladenosine Investigative T55922 DRUGINFO D03OLX 5'-Deoxy-5'-(N,N-dimethylamino)adenosine Investigative T55922 DRUGINFO D0V2QF 5'-deoxy-5'-[(3-hydrazinopropyl)methylamino]adenosine Investigative T55922 DRUGINFO D0I7IA 5'-Deoxy-5'-dimethylsulfonioadenosine chloride Investigative T55922 DRUGINFO D0BI4H Hydroxyalanine Investigative T55922 KEGGPATH hsa00270:Cysteine and methionine metabolism T55922 KEGGPATH hsa00330:Arginine and proline metabolism T55922 KEGGPATH hsa01100:Metabolic pathways T55922 WIKIPATH WP2693:Metabolism of amino acids and derivatives T55922 WHIZPATH PW000037:Spermidine and Spermine Biosynthesis T55922 WHIZPATH PW000056:Methionine Metabolism T55922 NET_PATH NetPath_4:EGFR1 Signaling Pathway T55922 BIOCPATH ARGSPECAT-PWY:Spermine biosynthesis T55922 BIOCPATH BSUBPOLYAMSYN-PWY:Spermidine biosynthesis T55922 BIOCPATH PWY-7527:Methionine salvage cycle III T59929 TARGETID T59929 T59929 FORMERID TTDR00251 T59929 UNIPROID TYPH_HUMAN T59929 TARGNAME Thymidine phosphorylase (TYMP) T59929 GENENAME TYMP T59929 TARGTYPE Successful target T59929 SYNONYMS TdRPase; TYMP; TP; Platelet-derived endothelial cell growth factor; PDECGF; PD-ECGF; Gliostatin T59929 FUNCTION Catalyzes the reversible phosphorolysis of thymidine. The produced molecules are then utilized as carbon and energy sources or in the rescue of pyrimidine bases for nucleotide synthesis. T59929 PDBSTRUC 2WK6; 2WK5; 2J0F; 1UOU T59929 BIOCLASS Pentosyltransferase T59929 ECNUMBER EC 2.4.2.4 T59929 SEQUENCE MAALMTPGTGAPPAPGDFSGEGSQGLPDPSPEPKQLPELIRMKRDGGRLSEADIRGFVAAVVNGSAQGAQIGAMLMAIRLRGMDLEETSVLTQALAQSGQQLEWPEAWRQQLVDKHSTGGVGDKVSLVLAPALAACGCKVPMISGRGLGHTGGTLDKLESIPGFNVIQSPEQMQVLLDQAGCCIVGQSEQLVPADGILYAARDVTATVDSLPLITASILSKKLVEGLSALVVDVKFGGAAVFPNQEQARELAKTLVGVGASLGLRVAAALTAMDKPLGRCVGHALEVEEALLCMDGAGPPDLRDLVTTLGGALLWLSGHAGTQAQGAARVAAALDDGSALGRFERMLAAQGVDPGLARALCSGSPAERRQLLPRAREQEELLAPADGTVELVRALPLALVLHELGAGRSRAGEPLRLGVGAELLVDVGQRLRRGTPWLRVHRDGPALSGPQSRALQEALVLSDRAPFAAPSPFAELVLPPQQ T59929 DRUGINFO D0Y7DP Uridine Approved T59929 DRUGINFO D03ITH 1-(cyclohexyl)methyl-5'-O-tritylinosine Investigative T59929 DRUGINFO D04OWX 1-(cyclopropyl)methyl-5'-O-tritylinosine Investigative T59929 DRUGINFO D06BMN 1-allyl-5'-O-tritylinosine Investigative T59929 DRUGINFO D0W6LJ 1-benzyl-5'-O-tritylinosine Investigative T59929 DRUGINFO D05OUP 1-propyl-5'-O-tritylinosine Investigative T59929 DRUGINFO D0CQ1J 2'-aminoimidazolylmethyluracils Investigative T59929 DRUGINFO D09TBA 5-benzyl-6-chloropyrimidine-2,4(1H,3H)-dione Investigative T59929 DRUGINFO D0Y5UF 5-bromo-6-(cyclopropylamino)uracil hydrochloride Investigative T59929 DRUGINFO D00PMF 5-bromo-6-hydrazinouracil hydrochloride Investigative T59929 DRUGINFO D0RE9X 5-butyl-6-chloropyrimidine-2,4(1H,3H)-dione Investigative T59929 DRUGINFO D0G1DS 5-chloro-6-hydrazinouracil hydrochloride Investigative T59929 DRUGINFO D01DAQ 5-fluoro-6-[(2-aminoimidazol-1-yl)methyl]uracil Investigative T59929 DRUGINFO D0X5RA 6-amino-5-bromouracil Investigative T59929 DRUGINFO D0VW6H 6-amino-5-chlorouracil hydrochloride Investigative T59929 DRUGINFO D0I7IF 6-bromo-5-phenylpyrimidine-2,4(1H,3H)-dione Investigative T59929 DRUGINFO D0C0HN 6-chloro-5-(2-thienyl)pyrimidine-2,4(1H,3H)-dione Investigative T59929 DRUGINFO D03IMY 6-chloro-5-heptylpyrimidine-2,4(1H,3H)-dione Investigative T59929 DRUGINFO D0CO5S 6-chloro-5-hexylpyrimidine-2,4(1H,3H)-dione Investigative T59929 DRUGINFO D0E7SH 6-chloro-5-pentylpyrimidine-2,4(1H,3H)-dione Investigative T59929 DRUGINFO D01IGW 6-chloro-5-phenylpyrimidine-2,4(1H,3H)-dione Investigative T59929 DRUGINFO D0DX8A 6-chloro-5-propylpyrimidine-2,4(1H,3H)-dione Investigative T59929 DRUGINFO D0E9PL 6-fluoro-5-phenylpyrimidine-2,4(1H,3H)-dione Investigative T59929 DRUGINFO D0F4KL Thymine Investigative T59929 KEGGPATH hsa00240:Pyrimidine metabolism T59929 KEGGPATH hsa00983:Drug metabolism - other enzymes T59929 KEGGPATH hsa01100:Metabolic pathways T59929 KEGGPATH hsa05219:Bladder cancer T59929 WIKIPATH WP1601:Fluoropyrimidine Activity T59929 WIKIPATH WP1851:Metabolism of nucleotides T59929 WIKIPATH WP2828:Bladder Cancer T59929 WHIZPATH PW000160:Pyrimidine Metabolism T59929 NET_PATH NetPath_23:TSH Signaling Pathway T59929 BIOCPATH PWY-7181:Pyrimidine deoxyribonucleosides degradation T67684 TARGETID T67684 T67684 FORMERID TTDS00004 T67684 UNIPROID ACM3_HUMAN T67684 TARGNAME Muscarinic acetylcholine receptor M3 (CHRM3) T67684 GENENAME CHRM3 T67684 TARGTYPE Successful target T67684 SYNONYMS M3 receptor; CHRM3 T67684 FUNCTION The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover. T67684 PDBSTRUC 2CSA T67684 BIOCLASS GPCR rhodopsin T67684 SEQUENCE MTLHNNSTTSPLFPNISSSWIHSPSDAGLPPGTVTHFGSYNVSRAAGNFSSPDGTTDDPLGGHTVWQVVFIAFLTGILALVTIIGNILVIVSFKVNKQLKTVNNYFLLSLACADLIIGVISMNLFTTYIIMNRWALGNLACDLWLAIDYVASNASVMNLLVISFDRYFSITRPLTYRAKRTTKRAGVMIGLAWVISFVLWAPAILFWQYFVGKRTVPPGECFIQFLSEPTITFGTAIAAFYMPVTIMTILYWRIYKETEKRTKELAGLQASGTEAETENFVHPTGSSRSCSSYELQQQSMKRSNRRKYGRCHFWFTTKSWKPSSEQMDQDHSSSDSWNNNDAAASLENSASSDEEDIGSETRAIYSIVLKLPGHSTILNSTKLPSSDNLQVPEEELGMVDLERKADKLQAQKSVDDGGSFPKSFSKLPIQLESAVDTAKTSDVNSSVGKSTATLPLSFKEATLAKRFALKTRSQITKRKRMSLVKEKKAAQTLSAILLAFIITWTPYNIMVLVNTFCDSCIPKTFWNLGYWLCYINSTVNPVCYALCNKTFRTTFKMLLLCQCDKKKRRKQQYQQRQSVIFHKRAPEQAL T67684 DRUGINFO D0R7WU ACECLIDINE Approved T67684 DRUGINFO D0Q4CS Cevimeline Approved T67684 DRUGINFO D0Y5AM Darifenacin Approved T67684 DRUGINFO D0S0AS Ipratropium Approved T67684 DRUGINFO D07KHH LAS-34273 Approved T67684 DRUGINFO D04MWJ Methacholine Chloride Approved T67684 DRUGINFO D04LHJ Methscopolamine Bromide Approved T67684 DRUGINFO D0M6VK Methylscopolamine Approved T67684 DRUGINFO D05KZK SMT-D002 Approved T67684 DRUGINFO D0L4YD Solifenacin Approved T67684 DRUGINFO D0Q7ZQ Succinylcholine Approved T67684 DRUGINFO D0P1WA Tiotropium Approved T67684 DRUGINFO D0BZ7W Tolterodine Approved T67684 DRUGINFO D04YEW Tarafenacin Phase 2 T67684 DRUGINFO D02TXV TRN-157 Phase 2 T67684 DRUGINFO D0V0JQ CHF 5407 Phase 1 T67684 DRUGINFO D04SBH Zamifenacin Discontinued in Phase 3 T67684 DRUGINFO D06GCP PSD-506 Discontinued in Phase 2 T67684 DRUGINFO D09LMX Revatropate Discontinued in Phase 1 T67684 DRUGINFO D0X8MZ Alvameline Terminated T67684 DRUGINFO D0G4CG [3H]oxotremorine-M Investigative T67684 DRUGINFO D02VGM [3H]QNB Investigative T67684 DRUGINFO D00JTE 1,1-diphenyl-2-(3-tropanyl)ethanol Investigative T67684 DRUGINFO D05EML 1'-Benzyl-3-phenyl-[3,4']bipiperidinyl-2,6-dione Investigative T67684 DRUGINFO D02PFJ 1-Methyl-1-(4-pyrrolidin-1-yl-but-2-ynyl)-urea Investigative T67684 DRUGINFO D05MDY 2,8-Dimethyl-1-oxa-8-aza-spiro[4.5]decan-3-one Investigative T67684 DRUGINFO D0U2IL 2-Methyl-6-pyrrolidin-1-yl-hex-4-ynal oxime Investigative T67684 DRUGINFO D06UOE 3-(1-carbamoyl-1,1-diphenylmethyl)-1-(4-methoxyphenylethyl)pyrrolidine (APP) Investigative T67684 DRUGINFO D07DEY 3-(3-benzylamino)-piperidin-2-one Investigative T67684 DRUGINFO D06VST 3-Methyl-7-pyrrolidin-1-yl-hept-5-yn-2-one Investigative T67684 DRUGINFO D0OE0K 3-Tetrazol-2-yl-1-aza-bicyclo[2.2.2]octane Investigative T67684 DRUGINFO D0T2RY 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Investigative T67684 DRUGINFO D0A2KT 4-DAMP Investigative T67684 DRUGINFO D08ZTA 6-Dimethylamino-2-methyl-hex-4-ynal oxime Investigative T67684 DRUGINFO D0QL1X 7-Dimethylamino-3-methyl-hept-5-yn-2-one Investigative T67684 DRUGINFO D0R8FS 7-Dimethylamino-hept-5-yn-2-one Investigative T67684 DRUGINFO D0B8AQ 7-Pyrrolidin-1-yl-hept-5-yn-2-one Investigative T67684 DRUGINFO D0F9QT A-987306 Investigative T67684 DRUGINFO D01UDC Acetic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester Investigative T67684 DRUGINFO D0IM7C AE-9C90CB Investigative T67684 DRUGINFO D0I9LU arecaidine propargyl ester Investigative T67684 DRUGINFO D0C9ZE Benzoic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester Investigative T67684 DRUGINFO D07VZG BRL-55473 Investigative T67684 DRUGINFO D0H2UT brucine Investigative T67684 DRUGINFO D0Z5RQ Cremastrine Investigative T67684 DRUGINFO D05EEV DAU-5750 Investigative T67684 DRUGINFO D0R8AZ DAU-5884 Investigative T67684 DRUGINFO D0HV3A FLUMEZAPINE Investigative T67684 DRUGINFO D06IUC FM1-10 Investigative T67684 DRUGINFO D0AR0H FM1-43 Investigative T67684 DRUGINFO D0PL0Y furtrethonium Investigative T67684 DRUGINFO D02EXX GNF-PF-5618 Investigative T67684 DRUGINFO D07OAK Go7874 Investigative T67684 DRUGINFO D0I9AL guanylpirenzepine Investigative T67684 DRUGINFO D0W8XI hexahydrodifenidol Investigative T67684 DRUGINFO D07LDP hexahydrosiladifenidol Investigative T67684 DRUGINFO D0P0IX ISOCLOZAPINE Investigative T67684 DRUGINFO D0Q2GP ISOLOXAPINE Investigative T67684 DRUGINFO D0BP7C J-104135 Investigative T67684 DRUGINFO D03DMR lithocholylcholine Investigative T67684 DRUGINFO D02BOW McN-A-343 Investigative T67684 DRUGINFO D0WO3A methylfurmethide Investigative T67684 DRUGINFO D00WNA ML381 Investigative T67684 DRUGINFO D0C9VH N-(4-Dimethylamino-but-2-ynyl)-N-methyl-acetamide Investigative T67684 DRUGINFO D08KNP N-benzyl brucine Investigative T67684 DRUGINFO D08BGK N-chloromethyl-brucine Investigative T67684 DRUGINFO D0R2JE N-methoxyquinuclidine-3-carboximidoyl chloride Investigative T67684 DRUGINFO D0X2JU N-methoxyquinuclidine-3-carboximidoyl fluoride Investigative T67684 DRUGINFO D02MJE NNC 11-1314 Investigative T67684 DRUGINFO D07CAB NNC 11-1585 Investigative T67684 DRUGINFO D08XBQ NNC 11-1607 Investigative T67684 DRUGINFO D09YBC NOCARDIMICIN A Investigative T67684 DRUGINFO D05YBO Nocardimicin C Investigative T67684 DRUGINFO D0I2XG Nocardimicin D Investigative T67684 DRUGINFO D0J4DJ Nocardimicin F Investigative T67684 DRUGINFO D07QGQ Noccardimicin E Investigative T67684 DRUGINFO D07TDE Olterodine Investigative T67684 DRUGINFO D0F5LH Oxybutynine Investigative T67684 DRUGINFO D0T6ID pentylthio-TZTP Investigative T67684 DRUGINFO D0K3VR p-F-HHSiD Investigative T67684 DRUGINFO D04XNH Propionic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester Investigative T67684 DRUGINFO D09AAZ PTAC Investigative T67684 DRUGINFO D00NRJ silahexocyclium Investigative T67684 DRUGINFO D0O1BN SULFOARECOLINE Investigative T67684 DRUGINFO D05WXF thiochrome Investigative T67684 DRUGINFO D07GPQ tripitramine Investigative T67684 DRUGINFO D02ZPV UCB-101333-3 Investigative T67684 DRUGINFO D03LSH UH-AH 37 Investigative T67684 DRUGINFO D0S4DT vinburnine Investigative T67684 DRUGINFO D02UNX VU0255035 Investigative T67684 DRUGINFO D05PSD WIN 51,708 Investigative T67684 DRUGINFO D02IIN WIN 62,577 Investigative T67684 KEGGPATH hsa04020:Calcium signaling pathway T67684 KEGGPATH hsa04080:Neuroactive ligand-receptor interaction T67684 KEGGPATH hsa04725:Cholinergic synapse T67684 KEGGPATH hsa04810:Regulation of actin cytoskeleton T67684 KEGGPATH hsa04911:Insulin secretion T67684 KEGGPATH hsa04970:Salivary secretion T67684 KEGGPATH hsa04971:Gastric acid secretion T67684 KEGGPATH hsa04972:Pancreatic secretion T67684 WIKIPATH WP117:GPCRs, Other T67684 WIKIPATH WP1824:GPCR downstream signaling T67684 WIKIPATH WP1825:GPCR ligand binding T67684 WIKIPATH WP1831:Integration of energy metabolism T67684 WIKIPATH WP2664:Gastrin-CREB signalling pathway via PKC and MAPK T67684 WIKIPATH WP455:GPCRs, Class A Rhodopsin-like T67684 WIKIPATH WP51:Regulation of Actin Cytoskeleton T67684 WIKIPATH WP536:Calcium Regulation in the Cardiac Cell T67684 WIKIPATH WP58:Monoamine GPCRs T67684 WHIZPATH PW000565:Gastric Acid Production T67684 REACPATH R-HSA-390648:Muscarinic acetylcholine receptors T67684 REACPATH R-HSA-399997:Acetylcholine regulates insulin secretion T67684 REACPATH R-HSA-416476:G alpha (q) signalling events T67684 PANTPATH P00003:Alzheimer disease-amyloid secretase pathway T67684 PANTPATH P00027:Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway T67684 PANTPATH P00042:Muscarinic acetylcholine receptor 1 and 3 signaling pathway T62193 TARGETID T62193 T62193 FORMERID TTDS00361 T62193 UNIPROID DDC_HUMAN T62193 TARGNAME Aromatic-L-amino-acid decarboxylase (DDC) T62193 GENENAME DDC T62193 TARGTYPE Successful target T62193 SYNONYMS DOPA decarboxylase; AADC T62193 FUNCTION Catalyzes the decarboxylation of L-3,4-dihydroxyphenylalanine (DOPA) to dopamine, L-5-hydroxytryptophan to serotonin and L-tryptophan to tryptamine. T62193 PDBSTRUC 3RCH; 3RBL; 3RBF T62193 BIOCLASS Carbon-carbon lyase T62193 ECNUMBER EC 4.1.1.28 T62193 SEQUENCE MNASEFRRRGKEMVDYMANYMEGIEGRQVYPDVEPGYLRPLIPAAAPQEPDTFEDIINDVEKIIMPGVTHWHSPYFFAYFPTASSYPAMLADMLCGAIGCIGFSWAASPACTELETVMMDWLGKMLELPKAFLNEKAGEGGGVIQGSASEATLVALLAARTKVIHRLQAASPELTQAAIMEKLVAYSSDQAHSSVERAGLIGGVKLKAIPSDGNFAMRASALQEALERDKAAGLIPFFMVATLGTTTCCSFDNLLEVGPICNKEDIWLHVDAAYAGSAFICPEFRHLLNGVEFADSFNFNPHKWLLVNFDCSAMWVKKRTDLTGAFRLDPTYLKHSHQDSGLITDYRHWQIPLGRRFRSLKMWFVFRMYGVKGLQAYIRKHVQLSHEFESLVRQDPRFEICVEVILGLVCFRLKGSNKVNEALLQRINSAKKIHLVPCHLRDKFVLRFAICSRTVESAHVQRAWEHIKELAADVLRAERE T62193 DRUGINFO D0P7JZ Carbidopa Approved T62193 DRUGINFO D07MUN Vitamin B6 Approved T62193 DRUGINFO D0X8ED Benserazide Phase 3 T62193 DRUGINFO D03QFN Patrome Phase 3 T62193 DRUGINFO D02ITL AV-201 Phase 2 T62193 DRUGINFO DX9KC2 GT-AADC Phase 2 T62193 DRUGINFO DH1W0G VY-AADC Phase 2 T62193 DRUGINFO D72UDH OXB-102 Phase 1/2 T62193 DRUGINFO D05ICS ProSavin Phase 1/2 T62193 DRUGINFO D0P9BM 3-hydroxybenzylhydrazine Investigative T62193 DRUGINFO D0IB8N Noradrenalone (arterenone) Investigative T62193 KEGGPATH hsa00340:Histidine metabolism T62193 KEGGPATH hsa00350:Tyrosine metabolism T62193 KEGGPATH hsa00360:Phenylalanine metabolism T62193 KEGGPATH hsa00380:Tryptophan metabolism T62193 KEGGPATH hsa01100:Metabolic pathways T62193 KEGGPATH hsa04726:Serotonergic synapse T62193 KEGGPATH hsa04728:Dopaminergic synapse T62193 KEGGPATH hsa05030:Cocaine addiction T62193 KEGGPATH hsa05031:Amphetamine addiction T62193 KEGGPATH hsa05034:Alcoholism T62193 WIKIPATH WP1602:Nicotine Activity on Dopaminergic Neurons T62193 WIKIPATH WP2371:Parkinsons Disease Pathway T62193 WIKIPATH WP2436:Dopamine metabolism T62193 WIKIPATH WP2693:Metabolism of amino acids and derivatives T62193 WIKIPATH WP2855:Dopaminergic Neurogenesis T62193 WIKIPATH WP465:Tryptophan metabolism T62193 WIKIPATH WP550:Biogenic Amine Synthesis T62193 WIKIPATH WP706:SIDS Susceptibility Pathways T62193 WHIZPATH PW000017:Catecholamine Biosynthesis T62193 WHIZPATH PW000142:Tyrosine Metabolism T62193 WHIZPATH PW000163:Tryptophan Metabolism T62193 PANTPATH P00001:Adrenaline and noradrenaline biosynthesis T62193 PANTPATH P04371:5-Hydroxytryptamine biosynthesis T62193 PANTPATH P05912:Dopamine receptor mediated signaling pathway T62193 PANTPATH P06587:Nicotine pharmacodynamics pathway T62193 BIOCPATH PWY-6030:Serotonin and melatonin biosynthesis T62193 BIOCPATH PWY-6307:Tryptophan degradation via tryptamine T62193 BIOCPATH PWY66-301:Catecholamine biosynthesis T62193 BIOCPATH PWY66-401:Superpathway of tryptophan utilization T13852 TARGETID T13852 T13852 FORMERID TTDC00258 T13852 UNIPROID S1PR1_HUMAN T13852 TARGNAME Sphingosine-1-phosphate receptor 1 (S1PR1) T13852 GENENAME S1PR1 T13852 TARGTYPE Successful target T13852 SYNONYMS Sphingosine 1-phosphate receptor Edg-1; S1P1; S1P receptor Edg-1; S1P receptor 1; Endothelial differentiation G-protein coupled receptor 1; CHEDG1; CD363 T13852 FUNCTION Signaling leads to the activation of RAC1, SRC, PTK2/FAK1 and MAP kinases. Plays an important role in cell migration, probably via its role in the reorganization of the actin cytoskeleton and the formation of lamellipodia in response to stimuli that increase the activity of the sphingosine kinase SPHK1. Required for normal chemotaxis toward sphingosine 1-phosphate. Required for normal embryonic heart development and normal cardiac morphogenesis. Plays an important role in the regulation of sprouting angiogenesis and vascular maturation. Inhibits sprouting angiogenesis to prevent excessive sprouting during blood vessel development. Required for normal egress of mature T-cells from the thymus into the blood stream and into peripheral lymphoid organs. Plays a role in the migration of osteoclast precursor cells, the regulation of bone mineralization and bone homeostasis. Plays a role in responses to oxidized 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine by pulmonary endothelial cells and in the protection against ventilator-induced lung injury. G-protein coupled receptor for the bioactive lysosphingolipid sphingosine 1-phosphate (S1P) that seems to be coupled to the G(i) subclass of heteromeric G proteins. T13852 PDBSTRUC 3V2Y; 3V2W T13852 BIOCLASS GPCR rhodopsin T13852 SEQUENCE MGPTSVPLVKAHRSSVSDYVNYDIIVRHYNYTGKLNISADKENSIKLTSVVFILICCFIILENIFVLLTIWKTKKFHRPMYYFIGNLALSDLLAGVAYTANLLLSGATTYKLTPAQWFLREGSMFVALSASVFSLLAIAIERYITMLKMKLHNGSNNFRLFLLISACWVISLILGGLPIMGWNCISALSSCSTVLPLYHKHYILFCTTVFTLLLLSIVILYCRIYSLVRTRSRRLTFRKNISKASRSSEKSLALLKTVIIVLSVFIACWAPLFILLLLDVGCKVKTCDILFRAEYFLVLAVLNSGTNPIIYTLTNKEMRRAFIRIMSCCKCPSGDSAGKFKRPIIAGMEFSRSKSDNSSHPQKDEGDNPETIMSSGNVNSSS T13852 DRUGINFO D07UHS Fingolimod Approved T13852 DRUGINFO D07EDB Ozanimod Approved T13852 DRUGINFO D0Y4SI Ponesimod Approved T13852 DRUGINFO D07FKQ Siponimod Approved T13852 DRUGINFO D0L9KH APD-334 Phase 3 T13852 DRUGINFO D0Y5ZT KRP-203 Phase 2 T13852 DRUGINFO D00ISN MT-1303 Phase 2 T13852 DRUGINFO D0I2RB ONO-4641 Phase 2 T13852 DRUGINFO D0Q0JI ASP-4058 Phase 1 T13852 DRUGINFO D0GG7L BMS-986104 Phase 1 T13852 DRUGINFO D0X8XT CS-0777 Phase 1 T13852 DRUGINFO D0B4CD GSK-2018682 Phase 1 T13852 DRUGINFO D0XE5M SAR247799 Phase 1 T13852 DRUGINFO D0KV2E Sonepcizumab Phase 1 T13852 DRUGINFO D07UGA Sphingosine-1-phosphate Phase 1 T13852 DRUGINFO D0N8AB PF-4629991 Discontinued in Phase 1 T13852 DRUGINFO D0Y0BC XL-541 Terminated T13852 DRUGINFO D06XMB (3-Tetradecylamino-cyclohexyl)-phosphonic acid Investigative T13852 DRUGINFO D0N0BN (3-Tetradecylamino-cyclopentyl)-phosphonic acid Investigative T13852 DRUGINFO D0O4JU (S)-FTY720P Investigative T13852 DRUGINFO D0D5QS [3-(4-Nonyl-benzylamino)-propyl]-phosphonic acid Investigative T13852 DRUGINFO D0P2AZ 1-(4-nonylbenzyl)azetidine-3-carboxylic acid Investigative T13852 DRUGINFO D0LO4T 1-(4-nonylbenzyl)pyrrolidin-3-ylphosphonic acid Investigative T13852 DRUGINFO D07EAB 1-(4-nonylbenzyl)pyrrolidine-3-carboxylic acid Investigative T13852 DRUGINFO D00VHN 3-(N-alkylamino) propylphosphonic acid derivative Investigative T13852 DRUGINFO D0P1TY 3-(tetradecylamino)propylphosphonic acid Investigative T13852 DRUGINFO D04XCB 3-amino-5-(4-octylphenyl)pentanoic acid Investigative T13852 DRUGINFO D08VLT 4-amino-6-(4-octylphenyl)hexanoic acid Investigative T13852 DRUGINFO D05KEE AFD(R) Investigative T13852 DRUGINFO D09NWW AMG-247 Investigative T13852 DRUGINFO D03BRM AUY954 Investigative T13852 DRUGINFO D0YC1R BMS-520 Investigative T13852 DRUGINFO D05SYL CYM5181 Investigative T13852 DRUGINFO D00ZXX CYM5442 Investigative T13852 DRUGINFO D06DYN FTY720-phosphate Investigative T13852 DRUGINFO D09ESF GNF-PF-78 Investigative T13852 DRUGINFO D0R2ZN GNF-PF-826 Investigative T13852 DRUGINFO D0T4LT GSK-1842799C Investigative T13852 DRUGINFO D0U7YK KRP 203-phosphate Investigative T13852 DRUGINFO D0IL7V KRP-107 Investigative T13852 DRUGINFO D0X0UR LPA Investigative T13852 DRUGINFO D02LTS NIBR-0213 Investigative T13852 DRUGINFO D02OCD NIBR-785 Investigative T13852 DRUGINFO D0G6KH NOX-S91 Investigative T13852 DRUGINFO D0ZU0O SEW2871 Investigative T13852 DRUGINFO D0W1ZW VPC03090-P Investigative T13852 DRUGINFO D05EDD VPC23019 Investigative T13852 DRUGINFO D06GFH VPC44116 Investigative T13852 DRUGINFO D03AAC W146 Investigative T13852 KEGGPATH hsa04068:FoxO signaling pathway T13852 KEGGPATH hsa04071:Sphingolipid signaling pathway T13852 KEGGPATH hsa04080:Neuroactive ligand-receptor interaction T13852 WIKIPATH WP117:GPCRs, Other T13852 WIKIPATH WP1824:GPCR downstream signaling T13852 WIKIPATH WP1825:GPCR ligand binding T13852 WIKIPATH WP247:Small Ligand GPCRs T13852 WIKIPATH WP26:Signal Transduction of S1P Receptor T13852 REACPATH R-HSA-418594:G alpha (i) signalling events T13852 REACPATH R-HSA-419408:Lysosphingolipid and LPA receptors T13852 NET_PATH NetPath_14:IL2 Signaling Pathway T13852 NET_PATH NetPath_16:IL4 Signaling Pathway T13852 NET_PATH NetPath_7:TGF_beta_Receptor Signaling Pathway T13852 INTEPATH fcer1pathway:Fc-epsilon receptor I signaling in mast cells T13852 INTEPATH pdgfrbpathway:PDGFR-beta signaling pathway T13852 INTEPATH s1p_meta_pathway:Sphingosine 1-phosphate (S1P) pathway T13852 INTEPATH s1p_s1p1_pathway:S1P1 pathway T13852 INTEPATH s1p_s1p3_pathway:S1P3 pathway T76904 TARGETID T76904 T76904 FORMERID TTDS00362 T76904 UNIPROID COMT_HUMAN T76904 TARGNAME Catechol-O-methyl-transferase (COMT) T76904 GENENAME COMT T76904 TARGTYPE Successful target T76904 SYNONYMS S-COMT; MB-COMT; Catechol-O-methyltransferase; COMT T76904 FUNCTION Catalyzes the O-methylation, and thereby the inactivation, of catecholamine neurotransmitters and catechol hormones. Also shortens the biological half-lives of certain neuroactive drugs, like L-DOPA, alpha-methyl DOPA and isoproterenol. T76904 PDBSTRUC 5LSA; 4XUE; 4XUD; 4XUC; 4PYK T76904 BIOCLASS Methyltransferase T76904 ECNUMBER EC 2.1.1.6 T76904 SEQUENCE MPEAPPLLLAAVLLGLVLLVVLLLLLRHWGWGLCLIGWNEFILQPIHNLLMGDTKEQRILNHVLQHAEPGNAQSVLEAIDTYCEQKEWAMNVGDKKGKIVDAVIQEHQPSVLLELGAYCGYSAVRMARLLSPGARLITIEINPDCAAITQRMVDFAGVKDKVTLVVGASQDIIPQLKKKYDVDTLDMVFLDHWKDRYLPDTLLLEECGLLRKGTVLLADNVICPGAPDFLAHVRGSSCFECTHYQSFLEYREVVDGLEKAIYKGPGSEAGP T76904 DRUGINFO D0J1VY Entacapone Approved T76904 DRUGINFO D01SGK Opicapone Approved T76904 DRUGINFO D0Y7PG Tolcapone Approved T76904 DRUGINFO D0R2NE Entacapone+levodopa+carbidopa Phase 3 T76904 DRUGINFO D0G4DE BIA 3-202 Phase 2 T76904 DRUGINFO D0P5TR CGP-28014 Phase 2 T76904 DRUGINFO D08LVF Nitecapone Discontinued in Phase 2 T76904 DRUGINFO D0U1CL PGX-200097 Preclinical T76904 DRUGINFO D0OE1R (3,4-DIHYDROXY-2-NITROPHENYL)(PHENYL)METHANONE Investigative T76904 DRUGINFO D0C0OT 1-(3,4-dihydroxy-2-nitrophenyl)-2-phenylethanone Investigative T76904 DRUGINFO D01AFH 1-(3,4-dihydroxy-5-nitrophenyl)-2-phenoxyethanone Investigative T76904 DRUGINFO D09AYR 3,5-Dinitrocatechol Investigative T76904 DRUGINFO D0HW3Y 5,6-dihydroxy-7-nitro-2,3-dihydroinden-1-one Investigative T76904 DRUGINFO D0M3PG 6,7-dihydroxy-8-nitro-1-tetralone Investigative T76904 DRUGINFO D06LED 7,8-dihydroxy-4-phenyl-2H-chromen-2-one Investigative T76904 DRUGINFO D0XT0I BIA Investigative T76904 KEGGPATH hsa00140:Steroid hormone biosynthesis T76904 KEGGPATH hsa00350:Tyrosine metabolism T76904 KEGGPATH hsa01100:Metabolic pathways T76904 KEGGPATH hsa04728:Dopaminergic synapse T76904 WIKIPATH WP1870:Neurotransmitter Clearance In The Synaptic Cleft T76904 WIKIPATH WP1880:Phase II conjugation T76904 WIKIPATH WP2436:Dopamine metabolism T76904 WIKIPATH WP550:Biogenic Amine Synthesis T76904 WIKIPATH WP697:Estrogen metabolism T76904 WIKIPATH WP702:Metapathway biotransformation T76904 WIKIPATH WP704:Methylation Pathways T76904 WHIZPATH PW000142:Tyrosine Metabolism T76904 PANTPATH P00001:Adrenaline and noradrenaline biosynthesis T76904 PANTPATH P05912:Dopamine receptor mediated signaling pathway T76904 BIOCPATH PWY-6334:L-dopa degradation T76904 BIOCPATH PWY-6342:Noradrenaline and adrenaline degradation T76904 BIOCPATH PWY6666-2:Dopamine degradation T76369 TARGETID T76369 T76369 FORMERID TTDR00274 T76369 UNIPROID EST1_HUMAN T76369 TARGNAME Liver carboxylesterase (CES1) T76369 GENENAME CES1 T76369 TARGTYPE Successful target T76369 SYNONYMS Serine esterase 1; Monocyte/macrophage serine esterase; Human carboxylesterase 1; HMSE; HCE1; CES1; Brain carboxylesterase hBr1; Acyl coenzyme A:cholesterol acyltransferase T76369 FUNCTION Involved in the detoxification of xenobiotics and in the activation of ester and amide prodrugs. Hydrolyzes aromatic and aliphatic esters, but has no catalytic activity toward amides or a fatty acyl coa ester. T76369 PDBSTRUC 5A7H; 5A7G; 5A7F; 4AB1; 3K9B T76369 BIOCLASS Carboxylic ester hydrolase T76369 ECNUMBER EC 3.1.1.1 T76369 SEQUENCE MWLRAFILATLSASAAWGHPSSPPVVDTVHGKVLGKFVSLEGFAQPVAIFLGIPFAKPPLGPLRFTPPQPAEPWSFVKNATSYPPMCTQDPKAGQLLSELFTNRKENIPLKLSEDCLYLNIYTPADLTKKNRLPVMVWIHGGGLMVGAASTYDGLALAAHENVVVVTIQYRLGIWGFFSTGDEHSRGNWGHLDQVAALRWVQDNIASFGGNPGSVTIFGESAGGESVSVLVLSPLAKNLFHRAISESGVALTSVLVKKGDVKPLAEQIAITAGCKTTTSAVMVHCLRQKTEEELLETTLKMKFLSLDLQGDPRESQPLLGTVIDGMLLLKTPEELQAERNFHTVPYMVGINKQEFGWLIPMQLMSYPLSEGQLDQKTAMSLLWKSYPLVCIAKELIPEATEKYLGGTDDTVKKKDLFLDLIADVMFGVPSVIVARNHRDAGAPTYMYEFQYRPSFSSDMKPKTVIGDHGDELFSVFGAPFLKEGASEEEIRLSKMVMKFWANFARNGNPNGEGLPHWPEYNQKEGYLQIGANTQAAQKLKDKEVAFWTNLFAKKAVEKPPQTEHIEL T76369 DRUGINFO D0OR2L Cholic Acid Approved T76369 DRUGINFO D02GWF PACTIMIBE Phase 2/3 T76369 DRUGINFO D0YB4D Eldacimibe Phase 2 T76369 DRUGINFO D03PYD K-604 Phase 2 T76369 DRUGINFO D05EMV GR148672X Clinical trial T76369 DRUGINFO D0O1KX Avasimibe Discontinued in Phase 3 T76369 DRUGINFO D0D1XG CI-976 Discontinued in Phase 2 T76369 DRUGINFO D0E1UZ CL-283796 Discontinued in Phase 2 T76369 DRUGINFO D01IDE E-5324 Discontinued in Phase 2 T76369 DRUGINFO D0W0ED Eflucimibe Discontinued in Phase 2 T76369 DRUGINFO D07DBS RP-64477 Discontinued in Phase 2 T76369 DRUGINFO D04ODQ 447C88 Discontinued in Phase 1 T76369 DRUGINFO D06FCR CL-277082 Discontinued in Phase 1 T76369 DRUGINFO D03QZB F-1394 Discontinued in Phase 1 T76369 DRUGINFO D0IZ7T YM-17E Discontinued in Phase 1 T76369 DRUGINFO D0D9AD YM-750 Discontinued in Phase 1 T76369 DRUGINFO D09MJO HL-004 Preclinical T76369 DRUGINFO D0J8TH CEB-925 Terminated T76369 DRUGINFO D0PG0S CI-999 Terminated T76369 DRUGINFO D0K8KJ DuP-129 Terminated T76369 DRUGINFO D00KQT FR-129169 Terminated T76369 DRUGINFO D0O2AC FR-145237 Terminated T76369 DRUGINFO D03EHR Lecimibide Terminated T76369 DRUGINFO D03JRJ NTE-122 Terminated T76369 DRUGINFO D03YPL RP-70676 Terminated T76369 DRUGINFO D06KFR RP-73163 Terminated T76369 DRUGINFO D0OK8M TEI-6522 Terminated T76369 DRUGINFO D0Y8RM (1r)-1,2,2-trimethylpropyl (r)-methylphosphinate Investigative T76369 DRUGINFO D0F0JI (E)-Octadec-9-enoic acid phenylamide Investigative T76369 DRUGINFO D0JI0H 1-(2-bromoethyl)-1H-indole-2,3-dione Investigative T76369 DRUGINFO D05PNO 1-(2-iodoethyl)-1H-indole-2,3-dione Investigative T76369 DRUGINFO D07EDG 1-(3,4-dichlorobenzyl)-1H-indole-2,3-dione Investigative T76369 DRUGINFO D0N8YZ 1-(3,4-Dimethyl-phenyl)-2-phenyl-ethane-1,2-dione Investigative T76369 DRUGINFO D0C9AD 1-(4-chlorobenzyl)-1H-indole-2,3-dione Investigative T76369 DRUGINFO D0F3RN 1-(4-Chloro-phenyl)-2-phenyl-ethane-1,2-dione Investigative T76369 DRUGINFO D0L1ST 1-(4-Chloro-phenyl)-2-p-tolyl-ethane-1,2-dione Investigative T76369 DRUGINFO D0T5XC 1-(4-Methoxy-phenyl)-2-phenyl-ethane-1,2-dione Investigative T76369 DRUGINFO D0D7FN 1-(4-Nitro-phenyl)-2-phenyl-ethane-1,2-dione Investigative T76369 DRUGINFO D0F7NU 1,1,1-trifluoro-3-(hexylsulfinyl)propan-2-one Investigative T76369 DRUGINFO D04JVA 1,1,1-trifluoro-3-(hexylsulfonyl)propan-2-one Investigative T76369 DRUGINFO D0Z7WK 1,1,1-trifluoro-3-(hexylthio)propan-2-one Investigative T76369 DRUGINFO D04UEN 1,1,1-trifluoro-3-(octylsulfinyl)propan-2-one Investigative T76369 DRUGINFO D00IAK 1,1,1-trifluoro-3-(octylsulfonyl)propan-2-one Investigative T76369 DRUGINFO D0Q3GH 1,1,1-trifluoro-3-(octylthio)propan-2-one Investigative T76369 DRUGINFO D0I7FF 1,1,1-trifluorododecan-2-one Investigative T76369 DRUGINFO D0JH7C 1,10-phenanthroline-5,6-dione Investigative T76369 DRUGINFO D06GYH 1,2-bis(2,3,4-trifluorophenyl)-2-hydroxyethanone Investigative T76369 DRUGINFO D0P1IK 1,2-bis(2,3,4-trifluorophenyl)ethane-1,2-dione Investigative T76369 DRUGINFO D0D2HH 1,2-bis(2,3,5-trifluorophenyl)-2-hydroxyethanone Investigative T76369 DRUGINFO D08UOB 1,2-bis(2,3,5-trifluorophenyl)ethane-1,2-dione Investigative T76369 DRUGINFO D0E2IG 1,2-bis(2,3,6-trifluorophenyl)ethane-1,2-dione Investigative T76369 DRUGINFO D0M2ZD 1,2-bis(2,3-difluorophenyl)-2-hydroxyethanone Investigative T76369 DRUGINFO D05LTW 1,2-bis(2,3-fluorophenyl)ethane-1,2-dione Investigative T76369 DRUGINFO D0ZT5C 1,2-bis(2,4-difluorophenyl)-2-hydroxyethanone Investigative T76369 DRUGINFO D02HQS 1,2-bis(2,4-difluorophenyl)ethane-1,2-dione Investigative T76369 DRUGINFO D00PLH 1,2-bis(2,5-difluorophenyl)-2-hydroxyethanone Investigative T76369 DRUGINFO D05EMT 1,2-bis(2,5-difluorophenyl)ethane-1,2-dione Investigative T76369 DRUGINFO D04CDV 1,2-bis(2,6-difluorophenyl)-2-hydroxyethanone Investigative T76369 DRUGINFO D01VCS 1,2-bis(2,6-difluorophenyl)ethane-1,2-dione Investigative T76369 DRUGINFO D03HZT 1,2-Bis-(2-chloro-phenyl)-ethane-1,2-dione Investigative T76369 DRUGINFO D05VUC 1,2-bis(2-fluorophenyl)-2-hydroxyethanone Investigative T76369 DRUGINFO D02GJG 1,2-bis(2-fluorophenyl)ethane-1,2-dione Investigative T76369 DRUGINFO D01HZN 1,2-bis(3,4,5-trifluorophenyl)-2-hydroxyethanone Investigative T76369 DRUGINFO D0CN8Z 1,2-bis(3,4,5-trifluorophenyl)ethane-1,2-dione Investigative T76369 DRUGINFO D0U0BV 1,2-bis(3,4-difluorophenyl)-2-hydroxyethanone Investigative T76369 DRUGINFO D0K6OM 1,2-bis(3,4-difluorophenyl)ethane-1,2-dione Investigative T76369 DRUGINFO D0L4MF 1,2-bis(3,5-difluorophenyl)-2-hydroxyethanone Investigative T76369 DRUGINFO D09LSR 1,2-bis(3,5-difluorophenyl)ethane-1,2-dione Investigative T76369 DRUGINFO D0AW4P 1,2-bis(3-fluorophenyl)-2-hydroxyethanon Investigative T76369 DRUGINFO D0Y6RZ 1,2-bis(3-fluorophenyl)ethane-1,2-dione Investigative T76369 DRUGINFO D01VAU 1,2-Bis-(3-methoxy-phenyl)-ethane-1,2-dione Investigative T76369 DRUGINFO D0UT1X 1,2-Bis-(3-nitro-phenyl)-ethane-1,2-dione Investigative T76369 DRUGINFO D06FFD 1,2-Bis-(4-bromo-phenyl)-ethane-1,2-dione Investigative T76369 DRUGINFO D05EYA 1,2-Bis-(4-chloro-phenyl)-ethane-1,2-dione Investigative T76369 DRUGINFO D0DW9J 1,2-bis(4-fluorophenyl)ethane-1,2-dione Investigative T76369 DRUGINFO D0UZ8R 1,2-Bis-(4-methoxy-phenyl)-ethane-1,2-dione Investigative T76369 DRUGINFO D0LJ2F 1,2-dicyclohexylethane-1,2-dione Investigative T76369 DRUGINFO D03WOU 1,2-Di-naphthalen-2-yl-ethane-1,2-dione Investigative T76369 DRUGINFO D0UK5A 1,2-Di-p-tolyl-ethane-1,2-dione Investigative T76369 DRUGINFO D01XGP 1,2-indanedione Investigative T76369 DRUGINFO D0W9VA 1,2-NAPHTHOQUINONE Investigative T76369 DRUGINFO D05XRY 11,12-dihydro-dibenzo[a,e]cyclooctene-5,6-dione Investigative T76369 DRUGINFO D0O0LU 1-benzyl-1H-indole-2,3-dione Investigative T76369 DRUGINFO D0M5NR 1-butyryl-1H-indole-2,3-dione Investigative T76369 DRUGINFO D00ANJ 1-dodecyl-1H-indole-2,3-dione Investigative T76369 DRUGINFO D0ZL6B 1-hexadecyl-1H-indole-2,3-dione Investigative T76369 DRUGINFO D0U3JD 1-methyl-1H-indole-2,3-dione Investigative T76369 DRUGINFO D01HRG 1-phenyl-1H-indole-2,3-dione Investigative T76369 DRUGINFO D0B8YX 1-Phenyl-2-p-tolyl-ethane-1,2-dione Investigative T76369 DRUGINFO D02TLP 1-Phenyl-propane-1,2-dione Investigative T76369 DRUGINFO D07CFJ 1-propionyl-1H-indole-2,3-dione Investigative T76369 DRUGINFO D08AOG 2,2-Dimethoxy-1,2-diphenyl-ethanone Investigative T76369 DRUGINFO D01NDE 2,2-dimethyl-3-methyleneheptadecane Investigative T76369 DRUGINFO D0H5II 2-methoxy-3,4-methylenedioxybenzophenone Investigative T76369 DRUGINFO D0O9EB 3-(butylsulfinyl)-1,1,1-trifluoropropan-2-one Investigative T76369 DRUGINFO D0FO4J 3-(butylthio)-1,1,1-trifluoropropan-2-one Investigative T76369 DRUGINFO D00VKB 3-(decylsulfinyl)-1,1,1-trifluoropropan-2-one Investigative T76369 DRUGINFO D0Y0FN 3-(decylsulfonyl)-1,1,1-trifluoropropan-2-one Investigative T76369 DRUGINFO D0E5CF 3-(decylthio)-1,1,1-trifluoropropan-2-one Investigative T76369 DRUGINFO D0B4GJ 3-(dodecylsulfinyl)-1,1,1-trifluoropropan-2-one Investigative T76369 DRUGINFO D02SDT 3-(dodecylsulfonyl)-1,1,1-trifluoropropan-2-one Investigative T76369 DRUGINFO D0N0HK 3,4,5,6-Tetrachloro-[1,2]benzoquinone Investigative T76369 DRUGINFO D0Z1WQ 3,5-Di-tert-butyl-[1,2]benzoquinone Investigative T76369 DRUGINFO D0BB2U 4-(2-Oxo-2-phenyl-acetyl)-benzoic acid Investigative T76369 DRUGINFO D0Z6CZ 4,5-dichloro-1H-indole-2,3-dione Investigative T76369 DRUGINFO D04EXR 4,6-dichloro-1H-indole-2,3-dione Investigative T76369 DRUGINFO D0EK7H 4,7-dichloro-1H-indole-2,3-dione Investigative T76369 DRUGINFO D04AXR 4-chloro-1H-indole-2,3-dione Investigative T76369 DRUGINFO D0B1TQ 4-chloro-7-methyl-1H-indole-2,3-dione Investigative T76369 DRUGINFO D07WHV 4-Piperidino-Piperidine Investigative T76369 DRUGINFO D0ZR2T 5-(trifluoromethoxy)-1H-indole-2,3-dione Investigative T76369 DRUGINFO D0WX6R 5,6-dinitroacenaphthoquinone Investigative T76369 DRUGINFO D0NJ4G 5,7-dichloro-1H-indole-2,3-dione Investigative T76369 DRUGINFO D03TPH 5-chloro-1H-indole-2,3-dione Investigative T76369 DRUGINFO D0Z8HX 6,7-dichloro-1H-indole-2,3-dione Investigative T76369 DRUGINFO D0N9ZR 6-bromo-5-methyl-1H-indole-2,3-dione Investigative T76369 DRUGINFO D0E5ZP 7-(trifluoromethyl)-1H-indole-2,3-dione Investigative T76369 DRUGINFO D0X0ER 7-chloro-1H-indole-2,3-dione Investigative T76369 DRUGINFO D0K6PO Acenanthrene-9,10-dione Investigative T76369 DRUGINFO D06VGD ACENAPHTHOQUINONE Investigative T76369 DRUGINFO D07LUR Alpha-D-Mannose Investigative T76369 DRUGINFO D0Y7FX BENZIL Investigative T76369 DRUGINFO D0Z5KQ Benzoin Investigative T76369 DRUGINFO D0D0BI CHLORANIL Investigative T76369 DRUGINFO D02VYI Dibutyl 2,2,2-trifluoro-1-phenylethyl phosphate Investigative T76369 DRUGINFO D01GSO Diethyl 2,2,2-trifluoro-1-phenylethyl phosphate Investigative T76369 DRUGINFO D0XP0J Dimethyl 2,2,2-trifluoro-1-phenylethyl phosphate Investigative T76369 DRUGINFO D05AVX Heptane-2,3-dione Investigative T76369 DRUGINFO D0V9MG KY-382 Investigative T76369 DRUGINFO D06ZPI N-Methylnaloxonium Investigative T76369 DRUGINFO D0F5VY NSC-23180 Investigative T76369 DRUGINFO D0T7YM Oleic acid anilide Investigative T76369 DRUGINFO D08WQM O-Sialic Acid Investigative T76369 DRUGINFO D0Q2YJ Phenanthrene-9,10-dione Investigative T76369 DRUGINFO D0A2NK PYRIPYROPENE A Investigative T76369 DRUGINFO D0W0PH SCH-48375 Investigative T76369 DRUGINFO D02EZF SMP-797 Investigative T76369 DRUGINFO D0F4QX Thenoyltrifluoroacetone Investigative T76369 DRUGINFO D05ZCX Thieno[3,2-e][1]benzothiophene-4,5-dione Investigative T76369 DRUGINFO D0OH1O VULM-1457 Investigative T76369 KEGGPATH hsa00983:Drug metabolism - other enzymes T76369 KEGGPATH hsa01100:Metabolic pathways T76369 WIKIPATH WP136:Phase I biotransformations, non P450 T76369 WIKIPATH WP1601:Fluoropyrimidine Activity T76369 WIKIPATH WP229:Irinotecan Pathway T76369 WIKIPATH WP2645:Heroin metabolism T76369 WIKIPATH WP2882:Nuclear Receptors Meta-Pathway T76369 WIKIPATH WP2884:NRF2 pathway T76369 INTEPATH e2f_pathway:E2F transcription factor network T60529 TARGETID T60529 T60529 FORMERID TTDS00040 T60529 UNIPROID PGH1_HUMAN T60529 TARGNAME Prostaglandin G/H synthase 1 (COX-1) T60529 GENENAME PTGS1 T60529 TARGTYPE Successful target T60529 SYNONYMS Prostaglandin-endoperoxide synthase 1; Prostaglandin H2 synthase 1; PHS 1; PGHS-1; PGH synthase 1; Cyclooxygenase-1; COX1; COX-1 T60529 FUNCTION Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Involved in the constitutive production of prostanoids in particular in the stomach and platelets. In gastric epithelial cells, it is a key step in the generation of prostaglandins, such as prostaglandin E2 (PGE2), which plays an important role in cytoprotection. In platelets, it is involved in the generation of thromboxane A2 (TXA2), which promotes platelet activation and aggregation, vasoconstriction and proliferation of vascular smooth muscle cells. T60529 BIOCLASS Paired donor oxygen oxidoreductase T60529 ECNUMBER EC 1.14.99.1 T60529 SEQUENCE MSRSLLLWFLLFLLLLPPLPVLLADPGAPTPVNPCCYYPCQHQGICVRFGLDRYQCDCTRTGYSGPNCTIPGLWTWLRNSLRPSPSFTHFLLTHGRWFWEFVNATFIREMLMRLVLTVRSNLIPSPPTYNSAHDYISWESFSNVSYYTRILPSVPKDCPTPMGTKGKKQLPDAQLLARRFLLRRKFIPDPQGTNLMFAFFAQHFTHQFFKTSGKMGPGFTKALGHGVDLGHIYGDNLERQYQLRLFKDGKLKYQVLDGEMYPPSVEEAPVLMHYPRGIPPQSQMAVGQEVFGLLPGLMLYATLWLREHNRVCDLLKAEHPTWGDEQLFQTTRLILIGETIKIVIEEYVQQLSGYFLQLKFDPELLFGVQFQYRNRIAMEFNHLYHWHPLMPDSFKVGSQEYSYEQFLFNTSMLVDYGVEALVDAFSRQIAGRIGGGRNMDHHILHVAVDVIRESREMRLQPFNEYRKRFGMKPYTSFQELVGEKEMAAELEELYGDIDALEFYPGLLLEKCHPNSIFGESMIEIGAPFSLKGLLGNPICSPEYWKPSTFGGEVGFNIVKTATLKKLVCLNTKTCPYVSFRVPDASQDDGPAVERPSTEL T60529 DRUGINFO D01WJL Aminosalicylic Acid Approved T60529 DRUGINFO D0A6KR Balsalazide Approved T60529 DRUGINFO D0U1OM Bromfenac Approved T60529 DRUGINFO D0Q5XX Eicosapentaenoic acid/docosa-hexaenoic acid Approved T60529 DRUGINFO D06LHG FENBUFEN Approved T60529 DRUGINFO D0B2WJ Flufenamic Acid Approved T60529 DRUGINFO D0O1TC Gamma-Homolinolenic acid Approved T60529 DRUGINFO D0MN9K Meclofenamate Sodium Approved T60529 DRUGINFO D0C4YC Mesalazine Approved T60529 DRUGINFO D0DJ1B Naproxen Approved T60529 DRUGINFO D00IBN Piroxicam Approved T60529 DRUGINFO D07HBX Salicyclic acid Approved T60529 DRUGINFO D0Y0JH Salsalate Approved T60529 DRUGINFO D07BPS Suprofen Approved T60529 DRUGINFO D0AL8M IMRECOXIB Phase 4 T60529 DRUGINFO D0G2IC (S)-FLURBIPROFEN Preregistration T60529 DRUGINFO D07SDQ Curcumin Phase 3 T60529 DRUGINFO D0U3EP Resveratrol Phase 3 T60529 DRUGINFO D0C4DZ ThermoProfen Phase 3 T60529 DRUGINFO D05TPI EPICATECHIN Phase 1/2 T60529 DRUGINFO D0F5BL EXO-230 Phase 1/2 T60529 DRUGINFO D0S8TB Carbamate derivative 2 Patented T60529 DRUGINFO D0Q5PL INDOPROFEN Withdrawn from market T60529 DRUGINFO D06JRD Metamizole Withdrawn from market T60529 DRUGINFO D0O2IE Phenacetin Withdrawn from market T60529 DRUGINFO D0BZ1Q CRx-401 Discontinued in Phase 2 T60529 DRUGINFO D0ZL4F R-ketoprofen Discontinued in Phase 2 T60529 DRUGINFO D0P3KA TEBUFELONE Discontinued in Phase 2 T60529 DRUGINFO D03AKL ATLIPROFEN METHYL ESTER Terminated T60529 DRUGINFO D0O9JX SC-58451 Terminated T60529 DRUGINFO D08BPE (-)-3-O-acetylspectaline Investigative T60529 DRUGINFO D0N0YS (11H-Dibenzo[b,e][1,4]dioxepin-2-yl)-acetic acid Investigative T60529 DRUGINFO D0X5RR (11H-Dibenzo[b,e][1,4]dioxepin-7-yl)-acetic acid Investigative T60529 DRUGINFO D0GF9J (11H-Dibenzo[b,e][1,4]dioxepin-8-yl)-acetic acid Investigative T60529 DRUGINFO D02HVL (3-Chloro-4-Propoxy-Phenyl)-Acetic Acid Investigative T60529 DRUGINFO D0A4LW (R)-2-(4-Isobutyl-phenyl)-N-phenyl-propionamide Investigative T60529 DRUGINFO D0D6UC (Z)-2'-des-methyl sulindac sulfide Investigative T60529 DRUGINFO D0LL9E 1-(4-(methylsulfonyl)phenyl)-3-phenylurea Investigative T60529 DRUGINFO D0T7BP 1-(4-(methylsulfonyl)phenyl)-3-p-tolylurea Investigative T60529 DRUGINFO D0V9AU 1-(4-aminosulfonylphenyl)-2-(2-pyridyl)acetylene Investigative T60529 DRUGINFO D0Q8TK 1-(4-aminosulfonylphenyl)-2-(4-pyridyl)acetylene Investigative T60529 DRUGINFO D0OX0B 1,2-dihydro-3-(2,3,4-trimethoxyphenyl)naphthalene Investigative T60529 DRUGINFO D06FTI 2-(1,1'-Biphenyl-4-Yl)Propanoic Acid Investigative T60529 DRUGINFO D0U0YE 2-(2-(2,6-dimethylphenylamino)phenyl)acetic acid Investigative T60529 DRUGINFO D02CCB 2-(2,3,4-trimethoxyphenyl)-1H-indene Investigative T60529 DRUGINFO D0N7OP 2-(2-methoxyphenyl)-1H-indene Investigative T60529 DRUGINFO D0R1UO 2-(2-Methylpropanoyl)-1,3,5-benzenetriol Investigative T60529 DRUGINFO D0M9RL 2-(3'-Allyl-biphenyl-4-yl)-propionic acid Investigative T60529 DRUGINFO D08QAH 2-(3'-Ethyl-biphenyl-4-yl)-propionic acid Investigative T60529 DRUGINFO D02GZX 2-(3'-Ethylsulfanyl-biphenyl-4-yl)-propionic acid Investigative T60529 DRUGINFO D0L4TM 2-(3-Phenyl-propyl)-1,2-dihydro-indazol-3-one Investigative T60529 DRUGINFO D0YI3V 2-(3'-Vinyl-biphenyl-4-yl)-propionic acid Investigative T60529 DRUGINFO D02FGY 2-(N-(2-Ffuorophenyl)pyrrol-3-yl) acetic acid Investigative T60529 DRUGINFO D07STC 2-(N-(2-fluorophenyl)pyrrol-2-yl) acetic acid Investigative T60529 DRUGINFO D00VBX 2-(p-Methylsulfonylbenzoyl)furan Investigative T60529 DRUGINFO D01JYF 2,4'-Dimethoxy-5,3'-di-(2-propenyl)-biphenyl Investigative T60529 DRUGINFO D0JQ1T 2-[4-(1H-Indol-5-yl)-phenyl]-propionic acid Investigative T60529 DRUGINFO D0J7YU 2-Benzyl-1,2-dihydro-indazol-3-one Investigative T60529 DRUGINFO D05DOM 2-Bromoacetyl Group Investigative T60529 DRUGINFO D05KYE 2'-epi-guianin Investigative T60529 DRUGINFO D0SJ3W 2-Furan-2-ylmethyl-1,2-dihydro-indazol-3-one Investigative T60529 DRUGINFO D0U8CM 2-Methyl-1,2-dihydro-indazol-3-one Investigative T60529 DRUGINFO D0X6SA 2-Naphthalen-2-ylmethyl-1,2-dihydro-indazol-3-one Investigative T60529 DRUGINFO D06HUQ 2-Phenethyl-1,2-dihydro-indazol-3-one Investigative T60529 DRUGINFO D0S0PB 2-Phenyl-1,2-dihydro-indazol-3-one Investigative T60529 DRUGINFO D0ZI8Y 3 beta-O-acetyloleanolic acid Investigative T60529 DRUGINFO D09HWQ 3-(4-Methanesulfonyl-phenyl)-1-phenyl-propynone Investigative T60529 DRUGINFO D0PQ3Q 4-(4-Chlorophenyl)-5-(4-methoxyphenyl)isothiazole Investigative T60529 DRUGINFO D09MDB 4-(4-Chlorophenyl)-5-p-tolyl-1,2-selenazole Investigative T60529 DRUGINFO D0G7RA 4-(4-Chlorophenyl)-5-p-tolyl-3H-1,2-dithiol-3-one Investigative T60529 DRUGINFO D0OW4W 4-(4-Chlorophenyl)-5-p-tolylisothiazole Investigative T60529 DRUGINFO D00VHS 4-(5-(4-Hydroxyphenyl)isothiazol-4-yl)phenol Investigative T60529 DRUGINFO D0E5MK 4,5-Bis(4-chlorophenyl)-1,2-selenazole Investigative T60529 DRUGINFO D01VRB 4,5-Bis(4-chlorophenyl)isothiazole Investigative T60529 DRUGINFO D0D0JE 4,5-Bis(4-methoxyphenyl)-1,2-selenazole Investigative T60529 DRUGINFO D0X4LI 4,5-Bis(4-methoxyphenyl)-3H-1,2-dithiol-3-one Investigative T60529 DRUGINFO D02PLG 4,5-Bis(4-methoxyphenyl)-3H-1,2-dithiole-3-thione Investigative T60529 DRUGINFO D0F0JU 4,5-Bis(4-methoxyphenyl)isothiazole Investigative T60529 DRUGINFO D0Y7ND 4-amino-N-(2-chlorophenyl)benzenesulfonamide Investigative T60529 DRUGINFO D02DYG 4-amino-N-(4-chlorophenyl)benzenesulfonamide Investigative T60529 DRUGINFO D04ORY 4-amino-N-p-tolylbenzenesulfonamide Investigative T60529 DRUGINFO D0S7ZQ 4'-Methoxy-5,3'-dipropyl-biphenyl-2ol Investigative T60529 DRUGINFO D07OAV 5-(2-1H-indenyl)-1,3-benzodioxole Investigative T60529 DRUGINFO D04ZGF 5-(2-Imidazol-1-yl-ethyl)-7,8-dihydro-quinoline Investigative T60529 DRUGINFO D0J6TU 5-(4-Chlorophenyl)-4-(4-methoxyphenyl)isothiazole Investigative T60529 DRUGINFO D08RYB 5-(4-Chlorophenyl)-4-p-tolyl-1,2-selenazole Investigative T60529 DRUGINFO D00XIX 5-(4-Chlorophenyl)-4-p-tolyl-3H-1,2-dithiol-3-one Investigative T60529 DRUGINFO D03TLR 5-(4-Chlorophenyl)-4-p-tolylisothiazole Investigative T60529 DRUGINFO D07RTV 5-(4-Methoxyphenyl)-4-p-tolyl-1,2-selenazole Investigative T60529 DRUGINFO D08RCQ 5-(4-Methoxyphenyl)-4-p-tolylisothiazole Investigative T60529 DRUGINFO D0R6ZC 5,3'-Dipropyl-biphenyl-2,4'-diol Investigative T60529 DRUGINFO D06WML 5-Ethyl-3,4-diphenyl-isoxazole Investigative T60529 DRUGINFO D04YPP 5-Methyl-3,4-diphenyl-isoxazole Investigative T60529 DRUGINFO D07ARK 5-Phenyl-pentanoic acid benzyl-hydroxy-amide Investigative T60529 DRUGINFO D02VLR Acetic acid 2-hept-2-ynylsulfanyl-phenyl ester Investigative T60529 DRUGINFO D0O8XG Acetic acid 2-hept-3-ynylsulfanyl-phenyl ester Investigative T60529 DRUGINFO D01EWD Acetic acid 2-heptylselanyl-phenyl ester Investigative T60529 DRUGINFO D0X9VY Acetic acid 2-heptylsulfanyl-phenyl ester Investigative T60529 DRUGINFO D00RCV Acetic acid 2-hex-2-ynylsulfanyl-phenyl ester Investigative T60529 DRUGINFO D04KAM Acetic acid 2-hexylsulfanyl-phenyl ester Investigative T60529 DRUGINFO D0M7EI Acetic acid 2-pentylsulfanyl-phenyl ester Investigative T60529 DRUGINFO D09XYZ Acetic Acid Salicyloyl-Amino-Ester Investigative T60529 DRUGINFO D07LUR Alpha-D-Mannose Investigative T60529 DRUGINFO D0HD9P Arachidonic Acid Investigative T60529 DRUGINFO D07ONX Beta-D-Glucose Investigative T60529 DRUGINFO D0SD9H Beta-D-Mannose Investigative T60529 DRUGINFO D02UVH B-Octylglucoside Investigative T60529 DRUGINFO D0V7AA CATECHIN Investigative T60529 DRUGINFO D03EDF DEMETHOXYCURCUMIN Investigative T60529 DRUGINFO D09CMJ FR122047 Investigative T60529 DRUGINFO D0UU1I Heme Investigative T60529 DRUGINFO D04DQJ HONOKIOL Investigative T60529 DRUGINFO D09VTJ Hyperforin Investigative T60529 DRUGINFO D02HSZ IODOINDOMETHACIN Investigative T60529 DRUGINFO D0T5DO IODOSUPROFEN Investigative T60529 DRUGINFO D01OFH METHYLHONOKIOL Investigative T60529 DRUGINFO D0J7YE N-(1H-indazol-5-yl)acetamide Investigative T60529 DRUGINFO D01WLL N-(3-(phenylthio)pyridin-4-yl)methanesulfonamide Investigative T60529 DRUGINFO D0BO9W N-(3-phenoxy-4-pyridinyl)ethanesulfonamide Investigative T60529 DRUGINFO D0L6TP N-(3-phenoxy-4-pyridinyl)propanesulfonamide Investigative T60529 DRUGINFO D0VF6F N-(3-phenoxypyridin-4-yl)methanesulfonamide Investigative T60529 DRUGINFO D06DRL N-(3-phenylamino-4-pyridinyl)methanesulfonamide Investigative T60529 DRUGINFO D04TNI Nitroflurbiprofen Investigative T60529 DRUGINFO D0IB5L O-Acetylserine Investigative T60529 DRUGINFO D0T9QW Oxametacin Investigative T60529 DRUGINFO D06GSY P-(2'-Iodo-5'-Thenoyl)Hydrotropic Acid Investigative T60529 DRUGINFO D03IRR Phenazone Investigative T60529 DRUGINFO D0P1LP PHENIDONE Investigative T60529 DRUGINFO D00GBX Prifelone Investigative T60529 DRUGINFO D0T4VL Primary alcohol metabolite of celecoxib Investigative T60529 DRUGINFO D07SAI Protoporphyrin Ix Containing Co Investigative T60529 DRUGINFO D02DBP RESORCINOL Investigative T60529 DRUGINFO D0CW3A Resveratrol Potassium3-Sulfate Investigative T60529 DRUGINFO D04JZY Resveratrol Potassium4,-Sulfate Investigative T60529 DRUGINFO D0M5MI SC-560 Investigative T60529 DRUGINFO D01HXN TRL-382 Investigative T60529 KEGGPATH hsa00590:Arachidonic acid metabolism T60529 KEGGPATH hsa01100:Metabolic pathways T60529 KEGGPATH hsa04611:Platelet activation T60529 KEGGPATH hsa04726:Serotonergic synapse T60529 WIKIPATH WP15:Selenium Micronutrient Network T60529 WIKIPATH WP167:Eicosanoid Synthesis T60529 WIKIPATH WP1879:Phase 1 - Functionalization of compounds T60529 WIKIPATH WP2650:Arachidonic acid metabolism T60529 WIKIPATH WP98:Prostaglandin Synthesis and Regulation T60529 WHIZPATH PW000044:Arachidonic Acid Metabolism T60529 NET_PATH NetPath_7:TGF_beta_Receptor Signaling Pathway T60529 PANTPATH P00031:Inflammation mediated by chemokine and cytokine signaling pathway T60529 BIOCPATH PWY66-374:C20 prostanoid biosynthesis T06569 TARGETID T06569 T06569 FORMERID TTDR00210 T06569 UNIPROID CAH6_HUMAN T06569 TARGNAME Carbonic anhydrase VI (CA-VI) T06569 GENENAME CA6 T06569 TARGTYPE Successful target T06569 SYNONYMS Secreted carbonic anhydrase; Salivary carbonic anhydrase; Carbonic anhydrase 6; Carbonate dehydratase VI T06569 FUNCTION Its role in saliva is unknown. Reversible hydration of carbon dioxide. T06569 PDBSTRUC 3FE4 T06569 BIOCLASS Alpha-carbonic anhydrase T06569 ECNUMBER EC 4.2.1.1 T06569 SEQUENCE MRALVLLLSLFLLGGQAQHVSDWTYSEGALDEAHWPQHYPACGGQRQSPINLQRTKVRYNPSLKGLNMTGYETQAGEFPMVNNGHTVQISLPSTMRMTVADGTVYIAQQMHFHWGGASSEISGSEHTVDGIRHVIEIHIVHYNSKYKSYDIAQDAPDGLAVLAAFVEVKNYPENTYYSNFISHLANIKYPGQRTTLTGLDVQDMLPRNLQHYYTYHGSLTTPPCTENVHWFVLADFVKLSRTQVWKLENSLLDHRNKTIHNDYRRTQPLNHRVVESNFPNQEYTLGSEFQFYLHKIEEILDYLRRALN T06569 DRUGINFO D07HBX Salicyclic acid Approved T06569 DRUGINFO D0K1QD Sulfamylon Approved T06569 DRUGINFO D07SDQ Curcumin Phase 3 T06569 DRUGINFO D0A8JP PARABEN Phase 3 T06569 DRUGINFO D0Y6OA Coumate Phase 2 T06569 DRUGINFO D43GZX SAR566658 Phase 2 T06569 DRUGINFO D03SLR FERULIC ACID Patented T06569 DRUGINFO D0LD9S SPERMINE Terminated T06569 DRUGINFO D0M3PO 2,4-Disulfamyltrifluoromethylaniline Investigative T06569 DRUGINFO D0OI1H 2-Amino-benzenesulfonamide Investigative T06569 DRUGINFO D0G0FJ 2-hydrazinylbenzenesulfonamide Investigative T06569 DRUGINFO D0TY8X 4-(2-aminopyrimidin-4-ylamino)benzenesulfonamide Investigative T06569 DRUGINFO D04VLI 4-(2-Hydroxy-ethyl)-benzenesulfonamide Investigative T06569 DRUGINFO D05XZM 4-(hydroxymethyl)benzenesulfonamide Investigative T06569 DRUGINFO D0P6AM 4-Amino-3-bromo-benzenesulfonamide Investigative T06569 DRUGINFO D0YU8J 4-Amino-3-chloro-benzenesulfonamide Investigative T06569 DRUGINFO D04CVC 4-Amino-3-fluoro-benzenesulfonamide Investigative T06569 DRUGINFO D01STY 4-Amino-3-iodo-benzenesulfonamide Investigative T06569 DRUGINFO D0Z1HY 4-amino-6-chlorobenzene-1,3-disulfonamide Investigative T06569 DRUGINFO D0X6IE 4-amino-N-(4-sulfamoylbenzyl)benzenesulfonamide Investigative T06569 DRUGINFO D00IUB 4-CYANOPHENOL Investigative T06569 DRUGINFO D0NN3Q 4-Hydrazino-benzenesulfonamide Investigative T06569 DRUGINFO D0N1AW 6-(aminomethyl)-2H-chromen-2-one Investigative T06569 DRUGINFO D0L5TZ 6-(hydroxymethyl)-2H-chromen-2-one Investigative T06569 DRUGINFO D0Q2LL 6-Hydroxy-benzothiazole-2-sulfonic acid amide Investigative T06569 DRUGINFO D0LU4S 7-butoxy-2H-chromen-2-one Investigative T06569 DRUGINFO D0OT5L 7-propoxy-2H-chromen-2-one Investigative T06569 DRUGINFO D0E8CC BENZOLAMIDE Investigative T06569 DRUGINFO D09PWX Carzenide Investigative T06569 DRUGINFO D0V7AA CATECHIN Investigative T06569 DRUGINFO D0VD7H CL-5343 Investigative T06569 DRUGINFO D03ZMQ COUMARIN Investigative T06569 DRUGINFO D00YEF Decane-1,10-diyl disulfamate Investigative T06569 DRUGINFO D09WSJ Decyl sulfamate Investigative T06569 DRUGINFO D0A1CM ELLAGIC ACID Investigative T06569 DRUGINFO D07TAJ Ethyl 7-methoxy-2-oxo-2H-chromene-3-carboxylate Investigative T06569 DRUGINFO D0Y3TZ GALLICACID Investigative T06569 DRUGINFO D0U4BB HERNIARIN Investigative T06569 DRUGINFO D09JPC Hexane-1,6-diamine Investigative T06569 DRUGINFO D09WVV N1-(2-aminoethyl)ethane-1,2-diamine Investigative T06569 DRUGINFO D0X5HL N1-(naphthalen-1-yl)ethane-1,2-diamine Investigative T06569 DRUGINFO D0D4OV Octane-1,8-diyl disulfamate Investigative T06569 DRUGINFO D05TLB Octyl sulfamate Investigative T06569 DRUGINFO D0AU0M P-Coumaric Acid Investigative T06569 DRUGINFO D02QGI Pentane-1,5-diamine Investigative T06569 DRUGINFO D0ZC3W P-toluenesulfonamide Investigative T06569 DRUGINFO D0Q7DJ Syringic Acid Investigative T06569 KEGGPATH hsa00910:Nitrogen metabolism T06569 WIKIPATH WP2770:Reversible Hydration of Carbon Dioxide T06569 REACPATH R-HSA-1475029:Reversible hydration of carbon dioxide T68334 TARGETID T68334 T68334 FORMERID TTDS00438 T68334 UNIPROID FSHR_HUMAN T68334 TARGNAME Follicle-stimulating hormone receptor (FSHR) T68334 GENENAME FSHR T68334 TARGTYPE Successful target T68334 SYNONYMS LGR1; Follitropin receptor; FSH-R T68334 FUNCTION G protein-coupled receptor for follitropin, the follicle-stimulating hormone. Through cAMP production activates the downstream PI3K-AKT and ERK1/ERK2 signaling pathways. T68334 PDBSTRUC 4MQW; 4AY9; 1XWD; 1XUN T68334 BIOCLASS GPCR rhodopsin T68334 SEQUENCE MALLLVSLLAFLSLGSGCHHRICHCSNRVFLCQESKVTEIPSDLPRNAIELRFVLTKLRVIQKGAFSGFGDLEKIEISQNDVLEVIEADVFSNLPKLHEIRIEKANNLLYINPEAFQNLPNLQYLLISNTGIKHLPDVHKIHSLQKVLLDIQDNINIHTIERNSFVGLSFESVILWLNKNGIQEIHNCAFNGTQLDELNLSDNNNLEELPNDVFHGASGPVILDISRTRIHSLPSYGLENLKKLRARSTYNLKKLPTLEKLVALMEASLTYPSHCCAFANWRRQISELHPICNKSILRQEVDYMTQARGQRSSLAEDNESSYSRGFDMTYTEFDYDLCNEVVDVTCSPKPDAFNPCEDIMGYNILRVLIWFISILAITGNIIVLVILTTSQYKLTVPRFLMCNLAFADLCIGIYLLLIASVDIHTKSQYHNYAIDWQTGAGCDAAGFFTVFASELSVYTLTAITLERWHTITHAMQLDCKVQLRHAASVMVMGWIFAFAAALFPIFGISSYMKVSICLPMDIDSPLSQLYVMSLLVLNVLAFVVICGCYIHIYLTVRNPNIVSSSSDTRIAKRMAMLIFTDFLCMAPISFFAISASLKVPLITVSKAKILLVLFHPINSCANPFLYAIFTKNFRRDFFILLSKCGCYEMQAQIYRTETSSTVHNTHPRNGHCSSAPRVTNGSTYILVPLSHLAQN T68334 DRUGINFO D0OM3A Follitropin beta Approved T68334 DRUGINFO D04WBY Menotropins Approved T68334 DRUGINFO D02SBQ Urofollitropin Approved T68334 DRUGINFO D0H2UB Suramin Phase 1 T68334 DRUGINFO D0W3SX FSHR NAM Investigative T68334 DRUGINFO D09HCE Long-acting FSH conjugate Investigative T68334 DRUGINFO D08MVV PRX-111 Investigative T68334 DRUGINFO D02FTU Recombinant follicle stimulating hormone Investigative T68334 KEGGPATH hsa04024:cAMP signaling pathway T68334 KEGGPATH hsa04080:Neuroactive ligand-receptor interaction T68334 KEGGPATH hsa04913:Ovarian steroidogenesis T68334 WIKIPATH WP117:GPCRs, Other T68334 WIKIPATH WP1824:GPCR downstream signaling T68334 WIKIPATH WP1825:GPCR ligand binding T68334 WIKIPATH WP2035:FSH signaling pathway T68334 WIKIPATH WP24:Peptide GPCRs T68334 WIKIPATH WP34:Ovarian Infertility Genes T68334 WIKIPATH WP455:GPCRs, Class A Rhodopsin-like T68334 WHIZPATH PW000447:Vasopressin Regulation of Water Homeostasis T68334 WHIZPATH PW000448:Intracellular Signalling Through FSH Receptor and Follicle Stimulating Hormone T68334 REACPATH R-HSA-375281:Hormone ligand-binding receptors T68334 REACPATH R-HSA-418555:G alpha (s) signalling events T83011 TARGETID T83011 T83011 FORMERID TTDS00341 T83011 UNIPROID AOFB_HUMAN T83011 TARGNAME Monoamine oxidase type B (MAO-B) T83011 GENENAME MAOB T83011 TARGTYPE Successful target T83011 SYNONYMS MAO-B; Amine oxidase [flavin-containing] B T83011 FUNCTION Catalyzes the oxidative deamination of biogenic and xenobiotic amines and has important functions in the metabolism of neuroactive and vasoactive amines in the central nervous system and peripheral tissues. MAOB preferentially degrades benzylamine and phenylethylamine. T83011 PDBSTRUC 6FWC; 6FW0; 6FVZ; 5MRL; 4CRT T83011 BIOCLASS CH-NH(2) donor oxidoreductase T83011 ECNUMBER EC 1.4.3.4 T83011 SEQUENCE MSNKCDVVVVGGGISGMAAAKLLHDSGLNVVVLEARDRVGGRTYTLRNQKVKYVDLGGSYVGPTQNRILRLAKELGLETYKVNEVERLIHHVKGKSYPFRGPFPPVWNPITYLDHNNFWRTMDDMGREIPSDAPWKAPLAEEWDNMTMKELLDKLCWTESAKQLATLFVNLCVTAETHEVSALWFLWYVKQCGGTTRIISTTNGGQERKFVGGSGQVSERIMDLLGDRVKLERPVIYIDQTRENVLVETLNHEMYEAKYVISAIPPTLGMKIHFNPPLPMMRNQMITRVPLGSVIKCIVYYKEPFWRKKDYCGTMIIDGEEAPVAYTLDDTKPEGNYAAIMGFILAHKARKLARLTKEERLKKLCELYAKVLGSLEALEPVHYEEKNWCEEQYSGGCYTTYFPPGILTQYGRVLRQPVDRIYFAGTETATHWSGYMEGAVEAGERAAREILHAMGKIPEDEIWQSEPESVDVPAQPITTTFLERHLPSVPGLLRLIGLTTIFSATALGFLAHKRGLLVRV T83011 DRUGINFO D0RM9Q Budipine Approved T83011 DRUGINFO D07TGY Indeloxazine Approved T83011 DRUGINFO D0R0UJ Pargyline Approved T83011 DRUGINFO D0P9AC Phenelzine Approved T83011 DRUGINFO D06OMW Rasagiline Approved T83011 DRUGINFO D0TV6I Safinamide Approved T83011 DRUGINFO D0XM1A Safinamide mesylate Approved T83011 DRUGINFO D0S2UG Selegiline Approved T83011 DRUGINFO D0J2MJ Selegiline Hydrochloride Approved T83011 DRUGINFO D07PAO Sulphadoxine Approved T83011 DRUGINFO D0H0HJ Tranylcypromine Approved T83011 DRUGINFO D01NKW P2B-001 Phase 3 T83011 DRUGINFO D00VUI Psoralen Phase 3 T83011 DRUGINFO D08CJK TRYPTAMINE Phase 3 T83011 DRUGINFO D04RCT CHF-3381 Phase 2 T83011 DRUGINFO D06PHS EVT302 Phase 2 T83011 DRUGINFO D0C3UC Ladostigil Phase 2 T83011 DRUGINFO D02PSS RG1577 Phase 2 T83011 DRUGINFO D0D1UQ Neu-120 Phase 1/2 T83011 DRUGINFO D0H7PW PIPERINE Phase 1/2 T83011 DRUGINFO D0W7LO PF9601N Phase 1 T83011 DRUGINFO D03VOJ 3,4-Dihydroxybenzaldehyde Patented T83011 DRUGINFO D00NDF 3-Hydroxy-2-butanone Patented T83011 DRUGINFO D03ZOH 4-Hydroxy-2,5-dimethyl-3(2H)-furanone Patented T83011 DRUGINFO D00BRD 4-hydroxybenzaldehyde Patented T83011 DRUGINFO D0NH9P 4-Hydroxybenzoicacid Patented T83011 DRUGINFO D0X7BT 4-Hydroxybenzylalcohol Patented T83011 DRUGINFO D09SWE 4-Methoxybenzaldehyde Patented T83011 DRUGINFO D0XV2A Benzylcinnamate Patented T83011 DRUGINFO D0BT3Y Coumaricacid Patented T83011 DRUGINFO D0L9FL Coumarin/resveratrol hybrid derivative 1 Patented T83011 DRUGINFO D0Z5VD Coumarin/resveratrol hybrid derivative 2 Patented T83011 DRUGINFO D04OEV Cyclic peptide derivative 1 Patented T83011 DRUGINFO D0N9JJ Ethylvanillin Patented T83011 DRUGINFO D0O4QB EUGENOL Patented T83011 DRUGINFO D03SLR FERULIC ACID Patented T83011 DRUGINFO D07NTA Heteroaryl-cyclopropylamine derivative 1 Patented T83011 DRUGINFO D06VMN Heteroaryl-cyclopropylamine derivative 3 Patented T83011 DRUGINFO D06QRW Lazabemide Patented T83011 DRUGINFO D0C7LB Lazabemide analog 1 Patented T83011 DRUGINFO D0UL9U N-(2-phenylcyclopropyl) amino acid derivative 1 Patented T83011 DRUGINFO D08IOP N-(2-phenylcyclopropyl) amino acid derivative 3 Patented T83011 DRUGINFO D0N3SU Piperonal Patented T83011 DRUGINFO D0AI6J PMID25399762-Compound-Table 6-10 Patented T83011 DRUGINFO D02WXS PMID25399762-Compound-Table 6-11 Patented T83011 DRUGINFO D0E7SF PMID25399762-Compound-Table 6-12 Patented T83011 DRUGINFO D06KBT PMID25399762-Compound-Table 6-13 Patented T83011 DRUGINFO D0PM2S PMID25399762-Compound-Table 6-14 Patented T83011 DRUGINFO D0Q1EG PMID25399762-Compound-Table 6-15 Patented T83011 DRUGINFO D0IO2A PMID25399762-Compound-Table 6-9 Patented T83011 DRUGINFO D0UA3V PMID25399762-Compound-Table 7-Vanillic acid Patented T83011 DRUGINFO D0ME4N PMID25399762-Compound-Table 7-Vanillyl alcohol Patented T83011 DRUGINFO D0TR7N PMID25399762-Compound-Table 7-Veratraldehyde Patented T83011 DRUGINFO D0Z6ZH PMID25399762-Compound-Table1-C1 Patented T83011 DRUGINFO D00VSX PMID25399762-Compound-Table1-C10 Patented T83011 DRUGINFO D0B2YJ PMID25399762-Compound-Table1-C11 Patented T83011 DRUGINFO D05UNM PMID25399762-Compound-Table1-C12 Patented T83011 DRUGINFO D01JDK PMID25399762-Compound-Table1-C13 Patented T83011 DRUGINFO D0V2NC PMID25399762-Compound-Table1-C14 Patented T83011 DRUGINFO D08YYW PMID25399762-Compound-Table1-C15 Patented T83011 DRUGINFO D0AF7J PMID25399762-Compound-Table1-C16 Patented T83011 DRUGINFO D00KTI PMID25399762-Compound-Table1-C17 Patented T83011 DRUGINFO D02FRR PMID25399762-Compound-Table1-C18 Patented T83011 DRUGINFO D01PCI PMID25399762-Compound-Table1-C19 Patented T83011 DRUGINFO D0K2LB PMID25399762-Compound-Table1-C2 Patented T83011 DRUGINFO D0UL2R PMID25399762-Compound-Table1-C20 Patented T83011 DRUGINFO D0S2LV PMID25399762-Compound-Table1-C21 Patented T83011 DRUGINFO D07GZU PMID25399762-Compound-Table1-C22 Patented T83011 DRUGINFO D0HR6P PMID25399762-Compound-Table1-C23 Patented T83011 DRUGINFO D04FJY PMID25399762-Compound-Table1-C24 Patented T83011 DRUGINFO D0J3JY PMID25399762-Compound-Table1-C25 Patented T83011 DRUGINFO D00YBT PMID25399762-Compound-Table1-C3 Patented T83011 DRUGINFO D0Q1MN PMID25399762-Compound-Table1-C4 Patented T83011 DRUGINFO D06BFA PMID25399762-Compound-Table1-C5 Patented T83011 DRUGINFO D0DM9L PMID25399762-Compound-Table1-C6 Patented T83011 DRUGINFO D0C2EW PMID25399762-Compound-Table1-C7 Patented T83011 DRUGINFO D0GY4F PMID25399762-Compound-Table1-C8 Patented T83011 DRUGINFO D06EIP PMID25399762-Compound-Table1-C9 Patented T83011 DRUGINFO D04OXC PMID29324067-Compound-38 Patented T83011 DRUGINFO D07UZL PMID29324067-Compound-40 Patented T83011 DRUGINFO D0AA7U PMID29757691-Compound-4 Patented T83011 DRUGINFO D05RJG Schiff base compound 1 Patented T83011 DRUGINFO D0DW5P Schiff base compound 2 Patented T83011 DRUGINFO D0J7HR Secondary and tertiary (hetero)arylamide derivative 1 Patented T83011 DRUGINFO D0B5YS T83193 Patented T83011 DRUGINFO D0T9JB Tacrine-coumarin hybrid derivative 1 Patented T83011 DRUGINFO D04OHC Tarnylcypromine derivative 2 Patented T83011 DRUGINFO D0O7IH Tarnylcypromine derivative 3 Patented T83011 DRUGINFO D04AXC Tetra-hydro-isoquinoline derivative 1 Patented T83011 DRUGINFO D0NB7Z Tetra-hydro-isoquinoline derivative 2 Patented T83011 DRUGINFO D02EME Tetra-hydro-isoquinoline derivative 3 Patented T83011 DRUGINFO D0R6RT Tetra-hydro-isoquinoline derivative 4 Patented T83011 DRUGINFO D0GQ2Z Tetra-hydro-oxazolopyridine derivative 1 Patented T83011 DRUGINFO D0DL1O Tetra-hydro-oxazolopyridine derivative 2 Patented T83011 DRUGINFO D01LAC MOFEGILINE Discontinued in Phase 3 T83011 DRUGINFO D01OLO AS602868 Discontinued in Phase 1 T83011 DRUGINFO D0P1WB EVT-301 Discontinued in Phase 1 T83011 DRUGINFO D0O5QL HT-1067 Discontinued in Phase 1 T83011 DRUGINFO D0E3JL SL-25.1188 Discontinued in Phase 1 T83011 DRUGINFO D0I9LO RWJ-416457 Preclinical T83011 DRUGINFO D07OLO Milacemide Terminated T83011 DRUGINFO D0T3ZS (+/-)-2-(4'-Benzyloxyphenyl)thiomorpholin-5-one Investigative T83011 DRUGINFO D0D6OR (+/-)-2-(4'-Benzyloxyphenyl)thiomorpholine Investigative T83011 DRUGINFO D0M4GR (+/-)-2-(4'-Butoxyphenyl)thiomorpholin-5-one Investigative T83011 DRUGINFO D0T3XC (+/-)-2-(4'-Butoxyphenyl)thiomorpholine Investigative T83011 DRUGINFO D0D5KD (+/-)-2-(4'-Ethoxyphenyl)thiomorpholin-5-one Investigative T83011 DRUGINFO D0J0QW (+/-)-2-(4'-Ethoxyphenyl)thiomorpholine Investigative T83011 DRUGINFO D0B1XZ (+/-)-2-(4-fluorophenyl)-7-methoxychroman-4-one Investigative T83011 DRUGINFO D04DCW (+/-)-2-(4-fluorophenyl)-7-methylchroman-4-one Investigative T83011 DRUGINFO D0ZH0T (+/-)-2-(4-fluorophenyl)chroman-4-one Investigative T83011 DRUGINFO D0O0MY (+/-)-2-(4-methoxyphenyl)-7-methylchroman-4-one Investigative T83011 DRUGINFO D0ID3Y (+/-)-2-(4'-Methoxyphenyl)thiomorpholin-5-one Investigative T83011 DRUGINFO D08TFN (+/-)-2-(4'-Methoxyphenyl)thiomorpholine Investigative T83011 DRUGINFO D0Z5BU (+/-)-2-(4'-Propoxyphenyl)thiomorpholin-5-one Investigative T83011 DRUGINFO D08FXH (+/-)-2-(4'-Propoxyphenyl)thiomorpholine Investigative T83011 DRUGINFO D04FLL (+/-)-2-Phenylthiomorpholin-5-one Investigative T83011 DRUGINFO D0HU4J (+/-)-2-Phenylthiomorpholine Investigative T83011 DRUGINFO D0R3LP (+/-)-2-p-tolylchroman-4-one Investigative T83011 DRUGINFO D0D2JH (+/-)-7-fluoro-2-(4-fluorophenyl)chroman-4-one Investigative T83011 DRUGINFO D03XQB (+/-)-7-fluoro-2-(4-methoxyphenyl)chroman-4-one Investigative T83011 DRUGINFO D0IK2S (+/-)-7-fluoro-2-phenylchroman-4-one Investigative T83011 DRUGINFO D0Y0KU (+/-)-7-fluoro-2-p-tolylchroman-4-one Investigative T83011 DRUGINFO D00HVZ (+/-)-7-methoxy-2-(4-methoxyphenyl)chroman-4-one Investigative T83011 DRUGINFO D0A2FO (+/-)-7-methoxy-2-phenylchroman-4-one Investigative T83011 DRUGINFO D02KXU (+/-)-7-methoxy-2-p-tolylchroman-4-one Investigative T83011 DRUGINFO D0T1GP (+/-)-7-methyl-2-phenylchroman-4-one Investigative T83011 DRUGINFO D0Z2XR (+/-)-7-methyl-2-p-tolylchroman-4-one Investigative T83011 DRUGINFO D03HXD (6-Benzyloxy-2-naphthyl)-2-aminopropane Investigative T83011 DRUGINFO D0L5EW (6-Ethoxy-2-naphthyl)-2-aminopropane Investigative T83011 DRUGINFO D02IDM (6-Methoxy-2-naphthyl)-2-aminopropane Investigative T83011 DRUGINFO D0IP7L (6-Propoxy-2-naphthyl)-2-aminopropane Investigative T83011 DRUGINFO D02TFD (7-Benzyloxy-2-oxo-2H-chromen-4-yl)acetonitrile Investigative T83011 DRUGINFO D06AJP (E)-5-(3-Chlorostyryl)isatin Investigative T83011 DRUGINFO D0X8HH (E)-5-(3-Fluorostyryl)isatin Investigative T83011 DRUGINFO D09XSB (E)-5-Styrylisatin Investigative T83011 DRUGINFO D07GUX (E)-6-Styrylisatin Investigative T83011 DRUGINFO D0TU7I (E)-8-(3-chlorostyryl)-caffeine Investigative T83011 DRUGINFO D0F2SM (R)(+)-2-(4-fluorophenyl)-7-methoxychroman-4-one Investigative T83011 DRUGINFO D07WIJ (R)(+)-7-fluoro-2-(4-fluorophenyl)chroman-4-one Investigative T83011 DRUGINFO D09PBW (R)(+)-7-fluoro-2-phenylchroman-4-one Investigative T83011 DRUGINFO D02WOQ (R)(+)-7-fluoro-2-p-tolylchroman-4-one Investigative T83011 DRUGINFO D0B3QN (R)(+)-7-methyl-2-phenylchroman-4-one Investigative T83011 DRUGINFO D0P1YC (R)(+)-7-methyl-2-p-tolylchroman-4-one Investigative T83011 DRUGINFO D07BAO (R)-3-Prop-2-ynylamino-indan-5-ol Investigative T83011 DRUGINFO D0S7FP (R)-Indan-1-yl-methyl-prop-2-ynyl-amine Investigative T83011 DRUGINFO D0JY9B (R)-N2-{4-[(3-chlorobenzyl)oxy]benzyl}alaninamide Investigative T83011 DRUGINFO D05ILO (R)-N2-{4-[(3-chlorobenzyl)oxy]benzyl}serinamide Investigative T83011 DRUGINFO D05HVV (R)-N2-{4-[(3-fluorobenzyl)oxy]benzyl}alaninamide Investigative T83011 DRUGINFO D0M0XR (R/R)BEFLOXATONE Investigative T83011 DRUGINFO D01KZF (S)(+)-2-(4-fluorophenyl)-7-methoxychroman-4-one Investigative T83011 DRUGINFO D0L6HE (S)(+)-7-fluoro-2-(4-fluorophenyl)chroman-4-one Investigative T83011 DRUGINFO D0I5CZ (S)(+)-7-fluoro-2-phenylchroman-4-one Investigative T83011 DRUGINFO D00PJT (S)(+)-7-fluoro-2-p-tolylchroman-4-one Investigative T83011 DRUGINFO D0N4DR (S)(+)-7-methyl-2-phenylchroman-4-one Investigative T83011 DRUGINFO D0TB1E (S)(+)-7-methyl-2-p-tolylchroman-4-one Investigative T83011 DRUGINFO D0Z0ZU (S)-2-amino-1-(4-butylthiophenyl)-propane Investigative T83011 DRUGINFO D08SSS (S)-2-amino-1-(4-propylthiophenyl)-propane Investigative T83011 DRUGINFO D05OTR (S)-N2-[4-(benzyloxy)benzyl]alaninamide Investigative T83011 DRUGINFO D0U4JD (S)-N2-[4-(benzyloxy)benzyl]serinamide Investigative T83011 DRUGINFO D03KYZ (S)-N2-{4-[(3-chlorobenzyl)oxy]benzyl}alaninamide Investigative T83011 DRUGINFO D0FR3X (S)-N2-{4-[(3-chlorobenzyl)oxy]benzyl}serinamide Investigative T83011 DRUGINFO D0IN0X (S)-N2-{4-[(3-fluorobenzyl)oxy]benzyl}serinamide Investigative T83011 DRUGINFO D0G5YA (S)-N2-{4-[(4-chlorobenzyl)oxy]benzyl}alaninamide Investigative T83011 DRUGINFO D0T8AD (S)-N2-{4-[(4-chlorobenzyl)oxy]benzyl}serinamide Investigative T83011 DRUGINFO D09GCE (S)-N2-{4-[(4-nitrobenzyl)oxy]benzyl}serinamide Investigative T83011 DRUGINFO D0G2LF [(1e)-4-Phenylbut-1-Enyl]Benzene Investigative T83011 DRUGINFO D01SBZ 1-(4-(benzyloxy)phenyl)propan-2-amine Investigative T83011 DRUGINFO D0UF1R 1,2,3,4-Tetrahydro-naphthalen-1-ylamine Investigative T83011 DRUGINFO D0C1SE 1,2,3,4-Tetrahydro-pyrazino[1,2-a]indole Investigative T83011 DRUGINFO D0J0MX 1,4-diphenyl-(1E,3E)-1,3-butadiene Investigative T83011 DRUGINFO D0SP2O 1H-Indole-2,3-dione Investigative T83011 DRUGINFO D01GAX 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine Investigative T83011 DRUGINFO D0Q3VS 2-(2,4-dichlorophenyl)-4,5-dihydro-1H-imidazole Investigative T83011 DRUGINFO D0Q1IP 2-(2-cycloheptylidenehydrazinyl)-4-phenylthiazole Investigative T83011 DRUGINFO D0E4HB 2-(2-cyclohexylidenehydrazinyl)-4-phenylthiazole Investigative T83011 DRUGINFO D0I2GP 2-(2-cyclohexylidenehydrazinyl)-4-p-tolylthiazole Investigative T83011 DRUGINFO D00WVG 2-(2-cyclopentylidenehydrazinyl)-4-phenylthiazole Investigative T83011 DRUGINFO D07YZD 2-(3-nitrophenyl)-4,5-dihydro-1H-imidazole Investigative T83011 DRUGINFO D0A4AB 2-(4,5-dihydro-1H-imidazol-2-yl)quinoline Investigative T83011 DRUGINFO D01FTB 2-(4-chlorophenyl)-4,5-dihydro-1H-imidazole Investigative T83011 DRUGINFO D0G6MA 2-(4-fluorophenyl)-7-methoxy-4H-chromen-4-one Investigative T83011 DRUGINFO D0P7SY 2-(4-methoxyphenyl)-4H-chromene-4-thione Investigative T83011 DRUGINFO D0P1UC 2-(5-phenyl-furan-2-yl)-4,5-dihydro-1H-imidazole Investigative T83011 DRUGINFO D04ZPU 2-(naphthalen-2-yl)-4,5-dihydro-1H-imidazole Investigative T83011 DRUGINFO D0M7WE 2,3,4,5-Tetrahydro-1H-pyrido[4,3-b]indole Investigative T83011 DRUGINFO D0S3QN 2-[7-(Benzyloxy)-2-oxo-2H-chromen-4-yl]acetamide Investigative T83011 DRUGINFO D0LI3J 2-BFi Investigative T83011 DRUGINFO D02BBT 2-Bromo-N-(2-morpholinoethyl)nicotinamide Investigative T83011 DRUGINFO D01JMW 2-Bromo-N-(3-morpholinopropyl)nicotinamide Investigative T83011 DRUGINFO D0R5EW 2-Chloro-N-(2-morpholinoethyl)nicotinamide Investigative T83011 DRUGINFO D0NS9X 2-Chloro-N-(3-morpholinopropyl)nicotinamide Investigative T83011 DRUGINFO D09ZDQ 2-Furan-2-yl-4,5-dihydro-1H-imidazole Investigative T83011 DRUGINFO D02VIV 2-Hydrazino-3-methyl-4(3H)-quinazolinone Investigative T83011 DRUGINFO D0FH5A 2-methyl-9H-indeno[2,1-d]pyrimidin-9-one Investigative T83011 DRUGINFO D00WSM 2-oxo-N-m-tolyl-2H-chromene-3-carboxamide Investigative T83011 DRUGINFO D03PXS 2-oxo-N-phenyl-2H-chromene-3-carboxamide Investigative T83011 DRUGINFO D0H0GZ 2-oxo-N-p-tolyl-2H-chromene-3-carboxamide Investigative T83011 DRUGINFO D0Z7NC 2-Phenethyl-4,5-dihydro-1H-imidazole Investigative T83011 DRUGINFO D0N9FH 2-Phenoxymethyl-4,5-dihydro-1H-imidazole Investigative T83011 DRUGINFO D0Q9NC 2-phenyl-9H-indeno[2,1-d]pyrimidine Investigative T83011 DRUGINFO D05LMT 2-Phenyl-cyclopropylamine hydrochloride Investigative T83011 DRUGINFO D01DEU 2-p-tolyl-4,5-dihydro-1H-imidazole Investigative T83011 DRUGINFO D03BQJ 2-p-tolyl-4H-chromen-4-one Investigative T83011 DRUGINFO D01VPZ 2-p-tolyl-4H-chromene-4-thione Investigative T83011 DRUGINFO D0U8ET 3-(2-Bromophenyl)-6-methylcoumarin Investigative T83011 DRUGINFO D0O1GE 3-(3-methoxyphenyl)-6-methyl-2H-chromen-2-one Investigative T83011 DRUGINFO D01HQV 3-(4-hydroxyphenyl)-6-methyl-2H-chromen-2-one Investigative T83011 DRUGINFO D0R9TX 3-(4-methoxyphenyl)-6-methyl-2H-chromen-2-one Investigative T83011 DRUGINFO D0I6GH 3-(phenoxymethyl)-5H-indeno[1,2-c]pyridazin-5-one Investigative T83011 DRUGINFO D0P4GF 3,4-Benzo-7-(beta-bromoallyloxy)-8-methylcoumarin Investigative T83011 DRUGINFO D0TL3S 3,4-Benzo-7-acetonyloxy-8-methoxycoumarin Investigative T83011 DRUGINFO D09NNZ 3,4-Dichloro-N-(2-methyl-1H-indol-5-yl)benzamide Investigative T83011 DRUGINFO D0D6QI 3-Chloro-N-(2-methyl-1H-indol-5-yl)benzamide Investigative T83011 DRUGINFO D08IDJ 3-phenyl-9H-indeno[1,2-e][1,2,4]triazin-9-one Investigative T83011 DRUGINFO D0E8IE 4-(2-oxo-2H-chromene-3-carboxamido)benzoic acid Investigative T83011 DRUGINFO D0T1FJ 4-(Aminomethyl)-7-(benzyloxy)-2H-chromen-2-one Investigative T83011 DRUGINFO D01LUB 4,8-Dimethyl-7-(2'-oxocyclohexyloxy)coumarin Investigative T83011 DRUGINFO D0G8BT 4,9-Dihydro-3H-beta-carboline Investigative T83011 DRUGINFO D07KIB 4-fluoroselegiline Investigative T83011 DRUGINFO D06ETG 4-HYDROXY-N-PROPARGYL-1(R)-AMINOINDAN Investigative T83011 DRUGINFO D0A1RE 4-methyl-7-(2-oxocyclopentyloxy)-2H-chromen-2-one Investigative T83011 DRUGINFO D04TGN 4-oxo-4H-chromene-3-carboxylic acid Investigative T83011 DRUGINFO D07AAZ 4-phenyl-1,2,3,6-tetrahydropyridine Investigative T83011 DRUGINFO D0R7UO 5-Aminomethyl-3-pyrrol-1-yl-oxazolidin-2-one Investigative T83011 DRUGINFO D0L8ND 5-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline Investigative T83011 DRUGINFO D08HAM 5-Bromo-4,9-dihydro-3H-beta-carboline Investigative T83011 DRUGINFO D08QVY 5-Hydroxymethyl-3-pyrrol-1-yl-oxazolidin-2-one Investigative T83011 DRUGINFO D00NSA 5-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Investigative T83011 DRUGINFO D0V6XA 5-Methoxy-4,9-dihydro-3H-beta-carboline Investigative T83011 DRUGINFO D08NQM 5-QUINOXALIN-6-YLMETHYLENE-THIAZOLIDINE-2,4-DIONE Investigative T83011 DRUGINFO D0S0JH 6-amino-9-methoxy-7H-furo[3,2-g]chromen-7-one Investigative T83011 DRUGINFO D05GQQ 6-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline Investigative T83011 DRUGINFO D04GVX 6-Bromo-4,9-dihydro-3H-beta-carboline Investigative T83011 DRUGINFO D0J3SN 6-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Investigative T83011 DRUGINFO D0C7PD 6-Methoxy-4,9-dihydro-3H-beta-carboline Investigative T83011 DRUGINFO D0C9WW 7-(3-chlorobenzyloxy)-4-carboxaldehyde-coumarin Investigative T83011 DRUGINFO D08FFH 7-Acetonyloxy-3,4-cyclohexene-8-methylcoumarin Investigative T83011 DRUGINFO D00OQL 7-Acetonyloxy-3,4-cyclopentene-8-methylcoumarin Investigative T83011 DRUGINFO D02UVG 7-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline Investigative T83011 DRUGINFO D0W4TW 7-Bromo-4,9-dihydro-3H-beta-carboline Investigative T83011 DRUGINFO D0Y5OB 7-fluoro-2-(4-fluorophenyl)-4H-chromene-4-thione Investigative T83011 DRUGINFO D0W7XK 7-fluoro-2-(4-methoxyphenyl)-4H-chromen-4-one Investigative T83011 DRUGINFO D0C9GI 7-fluoro-2-p-tolyl-4H-chromen-4-one Investigative T83011 DRUGINFO D0I9AA 7-fluoro-2-p-tolyl-4H-chromene-4-thione Investigative T83011 DRUGINFO D05GDP 7-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Investigative T83011 DRUGINFO D0ZI0S 7-methoxy-2-p-tolyl-4H-chromen-4-one Investigative T83011 DRUGINFO D07HFF 7-methoxy-2-p-tolyl-4H-chromene-4-thione Investigative T83011 DRUGINFO D05FQN 7-Methoxy-9H-beta-carboline Investigative T83011 DRUGINFO D08HKC 7-methyl-2-p-tolyl-4H-chromene-4-thione Investigative T83011 DRUGINFO D07NBB 8-(3-Bromobenzyloxy)caffeine Investigative T83011 DRUGINFO D08YCE 8-(3-Chlorobenzyloxy)caffeine Investigative T83011 DRUGINFO D04LPY 8-(3-Fluorobenzyloxy)caffeine Investigative T83011 DRUGINFO D0B6MV 8-(3-Methoxybenzyloxy)caffeine Investigative T83011 DRUGINFO D00OLX 8-(3-Methylbenzyloxy)caffeine Investigative T83011 DRUGINFO D02FJX 8-[(3-Trifluoromethyl)benzyloxy]caffeine Investigative T83011 DRUGINFO D0JN9R 8-Benzyloxycaffeine Investigative T83011 DRUGINFO D06BAC 8-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline Investigative T83011 DRUGINFO D0G2EF 8-Bromo-4,9-dihydro-3H-beta-carboline Investigative T83011 DRUGINFO D0H3RQ 8-Bromo-6-methyl-3-(4'-methoxyphenyl)coumarin Investigative T83011 DRUGINFO D0K1FE 8-Bromo-6-methyl-3-phenylcoumarin Investigative T83011 DRUGINFO D0Q3VI 8-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Investigative T83011 DRUGINFO D0Y1GL 8-Methoxy-4,9-dihydro-3H-beta-carboline Investigative T83011 DRUGINFO D0D2YR 9-Methyl-2,3,4,9-tetrahydro-1H-beta-carboline Investigative T83011 DRUGINFO D0Y0JM Benzyl-methyl-[1-(1H-pyrrol-2-yl)-vinyl]-amine Investigative T83011 DRUGINFO D0R7ZC Beta-methoxyamphetamine Investigative T83011 DRUGINFO D07KCC Butyl-methyl-prop-2-ynyl-amine hydrochloride Investigative T83011 DRUGINFO D05FMZ C-(1H-Indol-3-yl)-methylamine Investigative T83011 DRUGINFO D0D1PE CGS-19281A Investigative T83011 DRUGINFO D06ERH CHALCONE Investigative T83011 DRUGINFO D06AAA Cis-2-(4-chlorophenyl)-2-fluorocyclopropanamine Investigative T83011 DRUGINFO D0UL6Y Cis-2-(para-fluorophenyl)cyclopropylamine Investigative T83011 DRUGINFO D0B2TV Cis-2-Fluoro-2-(4-methoxyphenyl)cyclopropylamine Investigative T83011 DRUGINFO D04TZI Cis-2-fluoro-2-phenylcyclopropanamine Investigative T83011 DRUGINFO D0X8RN Cis-2-phenylcyclopropylamine Investigative T83011 DRUGINFO D0US0J CORDOIN Investigative T83011 DRUGINFO D0Y8AN Deprenyl Investigative T83011 DRUGINFO D0M0CF Farnesol Investigative T83011 DRUGINFO D0B4VE Flavanone Investigative T83011 DRUGINFO D00IMW Flavin-Adenine Dinucleotide Investigative T83011 DRUGINFO D0Z2NN Heptyl-methyl-prop-2-ynyl-amine hydrochloride Investigative T83011 DRUGINFO D0A4IY HYDRAZINECARBOXAMIDE Investigative T83011 DRUGINFO D08CNS IPRONIAZIDE Investigative T83011 DRUGINFO D0X3SE Isopropyl-methyl-prop-2-ynyl-amine hydrochloride Investigative T83011 DRUGINFO D09GQS JD-0100 Investigative T83011 DRUGINFO D0F7KG L-136662 Investigative T83011 DRUGINFO D0C7PY Lauryl Dimethylamine-N-Oxide Investigative T83011 DRUGINFO D0BV8Y LU-53439 Investigative T83011 DRUGINFO D0EX4L Methyl piperate Investigative T83011 DRUGINFO D0MX1T Methyl-(1,2,3,4-tetrahydro-naphthalen-1-yl)-amine Investigative T83011 DRUGINFO D0N6JE Methyl-pentyl-prop-2-ynyl-amine oxalic acid Investigative T83011 DRUGINFO D0I4ME MMDA Investigative T83011 DRUGINFO D00KDZ N-(1H-Indol-2-ylmethyl)-N-methyl-N-phenylamine Investigative T83011 DRUGINFO D01PES N-(1H-Indol-2-ylmethyl)-N-phenylamine Investigative T83011 DRUGINFO D02KGZ N-(2-aminoethyl)-2-oxo-2H-chromene-3-carboxamide Investigative T83011 DRUGINFO D0K0SA N-(2-aminoethyl)-p-chlorobenzamide Investigative T83011 DRUGINFO D08ILX N-(2-Methyl-1H-indol-5-yl)benzamide Investigative T83011 DRUGINFO D05WQN N-(2-Methyl-1H-indol-5-yl)cyclohexanecarboxamide Investigative T83011 DRUGINFO D0N8UE N-(2-phenylethyl),N-(pyrrol-2-ylmethyl)amine Investigative T83011 DRUGINFO D0YO7C N-(2-Phenylethyl)-1H-indole-2-carboxamide Investigative T83011 DRUGINFO D07LCU N-(3-Phenylpropyl)-1H-indole-2-carboxamide Investigative T83011 DRUGINFO D0B1WD N-(4-Ethylphenyl)-2-oxo-2H-chromene-3-carboxamide Investigative T83011 DRUGINFO D08HNJ N-(4-Phenylbutyl)-1H-indole-2-carboxamide Investigative T83011 DRUGINFO D0O2UK N-(benzyl),N-(pyrrol-2-ylmethyl)amine Investigative T83011 DRUGINFO D0G4BG N-(propargyl),N-(pyrrol-2-ylmethyl)amine Investigative T83011 DRUGINFO D0T6XC N2-[4-(benzyloxy)benzyl]glycinamide Investigative T83011 DRUGINFO D0T7EJ N2-{4-[(3-chlorobenzyl)oxy]benzyl}glycinamide Investigative T83011 DRUGINFO D02QBV N2-{4-[(3-fluorobenzyl)oxy]benzyl}glycinamide Investigative T83011 DRUGINFO D03XKJ N2-{4-[(4-chlorobenzyl)oxy]benzyl}glycinamide Investigative T83011 DRUGINFO D08BUB N2-{4-[(4-nitrobenzyl)oxy]benzyl}glycinamide Investigative T83011 DRUGINFO D0V0TN N-Benzyl,N-methyl-1H-indole-2-carboxamide Investigative T83011 DRUGINFO D0Z5YO N-Benzyl-1H-indole-2-carboxamide Investigative T83011 DRUGINFO D06QNN N-benzyl-2-oxo-2H-chromene-3-carboxamide Investigative T83011 DRUGINFO D05ANK N-Benzyl-N-(1H-indol-2-ylmethyl)-N-methylamine Investigative T83011 DRUGINFO D01UFM N-cyclohexyl-2-oxo-2H-chromene-3-carboxamide Investigative T83011 DRUGINFO D09FAD N-isobutyl-2-oxo-2H-chromene-3-carboxamide Investigative T83011 DRUGINFO D0MO1O N-methyl,N-(benzyl),N-(pyrrol-2-ylmethyl)amine Investigative T83011 DRUGINFO D03KDD N-methyl,N-(propargyl),N-(pyrrol-2-ylmethyl)amine Investigative T83011 DRUGINFO D0F7JK N-Methyl,N-phenyl-1H-indole-2-carboxamide Investigative T83011 DRUGINFO D0W1WE N-Methyl-N-phenyl-2-oxo-2H-chromene-3-carboxamide Investigative T83011 DRUGINFO D0A2AF N-Methyl-N-Propargyl-1(R)-Aminoindan Investigative T83011 DRUGINFO D0K9UN N-Phenyl-1H-indole-2-carboxamide Investigative T83011 DRUGINFO D0K5LJ N-Propargyl-1(S)-Aminoindan Investigative T83011 DRUGINFO D0T7VA NSC-50187 Investigative T83011 DRUGINFO D0K8EE NSC-93405 Investigative T83011 DRUGINFO D0OW5Y NW-1772 Investigative T83011 DRUGINFO D08SRB Phenyl 4-(4,5-dihydro-1H-imidazol-2-yl)benzoate Investigative T83011 DRUGINFO D04QRS PNU-22394 Investigative T83011 DRUGINFO D0K4GD RS-1636 Investigative T83011 DRUGINFO D00AHV SKL-PD Investigative T83011 DRUGINFO D0V3NT TOLOXATONE Investigative T83011 DRUGINFO D09BIV TRACIZOLINE Investigative T83011 DRUGINFO D03LGV Trans-2-(4-chlorophenyl)-2-fluorocyclopropanamine Investigative T83011 DRUGINFO D08PHY Trans-2-fluoro-2-(4-fluorophenyl)cyclopropanamine Investigative T83011 DRUGINFO D09HBX Trans-2-fluoro-2-phenylcyclopropylamin Investigative T83011 DRUGINFO D0F2DC Trans-2-fluoro-2-p-tolylcyclopropanamine Investigative T83011 DRUGINFO D03LPH TRYPTOLINE Investigative T83011 DRUGINFO D0V4KL VAR-10200 Investigative T83011 DRUGINFO D02AQM VAR-10300 Investigative T83011 KEGGPATH hsa00260:Glycine, serine and threonine metabolism T83011 KEGGPATH hsa00330:Arginine and proline metabolism T83011 KEGGPATH hsa00340:Histidine metabolism T83011 KEGGPATH hsa00350:Tyrosine metabolism T83011 KEGGPATH hsa00360:Phenylalanine metabolism T83011 KEGGPATH hsa00380:Tryptophan metabolism T83011 KEGGPATH hsa00982:Drug metabolism - cytochrome P450 T83011 KEGGPATH hsa01100:Metabolic pathways T83011 KEGGPATH hsa04726:Serotonergic synapse T83011 KEGGPATH hsa04728:Dopaminergic synapse T83011 KEGGPATH hsa05030:Cocaine addiction T83011 KEGGPATH hsa05031:Amphetamine addiction T83011 KEGGPATH hsa05034:Alcoholism T83011 WIKIPATH WP1879:Phase 1 - Functionalization of compounds T83011 WIKIPATH WP2436:Dopamine metabolism T83011 WIKIPATH WP465:Tryptophan metabolism T83011 INTEPATH alphasynuclein_pathway:Alpha-synuclein signaling T83011 PANTPATH P00001:Adrenaline and noradrenaline biosynthesis T83011 PANTPATH P04372:5-Hydroxytryptamine degredation T83011 PANTPATH P05912:Dopamine receptor mediated signaling pathway T83011 BIOCPATH PWY-0:Putrescine degradation III T83011 BIOCPATH PWY-6307:Tryptophan degradation via tryptamine T83011 BIOCPATH PWY-6342:Noradrenaline and adrenaline degradation T83011 BIOCPATH PWY66-401:Superpathway of tryptophan utilization T83011 BIOCPATH PWY6666-2:Dopamine degradation T31391 TARGETID T31391 T31391 FORMERID TTDS00093 T31391 UNIPROID DPP4_HUMAN T31391 TARGNAME Dipeptidyl peptidase 4 (DPP-4) T31391 GENENAME DPP4 T31391 TARGTYPE Successful target T31391 SYNONYMS Tcell activation antigen CD26; TP103; T-cell activation antigen CD26; Dipeptidyl peptidase IV; Dipeptidyl peptidase 4 soluble form; DPP-IV; DPP IV; DPP 4; CD26; Adenosine deaminase complexing protein-2; Adenosine deaminase complexing protein 2; ADCP2; ADCP-2; ADABP T31391 FUNCTION Acts as a positive regulator of T-cell coactivation, by binding at least ADA, CAV1, IGF2R, and PTPRC. Its binding to CAV1 and CARD11 induces T-cell proliferation and NF-kappa-B activation in a T-cell receptor/CD3-dependent manner. Its interaction with ADA also regulates lymphocyte-epithelial cell adhesion. In association with FAP is involved in the pericellular proteolysis of the extracellular matrix (ECM), the migration and invasion of endothelial cells into the ECM. May be involved in the promotion of lymphatic endothelial cells adhesion, migration and tube formation. When overexpressed, enhanced cell proliferation, a process inhibited by GPC3. Acts also as a serine exopeptidase with a dipeptidyl peptidase activity that regulates various physiological processes by cleaving peptides in the circulation, including many chemokines, mitogenic growth factors, neuropeptides and peptide hormones. Removes N-terminal dipeptides sequentially from polypeptides having unsubstituted N-termini provided that the penultimate residue is proline. Cell surface glycoprotein receptor involved in the costimulatory signal essential for T-cell receptor (TCR)-mediated T-cell activation. T31391 PDBSTRUC 6B1O; 6B1E; 5ZID; 5Y7K; 5Y7J T31391 BIOCLASS Peptidase T31391 ECNUMBER EC 3.4.14.5 T31391 SEQUENCE MKTPWKVLLGLLGAAALVTIITVPVVLLNKGTDDATADSRKTYTLTDYLKNTYRLKLYSLRWISDHEYLYKQENNILVFNAEYGNSSVFLENSTFDEFGHSINDYSISPDGQFILLEYNYVKQWRHSYTASYDIYDLNKRQLITEERIPNNTQWVTWSPVGHKLAYVWNNDIYVKIEPNLPSYRITWTGKEDIIYNGITDWVYEEEVFSAYSALWWSPNGTFLAYAQFNDTEVPLIEYSFYSDESLQYPKTVRVPYPKAGAVNPTVKFFVVNTDSLSSVTNATSIQITAPASMLIGDHYLCDVTWATQERISLQWLRRIQNYSVMDICDYDESSGRWNCLVARQHIEMSTTGWVGRFRPSEPHFTLDGNSFYKIISNEEGYRHICYFQIDKKDCTFITKGTWEVIGIEALTSDYLYYISNEYKGMPGGRNLYKIQLSDYTKVTCLSCELNPERCQYYSVSFSKEAKYYQLRCSGPGLPLYTLHSSVNDKGLRVLEDNSALDKMLQNVQMPSKKLDFIILNETKFWYQMILPPHFDKSKKYPLLLDVYAGPCSQKADTVFRLNWATYLASTENIIVASFDGRGSGYQGDKIMHAINRRLGTFEVEDQIEAARQFSKMGFVDNKRIAIWGWSYGGYVTSMVLGSGSGVFKCGIAVAPVSRWEYYDSVYTERYMGLPTPEDNLDHYRNSTVMSRAENFKQVEYLLIHGTADDNVHFQQSAQISKALVDVGVDFQAMWYTDEDHGIASSTAHQHIYTHMSHFIKQCFSLP T31391 DRUGINFO D0NJ5H Alogliptin Approved T31391 DRUGINFO D0T8XB Anagliptin Approved T31391 DRUGINFO D0Y6QC Dapagliflozin Propanediol; Saxagliptin Hydrochloride Approved T31391 DRUGINFO D05IPF Kombiglyze XR/Komboglyze FDC Approved T31391 DRUGINFO D02EYG Linagliptin Approved T31391 DRUGINFO D0K9MY Saxagliptin Approved T31391 DRUGINFO D0U2JP Sitagliptin Approved T31391 DRUGINFO D0L3DK Vildagliptin Approved T31391 DRUGINFO D04XIO Dutogliptin Phase 3 T31391 DRUGINFO D0ZD3C Gemigliptin Phase 3 T31391 DRUGINFO D0V0KJ IDDBCP161883 Phase 3 T31391 DRUGINFO D02ZBW LC-150444 Phase 3 T31391 DRUGINFO D0M3XR MK-3102 Phase 3 T31391 DRUGINFO D0N7JZ SAND-26 Phase 3 T31391 DRUGINFO D09XMX SaxaDapa FDC Phase 3 T31391 DRUGINFO D0N6SO SYR-472 Phase 3 T31391 DRUGINFO D06VCN Denagliptin Phase 2/3 T31391 DRUGINFO D0E3HY IP10 C8 Phase 2 T31391 DRUGINFO D03SKC KRP-104 Phase 2 T31391 DRUGINFO D06VMJ Melogliptin Phase 2 T31391 DRUGINFO D0H2IO P32/98 Phase 2 T31391 DRUGINFO D07HZG PF-00734200 Phase 2 T31391 DRUGINFO D05VXF YSCMA Phase 1/2 T31391 DRUGINFO D0Z1OS ARI-2243 Phase 1 T31391 DRUGINFO D05LPW DA-1229 Phase 1 T31391 DRUGINFO D03JWU REC-01 Phase 1 T31391 DRUGINFO D07EPV Teneligliptin Phase 1 T31391 DRUGINFO D0BA5E ZYDPLA 1 Phase 1 T31391 DRUGINFO D0A6LI Aminopiperidine derivative 1 Patented T31391 DRUGINFO D06PIP Aminopiperidine derivative 2 Patented T31391 DRUGINFO D0W6HL Beta-phe compound 1 Patented T31391 DRUGINFO D02UOW Beta-phe compound 2 Patented T31391 DRUGINFO D0IO0M Beta-phe compound 3 Patented T31391 DRUGINFO D0XB0Q Dihydropyrrolopyrazole derivative 1 Patented T31391 DRUGINFO D02SUS Imidazo cyclohexylamine derivative 1 Patented T31391 DRUGINFO D0KS8Y Imidazo cyclohexylamine derivative 2 Patented T31391 DRUGINFO D04UXC Imidazo cyclohexylamine derivative 3 Patented T31391 DRUGINFO D0UV3I Imidazo pyridine derivative 2 Patented T31391 DRUGINFO D0QE8Z Peptide analog 44 Patented T31391 DRUGINFO D0B4CH Peptide analog 45 Patented T31391 DRUGINFO D0E8WW Peptide analog 46 Patented T31391 DRUGINFO D0WE8K Peptide analog 47 Patented T31391 DRUGINFO D05LJQ Peptide analog 48 Patented T31391 DRUGINFO D04XXF Peptide analog 49 Patented T31391 DRUGINFO D0BY2H Peptide analog 50 Patented T31391 DRUGINFO D0J4KQ Peptide analog 51 Patented T31391 DRUGINFO D0N9CV PMID25482888-Compound-11 Patented T31391 DRUGINFO D0LG1I PMID25482888-Compound-12 Patented T31391 DRUGINFO D01MMT PMID25482888-Compound-13 Patented T31391 DRUGINFO D0E9MO PMID25482888-Compound-14 Patented T31391 DRUGINFO D02LNB PMID25482888-Compound-15 Patented T31391 DRUGINFO D06GQG PMID25482888-Compound-16 Patented T31391 DRUGINFO D0G3IL PMID25482888-Compound-17 Patented T31391 DRUGINFO D0KR7R PMID25482888-Compound-18 Patented T31391 DRUGINFO D05GEY PMID25482888-Compound-21 Patented T31391 DRUGINFO D0A5QV PMID25482888-Compound-34 Patented T31391 DRUGINFO D0BJ2X PMID25482888-Compound-37 Patented T31391 DRUGINFO D0XN3O PMID25482888-Compound-38 Patented T31391 DRUGINFO D0K5YJ PMID25482888-Compound-50 Patented T31391 DRUGINFO D06PDK PMID25482888-Compound-52 Patented T31391 DRUGINFO D0T6SD PMID25482888-Compound-56 Patented T31391 DRUGINFO D0JP6A PMID25482888-Compound-6 Patented T31391 DRUGINFO D0J0UN PMID25482888-Compound-69 Patented T31391 DRUGINFO D0T1WB PMID25482888-Compound-70 Patented T31391 DRUGINFO D0G1CF PMID25482888-Compound-71 Patented T31391 DRUGINFO D0PF2W PMID25482888-Compound-72 Patented T31391 DRUGINFO D0RT1R Pyrimidine derivative 30 Patented T31391 DRUGINFO D07JJT Pyrimidine derivative 31 Patented T31391 DRUGINFO D0CW9H Pyrimidine derivative 32 Patented T31391 DRUGINFO D04MAZ Pyrimidine derivative 33 Patented T31391 DRUGINFO D0J5EW Pyrimidinedione derivative 1 Patented T31391 DRUGINFO D0P3DS Pyrrolo[1,2-f]triazine derivative 1 Patented T31391 DRUGINFO D0EL5B Pyrrolo[1,2-f]triazine derivative 2 Patented T31391 DRUGINFO D05HLQ Quinazoline derivative 1 Patented T31391 DRUGINFO D06HJX Thiomorpholine derivative 1 Patented T31391 DRUGINFO D0D4BP Thiomorpholine derivative 2 Patented T31391 DRUGINFO D00GNP Triazole piperazine derivative 1 Patented T31391 DRUGINFO D0PM4N Triazolo-pyrimidinedione derivative 1 Patented T31391 DRUGINFO D0O6SK Triazolo-pyrimidinedione derivative 2 Patented T31391 DRUGINFO D0E8AS Tricyclic heterocycle derivative 6 Patented T31391 DRUGINFO D0ND5K Xanthine derivative 1 Patented T31391 DRUGINFO D0K2ZQ Xanthine/amino piperidine compound 1 Patented T31391 DRUGINFO D0H2KV ALS 2-0426 Discontinued in Phase 2 T31391 DRUGINFO D00FYF NVP-DPP728 Discontinued in Phase 2 T31391 DRUGINFO D0FD0B PSN-9301 Discontinued in Phase 2 T31391 DRUGINFO D0E4EZ R-1438 Discontinued in Phase 2 T31391 DRUGINFO D0JA1Z TA-6666 Discontinued in Phase 2 T31391 DRUGINFO D0A1NU ABT-279 Discontinued in Phase 1 T31391 DRUGINFO D0X5ZO SSR-162369 Discontinued in Phase 1 T31391 DRUGINFO D0Q4YP TAK-100 Discontinued in Phase 1 T31391 DRUGINFO D0Q6ED ASP8497 Preclinical T31391 DRUGINFO D0XL4I ER-319711-15 Preclinical T31391 DRUGINFO D0O6DC LY-2463665 Preclinical T31391 DRUGINFO D7K0GP PT630 Preclinical T31391 DRUGINFO D0M9SL DSP-7238 Terminated T31391 DRUGINFO D0F3TI PT-630 Terminated T31391 DRUGINFO D05UUA (+/-)-6-(2-chlorophenyl)cyclohex-3-enamine Investigative T31391 DRUGINFO D0W4GM (1-phenylcyclopentyl)methanamine Investigative T31391 DRUGINFO D0P5OE (1R,2R)-1,2-diphenylethane-1,2-diamine Investigative T31391 DRUGINFO D07HWI (1R,2S)-1,2-diphenylethane-1,2-diamine Investigative T31391 DRUGINFO D00HSG (2-(2-chlorophenyl)pyridin-3-yl)methanamine Investigative T31391 DRUGINFO D0X2JG (2-chloro-6-phenoxyphenyl)methanamine Investigative T31391 DRUGINFO D07VDJ (2s)-Pyrrolidin-2-Ylmethylamine Investigative T31391 DRUGINFO D09BYA (3S,4R)-3-butyl-1-phenylpiperidin-4-amine Investigative T31391 DRUGINFO D0N5CI (5-phenyl-3H-benzo[d]imidazol-4-yl)methanamine Investigative T31391 DRUGINFO D04CAR (R)-1-(2-aminoacetyl)pyrrolidin-2-ylboronic acid Investigative T31391 DRUGINFO D0O9RD (S)-2-Amino-1-azetidin-1-yl-2-cyclohexyl-ethanone Investigative T31391 DRUGINFO D0L5RI (S)-2-Amino-1-thiazolidin-3-yl-propane-1-thione Investigative T31391 DRUGINFO D07IJU (S)-pyrrolidin-1-yl(pyrrolidin-2-yl)methanone Investigative T31391 DRUGINFO D0R5OE (S)-pyrrolidin-2-yl(thiazolidin-3-yl)methanone Investigative T31391 DRUGINFO D0JI3S 1-benzhydryl-3-butylpiperidin-4-amine Investigative T31391 DRUGINFO D06AUB 1-benzyl-4-(2,4-dichlorophenyl)pyrrolidin-3-amine Investigative T31391 DRUGINFO D09MVE 1-biphenyl-2-ylmethanamine Investigative T31391 DRUGINFO D02WBC 2-(2-chlorophenyl)-2-morpholinoethanamine Investigative T31391 DRUGINFO D0L9XR 2-Amino-3-Methyl-1-Pyrrolidin-1-Yl-Butan-1-One Investigative T31391 DRUGINFO D00KMP 3-butyl-1-(naphthalen-1-yl)piperidin-4-amine Investigative T31391 DRUGINFO D06UKY 4-(2,4-dichlorophenyl)-1-phenylpyrrolidin-3-amine Investigative T31391 DRUGINFO D02RIE 4-(2,4-dichlorophenyl)-1-tosylpyrrolidin-3-amine Investigative T31391 DRUGINFO D0PB2M 4-iodophenyl-alaninyl-(S)-2-cyano-pyrrolidine Investigative T31391 DRUGINFO D04QDB ABT-341 Investigative T31391 DRUGINFO D07LUR Alpha-D-Mannose Investigative T31391 DRUGINFO D0N3YL ASC-201 Investigative T31391 DRUGINFO D01ZWF BPI-711001 Investigative T31391 DRUGINFO D06NRU C-(2'-Chloro-biphenyl-2-yl)-methylamine Investigative T31391 DRUGINFO D0T2EW Cyclohexylglycine-(2S)-cyanopyrrolidine Investigative T31391 DRUGINFO D0L1NF D-420720 Investigative T31391 DRUGINFO D0FH8R DB-160 Investigative T31391 DRUGINFO D03FDC Diisopropylphosphono Group Investigative T31391 DRUGINFO D0N1QQ DIPROTIN A Investigative T31391 DRUGINFO D01OUJ D-Val-L-boroPro Investigative T31391 DRUGINFO D0T8UH E-3024 Investigative T31391 DRUGINFO D01KRQ EMC-0901 Investigative T31391 DRUGINFO D05XWX FE 999011 Investigative T31391 DRUGINFO D0G6XS Fucose Investigative T31391 DRUGINFO D0D9ON Iodo-Phenylalanine Investigative T31391 DRUGINFO D05LYC KR-62436 Investigative T31391 DRUGINFO D0IQ4S L-Ala-L-boroPro Investigative T31391 DRUGINFO D0C2NQ L-Val-L-boroPro Investigative T31391 DRUGINFO D07ALM N4-(4-chlorobenzyl)-2,4-diaminobutanoylpiperidine Investigative T31391 DRUGINFO D0N1FU N-isoleucylthiazolidine Investigative T31391 DRUGINFO D05WKT PK-44 Investigative T31391 DRUGINFO D08NMS PMID20684603C24dd Investigative T31391 DRUGINFO D05TKO Retagliptin Investigative T31391 KEGGPATH hsa04974:Protein digestion and absorption T31391 NET_PATH NetPath_14:IL2 Signaling Pathway T31391 NET_PATH NetPath_7:TGF_beta_Receptor Signaling Pathway T61744 TARGETID T61744 T61744 FORMERID TTDS00280 T61744 UNIPROID PDE4A_HUMAN T61744 TARGNAME Phosphodiesterase 4A (PDE4A) T61744 GENENAME PDE4A T61744 TARGTYPE Successful target T61744 SYNONYMS cAMP-specific 3',5'-cyclic phosphodiesterase 4A; Type 4A cAMP phosphodiesterase; PDE46; DPDE2 T61744 FUNCTION Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes. T61744 PDBSTRUC 3TVX; 3I8V; 2QYK T61744 BIOCLASS Phosphoric diester hydrolase T61744 ECNUMBER EC 3.1.4.53 T61744 SEQUENCE MEPPTVPSERSLSLSLPGPREGQATLKPPPQHLWRQPRTPIRIQQRGYSDSAERAERERQPHRPIERADAMDTSDRPGLRTTRMSWPSSFHGTGTGSGGAGGGSSRRFEAENGPTPSPGRSPLDSQASPGLVLHAGAATSQRRESFLYRSDSDYDMSPKTMSRNSSVTSEAHAEDLIVTPFAQVLASLRSVRSNFSLLTNVPVPSNKRSPLGGPTPVCKATLSEETCQQLARETLEELDWCLEQLETMQTYRSVSEMASHKFKRMLNRELTHLSEMSRSGNQVSEYISTTFLDKQNEVEIPSPTMKEREKQQAPRPRPSQPPPPPVPHLQPMSQITGLKKLMHSNSLNNSNIPRFGVKTDQEELLAQELENLNKWGLNIFCVSDYAGGRSLTCIMYMIFQERDLLKKFRIPVDTMVTYMLTLEDHYHADVAYHNSLHAADVLQSTHVLLATPALDAVFTDLEILAALFAAAIHDVDHPGVSNQFLINTNSELALMYNDESVLENHHLAVGFKLLQEDNCDIFQNLSKRQRQSLRKMVIDMVLATDMSKHMTLLADLKTMVETKKVTSSGVLLLDNYSDRIQVLRNMVHCADLSNPTKPLELYRQWTDRIMAEFFQQGDRERERGMEISPMCDKHTASVEKSQVGFIDYIVHPLWETWADLVHPDAQEILDTLEDNRDWYYSAIRQSPSPPPEEESRGPGHPPLPDKFQFELTLEEEEEEEISMAQIPCTAQEALTAQGLSGVEEALDATIAWEASPAQESLEVMAQEASLEAELEAVYLTQQAQSTGSAPVAPDEFSSREEFVVAVSHSSPSALALQSPLLPAWRTLSVSEHAPGLPGLPSTAAEVEAQREHQAAKRACSACAGTFGEDTSALPAPGGGGSGGDPT T61744 DRUGINFO D02PWM Dyphylline Approved T61744 DRUGINFO D09AMZ Enprofylline Approved T61744 DRUGINFO D01XHG DENBUFYLLINE Phase 3 T61744 DRUGINFO D06VFP SOTB07 Phase 3 T61744 DRUGINFO D00JED AN-2898 Phase 2 T61744 DRUGINFO D0F4TV AWD-12-281 Phase 2 T61744 DRUGINFO D0U2DH CC-1088 Phase 2 T61744 DRUGINFO D01XFZ GPD-1116 Phase 2 T61744 DRUGINFO D07OCV HT-0712 Phase 2 T61744 DRUGINFO D0F5IY LIRIMILAST Phase 2 T61744 DRUGINFO D0M7CB MK-0873 Phase 2 T61744 DRUGINFO D0L8KJ Oglemilast Phase 2 T61744 DRUGINFO D0RJ1W OX-914 Phase 2 T61744 DRUGINFO D0Z2FB Piclamilast Phase 2 T61744 DRUGINFO D0X0PW Revamilast Phase 2 T61744 DRUGINFO D02POH TA-7906 Phase 2 T61744 DRUGINFO D09TFB TOFIMILAST Phase 2 T61744 DRUGINFO DB82TO Tofisopam Phase 2 T61744 DRUGINFO D01WZL AVE-8112 Phase 1 T61744 DRUGINFO D0K9DI GSK-356278 Phase 1 T61744 DRUGINFO D03CWX MEM-1414 Phase 1 T61744 DRUGINFO D0O8JW Ronomilast Phase 1 T61744 DRUGINFO D02EMR Cilomilast Discontinued in Phase 3 T61744 DRUGINFO D0UG4T CDP840 Discontinued in Phase 2 T61744 DRUGINFO D00DBE CI-1018 Discontinued in Phase 2 T61744 DRUGINFO D0I0GM Daxalipram Discontinued in Phase 2 T61744 DRUGINFO D0U7PS GSK256066 Discontinued in Phase 2 T61744 DRUGINFO D03ZVD KW-4490 Discontinued in Phase 2 T61744 DRUGINFO D0V2CN LAS-37779 Discontinued in Phase 2 T61744 DRUGINFO D08SNX V-11294A Discontinued in Phase 2 T61744 DRUGINFO D0K1OA D-4418 Discontinued in Phase 1 T61744 DRUGINFO D01FXD SCH-351591 Discontinued in Phase 1 T61744 DRUGINFO D0C7JT YM-976 Discontinued in Phase 1 T61744 DRUGINFO D0R1QJ D-22888 Terminated T61744 DRUGINFO D01QUF GW-3600 Terminated T61744 DRUGINFO D07UHY NIK-616 Terminated T61744 DRUGINFO D01OUA TJN-598 Terminated T61744 DRUGINFO D0F7TV Torbafylline Terminated T61744 DRUGINFO D0W7BI (2,5-Diphenyl-furan-3-yl)-phenyl-methanone Investigative T61744 DRUGINFO D01RUN (R)-Rolipram Investigative T61744 DRUGINFO D02FZD (S)-Rolipram Investigative T61744 DRUGINFO D00JBC 1-Butyl-3-methyl-3,7-dihydro-purine-2,6-dione Investigative T61744 DRUGINFO D00TQR 1-Methyl-3-propyl-3,7-dihydro-purine-2,6-dione Investigative T61744 DRUGINFO D01CAY 2,5-Bis-(3,4-dimethoxy-phenyl)-furan Investigative T61744 DRUGINFO D0N2KP 2,5-Bis-(3-cyclopentyloxy-4-methoxy-phenyl)-furan Investigative T61744 DRUGINFO D0J4AT 4-(2,5-Diphenyl-furan-3-yl)-morpholine Investigative T61744 DRUGINFO D04XRV 6-Azido-8-(3-iodo-phenyl)-quinoline Investigative T61744 DRUGINFO D0L0NY 6-Imidazol-1-ylmethyl-8-phenyl-quinoline Investigative T61744 DRUGINFO D0V8DB 8-(3-Azido-phenyl)-6-iodo-quinoline Investigative T61744 DRUGINFO D0Z5SB 8-(3-Azido-phenyl)-6-pyridin-4-ylmethyl-quinoline Investigative T61744 DRUGINFO D02NKD 8-(3-Nitro-phenyl)-6-phenyl-[1,7]naphthyridine Investigative T61744 DRUGINFO D0K4HG 8-(3-Nitro-phenyl)-6-pyridin-4-ylmethyl-quinoline Investigative T61744 DRUGINFO D04BMR AL-59640 Investigative T61744 DRUGINFO D0N7HS ASP-3258 Investigative T61744 DRUGINFO D09AUL Benzyl-(2-imidazol-1-yl-quinazolin-4-yl)-amine Investigative T61744 DRUGINFO D0J7GF Benzyl-(2-phenyl-quinazolin-4-yl)-amine Investigative T61744 DRUGINFO D01TOR Benzyl-(2-pyridin-3-yl-quinazolin-4-yl)-amine Investigative T61744 DRUGINFO D0U8YQ Benzyl-(2-pyridin-4-yl-quinazolin-4-yl)-amine Investigative T61744 DRUGINFO D02NWF Benzyl-(2-thiophen-2-yl-quinazolin-4-yl)-amine Investigative T61744 DRUGINFO D0U4SS CD-160130 Investigative T61744 DRUGINFO D05YEL CH-3697 Investigative T61744 DRUGINFO D0K9PS CHF-5480 Investigative T61744 DRUGINFO D0DL6J CI-1044 Investigative T61744 DRUGINFO D0R6MT isobutylmethylxanthine Investigative T61744 DRUGINFO D0E5VP KF-66490 Investigative T61744 DRUGINFO D06GUJ KURAIDIN Investigative T61744 DRUGINFO D0W4ZU KURARINOL Investigative T61744 DRUGINFO D0JD4C L-454560 Investigative T61744 DRUGINFO D0V1IM L-791943 Investigative T61744 DRUGINFO D0W7WV L-869298 Investigative T61744 DRUGINFO D0Y3PP NIS-62949 Investigative T61744 DRUGINFO D0V5BX NITRAQUAZONE Investigative T61744 DRUGINFO D0S6MA OCID-2987 Investigative T61744 DRUGINFO D0T5PO ROLIPRAM Investigative T61744 DRUGINFO D0O3BL RS-14491 Investigative T61744 DRUGINFO D0P2HX RS-25344 Investigative T61744 DRUGINFO D00QCL SOPHOFLAVESCENOL Investigative T61744 DRUGINFO D0S1HX TAS-203 Investigative T61744 DRUGINFO D02ZPV UCB-101333-3 Investigative T61744 DRUGINFO D04JNC ZL-N-91 Investigative T61744 KEGGPATH hsa00230:Purine metabolism T61744 KEGGPATH hsa04024:cAMP signaling pathway T61744 KEGGPATH hsa05032:Morphine addiction T61744 WIKIPATH WP35:G Protein Signaling Pathways T61744 REACPATH R-HSA-180024:DARPP-32 events T61744 REACPATH R-HSA-418555:G alpha (s) signalling events T92072 TARGETID T92072 T92072 FORMERID TTDS00186 T92072 UNIPROID AA1R_HUMAN T92072 TARGNAME Adenosine A1 receptor (ADORA1) T92072 GENENAME ADORA1 T92072 TARGTYPE Successful target T92072 SYNONYMS Adenosine receptor A1; A(1) adenosine receptor T92072 FUNCTION The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase. Receptor for adenosine. T92072 PDBSTRUC 6D9H; 5UEN; 5N2S T92072 BIOCLASS GPCR rhodopsin T92072 SEQUENCE MPPSISAFQAAYIGIEVLIALVSVPGNVLVIWAVKVNQALRDATFCFIVSLAVADVAVGALVIPLAILINIGPQTYFHTCLMVACPVLILTQSSILALLAIAVDRYLRVKIPLRYKMVVTPRRAAVAIAGCWILSFVVGLTPMFGWNNLSAVERAWAANGSMGEPVIKCEFEKVISMEYMVYFNFFVWVLPPLLLMVLIYLEVFYLIRKQLNKKVSASSGDPQKYYGKELKIAKSLALILFLFALSWLPLHILNCITLFCPSCHKPSILTYIAIFLTHGNSAMNPIVYAFRIQKFRVTFLKIWNDHFRCQPAPPIDEDLPEERPDD T92072 DRUGINFO D0B3HD Caffeine Approved T92072 DRUGINFO D0X0IY Rolofylline Phase 3 T92072 DRUGINFO D0QH7H AMP-579 Phase 2 T92072 DRUGINFO D0BA5K Apaxifylline Phase 2 T92072 DRUGINFO D0M7BL BAY 1067197 Phase 2 T92072 DRUGINFO D0I3YX Capadenoson Phase 2 T92072 DRUGINFO D0I1EX DTI-0009 Phase 2 T92072 DRUGINFO D04YAJ SELODENOSON Phase 2 T92072 DRUGINFO D0F5UN SLV320 Phase 2 T92072 DRUGINFO D00SUK Tonapofylline Phase 2 T92072 DRUGINFO D05KBP INO-8875 Phase 1/2 T92072 DRUGINFO D0Z9RJ GS 9667 Phase 1 T92072 DRUGINFO D0L5VS KF-17837 Phase 1 T92072 DRUGINFO D02YQO SCH-442416 Phase 1 T92072 DRUGINFO D0T0YA PMID27387065-Compound-6 Patented T92072 DRUGINFO D09GGJ CVT-124 Discontinued in Phase 3 T92072 DRUGINFO D07VZV N-0861 Discontinued in Phase 3 T92072 DRUGINFO D00YSJ Tecadenoson Discontinued in Phase 3 T92072 DRUGINFO D0K2BQ BRL-61063 Discontinued in Phase 2 T92072 DRUGINFO D03JHJ FK-352 Discontinued in Phase 2 T92072 DRUGINFO D01VPK FK-453 Discontinued in Phase 2 T92072 DRUGINFO D0EK6D FK-838 Discontinued in Phase 2 T92072 DRUGINFO D0UH4T GW-493838 Discontinued in Phase 2 T92072 DRUGINFO D0V5DX GR-79236 Discontinued in Phase 1 T92072 DRUGINFO D08ZBT SDZ-WAG-994 Discontinued in Phase 1 T92072 DRUGINFO D0HE1P BAY 60-6583 Preclinical T92072 DRUGINFO D0I7BL ARISTEROMYCIN Terminated T92072 DRUGINFO D0E4WF METHYLTHIOADENOSINE Terminated T92072 DRUGINFO D0NQ5I METRIFUDIL Terminated T92072 DRUGINFO D0Y6GJ ZM-241385 Terminated T92072 DRUGINFO D0VB6X (1H-Imidazo[4,5-c]quinolin-4-yl)-phenyl-amine HCl Investigative T92072 DRUGINFO D09FUO (1-Phenyl-propyl)-(9-phenyl-9H-purin-6-yl)-amine Investigative T92072 DRUGINFO D0UM4R (2-Chloro-9-methyl-9H-purin-6-yl)-phenyl-amine Investigative T92072 DRUGINFO D0D8WN (9-Methyl-9H-purin-6-yl)-phenyl-amine Investigative T92072 DRUGINFO D0TU7I (E)-8-(3-chlorostyryl)-caffeine Investigative T92072 DRUGINFO D0V9OO (R,S)-PHPNECA Investigative T92072 DRUGINFO D0E9QX (S)-PIA Investigative T92072 DRUGINFO D0R1XY [3H]CCPA Investigative T92072 DRUGINFO D08RSU [3H]DPCPX Investigative T92072 DRUGINFO D08EBT [3H]HEMADO Investigative T92072 DRUGINFO D0K8ZZ [3H]NECA Investigative T92072 DRUGINFO D0K6ZA [3H]OSIP339391 Investigative T92072 DRUGINFO D07HNM 1,3-Diallyl-3,7-dihydro-purine-2,6-dione Investigative T92072 DRUGINFO D02RMR 1,3-Diethyl-3,7-dihydro-purine-2,6-dione Investigative T92072 DRUGINFO D0T6XM 1,3-Diisobutyl-3,7-dihydro-purine-2,6-dione Investigative T92072 DRUGINFO D03KKK 1,3-Dipropyl-3,7-dihydro-purine-2,6-dione Investigative T92072 DRUGINFO D0U8DW 1-Butyl-8-phenyl-3,7-dihydro-purine-2,6-dione Investigative T92072 DRUGINFO D08MRB 1H-Imidazo[4,5-c]quinolin-4-ylamine HCl Investigative T92072 DRUGINFO D0BA7Q 1-Methyl-8-phenyl-3,7-dihydro-purine-2,6-dione Investigative T92072 DRUGINFO D0F1AS 1-METHYLXANTHINE Investigative T92072 DRUGINFO D0LD0X 1-Propyl-3,7-dihydro-purine-2,6-dione Investigative T92072 DRUGINFO D0PU6F 2-(1H-benzo[d]imidazol-2-yl)quinoxaline Investigative T92072 DRUGINFO D08CIY 2-(2-furyl)-6-(1H-pyrazol-1-yl)pyrimidin-4-amine Investigative T92072 DRUGINFO D0KJ3H 2-(2''-indolylethyloxy)adenosine Investigative T92072 DRUGINFO D03HBG 2-(3''-(4''-bromo-indolyl)ethyloxy)adenosine Investigative T92072 DRUGINFO D0L6YI 2-(3''-(5''-bromo-indolyl)ethyloxy)adenosine Investigative T92072 DRUGINFO D0Q1RD 2-(3''(5''-chloro-indolyl)ethyloxy)adenosine Investigative T92072 DRUGINFO D0I1IW 2-(3''-(5''-fluoro-indolyl)ethyloxy)adenosine Investigative T92072 DRUGINFO D0P0BV 2-(3''-(5''-hydroxyindolyl)ethyloxy)adenosine Investigative T92072 DRUGINFO D0G6VT 2-(3''-(5''-iodo-indolyl)ethyloxy)adenosine Investigative T92072 DRUGINFO D09VOP 2-(3''-(5''-methoxy-indolyl)ethyloxy)adenosine Investigative T92072 DRUGINFO D0G6BI 2-(3''-(6''-bromo-indolyl)ethyloxy)adenosine Investigative T92072 DRUGINFO D02JMR 2-(3''-(6''-chloro-indolyl)ethyloxy)adenosine Investigative T92072 DRUGINFO D0QN4U 2-(3''(7''-bromo-indolyl)ethyloxy)adenosine Investigative T92072 DRUGINFO D06RCT 2-(3''-indolylethyloxy)adenosine Investigative T92072 DRUGINFO D00ASZ 2-(3''-pyrrolylethyloxy)adenosine Investigative T92072 DRUGINFO D0N1PT 2-(4-chloro-1H-benzo[d]imidazol-2-yl)quinoxaline Investigative T92072 DRUGINFO D0L2MN 2-(4-chlorophenyl)-6-phenyl-9H-purine Investigative T92072 DRUGINFO D0OX0V 2-(4-ethylthiobenzimidazol-2-yl)quinoxaline Investigative T92072 DRUGINFO D07IPZ 2-(4-hydroxypent-1-yl)-N6-methoxyadenosine Investigative T92072 DRUGINFO D0R4LZ 2-(4-methoxyphenyl)-6-phenyl-9H-purine Investigative T92072 DRUGINFO D09VRX 2-(4-methyl-1H-benzo[d]imidazol-2-yl)quinoxaline Investigative T92072 DRUGINFO D0E4LB 2-(5-cyano-1-pent-1-ynyl)-N6-methoxyadenosine Investigative T92072 DRUGINFO D0P8MK 2-(6-amino-8-bromo-9H-purin-9-yl)ethanol Investigative T92072 DRUGINFO D0NH5X 2-(6-Cyclopentylamino-purin-9-yl)-ethanol Investigative T92072 DRUGINFO D01PGY 2-(hex-1-ynyl)-N6-methoxyadenosine Investigative T92072 DRUGINFO D0T5FY 2,4-Dichloro-N-(4-phenyl-thiazol-2-yl)-benzamide Investigative T92072 DRUGINFO D0IG5E 2,5'-dichloro-5'-deoxy-N6-cyclopentyladenosine Investigative T92072 DRUGINFO D0E7YE 2,6,8-triphenyl-9H-purine Investigative T92072 DRUGINFO D07FGB 2,6-bis(4-tolyl)-9H-purine Investigative T92072 DRUGINFO D03KLO 2,6-dimethyl-8-ethyl-1-deazapurine Investigative T92072 DRUGINFO D0N1QP 2,6-diphenyl-1-deazapurine Investigative T92072 DRUGINFO D00GNW 2,6-diphenyl-8-(1-ethylpropyl)-1-deazapurine Investigative T92072 DRUGINFO D00NFW 2,6-diphenyl-8-ethyl-1-deazapurine Investigative T92072 DRUGINFO D0I2EQ 2,6-diphenyl-8-methyl-1-deazapurine Investigative T92072 DRUGINFO D01NHH 2,6-diphenyl-8-tButyl-1-deazapurine Investigative T92072 DRUGINFO D0RZ2M 2,6-diphenyl-9H-purine Investigative T92072 DRUGINFO D08INY 2,6-Diphenyl-pyrimidin-4-ylamine Investigative T92072 DRUGINFO D02FLH 2,6-dphenyl-8-propyl-1-deazapurine Investigative T92072 DRUGINFO D08JYX 2-[(4-acetylphenyl)ethynyl]-N6-methoxyadenosine Investigative T92072 DRUGINFO D0KT3L 2-[(4-fluorophenyl)ethynyl]-N6-methoxyadenosine Investigative T92072 DRUGINFO D0F4XB 2-Amino-4,6-di-furan-2-yl-nicotinonitrile Investigative T92072 DRUGINFO D0N2VO 2-Amino-4,6-diphenyl-nicotinonitrile Investigative T92072 DRUGINFO D00HYS 2-Amino-4,6-diphenyl-pyrimidin-5-carbonitrile Investigative T92072 DRUGINFO D0QD3O 2-Amino-4,6-diphenyl-pyrimidine Investigative T92072 DRUGINFO D04ZTH 2-Amino-4,6-di-thiophen-2-yl-nicotinonitrile Investigative T92072 DRUGINFO D0P7FK 2-Amino-4-furan-2-yl-6-phenyl-nicotinonitrile Investigative T92072 DRUGINFO D0KM0Y 2-Amino-4-phenyl-6-thiophen-2-yl-nicotinonitrile Investigative T92072 DRUGINFO D0V9EE 2-Amino-6-furan-2-yl-4-phenyl-nicotinonitrile Investigative T92072 DRUGINFO D06NQD 2-amino-6-phenyl-4-p-tolylnicotinonitrile Investigative T92072 DRUGINFO D0BC7P 2-Amino-6-phenyl-4-thiophen-2-yl-nicotinonitrile Investigative T92072 DRUGINFO D04XLX 2-amino-N-benzyl-6-phenyl-9H-purine-9-carboxamide Investigative T92072 DRUGINFO D0A5KG 2-azido-N6-methyl-9-(beta-D-ribofuranosyl)adenine Investigative T92072 DRUGINFO D0Z1WY 2-chloro-2'-C-methyl-tecadenoson Investigative T92072 DRUGINFO D0UM6O 2-chloro-4-(thiazol-2-yl)thieno[3,2-d]pyrimidine Investigative T92072 DRUGINFO D09UDF 2-chloro-4-(thiophen-2-yl)thieno[3,2-d]pyrimidine Investigative T92072 DRUGINFO D0C2UJ 2-chloroadenosine Investigative T92072 DRUGINFO D0B1RV 2-Cyclopentyl-1H-imidazo[4,5-c]quinolin-4-ylamine Investigative T92072 DRUGINFO D05TFM 2-ethyl-4-(furan-2-yl)thieno[3,2-d]pyrimidine Investigative T92072 DRUGINFO D0Y7AV 2-ethyl-4-(furan-3-yl)thieno[3,2-d]pyrimidine Investigative T92072 DRUGINFO D0J6ME 2-ethyl-4-(pyridin-2-yl)thieno[3,2-d]pyrimidine Investigative T92072 DRUGINFO D0O4KI 2-ethyl-4-(thiazol-2-yl)thieno[3,2-d]pyrimidine Investigative T92072 DRUGINFO D07YKU 2-ethyl-4-(thiophen-2-yl)thieno[3,2-d]pyrimidine Investigative T92072 DRUGINFO D01VXP 2-ethynyl-N6-methoxyadenosine Investigative T92072 DRUGINFO D07DOE 2'-Me-tecadenoson Investigative T92072 DRUGINFO D0J3TY 2-m-tolyl-2H-pyrazolo[3,4-c]quinolin-4(5H)-one Investigative T92072 DRUGINFO D04PJO 2-m-tolyl-2H-pyrazolo[3,4-c]quinolin-4-amine Investigative T92072 DRUGINFO D0LP5G 2-Phenyl-1H-imidazo[4,5-c]quinolin-4-ylamine Investigative T92072 DRUGINFO D06ZWQ 2-phenyl-2H-pyrazolo[3,4-c]quinolin-4(5H)-one Investigative T92072 DRUGINFO D09HAM 2-phenyl-2H-pyrazolo[3,4-c]quinolin-4-amine Investigative T92072 DRUGINFO D0I7HL 2-phenylpropoxyadenosine Investigative T92072 DRUGINFO D0J4SW 2-p-tolyl-2H-pyrazolo[3,4-c]quinolin-4(5H)-one Investigative T92072 DRUGINFO D02TEW 2-p-tolyl-2H-pyrazolo[3,4-c]quinolin-4-amine Investigative T92072 DRUGINFO D08JUQ 2-tolyl-6-phenyl-9H-purine Investigative T92072 DRUGINFO D08AJS 3-(3-chloro-1H-pyrazol-5-yl)quinoxalin-2(1H)-one Investigative T92072 DRUGINFO D0K2QF 3,4-Dichloro-N-(4-phenyl-thiazol-2-yl)-benzamide Investigative T92072 DRUGINFO D00YOM 3-Benzyl-7-methyl-[1,8]naphthyridin-4-ol Investigative T92072 DRUGINFO D08RGW 3-Benzyl-7-methyl-[1,8]naphthyridine-4-thiol Investigative T92072 DRUGINFO D0YB3X 3-Chloro-N-(4-phenyl-thiazol-2-yl)-benzamide Investigative T92072 DRUGINFO D02PBY 3-noradamantyl-1,3-dipropylxanthine Investigative T92072 DRUGINFO D0T2RY 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Investigative T92072 DRUGINFO D00OFN 4-(ethylthio)-6-phenyl-1,3,5-triazin-2-amine Investigative T92072 DRUGINFO D0W5CZ 4-(furan-2-yl)-7H-pyrrolo[2,3-d]pyrimidin-2-amine Investigative T92072 DRUGINFO D0QN5I 4-(furan-2-yl)thieno[3,2-d]pyrimidin-2-amine Investigative T92072 DRUGINFO D0CB9B 4-(thiazol-2-yl)thieno[3,2-d]pyrimidin-2-amine Investigative T92072 DRUGINFO D00NYG 4-Amino-2,6-diphenyl-pyrimidine-5-carbonitrile Investigative T92072 DRUGINFO D04LPX 4-Bromo-N-(4-phenyl-thiazol-2-yl)-benzamide Investigative T92072 DRUGINFO D09KUY 4-Chloro-7-methyl-2-phenyl-[1,8]naphthyridine Investigative T92072 DRUGINFO D00UFJ 4-Chloro-N-(4-phenyl-thiazol-2-yl)-benzamide Investigative T92072 DRUGINFO D07VCN 4-Ethoxy-7-((E)-styryl)-furo[3,2-g]chromen-5-one Investigative T92072 DRUGINFO D0O8QS 4-Methoxy-N-(3-phenyl-isoquinolin-1-yl)-benzamide Investigative T92072 DRUGINFO D0W0QF 4-Methyl-N-(4-phenyl-thiazol-2-yl)-benzamide Investigative T92072 DRUGINFO D0H3QX 4-Nitro-N-(4-phenyl-thiazol-2-yl)-benzamide Investigative T92072 DRUGINFO D04QAD 4-tert-Butyl-N-(4-phenyl-thiazol-2-yl)-benzamide Investigative T92072 DRUGINFO D04TTP 5,7-dibromo-9H-pyrido[3,4-b]indol-6-ol Investigative T92072 DRUGINFO D0ZW9L 5,7-diphenyl-3H-imidazo[4,5-b]pyridin-2-ol Investigative T92072 DRUGINFO D0G8XJ 5-Cl-5-deoxy-(+/-)-ENBA Investigative T92072 DRUGINFO D00MPA 6-(furan-2-yl)-9H-purin-2-amine Investigative T92072 DRUGINFO D0P1JJ 6-ethylamino-2-(3''-indolyl)ethyloxy)adenosine Investigative T92072 DRUGINFO D0Q5CS 6-guanidino-2-(3''-indolylethyloxy)adenosine Investigative T92072 DRUGINFO D0N0OE 7-(3,6,9,12-tetraoxatricos-22-enyl)theophylline Investigative T92072 DRUGINFO D05SYY 7-Bromo-2-phenyl-[1,8]naphthyridin-4-ol Investigative T92072 DRUGINFO D05MCK 7-Chloro-2-phenyl-[1,8]naphthyridin-4-ol Investigative T92072 DRUGINFO D06QRI 7-Dimethylamino-2-phenyl-[1,8]naphthyridin-4-ol Investigative T92072 DRUGINFO D01MOQ 7-Methyl-2-propyl-[1,8]naphthyridin-4-ol Investigative T92072 DRUGINFO D0E8RA 8-Bromo-9-(2,3-dihydroxypropyl)-9H-adenine Investigative T92072 DRUGINFO D0S6QA 8-Bromo-9-(2-butyl)-9H-adenine Investigative T92072 DRUGINFO D0W6FC 8-Bromo-9-(2-hydroxypropyl)-9H-adenine Investigative T92072 DRUGINFO D0CX7N 8-Bromo-9-(3-hydroxypropyl)-9H-adenine Investigative T92072 DRUGINFO D0W8RB 8-Bromo-9-(but-3-enyl)-9H-adenine Investigative T92072 DRUGINFO D0Z8VU 8-Bromo-9-(sec-butyl)-9H-adenine Investigative T92072 DRUGINFO D04LZN 8-Bromo-9-cyclobutyl-9H-adenine Investigative T92072 DRUGINFO D01QBK 8-Bromo-9-cyclohexyl-9H-adenine Investigative T92072 DRUGINFO D0AI8F 8-Bromo-9-cyclopentyl-9H-adenine Investigative T92072 DRUGINFO D01WNA 8-Bromo-9-ethyl-9H-adenine Investigative T92072 DRUGINFO D0B0TX 8-bromo-9-isobutyl-9H-purin-6-amine Investigative T92072 DRUGINFO D06KYP 8-Bromo-9-isopropyl-9H-adenine Investigative T92072 DRUGINFO D0R8OK 8-Bromo-9-methyl-9H-adenine Investigative T92072 DRUGINFO D00CJJ 8-Bromo-9-phenylethyl-9H-adenine Investigative T92072 DRUGINFO D02HOL 8-Bromo-9-propyl-9H-adenine Investigative T92072 DRUGINFO D0L7DL 8-cyclohexyl-6-(4-tolyl)-2-phenyl-9H-purine Investigative T92072 DRUGINFO D0L5JL 8-cyclopentyltheophylline Investigative T92072 DRUGINFO D0V8MD 8-PHENYL THEOPHYLLINE Investigative T92072 DRUGINFO D0B1YW 8-Phenyl-1-propyl-3,7-dihydro-purine-2,6-dione Investigative T92072 DRUGINFO D0L8DZ 8-Phenyl-3,7-dihydro-purine-2,6-dione Investigative T92072 DRUGINFO D0W3MT 8-propyl-2,6-diphenyl-9H-purine Investigative T92072 DRUGINFO D05ZRR 9-(3-aminobenzyl)-6-(furan-2-yl)-9H-purin-2-amine Investigative T92072 DRUGINFO D02NBB 9-(3-nitrobenzyl)-6-(furan-2-yl)-9H-purin-2-amine Investigative T92072 DRUGINFO D08AXT 9-(4-nitrobenzyl)-6-(furan-2-yl)-9H-purin-2-amine Investigative T92072 DRUGINFO D0S5XP 9-Allyl-8-bromo-9H-adenine Investigative T92072 DRUGINFO D0D3WR 9-benzyl-6-(furan-2-yl)-9H-purin-2-amine Investigative T92072 DRUGINFO D02RBK 9-Benzyl-8-bromo-9H-adenine Investigative T92072 DRUGINFO D0A6JX 9-Cyclobutyl-9H-adenine Investigative T92072 DRUGINFO D0B3UE 9-Cyclopentyl-9H-adenine Investigative T92072 DRUGINFO D01VEU 9-Ethyl-8-phenylethynyl-9H-purin-6-ylamine Investigative T92072 DRUGINFO D03JFX 9-Ethyl-9H-adenine Investigative T92072 DRUGINFO D0DB7A 9-Isopropyl-9H-adenine Investigative T92072 DRUGINFO D02BGA 9-Methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine Investigative T92072 DRUGINFO D04JIR 9-Methyl-9H-adenine Investigative T92072 DRUGINFO D0G8GA 9-Phenyl-9H-purin-6-ylamine Investigative T92072 DRUGINFO D04WHE 9-Propyl-9H-adenine Investigative T92072 DRUGINFO D0F9QT A-987306 Investigative T92072 DRUGINFO D0XE8T Anthoptilide C Investigative T92072 DRUGINFO D0A4MK AS100 Investigative T92072 DRUGINFO D0Q9GL AS70 Investigative T92072 DRUGINFO D07FZA AS99 Investigative T92072 DRUGINFO D05QNV ATL802 Investigative T92072 DRUGINFO D0ZO1R Cirsimarin Investigative T92072 DRUGINFO D02HHW CP608,039 Investigative T92072 DRUGINFO D0G2JG CPFPX Investigative T92072 DRUGINFO D08LZN Cyclohexyl-(2-phenylsulfanyl-9H-purin-6-yl)-amine Investigative T92072 DRUGINFO D09ETC Cyclohexyl-(9-ethyl-9H-purin-6-yl)-amine Investigative T92072 DRUGINFO D08VXF Cyclohexyl-(9-methyl-9H-purin-6-yl)-amine Investigative T92072 DRUGINFO D0N1PS Cyclopentyl-(9-cyclopentyl-9H-purin-6-yl)-amine Investigative T92072 DRUGINFO D05ZYN Cyclopentyl-(9-ethyl-9H-purin-6-yl)-amine Investigative T92072 DRUGINFO D01EHP Cyclopentyl-(9-methyl-9H-purin-6-yl)-amine Investigative T92072 DRUGINFO D01GUK Cyclopentyl-(9-phenyl-9H-purin-6-yl)-amine Investigative T92072 DRUGINFO D07HKU DEPX Investigative T92072 DRUGINFO D0NO5E Ethyl 5-benzoyl-4-phenylthiazol-2-ylcarbamate Investigative T92072 DRUGINFO D0S0RK flavone Investigative T92072 DRUGINFO D0F9JF FR-166124 Investigative T92072 DRUGINFO D0S2MO FR194921 Investigative T92072 DRUGINFO D0K0OT GNF-PF-2224 Investigative T92072 DRUGINFO D0O1CW GNF-PF-2700 Investigative T92072 DRUGINFO D02WTN Hexanoic Acid (2,6-diphenylpyrimidin-4-yl)amide Investigative T92072 DRUGINFO D0R6MT isobutylmethylxanthine Investigative T92072 DRUGINFO D0Y2RM Isoguanosine Investigative T92072 DRUGINFO D0I3HE KF26777 Investigative T92072 DRUGINFO D0M8NW Kuanoniamine D Investigative T92072 DRUGINFO D0Y8SB L-249313 Investigative T92072 DRUGINFO D07DTC L-97-1 intravenous Investigative T92072 DRUGINFO D0P7CS LUF-5417 Investigative T92072 DRUGINFO D02VQK LUF-5433 Investigative T92072 DRUGINFO D0Z3YY LUF-5735 Investigative T92072 DRUGINFO D00WFU LUF-5737 Investigative T92072 DRUGINFO D0Z3BT LUF-5764 Investigative T92072 DRUGINFO D0B8RQ LUF-5767 Investigative T92072 DRUGINFO D0T7GG LUF-5816 Investigative T92072 DRUGINFO D06TSQ LUF5831 Investigative T92072 DRUGINFO D0H2VA LUF-5853 Investigative T92072 DRUGINFO D0LP5V LUF-5956 Investigative T92072 DRUGINFO D09IRV LUF-5957 Investigative T92072 DRUGINFO D0WI4D LUF-5962 Investigative T92072 DRUGINFO D05KEF LUF-5978 Investigative T92072 DRUGINFO D0W1PF LUF-5980 Investigative T92072 DRUGINFO D0Z8NC LUF-5981 Investigative T92072 DRUGINFO D0U8KW LUF-6258 Investigative T92072 DRUGINFO D0L0VU MRE 2029F20 Investigative T92072 DRUGINFO D0A6IO MRE 3008F20 Investigative T92072 DRUGINFO D02SKN MRS1041 Investigative T92072 DRUGINFO D0XC9U MRS1042 Investigative T92072 DRUGINFO D0G6SL MRS1062 Investigative T92072 DRUGINFO D09TBE MRS1065 Investigative T92072 DRUGINFO D0L3BI MRS1084 Investigative T92072 DRUGINFO D04RHI MRS1086 Investigative T92072 DRUGINFO D0B8DR MRS1093 Investigative T92072 DRUGINFO D04GFX MRS1132 Investigative T92072 DRUGINFO D0J1BA MRS1191 Investigative T92072 DRUGINFO D0ZL2A MRS1523 Investigative T92072 DRUGINFO D06KMJ MRS5151 Investigative T92072 DRUGINFO D07RSH MRS923 Investigative T92072 DRUGINFO D0I1EP MRS928 Investigative T92072 DRUGINFO D00JWA N-(2-(furan-2-yl)-3,4'-bipyridin-6-yl)acetamide Investigative T92072 DRUGINFO D0ZV1T N-(2,6-diphenylpyrimidin-4-yl)-2-ethylbutyramide Investigative T92072 DRUGINFO D08EZI N-(2,6-diphenylpyrimidin-4-yl)-3-methylbutyramide Investigative T92072 DRUGINFO D0Z3XC N-(2,6-diphenylpyrimidin-4-yl)acetamide Investigative T92072 DRUGINFO D02HZJ N-(2,6-diphenylpyrimidin-4-yl)benzamide Investigative T92072 DRUGINFO D08HBH N-(2,6-diphenylpyrimidin-4-yl)butyramide Investigative T92072 DRUGINFO D00GQI N-(2,6-diphenylpyrimidin-4-yl)isobutyramide Investigative T92072 DRUGINFO D02HYT N-(2,6-diphenylpyrimidin-4-yl)propionamide Investigative T92072 DRUGINFO D01WXR N-(4,5-diphenylpyrimidin-2-yl)acetamide Investigative T92072 DRUGINFO D0WN3O N-(4,6-diphenylpyrimidin-2-yl)-2-ethylbutyramide Investigative T92072 DRUGINFO D0N9WG N-(4,6-diphenylpyrimidin-2-yl)-3-chlorobenzamide Investigative T92072 DRUGINFO D0L4TY N-(4,6-diphenylpyrimidin-2-yl)-3-methylbutyramide Investigative T92072 DRUGINFO D0C3ID N-(4,6-diphenylpyrimidin-2-yl)benzamide Investigative T92072 DRUGINFO D01VXC N-(4,6-diphenylpyrimidin-2-yl)propionamide Investigative T92072 DRUGINFO D00JXL N-(4-Phenyl-thiazol-2-yl)-benzamide Investigative T92072 DRUGINFO D0B3NZ N-(5-Benzoyl-4-phenylthiazol-2-yl)benzamide Investigative T92072 DRUGINFO D02JCM N(6)-cyclohexyladenosine Investigative T92072 DRUGINFO D0Z3IZ N*6*-Cyclohexyl-N*2*-ethyl-9H-purine-2,6-diamine Investigative T92072 DRUGINFO D02EAO N*6*-Cyclohexyl-N*2*-phenyl-9H-purine-2,6-diamine Investigative T92072 DRUGINFO D0N2DP N*6*-Cyclooctyl-N*2*-phenyl-9H-purine-2,6-diamine Investigative T92072 DRUGINFO D0JJ6T N6-((+/-)-endo-norborn-2-yl)adenosine Investigative T92072 DRUGINFO D0I6MT N6-[(4-Amino)-phenyl]-9-benzyl-2-phenyladenine Investigative T92072 DRUGINFO D04MMG N6-[(4-Nitro)-phenyl]-9-benzyl-2-phenyladenine Investigative T92072 DRUGINFO D03RFA N6-CYCLOPENTYLADENOSINE Investigative T92072 DRUGINFO D0G5ZF N6-methoxy-2-[(2-pyridinyl)ethynyl]adenosine Investigative T92072 DRUGINFO D0Y6HQ N6-methoxy-2-[(3-pyridinyl)ethynyl]-adenosine Investigative T92072 DRUGINFO D0N1QO N6-methoxy-2-[(4-methoxyphenyl)ethynyl]adenosine Investigative T92072 DRUGINFO D0Q5HW N6-methoxy-2-[(4-methylphenyl)ethynyl]adenosine Investigative T92072 DRUGINFO D0B0QW N6-methoxy-2-[(4-pentylphenyl)ethynyl]adenosine Investigative T92072 DRUGINFO D03FVK N6-methoxy-2-[(4-pyridinyl)ethynyl]adenosine Investigative T92072 DRUGINFO D0Q3LM N6-methoxy-2-[2-(trimethylsilyl)ethynyl]adenosine Investigative T92072 DRUGINFO D03POP N6-methoxy-2-phenylethynyladenosine Investigative T92072 DRUGINFO D0PD0F Paeoniflorin Investigative T92072 DRUGINFO D07DNX PD-115199 Investigative T92072 DRUGINFO D07HXL PD-81723 Investigative T92072 DRUGINFO D0TC7N PENECA Investigative T92072 DRUGINFO D07DGH Pentanoic acid (4,6-diphenylpyrimidin-2-yl)amide Investigative T92072 DRUGINFO D04AGC Phenyl(2-(trifluoromethyl)quinolin-4-yl)methanol Investigative T92072 DRUGINFO D0BZ3S Phenyl-(9-phenyl-9H-purin-6-yl)-amine Investigative T92072 DRUGINFO D0L8SN P-IODOAMPHETAMINE Investigative T92072 DRUGINFO D05XGF PSB-0788 Investigative T92072 DRUGINFO D07PPM PSB-10 Investigative T92072 DRUGINFO D09RKX PSB-11 Investigative T92072 DRUGINFO D08FOT PSB-1115 Investigative T92072 DRUGINFO D00IOF PSB36 Investigative T92072 DRUGINFO D0A9BZ PSB-601 Investigative T92072 DRUGINFO D0Y5WQ PSB603 Investigative T92072 DRUGINFO D0M3CG R-N6-(phenylisopropyl)adenosine Investigative T92072 DRUGINFO D0B7OW sakuranetin Investigative T92072 DRUGINFO D0Y9WZ SB-298 Investigative T92072 DRUGINFO D0HK5B SCH-63390 Investigative T92072 DRUGINFO D0O0FP ST-1535 Investigative T92072 DRUGINFO D08BCH TCPA Investigative T92072 DRUGINFO D0Z7BC VCP-28 Investigative T92072 DRUGINFO D01AAI VUF5574 Investigative T92072 DRUGINFO D04PLH VUF-8507 Investigative T92072 DRUGINFO D0YV1R WRC-0571 Investigative T92072 DRUGINFO D0H9BP xanthine amine congener Investigative T92072 KEGGPATH hsa04022:cGMP-PKG signaling pathway T92072 KEGGPATH hsa04024:cAMP signaling pathway T92072 KEGGPATH hsa04071:Sphingolipid signaling pathway T92072 KEGGPATH hsa04080:Neuroactive ligand-receptor interaction T92072 KEGGPATH hsa05032:Morphine addiction T92072 WIKIPATH WP1824:GPCR downstream signaling T92072 WIKIPATH WP1825:GPCR ligand binding T92072 WIKIPATH WP455:GPCRs, Class A Rhodopsin-like T92072 WIKIPATH WP80:Nucleotide GPCRs T92072 REACPATH R-HSA-417973:Adenosine P1 receptors T92072 REACPATH R-HSA-418594:G alpha (i) signalling events T92072 NET_PATH NetPath_11:TCR Signaling Pathway T92072 NET_PATH NetPath_21:RANKL Signaling Pathway T92072 PANTPATH P00026:Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway T92072 PANTPATH P00027:Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway T74456 TARGETID T74456 T74456 FORMERID TTDS00267 T74456 UNIPROID AGTR1_HUMAN T74456 TARGNAME Angiotensin II receptor type-1 (AGTR1) T74456 GENENAME AGTR1 T74456 TARGTYPE Successful target T74456 SYNONYMS Type-1 angiotensin II receptor; Angiotensin II type-1 receptor; Angiotensin II receptor 1; Angiotensin 1 receptor; AT2R1B; AT2R1; AT1BR; AT1AR; AT1; AGTR1B; AGTR1A T74456 FUNCTION Mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Receptor for angiotensin II. T74456 PDBSTRUC 6DO1; 4ZUD; 4YAY; 1ZV0 T74456 BIOCLASS GPCR rhodopsin T74456 SEQUENCE MILNSSTEDGIKRIQDDCPKAGRHNYIFVMIPTLYSIIFVVGIFGNSLVVIVIYFYMKLKTVASVFLLNLALADLCFLLTLPLWAVYTAMEYRWPFGNYLCKIASASVSFNLYASVFLLTCLSIDRYLAIVHPMKSRLRRTMLVAKVTCIIIWLLAGLASLPAIIHRNVFFIENTNITVCAFHYESQNSTLPIGLGLTKNILGFLFPFLIILTSYTLIWKALKKAYEIQKNKPRNDDIFKIIMAIVLFFFFSWIPHQIFTFLDVLIQLGIIRDCRIADIVDTAMPITICIAYFNNCLNPLFYGFLGKKFKRYFLQLLKYIPPKAKSHSNLSTKMSTLSYRPSDNVSSSTKKPAPCFEVE T74456 DRUGINFO D0G6SE ANGIOTENSIN II Approved T74456 DRUGINFO D05FGG Azilsartan Approved T74456 DRUGINFO D0D5SQ Candesartan Approved T74456 DRUGINFO D0T7US Eprosartan Approved T74456 DRUGINFO D00NVX Forasartan Approved T74456 DRUGINFO D00JAU Irbesartan Approved T74456 DRUGINFO D0DD0K Losartan Approved T74456 DRUGINFO D0I7PO Micardis telmisartan Approved T74456 DRUGINFO D07UBG Olmesartan medoxomil Approved T74456 DRUGINFO D0B9AO Saprisartan Approved T74456 DRUGINFO D0K0AT SARALASIN Approved T74456 DRUGINFO D00VFE Saralasin Acetate Approved T74456 DRUGINFO D0M7TO Tasosartan Approved T74456 DRUGINFO D0N6RF Telmisartan Approved T74456 DRUGINFO D06UDG Valsartan Approved T74456 DRUGINFO D05FUU Pratosartan Phase 3 T74456 DRUGINFO D0H9QC S-474474 Phase 3 T74456 DRUGINFO D0YS1U sparsentan Phase 3 T74456 DRUGINFO D0A2RA TAK-491 Phase 3 T74456 DRUGINFO D02BBC CL-329167 Phase 2 T74456 DRUGINFO D06LRG TRV027 Phase 2 T74456 DRUGINFO D0C3BA YM-358 Phase 2 T74456 DRUGINFO D0J2NB KRH-594 Discontinued in Phase 2 T74456 DRUGINFO D0DL2S MILFASARTAN Discontinued in Phase 2 T74456 DRUGINFO D06TZT RIPISARTAN Discontinued in Phase 2 T74456 DRUGINFO D0E3XG Zolasartan Discontinued in Phase 2 T74456 DRUGINFO D0A8EG TAK-591 Discontinued in Phase 1 T74456 DRUGINFO D00XZP UR-7198 Discontinued in Phase 1 T74456 DRUGINFO D06MUI A-81988 Terminated T74456 DRUGINFO D00XTS CR-3834 Terminated T74456 DRUGINFO D0Q6YP HELENALIN Terminated T74456 DRUGINFO D0GS7N L-158809 Terminated T74456 DRUGINFO D00UBK L-159689 Terminated T74456 DRUGINFO D0Q7SO RS-66252 Terminated T74456 DRUGINFO D0N0JE UP-275-22 Terminated T74456 DRUGINFO D06EQN XR-510 Terminated T74456 DRUGINFO D0N7HN (E)-N-(3-iodoprop-2-enyl)-2beta-carbomethoxy-3beta-(4'-methylphenyl)n Investigative T74456 DRUGINFO D00TWV [125I]EXP985 Investigative T74456 DRUGINFO D07OOI [3H]GBR12935 Investigative T74456 DRUGINFO D0N2WA [Bpa1]AngII Investigative T74456 DRUGINFO D06PJZ [Sar1,Bpa2]AngII Investigative T74456 DRUGINFO D07EWK [Sar1,Bpa3]AngII Investigative T74456 DRUGINFO D0XO1T [Sar1,Bpa8]AngII Investigative T74456 DRUGINFO D0O1YO [Sar1,Tdf2]AngII Investigative T74456 DRUGINFO D06DRC [Sar1,Tdf3]AngII Investigative T74456 DRUGINFO D00LWG [Sar1,Tdf8]AngII Investigative T74456 DRUGINFO D0U7QE [Tdf1]AngII Investigative T74456 DRUGINFO D0T6WV 4-(2-Butyl-benzoimidazol-1-ylmethyl)-phenol Investigative T74456 DRUGINFO D0RE7T 4-[(diphenylmethyl)amino]-2-phenylquinazoline Investigative T74456 DRUGINFO D04FQA 4-hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketone Investigative T74456 DRUGINFO D0I9IB 5-butyl-methyl immidazole carboxylate 30 Investigative T74456 DRUGINFO D0L2HK 5-oxo-1-2-4-oxadiazol biphenyl Investigative T74456 DRUGINFO D0D9AS angiotensin III Investigative T74456 DRUGINFO D00DIJ CGP-49870 Investigative T74456 DRUGINFO D0OO4P CV-11194 Investigative T74456 DRUGINFO D0D1FT EXP3174 Investigative T74456 DRUGINFO D0T1YO GNF-PF-2307 Investigative T74456 DRUGINFO D0F3VE GNF-PF-2812 Investigative T74456 DRUGINFO D01YPD GNF-PF-3832 Investigative T74456 DRUGINFO D0I6HJ INC-106 Investigative T74456 DRUGINFO D04SVT L-159093 Investigative T74456 DRUGINFO D0A4NO L-162313 Investigative T74456 DRUGINFO D0Z7AF L-162782 Investigative T74456 DRUGINFO D0U3WW L-163,101 Investigative T74456 DRUGINFO D05EQC LY301875 Investigative T74456 DRUGINFO D0AD7P LY303336 Investigative T74456 DRUGINFO D0K0TY N,N`-bis-alkyl butylimmidazole 12b Investigative T74456 KEGGPATH hsa04020:Calcium signaling pathway T74456 KEGGPATH hsa04022:cGMP-PKG signaling pathway T74456 KEGGPATH hsa04080:Neuroactive ligand-receptor interaction T74456 KEGGPATH hsa04261:Adrenergic signaling in cardiomyocytes T74456 KEGGPATH hsa04270:Vascular smooth muscle contraction T74456 KEGGPATH hsa04614:Renin-angiotensin system T74456 KEGGPATH hsa04924:Renin secretion T74456 KEGGPATH hsa05200:Pathways in cancer T74456 WIKIPATH WP1824:GPCR downstream signaling T74456 WIKIPATH WP1825:GPCR ligand binding T74456 WIKIPATH WP2328:Allograft Rejection T74456 WIKIPATH WP24:Peptide GPCRs T74456 WIKIPATH WP2664:Gastrin-CREB signalling pathway via PKC and MAPK T74456 WIKIPATH WP455:GPCRs, Class A Rhodopsin-like T74456 WIKIPATH WP554:ACE Inhibitor Pathway T74456 WHIZPATH PW000563:Angiotensin Metabolism T74456 WHIZPATH PW000564:Muscle/Heart Contraction T74456 REACPATH R-HSA-375276:Peptide ligand-binding receptors T74456 REACPATH R-HSA-416476:G alpha (q) signalling events T74456 NET_PATH NetPath_7:TGF_beta_Receptor Signaling Pathway T74456 INTEPATH angiopoietinreceptor_pathway:Angiopoietin receptor Tie2-mediated signaling T74456 INTEPATH arf6_pathway:Arf6 signaling events T74456 INTEPATH arf6_traffickingpathway:Arf6 trafficking events T74456 PANTPATH P05911:Angiotensin II-stimulated signaling through G proteins and beta-arrestin T38301 TARGETID T38301 T38301 FORMERID TTDS00421 T38301 UNIPROID RIR2_HUMAN T38301 TARGNAME Ribonucleoside-diphosphate reductase M2 (RRM2) T38301 GENENAME RRM2 T38301 TARGTYPE Successful target T38301 SYNONYMS Ribonucleotide reductase small subunit; Ribonucleotide reductase small chain; Ribonucleoside-diphosphate reductase subunit M2; RR2 T38301 FUNCTION Catalyzes the biosynthesis of deoxyribonucleotides from the corresponding ribonucleotides. Inhibits Wnt signaling. Provides the precursors necessary for DNA synthesis. T38301 PDBSTRUC 3VPO; 3VPN; 3VPM; 3OLJ; 2UW2 T38301 BIOCLASS CH/CH(2) oxidoreductase T38301 ECNUMBER EC 1.17.4.1 T38301 SEQUENCE MLSLRVPLAPITDPQQLQLSPLKGLSLVDKENTPPALSGTRVLASKTARRIFQEPTEPKTKAAAPGVEDEPLLRENPRRFVIFPIEYHDIWQMYKKAEASFWTAEEVDLSKDIQHWESLKPEERYFISHVLAFFAASDGIVNENLVERFSQEVQITEARCFYGFQIAMENIHSEMYSLLIDTYIKDPKEREFLFNAIETMPCVKKKADWALRWIGDKEATYGERVVAFAAVEGIFFSGSFASIFWLKKRGLMPGLTFSNELISRDEGLHCDFACLMFKHLVHKPSEERVREIIINAVRIEQEFLTEALPVKLIGMNCTLMKQYIEFVADRLMLELGFSKVFRVENPFDFMENISLEGKTNFFEKRVGEYQRMGVMSSPTENSFTLDADF T38301 DRUGINFO D03UVS Gemcitabine Approved T38301 DRUGINFO D07CWD Hydroxyurea Approved T38301 DRUGINFO D0V0CJ CO-101 Phase 2 T38301 DRUGINFO D0DT1R Triapine Phase 2 T38301 DRUGINFO D0A1GR CALAA-01 Phase 1 T38301 DRUGINFO D0F2JY LY-2334737 Phase 1 T38301 DRUGINFO D05ACQ Gallium maltolate Discontinued in Phase 2 T38301 DRUGINFO D05HZI MDL 101,731 Discontinued in Phase 2 T38301 DRUGINFO D0V2RK NKP-46 Preclinical T38301 KEGGPATH hsa00230:Purine metabolism T38301 KEGGPATH hsa00240:Pyrimidine metabolism T38301 KEGGPATH hsa00480:Glutathione metabolism T38301 KEGGPATH hsa01100:Metabolic pathways T38301 KEGGPATH hsa04115:p53 signaling pathway T38301 WIKIPATH WP1601:Fluoropyrimidine Activity T38301 WIKIPATH WP1851:Metabolism of nucleotides T38301 WIKIPATH WP2446:Retinoblastoma (RB) in Cancer T38301 WIKIPATH WP404:Nucleotide Metabolism T38301 WHIZPATH PW000052:Purine Metabolism T38301 WHIZPATH PW000160:Pyrimidine Metabolism T38301 REACPATH R-HSA-113510:E2F mediated regulation of DNA replication T38301 REACPATH R-HSA-69205:G1/S-Specific Transcription T38301 NET_PATH NetPath_4:EGFR1 Signaling Pathway T38301 INTEPATH e2f_pathway:E2F transcription factor network T38301 PANTPATH P00059:p53 pathway T38301 PANTPATH P02738:De novo purine biosynthesis T38301 PANTPATH P02739:De novo pyrimidine deoxyribonucleotide biosynthesis T38301 BIOCPATH PWY66-409:Superpathway of purine nucleotide salvage T38301 BIOCPATH PWY-7184:Pyrimidine deoxyribonucleotides de novo biosynthesis T38301 BIOCPATH PWY-7210:Pyrimidine deoxyribonucleotides biosynthesis from CTP T38301 BIOCPATH PWY-7211:Superpathway of pyrimidine deoxyribonucleotides de novo biosynthesis T38301 BIOCPATH PWY-7226:Guanosine deoxyribonucleotides de novo biosynthesis T38301 BIOCPATH PWY-7227:Adenosine deoxyribonucleotides de novo biosynthesis T38301 BIOCPATH PWY-7228:Guanosine nucleotides de novo biosynthesis T38301 BIOCPATH PWY-841:Purine nucleotides de novo biosynthesis T05849 TARGETID T05849 T05849 FORMERID TTDS00043 T05849 UNIPROID GASR_HUMAN T05849 TARGNAME Gastrin/cholecystokinin type B receptor (CCKBR) T05849 GENENAME CCKBR T05849 TARGTYPE Successful target T05849 SYNONYMS Cholecystokinin-2 receptor; CCKRB; CCK2-R; CCK-BR; CCK-B receptor T05849 FUNCTION The CCK-B receptors occur throughout the central nervous system where they modulate anxiety, analgesia, arousal, and neuroleptic activity. This receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Receptor for gastrin and cholecystokinin. T05849 PDBSTRUC 1L4T T05849 BIOCLASS GPCR rhodopsin T05849 SEQUENCE MELLKLNRSVQGTGPGPGASLCRPGAPLLNSSSVGNLSCEPPRIRGAGTRELELAIRITLYAVIFLMSVGGNMLIIVVLGLSRRLRTVTNAFLLSLAVSDLLLAVACMPFTLLPNLMGTFIFGTVICKAVSYLMGVSVSVSTLSLVAIALERYSAICRPLQARVWQTRSHAARVIVATWLLSGLLMVPYPVYTVVQPVGPRVLQCVHRWPSARVRQTWSVLLLLLLFFIPGVVMAVAYGLISRELYLGLRFDGDSDSDSQSRVRNQGGLPGAVHQNGRCRPETGAVGEDSDGCYVQLPRSRPALELTALTAPGPGSGSRPTQAKLLAKKRVVRMLLVIVVLFFLCWLPVYSANTWRAFDGPGAHRALSGAPISFIHLLSYASACVNPLVYCFMHRRFRQACLETCARCCPRPPRARPRALPDEDPPTPSIASLSRLSYTTISTLGPG T05849 DRUGINFO D0Y9TS Ceruletide Approved T05849 DRUGINFO D0O5TQ Pentagastrin Approved T05849 DRUGINFO D09XUH GASTRAZOLE Phase 3 T05849 DRUGINFO D0TL7L Dexloxiglumide Phase 2 T05849 DRUGINFO D0K2RY Itriglumide Phase 2 T05849 DRUGINFO D0H5WM S-0509 Phase 2 T05849 DRUGINFO D04KHY Spiroglumide Phase 2 T05849 DRUGINFO D02FYE TT-223 Phase 2 T05849 DRUGINFO D0H7FW YF-476 Phase 2 T05849 DRUGINFO D02RPK Z 360 Phase 2 T05849 DRUGINFO D0QJ6L Demogastrin Phase 1 T05849 DRUGINFO D0X4AV GV-150013 Discontinued in Phase 2 T05849 DRUGINFO D0Z1RQ L-365260 Discontinued in Phase 2 T05849 DRUGINFO D0XJ0S PD-134308 Discontinued in Phase 2 T05849 DRUGINFO D07YHY CR-2093 Discontinued in Phase 1 T05849 DRUGINFO D0W4OZ GG-8573 Preclinical T05849 DRUGINFO D0E8QK JNJ-26070109 Preclinical T05849 DRUGINFO D06DPS PD-170292 Preclinical T05849 DRUGINFO D07SXO AG-041R Terminated T05849 DRUGINFO D01ZDR FR-208419 Terminated T05849 DRUGINFO D0EG1F GR-199114X Terminated T05849 DRUGINFO D05HGU IQM-95333 Terminated T05849 DRUGINFO D00UEG LY288513 Terminated T05849 DRUGINFO D0I3BT PD-135666 Terminated T05849 DRUGINFO D00COB PD136450 Terminated T05849 DRUGINFO D0W8TS SNF-9007 Terminated T05849 DRUGINFO D05HYL YM-022 Terminated T05849 DRUGINFO D0Z4SS [125I]-BDZ2 Investigative T05849 DRUGINFO D02ZWC [125I]PD142308 Investigative T05849 DRUGINFO D0F5WV [3H]JB-93182 Investigative T05849 DRUGINFO D0J0NS [3H]PBC-264 Investigative T05849 DRUGINFO D0IU6I [3H]PD140376 Investigative T05849 DRUGINFO D0T2RY 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Investigative T05849 DRUGINFO D0CE9U Asp-Tyr(OSO3H)-Met-Gly-Trp-Met-Asp-Phe Investigative T05849 DRUGINFO D0Z4HK BC-264 Investigative T05849 DRUGINFO D0M6ZF Boc-Asp-Tyr(So3-)-Nle-Gly-Trp-Asp-Phe-NH2 Investigative T05849 DRUGINFO D05OUQ CCK-33 Investigative T05849 DRUGINFO D0I8AF CCK-8 Investigative T05849 DRUGINFO D0A7RT Cholecystokinin-9 Investigative T05849 DRUGINFO D0C2KS CI-1015 Investigative T05849 DRUGINFO D02VGS desulfated cholecystokinin-8 Investigative T05849 DRUGINFO D02ZML GW-5823 Investigative T05849 DRUGINFO D0S7SO H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-Bo Investigative T05849 DRUGINFO D0V9DY H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-H Investigative T05849 DRUGINFO D0J7GJ H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-H Investigative T05849 DRUGINFO D03WGS H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Ac Investigative T05849 DRUGINFO D0N6DN H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Boc Investigative T05849 DRUGINFO D0L9RP PBC-264 Investigative T05849 DRUGINFO D0O0IZ PD-135118 Investigative T05849 DRUGINFO D0D2ZM PD-135158 Investigative T05849 DRUGINFO D04VOM PD-136621 Investigative T05849 DRUGINFO D0E4JX PD-137337 Investigative T05849 DRUGINFO D0G7RE PD-137342 Investigative T05849 DRUGINFO D02MIN PD-138915 Investigative T05849 DRUGINFO D0L9OU PD-138916 Investigative T05849 DRUGINFO D0A9EA PD-138917 Investigative T05849 DRUGINFO D00FLQ PD-140547 Investigative T05849 DRUGINFO D08EYZ PD-140548 Investigative T05849 DRUGINFO D0G1CK PD-140723 Investigative T05849 DRUGINFO D08VRJ PD-149164 Investigative T05849 DRUGINFO D09TNC RB-400 Investigative T05849 DRUGINFO D0U5NA RP-69758 Investigative T05849 DRUGINFO D0O0AR RP-71483 Investigative T05849 DRUGINFO D06WOQ RP-72540 Investigative T05849 DRUGINFO D0Y8KY RP73870 Investigative T05849 DRUGINFO D00UPU RPR-107836 Investigative T05849 DRUGINFO D05XXE Tetragastrin Investigative T05849 DRUGINFO D0R4TA tetronothiodin Investigative T05849 DRUGINFO D0ES2U TP-680 Investigative T05849 DRUGINFO D06BRA Tyr-D-Ala-Gly-D-Trp-Nle-Asp-Phe-NH2 Investigative T05849 DRUGINFO D07ICW Tyr-D-Ala-Gly-D-Trp-NMeNle-Asp-Phe-NH2 Investigative T05849 DRUGINFO D0QP2S Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-NMeNle-D-Trp-Boc Investigative T05849 DRUGINFO D0U6OA Tyr-D-Ala-Gly-Trp-Nle-Asp-Phe-NH2 Investigative T05849 DRUGINFO D0R4GI Tyr-D-Ala-Gly-Trp-NMeNle-Asp-Phe-NH2 Investigative T05849 DRUGINFO D0V0RB Tyr-D-Nle-Gly-D-Trp-Nle-Asp-Phe-NH2 Investigative T05849 DRUGINFO D0E2OG Tyr-D-Nle-Gly-D-Trp-NMeNle-Asp-Phe-NH2 Investigative T05849 DRUGINFO D07LQQ Tyr-D-Nle-Gly-Trp-Nle-Asp-Phe-NH2 Investigative T05849 DRUGINFO D08QKT Tyr-D-Nle-Gly-Trp-NMeNle-Asp-Phe-NH2 Investigative T05849 DRUGINFO D09EMR Tyr-D-Phe-Gly-D-Trp-Nle-Asp-Phe-NH2 Investigative T05849 DRUGINFO D0TR0U Tyr-D-Phe-Gly-D-Trp-NMeNle-Asp-Phe-NH2 Investigative T05849 DRUGINFO D03EPA Tyr-D-Phe-Gly-Trp-Nle-Asp-Phe-NH2 Investigative T05849 DRUGINFO D01AQC Tyr-D-Phe-Gly-Trp-NMeNle-Asp-Phe-NH2 Investigative T05849 DRUGINFO D01ADK Tyr-D-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2 Investigative T05849 DRUGINFO D0X7LC Tyr-Gly-Gly-Trp-NMeNle-Asp-Phe-NH2 Investigative T05849 DRUGINFO D06NIP Tyr-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2 Investigative T05849 KEGGPATH hsa04020:Calcium signaling pathway T05849 KEGGPATH hsa04080:Neuroactive ligand-receptor interaction T05849 KEGGPATH hsa04971:Gastric acid secretion T05849 WIKIPATH WP117:GPCRs, Other T05849 WIKIPATH WP1824:GPCR downstream signaling T05849 WIKIPATH WP1825:GPCR ligand binding T05849 WIKIPATH WP24:Peptide GPCRs T05849 WIKIPATH WP2597:Secretion of Hydrochloric Acid in Parietal Cells T05849 WIKIPATH WP2664:Gastrin-CREB signalling pathway via PKC and MAPK T05849 WIKIPATH WP455:GPCRs, Class A Rhodopsin-like T05849 WHIZPATH PW000565:Gastric Acid Production T05849 REACPATH R-HSA-375276:Peptide ligand-binding receptors T05849 REACPATH R-HSA-416476:G alpha (q) signalling events T05849 REACPATH R-HSA-881907:Gastrin-CREB signalling pathway via PKC and MAPK T05849 PANTPATH P06959:CCKR signaling map ST T72458 TARGETID T72458 T72458 FORMERID TTDC00072 T72458 UNIPROID MC4R_HUMAN T72458 TARGNAME Melanocortin receptor 4 (MC4R) T72458 GENENAME MC4R T72458 TARGTYPE Successful target T72458 SYNONYMS MC4-R T72458 FUNCTION Plays a central role in energy homeostasis and somatic growth. This receptor is mediated by G proteins that stimulate adenylate cyclase (cAMP). Receptor specific to the heptapeptide core common to adrenocorticotropic hormone and alpha-, beta-, and gamma-MSH. T72458 PDBSTRUC 2IQW; 2IQV; 2IQU; 2IQS; 2IQR T72458 BIOCLASS GPCR rhodopsin T72458 SEQUENCE MVNSTHRGMHTSLHLWNRSSYRLHSNASESLGKGYSDGGCYEQLFVSPEVFVTLGVISLLENILVIVAIAKNKNLHSPMYFFICSLAVADMLVSVSNGSETIVITLLNSTDTDAQSFTVNIDNVIDSVICSSLLASICSLLSIAVDRYFTIFYALQYHNIMTVKRVGIIISCIWAACTVSGILFIIYSDSSAVIICLITMFFTMLALMASLYVHMFLMARLHIKRIAVLPGTGAIRQGANMKGAITLTILIGVFVVCWAPFFLHLIFYISCPQNPYCVCFMSHFNLYLILIMCNSIIDPLIYALRSQELRKTFKEIICCYPLGGLCDLSSRY T72458 DRUGINFO D0X9PF Bremelanotide Approved T72458 DRUGINFO D03YVO Methylnaltrexone bromide Approved T72458 DRUGINFO D0YP7B Setmelanotide Approved T72458 DRUGINFO D0PI8W Amylin Phase 4 T72458 DRUGINFO D0K8NR AMG 386 Phase 3 T72458 DRUGINFO D04QUX PF-446687 Phase 2 T72458 DRUGINFO D0G2XE PMX-53 Phase 2 T72458 DRUGINFO D0H3HV AP-1030 Phase 1/2 T72458 DRUGINFO D09XVQ PT-14 Discontinued in Phase 2 T72458 DRUGINFO D0J9CF IDDBCP-150101 Preclinical T72458 DRUGINFO D06SDP Melanotetan II Preclinical T72458 DRUGINFO D0N0IQ Ro-27-3225 Preclinical T72458 DRUGINFO D0D8YP 1-Benzyl-4-methyl-piperazine Investigative T72458 DRUGINFO D00XMP 1-Methyl-4-(1-phenyl-ethyl)-piperazine Investigative T72458 DRUGINFO D0T2RY 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Investigative T72458 DRUGINFO D0A8ME Ac-[CEHdFRWC]-NH2 Investigative T72458 DRUGINFO D07DWH Ac-dR[CEHdFRWC]-NH2 Investigative T72458 DRUGINFO D0B8GR Ac-His-D-Phe-Arg-2-Nal-NHCH3 Investigative T72458 DRUGINFO D0U5KM Ac-His-DPhe-Arg-Trp-NH2 Investigative T72458 DRUGINFO D0U6XP Ac-Nle-c[Asp-His-DNaI(2')-Pro-Trp-Lys]-NH2 Investigative T72458 DRUGINFO D0CK0K Ac-Nle-c[Asp-His-DNal(2')-Pro-Trp-Lys]-NH2 Investigative T72458 DRUGINFO D0N6AS AC-Nle-c[Asp-His-DPhe-Pro-Trp-Lys]-NH2 Investigative T72458 DRUGINFO D05XRI Ac-R[CEHdFRWC]-NH2 Investigative T72458 DRUGINFO D0F6GX Ac-Tyr-D-Phe-Arg-2-Nal-NHCH3 Investigative T72458 DRUGINFO D0ZD3M Ac-YCit[CEHdFRWC]-NH2 Investigative T72458 DRUGINFO D09OMI Ac-YK[CEHdFRWC]-NH2 Investigative T72458 DRUGINFO D07IBF Ac-YR[CE(1-Me-H)dFRWC]-NH2 Investigative T72458 DRUGINFO D07TBR Ac-YR[CEH(d-2alpha-Nal)RWC]-NH2 Investigative T72458 DRUGINFO D0R0BY Ac-YR[CEH(pCl-dF)RWC]-NH2 Investigative T72458 DRUGINFO D0WG8P Ac-YR[CEH(pF-dF)RWC]-NH2 Investigative T72458 DRUGINFO D00VYC Ac-YR[CEHdFRWC]-NH2 Investigative T72458 DRUGINFO D0C7VI Ac-YR[CEHdFRWC]SPPKD-NH2 Investigative T72458 DRUGINFO D09XCH Ac-YR[CEHFRWC]-NH2 Investigative T72458 DRUGINFO D0X1YL Ac-YRC(Me)*EHdFRWC(Me)NH2 Investigative T72458 DRUGINFO D03AZC Ac-YRMEHdFRWG-NH2 Investigative T72458 DRUGINFO D0B4OL Ac-YRMEHdFRWGSPPKD-NH2 Investigative T72458 DRUGINFO D0AU4C AEKKDEGPYRMEHFRWGSPPKD Investigative T72458 DRUGINFO D02TOS AMSH Investigative T72458 DRUGINFO D08QRO BL-6020 Investigative T72458 DRUGINFO D0U1UZ C(his-D-phe-arg-trp-Abu) Investigative T72458 DRUGINFO D0M2QK C(his-D-phe-arg-trp-Ahp) Investigative T72458 DRUGINFO D0R5KO C(his-D-phe-arg-trp-Ahx) Investigative T72458 DRUGINFO D09LHF C(his-D-phe-arg-trp-Aoc) Investigative T72458 DRUGINFO D0V5YV C(his-L-phe-arg-trp-Aoc) Investigative T72458 DRUGINFO D0WI8M C[CO-(CH2)2-CO-Nle-D-Nal(2)-Arg-Trp-Lys]-NH2 Investigative T72458 DRUGINFO D08DND C[CO-(CH2)2-CO-Nle-D-Phe-Arg-Trp-Lys]-NH2 Investigative T72458 DRUGINFO D04YZZ C[CO-(CH2)3-CO-Pro-D-Nal(2)-Arg-Trp-Lys]-NH2 Investigative T72458 DRUGINFO D09PDT C[CO-o-C6H4-CO-Pro-D-Nal(2)-Arg-Trp-Lys]-NH2 Investigative T72458 DRUGINFO D0QW4A C[CO-o-C6H4-CO-Pro-D-Phe-Arg-Trp-Lys]-NH2 Investigative T72458 DRUGINFO D02JVA C[Nle-Arg-D-Nal(2')-Arg-Trp-Glu]-NH2 Investigative T72458 DRUGINFO D07SFD C[Nle-Arg-D-Phe-Arg-Trp-Glu]-NH2 Investigative T72458 DRUGINFO D07UXW C[Nle-Asp-D-Nal(2')-Arg-Trp-Glu]-NH2 Investigative T72458 DRUGINFO D04BOG C[Nle-Asp-D-Phe-Arg-Trp-Glu]-NH2 Investigative T72458 DRUGINFO D05LLI C[Nle-Gln-D-Nal(2')-Arg-Trp-Glu]-NH2 Investigative T72458 DRUGINFO D05WNC C[Nle-Glu-D-Nal(2')-Arg-Trp-Glu]-NH2 Investigative T72458 DRUGINFO D00TSX C[Nle-His-D-Nal(2')-Arg-Trp-Glu]-NH2 Investigative T72458 DRUGINFO D02MPZ C[Nle-His-D-Phe-Arg-Trp-Glu]-NH2 Investigative T72458 DRUGINFO D0L1MJ C[Nle-Nle-D-Nal(2')-Arg-Trp-Glu]-NH2 Investigative T72458 DRUGINFO D01HTX C[Nle-Nle-D-Phe-Arg-Trp-Glu]-NH2 Investigative T72458 DRUGINFO D0P4GI C[Nle-Pro-D-Nal(2')-Arg-Trp-Glu]-NH2 Investigative T72458 DRUGINFO D0VD7R C[Nle-Pro-D-Phe-Arg-Trp-Glu]-NH2 Investigative T72458 DRUGINFO D06RTP C[Nle-Val-D-Nal(2')-Arg-Trp-Glu]-NH2 Investigative T72458 DRUGINFO D0M4EF C[Nle-Val-D-Phe-Arg-Trp-Glu]-NH2 Investigative T72458 DRUGINFO D08EBV C[Ser-Tyr-Thr-His-Dphe-Arg-Trp-Thr-Ile-Pro] Investigative T72458 DRUGINFO D07RRN C[Thr-Tyr-Thr-His-DNaf-Arg-Trp-Thr-Ile-Pro] Investigative T72458 DRUGINFO D0R3GC D-Phe-Arg-2-Nal-NHCH3 Investigative T72458 DRUGINFO D0ID5M GPYRMEHFRWGSPPKD-NH2 Investigative T72458 DRUGINFO D07SRW His-DPhe-Arg-Trp Investigative T72458 DRUGINFO D00HAJ Hoo-Phe-Orn-Pro-hle-Pff-Phe-NH2 Investigative T72458 DRUGINFO D0J0ZG HS014 Investigative T72458 DRUGINFO D00GCC MCL0129 Investigative T72458 DRUGINFO D0Z1QU MCL-129 Investigative T72458 DRUGINFO D0D1BC Melanocortin-4 Receptor antagonist Investigative T72458 DRUGINFO D09UUC MK-10 Investigative T72458 DRUGINFO D00NOG MK-11 Investigative T72458 DRUGINFO D09HHW ML-253764 Investigative T72458 DRUGINFO D0YB7F MT-II Investigative T72458 DRUGINFO D0GH5N NDP-alpha-MSH Investigative T72458 DRUGINFO D0I8SJ NDP-SYSMEHFRWGKPVG Investigative T72458 DRUGINFO D0D7ZA Ser-Tyr-Ser-Nle-Glu-His-Dphe-Arg Investigative T72458 DRUGINFO D0N6KO THIQ Investigative T72458 DRUGINFO D06PNU Tic-D-Phe-Arg-2-Nal-NHCH3 Investigative T72458 KEGGPATH hsa04080:Neuroactive ligand-receptor interaction T72458 WIKIPATH WP1824:GPCR downstream signaling T72458 WIKIPATH WP1825:GPCR ligand binding T72458 WIKIPATH WP24:Peptide GPCRs T72458 WIKIPATH WP455:GPCRs, Class A Rhodopsin-like T72458 REACPATH R-HSA-375276:Peptide ligand-binding receptors T72458 REACPATH R-HSA-418555:G alpha (s) signalling events T72458 INTEPATH syndecan_3_pathway:Syndecan-3-mediated signaling events T11288 TARGETID T11288 T11288 FORMERID TTDS00288 T11288 UNIPROID MRP1_HUMAN T11288 TARGNAME Multidrug resistance-associated protein 1 (ABCC1) T11288 GENENAME ABCC1 T11288 TARGTYPE Successful target T11288 SYNONYMS MRP1; MRP; Leukotriene C(4) transporter; LTC4 transporter; ATP-binding cassette sub-family C member 1 T11288 FUNCTION Mediates ATP-dependent transport of glutathione and glutathione conjugates, leukotriene C4, estradiol-17-beta-o-glucuronide, methotrexate, antiviral drugs and other xenobiotics. Confers resistance to anticancer drugs. Hydrolyzes ATP with low efficiency. Mediates export of organic anions and drugs from the cytoplasm. T11288 PDBSTRUC 4C3Z; 2CBZ T11288 BIOCLASS ABC transporter T11288 ECNUMBER EC 7.6.2.2 T11288 SEQUENCE MALRGFCSADGSDPLWDWNVTWNTSNPDFTKCFQNTVLVWVPCFYLWACFPFYFLYLSRHDRGYIQMTPLNKTKTALGFLLWIVCWADLFYSFWERSRGIFLAPVFLVSPTLLGITMLLATFLIQLERRKGVQSSGIMLTFWLVALVCALAILRSKIMTALKEDAQVDLFRDITFYVYFSLLLIQLVLSCFSDRSPLFSETIHDPNPCPESSASFLSRITFWWITGLIVRGYRQPLEGSDLWSLNKEDTSEQVVPVLVKNWKKECAKTRKQPVKVVYSSKDPAQPKESSKVDANEEVEALIVKSPQKEWNPSLFKVLYKTFGPYFLMSFFFKAIHDLMMFSGPQILKLLIKFVNDTKAPDWQGYFYTVLLFVTACLQTLVLHQYFHICFVSGMRIKTAVIGAVYRKALVITNSARKSSTVGEIVNLMSVDAQRFMDLATYINMIWSAPLQVILALYLLWLNLGPSVLAGVAVMVLMVPVNAVMAMKTKTYQVAHMKSKDNRIKLMNEILNGIKVLKLYAWELAFKDKVLAIRQEELKVLKKSAYLSAVGTFTWVCTPFLVALCTFAVYVTIDENNILDAQTAFVSLALFNILRFPLNILPMVISSIVQASVSLKRLRIFLSHEELEPDSIERRPVKDGGGTNSITVRNATFTWARSDPPTLNGITFSIPEGALVAVVGQVGCGKSSLLSALLAEMDKVEGHVAIKGSVAYVPQQAWIQNDSLRENILFGCQLEEPYYRSVIQACALLPDLEILPSGDRTEIGEKGVNLSGGQKQRVSLARAVYSNADIYLFDDPLSAVDAHVGKHIFENVIGPKGMLKNKTRILVTHSMSYLPQVDVIIVMSGGKISEMGSYQELLARDGAFAEFLRTYASTEQEQDAEENGVTGVSGPGKEAKQMENGMLVTDSAGKQLQRQLSSSSSYSGDISRHHNSTAELQKAEAKKEETWKLMEADKAQTGQVKLSVYWDYMKAIGLFISFLSIFLFMCNHVSALASNYWLSLWTDDPIVNGTQEHTKVRLSVYGALGISQGIAVFGYSMAVSIGGILASRCLHVDLLHSILRSPMSFFERTPSGNLVNRFSKELDTVDSMIPEVIKMFMGSLFNVIGACIVILLATPIAAIIIPPLGLIYFFVQRFYVASSRQLKRLESVSRSPVYSHFNETLLGVSVIRAFEEQERFIHQSDLKVDENQKAYYPSIVANRWLAVRLECVGNCIVLFAALFAVISRHSLSAGLVGLSVSYSLQVTTYLNWLVRMSSEMETNIVAVERLKEYSETEKEAPWQIQETAPPSSWPQVGRVEFRNYCLRYREDLDFVLRHINVTINGGEKVGIVGRTGAGKSSLTLGLFRINESAEGEIIIDGINIAKIGLHDLRFKITIIPQDPVLFSGSLRMNLDPFSQYSDEEVWTSLELAHLKDFVSALPDKLDHECAEGGENLSVGQRQLVCLARALLRKTKILVLDEATAAVDLETDDLIQSTIRTQFEDCTVLTIAHRLNTIMDYTRVIVLDKGEIQEYGAPSDLLQQRGLFYSMAKDAGLV T11288 DRUGINFO D0Z3DY Benzbromarone Approved T11288 DRUGINFO D03DEI Sulfinpyrazone Approved T11288 DRUGINFO D0KX3H Pyrrolopyrimidine Investigative T11288 DRUGINFO D04GYT XR-9456 Investigative T11288 DRUGINFO D09HIM XR-9504 Investigative T11288 DRUGINFO D0A4TF XR-9544 Investigative T11288 DRUGINFO D0S8CE XR-9577 Investigative T11288 KEGGPATH hsa02010:ABC transporters T11288 KEGGPATH hsa04071:Sphingolipid signaling pathway T11288 KEGGPATH hsa04977:Vitamin digestion and absorption T11288 KEGGPATH hsa05206:MicroRNAs in cancer T11288 WIKIPATH WP1857:Metabolism of water-soluble vitamins and cofactors T11288 WIKIPATH WP229:Irinotecan Pathway T11288 WIKIPATH WP2650:Arachidonic acid metabolism T11288 REACPATH R-HSA-196741:Cobalamin (Cbl, vitamin B12) transport and metabolism T11288 REACPATH R-HSA-382556:ABC-family proteins mediated transport T11288 NET_PATH NetPath_18:IL6 Signaling Pathway T11288 INTEPATH s1p_meta_pathway:Sphingosine 1-phosphate (S1P) pathway T11288 INTEPATH s1p_s1p1_pathway:S1P1 pathway T37693 TARGETID T37693 T37693 FORMERID TTDC00314 T37693 UNIPROID CNR2_HUMAN T37693 TARGNAME Cannabinoid receptor 2 (CB2) T37693 GENENAME CNR2 T37693 TARGTYPE Successful target T37693 SYNONYMS hCB2; Cannabinoid CB2 receptor; CX5; CB2B; CB2A; CB-2 T37693 FUNCTION May function in inflammatory response, nociceptive transmission and bone homeostasis. Heterotrimeric G protein-coupled receptor for endocannabinoid 2-arachidonoylglycerol mediating inhibition of adenylate cyclase. T37693 PDBSTRUC 5ZTY; 2KI9 T37693 BIOCLASS GPCR rhodopsin T37693 SEQUENCE MEECWVTEIANGSKDGLDSNPMKDYMILSGPQKTAVAVLCTLLGLLSALENVAVLYLILSSHQLRRKPSYLFIGSLAGADFLASVVFACSFVNFHVFHGVDSKAVFLLKIGSVTMTFTASVGSLLLTAIDRYLCLRYPPSYKALLTRGRALVTLGIMWVLSALVSYLPLMGWTCCPRPCSELFPLIPNDYLLSWLLFIAFLFSGIIYTYGHVLWKAHQHVASLSGHQDRQVPGMARMRLDVRLAKTLGLVLAVLLICWFPVLALMAHSLATTLSDQVKKAFAFCSMLCLINSMVNPVIYALRSGEIRSSAHHCLAHWKKCVRGLGSEAKEEAPRSSVTETEADGKITPWPDSRDLDLSDC T37693 DRUGINFO D07ILQ Guanfacine extended release Approved T37693 DRUGINFO D0L7AS NABILONE Approved T37693 DRUGINFO D0Q7NB 842166X Phase 2 T37693 DRUGINFO D0I4PW APD371 Phase 2 T37693 DRUGINFO D53QMP Beta-caryophyllene Phase 2 T37693 DRUGINFO D05BMC GW-42004 Phase 2 T37693 DRUGINFO D00FBC KHK-6188 Phase 2 T37693 DRUGINFO D06UIS LY-2828360 Phase 2 T37693 DRUGINFO D0J6KZ S-777469 Phase 2 T37693 DRUGINFO D0Q8WG Tedalinab Phase 1 T37693 DRUGINFO D0HG0F 1,3,5-triazine derivative 1 Patented T37693 DRUGINFO D05CEL 2-cycloalkyl resorcinol cannabinoid ligand derivative 1 Patented T37693 DRUGINFO D0H0XC 2-cycloalkyl resorcinol cannabinoid ligand derivative 2 Patented T37693 DRUGINFO D0T9OL Adamantyl derivative 1 Patented T37693 DRUGINFO D0GQ8W Carbazole-3-carboxamide analog 1 Patented T37693 DRUGINFO D0LN9D Cyano(dimethyl)methyl isoxazoles and [1,3,4]-thiadiazoles derivative 1 Patented T37693 DRUGINFO D0X5ZS Cyano(dimethyl)methyl isoxazoles and [1,3,4]-thiadiazoles derivative 2 Patented T37693 DRUGINFO D0TC7X Isoquinoline derivative 1 Patented T37693 DRUGINFO D0D1TS Isoquinoline derivative 2 Patented T37693 DRUGINFO D0ZM1H Isoquinoline derivative 3 Patented T37693 DRUGINFO D0YZ8I JWH-015 Patented T37693 DRUGINFO D07IHT N,N-methylenebis-2-phenylacetamide and benzenesulfonamide derivative 1 Patented T37693 DRUGINFO D0WJ3F N,N-methylenebis-2-phenylacetamide and benzenesulfonamide derivative 2 Patented T37693 DRUGINFO D0FA2L N,N-methylenebis-2-phenylacetamide and benzenesulfonamide derivative 3 Patented T37693 DRUGINFO D0RZ4M Phytocannabinoid/aminoalkylindole derivative 1 Patented T37693 DRUGINFO D09WPA Phytocannabinoid/aminoalkylindole derivative 2 Patented T37693 DRUGINFO D0EX1T PMID27215781-Compound-11 Patented T37693 DRUGINFO D0Q9TO PMID27215781-Compound-12 Patented T37693 DRUGINFO D0O2TY PMID27215781-Compound-13 Patented T37693 DRUGINFO D0SR5L PMID27215781-Compound-19 Patented T37693 DRUGINFO D0W9PY PMID27215781-Compound-2 Patented T37693 DRUGINFO D07ULI PMID27215781-Compound-25 Patented T37693 DRUGINFO D0E6YT PMID27215781-Compound-27 Patented T37693 DRUGINFO D03YAA PMID27215781-Compound-28 Patented T37693 DRUGINFO D0XG7K PMID27215781-Compound-29 Patented T37693 DRUGINFO D03YWY PMID27215781-Compound-30 Patented T37693 DRUGINFO D0CR0Y PMID27215781-Compound-31 Patented T37693 DRUGINFO D01PUS PMID27215781-Compound-32 Patented T37693 DRUGINFO D0OE0D PMID27215781-Compound-33 Patented T37693 DRUGINFO D00TIB PMID27215781-Compound-34 Patented T37693 DRUGINFO D07BFP PMID27215781-Compound-37 Patented T37693 DRUGINFO D08XES PMID27215781-Compound-4 Patented T37693 DRUGINFO D09GJQ Tricyclic phytocannabinoid derivative 1 Patented T37693 DRUGINFO D02TOI Tricyclic phytocannabinoid derivative 2 Patented T37693 DRUGINFO D0LF5B KN-38-7271 Discontinued in Phase 2 T37693 DRUGINFO D03ACT PRS-211375 iv Discontinued in Phase 2 T37693 DRUGINFO D03KTK TAK-937 Discontinued in Phase 1 T37693 DRUGINFO D07XGT AM-577 Terminated T37693 DRUGINFO D0A4XN PRS-639058 Terminated T37693 DRUGINFO D01DTQ PXS-2076 Terminated T37693 DRUGINFO D0J7RW WIN-55212-2 Terminated T37693 DRUGINFO D03HFM (1R,2R)-N-Arachidonoylcyclopropanolamide Investigative T37693 DRUGINFO D0R7QF (1R,2S)-N-Arachidonoylcyclopropanolamide Investigative T37693 DRUGINFO D0Q0XV (1R,2S)-N-Oleoylcyclopropanolamide Investigative T37693 DRUGINFO D0G2EQ (1S,2S)-N-Arachidonoylcyclopropanolamide Investigative T37693 DRUGINFO D0K7QP (1S,2S)-N-Oleoylcyclopropanolamide Investigative T37693 DRUGINFO D01MCD (2R)-N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-2-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX) Investigative T37693 DRUGINFO D01PEC (2R)-N-(7'-(2-CHLOROPHENYL)-6'-(4-CHLOROPHENYL)-3',4'-DIHYDROSPIRO[CYCLOHEXANE-1,2'-PYRANO[2,3-B]PYRIDINE]-4'-YL)-2-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX) Investigative T37693 DRUGINFO D06DTC (2S)-N-(7'-(2-CHLOROPHENYL)-6'-(4-CHLOROPHENYL)-3',4'-DIHYDROSPIRO[CYCLOHEXANE-1,2'-PYRANO[2,3-B]PYRIDINE]-4'-YL)-2-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX) Investigative T37693 DRUGINFO D01VIA (4-benzhydrylpiperazin-1-yl)(cyclohexyl)methanone Investigative T37693 DRUGINFO D0Z7OB (E)-N-(3,5-dimethoxyphenethyl)undec-2-enamide Investigative T37693 DRUGINFO D0T4SE (E)-N-(4-methoxyphenethyl)undec-2-enamide Investigative T37693 DRUGINFO D08BNY (E)-N-(4-methoxyphenyl)undec-2-enamide Investigative T37693 DRUGINFO D0D6OH [3H]CP55940 Investigative T37693 DRUGINFO D0K8VR [3H]HU-243 Investigative T37693 DRUGINFO D06BXT [3H]WIN55212-2 Investigative T37693 DRUGINFO D0V7QA 1,4-dihydroindeno[1,2-c]-pyrazole Investigative T37693 DRUGINFO D04XGX 2-(2-Methoxybenzyl)-3H-benzo[f]chromen-3-one Investigative T37693 DRUGINFO D01JHA 2'-amino-4-(1,1-dimethyl-heptyl)-biphenyl-2-ol Investigative T37693 DRUGINFO D0V3YB 3,4-diarylpyrazoline derivative Investigative T37693 DRUGINFO D0G7GF 3'-amino-4-(1,1-dimethyl-heptyl)-biphenyl-2-ol Investigative T37693 DRUGINFO D08JFL 3-benzoyl-1-pentyl-1,4-dihydroquinolin-4-one Investigative T37693 DRUGINFO D01RWS 3-Benzyl-5-isopropyl-8-methylchromen-2-one Investigative T37693 DRUGINFO D08VLG 4-(1,1-dimethyl-heptyl)-2'-methoxy-biphenyl-2-ol Investigative T37693 DRUGINFO D0U3ME 4'-(1,1-dimethyl-heptyl)-3,5-dimethyl-biphenyl Investigative T37693 DRUGINFO D08OAQ 4-(1,1-dimethyl-heptyl)-3'-methoxy-biphenyl-2-ol Investigative T37693 DRUGINFO D08GLU 4'-amino-4-(1,1-dimethyl-heptyl)-biphenyl-2-ol Investigative T37693 DRUGINFO D0N0ME 4-benzhydryl-N-butylpiperazine-1-carboxamide Investigative T37693 DRUGINFO D04ICJ 4-benzhydryl-N-cyclohexylpiperazine-1-carboxamide Investigative T37693 DRUGINFO D02POA 5-(1,1-dimethyl-heptyl)-2-pyridin-3-yl-phenol Investigative T37693 DRUGINFO D03SCD 5-Biphenyl-4-ylmethyl-1-isobutyl-1H-tetrazole Investigative T37693 DRUGINFO D0K8MN 5-Biphenyl-4-ylmethyl-2-isobutyl-2H-tetrazole Investigative T37693 DRUGINFO D03REA 5-Methoxy-3-(2-methoxybenzyl)-2H-chromen-2-one Investigative T37693 DRUGINFO D0R6MB 6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX) Investigative T37693 DRUGINFO D0K4PV 6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-N-((R)-1-HYDROXYETHYL)-1,2,2-TRIMETHYL-1,2,3,4-TETRAHYDRO-1,8-NAPHTHYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX) Investigative T37693 DRUGINFO D0R9VY 6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-N-(1-HYDROXY-2-METHYLPROPAN-2-YL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX) Investigative T37693 DRUGINFO D0OQ5H 6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-N-(HYDROXYMETHYL)-1,2,2-TRIMETHYL-1,2,3,4-TETRAHYDRO-1,8-NAPHTHYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX) Investigative T37693 DRUGINFO D08TXL A-796260 Investigative T37693 DRUGINFO D0O3NY AM-1241 Investigative T37693 DRUGINFO D04AUM AM-1710 Investigative T37693 DRUGINFO D0E3ET AM-1714 Investigative T37693 DRUGINFO D03GDP AM-1715 Investigative T37693 DRUGINFO D0UD9H AM-281 Investigative T37693 DRUGINFO D02GOH AM-404 Investigative T37693 DRUGINFO D09CKZ AM-411 Investigative T37693 DRUGINFO D03AWH AM-4768 Investigative T37693 DRUGINFO D09FMK AM-630 Investigative T37693 DRUGINFO D02GTT AR-XYZ Investigative T37693 DRUGINFO D0Z1NH Cis-N-oleoylcyclopropanolamide Investigative T37693 DRUGINFO D04GDY DELTA 8-TETRAHYDROCANNOBINOL Investigative T37693 DRUGINFO D0EC6B Dodeca-2E,4E-dienoic acid isobutylamide Investigative T37693 DRUGINFO D0R1UA GNF-PF-5188 Investigative T37693 DRUGINFO D0UX4A HU-433 Investigative T37693 DRUGINFO D09DSK JWH-051 Investigative T37693 DRUGINFO D0O7ZJ JWH-120 Investigative T37693 DRUGINFO D02VSL JWH-133 Investigative T37693 DRUGINFO D0S3UA JWH-145 Investigative T37693 DRUGINFO D0TN1L JWH-146 Investigative T37693 DRUGINFO D0S2ZR JWH-147 Investigative T37693 DRUGINFO D0GG4T JWH-150 Investigative T37693 DRUGINFO D0F3CH JWH-151 Investigative T37693 DRUGINFO D03RGV JWH-156 Investigative T37693 DRUGINFO D05EWD JWH-167 Investigative T37693 DRUGINFO D00TPO JWH-201 Investigative T37693 DRUGINFO D0P6NA JWH-202 Investigative T37693 DRUGINFO D0M1MQ JWH-203 Investigative T37693 DRUGINFO D08JCV JWH-204 Investigative T37693 DRUGINFO D0WD1F JWH-205 Investigative T37693 DRUGINFO D0X0FB JWH-206 Investigative T37693 DRUGINFO D0GD9G JWH-207 Investigative T37693 DRUGINFO D0Q8SO JWH-208 Investigative T37693 DRUGINFO D0YM8O JWH-209 Investigative T37693 DRUGINFO D09KFJ JWH-229 Investigative T37693 DRUGINFO D0Q4IM JWH-237 Investigative T37693 DRUGINFO D0Z6BY JWH-243 Investigative T37693 DRUGINFO D0I7MW JWH-244 Investigative T37693 DRUGINFO D0TS5I JWH-245 Investigative T37693 DRUGINFO D0Z7FF JWH-246 Investigative T37693 DRUGINFO D0X1EC JWH-248 Investigative T37693 DRUGINFO D0Q6FF JWH-249 Investigative T37693 DRUGINFO D0D4HH JWH-250 Investigative T37693 DRUGINFO D05DXW JWH-251 Investigative T37693 DRUGINFO D0P9KU JWH-252 Investigative T37693 DRUGINFO D01IUI JWH-253 Investigative T37693 DRUGINFO D06EHU JWH-268 Investigative T37693 DRUGINFO D03SRV JWH-292 Investigative T37693 DRUGINFO D0T5WY JWH-293 Investigative T37693 DRUGINFO D04EOZ JWH-294 Investigative T37693 DRUGINFO D0G9EU JWH-295 Investigative T37693 DRUGINFO D0Q4YR JWH-296 Investigative T37693 DRUGINFO D0Y6MS JWH-297 Investigative T37693 DRUGINFO D0I9XR JWH-302 Investigative T37693 DRUGINFO D03DDL JWH-303 Investigative T37693 DRUGINFO D0IW4Q JWH-305 Investigative T37693 DRUGINFO D0L5IM JWH-306 Investigative T37693 DRUGINFO D02QTB JWH-307 Investigative T37693 DRUGINFO D0Q9FB JWH-308 Investigative T37693 DRUGINFO D0O8IC JWH-309 Investigative T37693 DRUGINFO D02UEJ JWH-311 Investigative T37693 DRUGINFO D0RI8G JWH-312 Investigative T37693 DRUGINFO D01JTY JWH-313 Investigative T37693 DRUGINFO D0W9BD JWH-314 Investigative T37693 DRUGINFO D08BGZ JWH-315 Investigative T37693 DRUGINFO D0PC1Z JWH-323 Investigative T37693 DRUGINFO D0Z1XE JWH-324 Investigative T37693 DRUGINFO D0E4OT JWH-325 Investigative T37693 DRUGINFO D0U4JI JWH-337 Investigative T37693 DRUGINFO D01JQX JWH-342 Investigative T37693 DRUGINFO D0M1ZC JWH-343 Investigative T37693 DRUGINFO D09JER JWH-344 Investigative T37693 DRUGINFO D07QUV JWH-345 Investigative T37693 DRUGINFO D0F3XG JWH-346 Investigative T37693 DRUGINFO D0B8AN JWH-347 Investigative T37693 DRUGINFO D0V3TO JWH-348 Investigative T37693 DRUGINFO D0Y9HT JWH-363 Investigative T37693 DRUGINFO D07KZW JWH-364 Investigative T37693 DRUGINFO D0DQ3F JWH-365 Investigative T37693 DRUGINFO D0EE0Q JWH-366 Investigative T37693 DRUGINFO D09PIQ JWH-367 Investigative T37693 DRUGINFO D0DE9L JWH-368 Investigative T37693 DRUGINFO D0ZL2P JWH-369 Investigative T37693 DRUGINFO D04LZA JWH-370 Investigative T37693 DRUGINFO D0R1NR JWH-371 Investigative T37693 DRUGINFO D0E3OY JWH-372 Investigative T37693 DRUGINFO D0R3GN JWH-373 Investigative T37693 DRUGINFO D0A2BC JWH-385 Investigative T37693 DRUGINFO D04TSL JWH-392 Investigative T37693 DRUGINFO D0E0JU JWH-401 Investigative T37693 DRUGINFO D0Y0MY JWH-402 Investigative T37693 DRUGINFO D0N5VO JWH-403 Investigative T37693 DRUGINFO D01MJF JWH-404 Investigative T37693 DRUGINFO D00LZJ JWH-405 Investigative T37693 DRUGINFO D00DNT JWH-406 Investigative T37693 DRUGINFO D00TRZ JWH-407 Investigative T37693 DRUGINFO D06SKK JWH-440 Investigative T37693 DRUGINFO D0X1FX JWH-441 Investigative T37693 DRUGINFO D0EX7J JWH-442 Investigative T37693 DRUGINFO D0P5VJ KM-233 Investigative T37693 DRUGINFO D0D7OR KM-233-M Investigative T37693 DRUGINFO D0BS7G L-759,633 Investigative T37693 DRUGINFO D02INF L-759,656 Investigative T37693 DRUGINFO D06SRX MDA-19 Investigative T37693 DRUGINFO D0PE8U N-(1H-indazol-5-yl)icosa-5,8,11,14-tetraenamide Investigative T37693 DRUGINFO D0C4CG N-(2-chloroethyl)icosa-5,8,11,14-tetraenamide Investigative T37693 DRUGINFO D0Z5CX N-(3,3-Diphenyl)propyl-2,2-diphenylacetamide Investigative T37693 DRUGINFO D0J3XJ N-(3-Phenyl)propyl-2-(4-bromophenylacetamide) Investigative T37693 DRUGINFO D0L1UA N-(4-hydroxybenzyl)icosa-5,8,11,14-tetraenamide Investigative T37693 DRUGINFO D09BYO N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-2-HYDROXYACETAMIDE (ENANTIOMERIC MIX) Investigative T37693 DRUGINFO D0I4AF N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-3-HYDROXY-2,2-DIMETHYLPROPANAMIDE (ENANTIOMERIC MIX) Investigative T37693 DRUGINFO D0FJ1I N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-3-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX) Investigative T37693 DRUGINFO D0E0AA N-(7-(2-CHLOROPHENYL)-6-(4-CHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-2-HYDROXYACETAMIDE (ENANTIOMERIC MIX) Investigative T37693 DRUGINFO D02NAW N-(7'-(2-CHLOROPHENYL)-6'-(4-CHLOROPHENYL)-3',4'-DIHYDROSPIRO[CYCLOHEXANE-1,2'-PYRANO[2,3-B]PYRIDINE]-4'-YL)-2-HYDROXY-2-METHYLPROPANAMIDE (ENANTIOMERIC MIX) Investigative T37693 DRUGINFO D06NXC N-[6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDINE-4-YL]-4,4,4-TRIFLUORO-3-HYDROXYBUTANAMIDE (DIASTEREOMERIC MIX) Investigative T37693 DRUGINFO D06GAF N1-(4-bromophenyl)-N2,N2-dipentylphthalamide Investigative T37693 DRUGINFO D0CO6T NAPHTHYRIDINONE Investigative T37693 DRUGINFO D04AMC N-arachidonoyl-N-(2-hydroxyethyl)hydroxylamine Investigative T37693 DRUGINFO D0Y1MM N-arachidonoyl-O-(2-hydroxyethyl)hydroxylamine Investigative T37693 DRUGINFO D06JFN N-benzyl-4-bromo-3-(morpholinosulfonyl)benzamide Investigative T37693 DRUGINFO D0Q8QH N-oleoyl-N-(2-hydroxyethyl)hydroxylamine Investigative T37693 DRUGINFO D0T3CP N-oleoyl-O-(2-hydroxyethyl)hydroxylamine Investigative T37693 DRUGINFO D0F4BE O-arachidonoyl-N-(2-hydroxyethyl)hydroxylamine Investigative T37693 DRUGINFO D05TQX O-oleoyl-N-(2-hydroxyethyl)hydroxylamine Investigative T37693 DRUGINFO D0L6RT PRAVADOLINE Investigative T37693 DRUGINFO D0J7CR Rac-cis-N-arachidonoylcyclopropanolamide Investigative T37693 DRUGINFO D04ECZ Rac-trans-N-oleoylcyclopropanolamide Investigative T37693 DRUGINFO D08RYN RQ-00202730 Investigative T37693 DRUGINFO D05RKV Sch-036 Investigative T37693 DRUGINFO D00ECV SCH-225336 Investigative T37693 DRUGINFO D0G4VV SCH-356036 Investigative T37693 DRUGINFO D0J8KW SR144528 Investigative T37693 DRUGINFO D0PC5A VER-156084 Investigative T37693 DRUGINFO D0ZM1T VER-156085 Investigative T37693 KEGGPATH hsa04080:Neuroactive ligand-receptor interaction T37693 WIKIPATH WP1824:GPCR downstream signaling T37693 WIKIPATH WP1825:GPCR ligand binding T37693 WIKIPATH WP247:Small Ligand GPCRs T37693 WIKIPATH WP455:GPCRs, Class A Rhodopsin-like T37693 REACPATH R-HSA-373076:Class A/1 (Rhodopsin-like receptors) T37693 REACPATH R-HSA-418594:G alpha (i) signalling events T77913 TARGETID T77913 T77913 FORMERID TTDS00086 T77913 UNIPROID HRH1_HUMAN T77913 TARGNAME Histamine H1 receptor (H1R) T77913 GENENAME HRH1 T77913 TARGTYPE Successful target T77913 SYNONYMS HH1R; H1R T77913 FUNCTION In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system. T77913 PDBSTRUC 3RZE T77913 BIOCLASS GPCR rhodopsin T77913 SEQUENCE MSLPNSSCLLEDKMCEGNKTTMASPQLMPLVVVLSTICLVTVGLNLLVLYAVRSERKLHTVGNLYIVSLSVADLIVGAVVMPMNILYLLMSKWSLGRPLCLFWLSMDYVASTASIFSVFILCIDRYRSVQQPLRYLKYRTKTRASATILGAWFLSFLWVIPILGWNHFMQQTSVRREDKCETDFYDVTWFKVMTAIINFYLPTLLMLWFYAKIYKAVRQHCQHRELINRSLPSFSEIKLRPENPKGDAKKPGKESPWEVLKRKPKDAGGGSVLKSPSQTPKEMKSPVVFSQEDDREVDKLYCFPLDIVHMQAAAEGSSRDYVAVNRSHGQLKTDEQGLNTHGASEISEDQMLGDSQSFSRTDSDTTTETAPGKGKLRSGSNTGLDYIKFTWKRLRSHSRQYVSGLHMNRERKAAKQLGFIMAAFILCWIPYFIFFMVIAFCKNCCNEHLHMFTIWLGYINSTLNPLIYPLCNENFKKTFKRILHIRS T77913 DRUGINFO D0ZJ1C (S)-(+)-Dimethindene maleate Approved T77913 DRUGINFO D06EQP Aceprometazine Approved T77913 DRUGINFO D0O4EU Acrivastine Approved T77913 DRUGINFO D0O7JW Alcaftadine Approved T77913 DRUGINFO D06FZX Antazoline Approved T77913 DRUGINFO D0N7AD Azatadine Approved T77913 DRUGINFO D00JVR Azelastine Approved T77913 DRUGINFO D0U5VZ Bepotastine Approved T77913 DRUGINFO D0Y5GK Bromodiphenhydramine Approved T77913 DRUGINFO D08VXO Brompheniramine Approved T77913 DRUGINFO D03XSJ Buclizine Approved T77913 DRUGINFO D00FGV Carbinoxamine Approved T77913 DRUGINFO D0DK8V Cetirizine Approved T77913 DRUGINFO D0EC6Q Chlophedianol Approved T77913 DRUGINFO D0B7NG Chlorpheniramine Approved T77913 DRUGINFO D0Q3YO Cinnarizine Approved T77913 DRUGINFO D0C5XC Clemastine Approved T77913 DRUGINFO D08HRJ Cyclizine Approved T77913 DRUGINFO D00TLN Cyproheptadine Approved T77913 DRUGINFO D01GBY Desloratadine Approved T77913 DRUGINFO D02WIW Dexbrompheniramine Approved T77913 DRUGINFO D05ZGQ Dexchlorpheniramine Maleate Approved T77913 DRUGINFO D0U8UV Dimenhydrinate Approved T77913 DRUGINFO D08CTT Dimethindene Approved T77913 DRUGINFO D01FGR Diphenhydramine Approved T77913 DRUGINFO D0W6DY Diphenylpyraline Approved T77913 DRUGINFO D06FES Doxepin Approved T77913 DRUGINFO D0Y2LR Doxylamine Approved T77913 DRUGINFO D02XJI Emedastine Approved T77913 DRUGINFO D0DV3O Epinastine Approved T77913 DRUGINFO D04USC Ergotidine Approved T77913 DRUGINFO D0Q0RC Ethopropazine Approved T77913 DRUGINFO D01KPV Fexofenadine Approved T77913 DRUGINFO D0O6SX Hydroxyzine Approved T77913 DRUGINFO D0YG7M Ketotifen Approved T77913 DRUGINFO D08SEI Levocabastine Approved T77913 DRUGINFO D0M8PW Levocetirizine dihydrochloride Approved T77913 DRUGINFO D06ABF Loratadine Approved T77913 DRUGINFO D08JZS Mepyramine Approved T77913 DRUGINFO D01NJI Mepyramine maleate Approved T77913 DRUGINFO D09IMS Mequitazine Approved T77913 DRUGINFO D0LR0R Methdilazine Approved T77913 DRUGINFO D06MAJ Mizolastine Approved T77913 DRUGINFO D05GPO Olopatadine Approved T77913 DRUGINFO D0AJ5L Oxatomide Approved T77913 DRUGINFO D0K5LQ Pemirolast Approved T77913 DRUGINFO D06UDO Phenindamine Approved T77913 DRUGINFO D04OBB Pheniramine Approved T77913 DRUGINFO D0T2XU Promethazine Approved T77913 DRUGINFO D0R9ZB Propiomazine Approved T77913 DRUGINFO D0E6OC Tranilast Approved T77913 DRUGINFO D08HZL Trimeprazine Approved T77913 DRUGINFO D0B4JQ Tripelennamine Approved T77913 DRUGINFO D0E8CI Triprolidine Approved T77913 DRUGINFO D0S1CQ RUPATADINE Phase 4 T77913 DRUGINFO D01JFM AC-170 Phase 3 T77913 DRUGINFO D0LK4X Carebastine Phase 3 T77913 DRUGINFO D08TLI E-4716 Phase 2 T77913 DRUGINFO D04HAF LY-2624803 Phase 2 T77913 DRUGINFO D03DRR Noberastine Phase 2 T77913 DRUGINFO D08WOJ OBE-101 Phase 2 T77913 DRUGINFO D05XEA RP5063 Phase 2 T77913 DRUGINFO D04JIM UCB-35440 Phase 2 T77913 DRUGINFO D0E8ZY Vapitadine Phase 2 T77913 DRUGINFO D0R6LF Citalopram derivative 1 Patented T77913 DRUGINFO D0VX6P Piperidine derivative 1 Patented T77913 DRUGINFO D0FA3G PMID29334795-Compound-61 Patented T77913 DRUGINFO D0Y2HR Astemizole Withdrawn from market T77913 DRUGINFO D08SOF Terfenadine Withdrawn from market T77913 DRUGINFO D0I5UU Norastemizole Discontinued in Preregistration T77913 DRUGINFO D04IFU GSK835726 Discontinued in Phase 2 T77913 DRUGINFO D08RZV HSR-609 Discontinued in Phase 2 T77913 DRUGINFO D02YBP Mequitamium iodide Discontinued in Phase 2 T77913 DRUGINFO D09TEI ReN-1869 Discontinued in Phase 2 T77913 DRUGINFO D00WJE SUN-1334H Discontinued in Phase 2 T77913 DRUGINFO D09UXP AZD-1744 Discontinued in Phase 1 T77913 DRUGINFO D0B4TT GSK1004723 Discontinued in Phase 1 T77913 DRUGINFO D0VZ8S KA-398 Terminated T77913 DRUGINFO D0FQ4M Selenotifen Terminated T77913 DRUGINFO D01XZI (-)-trans-H2-PAT Investigative T77913 DRUGINFO D0QW5N (+)-cis-H2-PAT Investigative T77913 DRUGINFO D0PC7A (+)-trans-H2-PAT Investigative T77913 DRUGINFO D0B9TV (+/-)-cis-H2-PAT Investigative T77913 DRUGINFO D0Z1WW (S)-cetirizine Investigative T77913 DRUGINFO D0I0UW 1-(4-p-Tolyl-butyl)-piperidine Investigative T77913 DRUGINFO D08NXC 1-[(Furan-2(5H)-one)-4-methyl]-desloratadine Investigative T77913 DRUGINFO D0XY3G 2-(2-thiazolyl)ethanamine Investigative T77913 DRUGINFO D0G6AQ 2-(3-bromophenyl)histamine Investigative T77913 DRUGINFO D0T7AR 2-(3-chlorophenyl)histamine Investigative T77913 DRUGINFO D0A6IQ 2-(3-iodophenyl)histamine Investigative T77913 DRUGINFO D03VUU 2-(9,10-dihydroanthracen-9-yl)-N-methylethanamine Investigative T77913 DRUGINFO D0BT1A 2-pyridylethylamine Investigative T77913 DRUGINFO D0B0PP 3,3-diphenylpropan-1-amine Investigative T77913 DRUGINFO D0T2RY 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Investigative T77913 DRUGINFO D04SCQ 4,4-Diphenylbutan-1-amine Investigative T77913 DRUGINFO D0Y5QR 8R-Lisuride Investigative T77913 DRUGINFO D05YFZ 9-(2-aminoethyl)-9,10-dihydroanthracene Investigative T77913 DRUGINFO D0S0WX 9-(2-aminopropyl)-9,10-dihydroanthracene Investigative T77913 DRUGINFO D01CXD 9-(Aminomethyl)-9,10-dihydroanthracene Investigative T77913 DRUGINFO D0Y4MC 9-OH-risperidone Investigative T77913 DRUGINFO D05IHR 9-Phenyl-2,3-dihydro-1H-indeno[2,1-c]pyridine Investigative T77913 DRUGINFO D08SLS arpromidine Investigative T77913 DRUGINFO D0K9KJ BU-E 47 Investigative T77913 DRUGINFO D02YSX DIMEBOLIN Investigative T77913 DRUGINFO D0PB6B dimethylhistaprodifen Investigative T77913 DRUGINFO D08TBU Diphenyl(piperidin-4-yl)methanol Investigative T77913 DRUGINFO D0RG8O histaprodifen Investigative T77913 DRUGINFO D06QQS Hydroxyclemastine Investigative T77913 DRUGINFO D0B4SF impromidine Investigative T77913 DRUGINFO D08RCH KF-A6 Investigative T77913 DRUGINFO D0A1DE MDL-28163 Investigative T77913 DRUGINFO D0G3OY methylhistaprodifen Investigative T77913 DRUGINFO D01HJZ N,N-dimethyl-2,2-diphenylethanamine Investigative T77913 DRUGINFO D02SDX N,N-Dimethyl-3,3-diphenylpropan-1-amine Investigative T77913 DRUGINFO D0S3WR N,N-dimethyl-4,4-diphenylbutan-1-amine Investigative T77913 DRUGINFO D02GNN N-methyl-3,3-diphenylpropan-1-amine Investigative T77913 DRUGINFO D05RKS N-methyl-4,4-diphenylbutan-1-amine Investigative T77913 DRUGINFO D0D3YN OCTOCLOTHEPIN Investigative T77913 DRUGINFO D04WXI oxo-arpromidine Investigative T77913 DRUGINFO D0PN9R R-226161 Investigative T77913 DRUGINFO D0H8XV R-dimethindene Investigative T77913 DRUGINFO D01HUN UR-PG131A Investigative T77913 DRUGINFO D0AU0F UR-PG146 Investigative T77913 DRUGINFO D0Y9IB UR-PG153 Investigative T77913 DRUGINFO D0UG1U UR-PG55B Investigative T77913 DRUGINFO D03SNI VUF-10148 Investigative T77913 KEGGPATH hsa04020:Calcium signaling pathway T77913 KEGGPATH hsa04080:Neuroactive ligand-receptor interaction T77913 KEGGPATH hsa04750:Inflammatory mediator regulation of TRP channels T77913 WIKIPATH WP1824:GPCR downstream signaling T77913 WIKIPATH WP1825:GPCR ligand binding T77913 WIKIPATH WP2664:Gastrin-CREB signalling pathway via PKC and MAPK T77913 WIKIPATH WP395:IL-4 Signaling Pathway T77913 WIKIPATH WP455:GPCRs, Class A Rhodopsin-like T77913 WIKIPATH WP58:Monoamine GPCRs T77913 REACPATH R-HSA-390650:Histamine receptors T77913 REACPATH R-HSA-416476:G alpha (q) signalling events T77913 PANTPATH P04385:Histamine H1 receptor mediated signaling pathway T58921 TARGETID T58921 T58921 FORMERID TTDS00338 T58921 UNIPROID PPARG_HUMAN T58921 TARGNAME Peroxisome proliferator-activated receptor gamma (PPAR-gamma) T58921 GENENAME PPARG T58921 TARGTYPE Successful target T58921 SYNONYMS PPAR-gamma; Nuclear receptor subfamily 1 group C member 3; NR1C3 T58921 FUNCTION Nuclear receptor that binds peroxisome proliferators such as hypolipidemic drugs and fatty acids. Once activated by a ligand, the nuclear receptor binds to DNA specific PPAR response elements (PPRE) and modulates the transcription of its target genes, such as acyl-CoA oxidase. It therefore controls the peroxisomal beta-oxidation pathway of fatty acids. Key regulator of adipocyte differentiation and glucose homeostasis. ARF6 acts as a key regulator of the tissue-specific adipocyte P2 (aP2) enhancer. Acts as a critical regulator of gut homeostasis by suppressing NF-kappa-B-mediated proinflammatory responses. Plays a role in the regulation of cardiovascular circadian rhythms by regulating the transcription of ARNTL/BMAL1 in the blood vessels (By similarity). T58921 PDBSTRUC 6MD4; 6MD2; 6MD1; 6MD0; 6MCZ T58921 BIOCLASS Nuclear hormone receptor T58921 SEQUENCE MGETLGDSPIDPESDSFTDTLSANISQEMTMVDTEMPFWPTNFGISSVDLSVMEDHSHSFDIKPFTTVDFSSISTPHYEDIPFTRTDPVVADYKYDLKLQEYQSAIKVEPASPPYYSEKTQLYNKPHEEPSNSLMAIECRVCGDKASGFHYGVHACEGCKGFFRRTIRLKLIYDRCDLNCRIHKKSRNKCQYCRFQKCLAVGMSHNAIRFGRMPQAEKEKLLAEISSDIDQLNPESADLRALAKHLYDSYIKSFPLTKAKARAILTGKTTDKSPFVIYDMNSLMMGEDKIKFKHITPLQEQSKEVAIRIFQGCQFRSVEAVQEITEYAKSIPGFVNLDLNDQVTLLKYGVHEIIYTMLASLMNKDGVLISEGQGFMTREFLKSLRKPFGDFMEPKFEFAVKFNALELDDSDLAIFIAVIILSGDRPGLLNVKPIEDIQDNLLQALELQLKLNHPESSQLFAKLLQKMTDLRQIVTEHVQLLQVIKKTETDMSLHPLLQEIYKDLY T58921 DRUGINFO D04BCB Lobeglitazone Approved T58921 DRUGINFO D03OFF Pioglitazone Approved T58921 DRUGINFO D0K5ER Rosiglitazone XR Approved T58921 DRUGINFO D0K8IX Thiazolidinedione Approved T58921 DRUGINFO D06XZW Troglitazone Approved T58921 DRUGINFO D0S2BV Glitazone Phase 4 T58921 DRUGINFO D0F3NH Balaglitazone Phase 3 T58921 DRUGINFO D0F5JH CS-038 Phase 3 T58921 DRUGINFO D0M0SS FARGLITAZAR Phase 3 T58921 DRUGINFO D0VU5M Imiglitazar Phase 3 T58921 DRUGINFO D0M3UT MURAGLITAZAR Phase 3 T58921 DRUGINFO D02NHD Ragaglitazar Phase 3 T58921 DRUGINFO D08PFA Rivoglitazone Phase 3 T58921 DRUGINFO D0A1AQ Rosiglitazone + metformin Phase 3 T58921 DRUGINFO D0Q6IW Rosiglitazone + simvastatin Phase 3 T58921 DRUGINFO D0H1NL TESAGLITAZAR Phase 3 T58921 DRUGINFO D0T7MN ZYH-1 Phase 3 T58921 DRUGINFO D0X7VB MBX-102 Phase 2/3 T58921 DRUGINFO D0P5SU CHS-131 Phase 2 T58921 DRUGINFO D00PJJ FK-614 Phase 2 T58921 DRUGINFO D0E6ME GED-0507-34-Levo Phase 2 T58921 DRUGINFO D08NPG MBX-2044 Phase 2 T58921 DRUGINFO D04BPS Naveglitazar Phase 2 T58921 DRUGINFO D02TGD Netoglitazone Phase 2 T58921 DRUGINFO D0W0JP OMS405 Phase 2 T58921 DRUGINFO D0PP8G ONO-5129 Phase 2 T58921 DRUGINFO D0ZT8A T3D-959 Phase 1/2 T58921 DRUGINFO D06TWE CLX-0921 Phase 1 T58921 DRUGINFO D07IGC DSP-8658 Phase 1 T58921 DRUGINFO D08EEU Englitazone sodium Phase 1 T58921 DRUGINFO D0AX9S GW-409544 Phase 1 T58921 DRUGINFO D03RJZ Oxeglitazar Phase 1 T58921 DRUGINFO D0U6AW 1-(biphenyl-4-yl-methyl)-1H-imidazole derivative 1 Patented T58921 DRUGINFO D0SV6U 3-phenyl acrylic acid derivative 1 Patented T58921 DRUGINFO D0E9GF A-substituted phenylpropionic acid derivative 1 Patented T58921 DRUGINFO D0M5YQ A-substituted phenylpropionic acid derivative 2 Patented T58921 DRUGINFO D0O8PR Biaromatic compound 1 Patented T58921 DRUGINFO D0ZO0D Cannabinoid quinone derivative 1 Patented T58921 DRUGINFO D0M4RD Crystalline anhydrous toluene derivative 1 Patented T58921 DRUGINFO D0HW6Y Flavonoid derivative 8 Patented T58921 DRUGINFO D0UG1W Fused aromatic compound 1 Patented T58921 DRUGINFO D0SL0K Fused ring compound 1 Patented T58921 DRUGINFO D0PO7F MRL20 Patented T58921 DRUGINFO D0H5FI MRL24 Patented T58921 DRUGINFO D09OXG Phenylpropionic acid derivative 1 Patented T58921 DRUGINFO D0NF8V Phenylpyridine derivative 3 Patented T58921 DRUGINFO D0UH5B PMID25416646-Compound-Figure2-J Patented T58921 DRUGINFO D0G3KY PMID25416646-Compound-Figure2-K Patented T58921 DRUGINFO D0GG5K PMID25416646-Compound-Figure2-N Patented T58921 DRUGINFO D0O5IN PMID25416646-Compound-Figure5-A Patented T58921 DRUGINFO D0V0JN PMID25416646-Compound-Figure5-C Patented T58921 DRUGINFO D0LA6O PMID25416646-Compound-Figure5-E Patented T58921 DRUGINFO D05AUY PMID25416646-Compound-Figure5-H Patented T58921 DRUGINFO D03GFB Spirolaxine derivative 1 Patented T58921 DRUGINFO D0HT9C Sulfonamide derivative 18 Patented T58921 DRUGINFO D0TF0T Thiazolidine dione crystalline derivative 1 Patented T58921 DRUGINFO D0W2IU AVE-0847 Discontinued in Phase 2 T58921 DRUGINFO D0S6KX GSK-677954 Discontinued in Phase 2 T58921 DRUGINFO D09OHP Indeglitazar Discontinued in Phase 2 T58921 DRUGINFO D02RAU KRP-297 Discontinued in Phase 2 T58921 DRUGINFO D02ZKL Reglixane Discontinued in Phase 2 T58921 DRUGINFO D01JGG Sodelglitazar Discontinued in Phase 2 T58921 DRUGINFO D0KL3K YM-440 Discontinued in Phase 2 T58921 DRUGINFO D0Z6OI DS-6930 Discontinued in Phase 1 T58921 DRUGINFO D06PHO E-3030 Discontinued in Phase 1 T58921 DRUGINFO D0B0EB LY-929 Discontinued in Phase 1 T58921 DRUGINFO D03GWY Ciglitazone Preclinical T58921 DRUGINFO D08WOE MC-3002 Preclinical T58921 DRUGINFO D0LB4T AD-5075 Terminated T58921 DRUGINFO D04JVX AKP-320 Terminated T58921 DRUGINFO D0I0RF BVT-142 Terminated T58921 DRUGINFO D0V0TT CS-204 Terminated T58921 DRUGINFO D0N1EF DARGLITAZONE Terminated T58921 DRUGINFO D08VKZ Edaglitazone Terminated T58921 DRUGINFO D00YGA SB-219994 Terminated T58921 DRUGINFO D0OW6Z Sipoglitazar Terminated T58921 DRUGINFO D0J3UU (2S)-2-(4-chlorophenoxy)-3-phenylpropanoic acid Investigative T58921 DRUGINFO D0H4US (2S)-2-(4-ethylphenoxy)-3-phenylpropanoic acid Investigative T58921 DRUGINFO D06MDX (2S)-2-(biphenyl-4-yloxy)-3-phenylpropanoic acid Investigative T58921 DRUGINFO D0Z5TV (9Z,11E,13S)-13-hydroxyoctadeca-9,11-dienoic acid Investigative T58921 DRUGINFO D01PGU 15-deoxy-Delta(12, 14)-prostaglandin J(2) Investigative T58921 DRUGINFO D00ACX 2-chloro-5-nitro-N-phenylbenzamide Investigative T58921 DRUGINFO D0E5HC 3-(5-methoxy-1H-indol-3-yl)propanoic acid Investigative T58921 DRUGINFO D0SZ4T 9-hydroxyoctadecadienoic acid Investigative T58921 DRUGINFO D01ARG DB-900 Investigative T58921 DRUGINFO D01POG GW-2331 Investigative T58921 DRUGINFO D0O2US GW7845 Investigative T58921 DRUGINFO D0Z4MH ZY H2 Investigative T58921 KEGGPATH hsa03320:PPAR signaling pathway T58921 KEGGPATH hsa04152:AMPK signaling pathway T58921 KEGGPATH hsa04380:Osteoclast differentiation T58921 KEGGPATH hsa05016:Huntington's disease T58921 KEGGPATH hsa05200:Pathways in cancer T58921 KEGGPATH hsa05202:Transcriptional misregulation in cancer T58921 KEGGPATH hsa05216:Thyroid cancer T58921 WIKIPATH WP170:Nuclear Receptors T58921 WIKIPATH WP1982:SREBP signalling T58921 WIKIPATH WP236:Adipogenesis T58921 WIKIPATH WP2751:Transcriptional Regulation of White Adipocyte Differentiation T58921 WIKIPATH WP2797:Regulation of Lipid Metabolism by Peroxisome proliferator-activated receptor alpha (PPARalpha) T58921 WIKIPATH WP2895:Differentiation of white and brown adipocyte T58921 WIKIPATH WP299:Nuclear Receptors in Lipid Metabolism and Toxicity T58921 WIKIPATH WP363:Wnt Signaling Pathway Netpath T58921 REACPATH R-HSA-1989781:PPARA activates gene expression T58921 REACPATH R-HSA-381340:Transcriptional regulation of white adipocyte differentiation T58921 REACPATH R-HSA-383280:Nuclear Receptor transcription pathway T58921 NET_PATH NetPath_13:IL1 Signaling Pathway T58921 NET_PATH NetPath_22:Leptin Signaling Pathway T58921 NET_PATH NetPath_7:TGF_beta_Receptor Signaling Pathway T58921 INTEPATH hdac_classi_pathway:Signaling events mediated by HDAC Class I T58921 INTEPATH nfat_tfpathway:Calcineurin-regulated NFAT-dependent transcription in lymphocytes T58921 INTEPATH rb_1pathway:Regulation of retinoblastoma protein T58921 INTEPATH rxr_vdr_pathway:RXR and RAR heterodimerization with other nuclear receptor T58921 INTEPATH wnt_noncanonical_pathway:Noncanonical Wnt signaling pathway T58921 PANTPATH P06959:CCKR signaling map ST T60857 TARGETID T60857 T60857 FORMERID TTDR00033 T60857 UNIPROID AK1C3_HUMAN T60857 TARGNAME Dihydrodiol dehydrogenase type I (AKR1C3) T60857 GENENAME AKR1C3 T60857 TARGTYPE Successful target T60857 SYNONYMS Trans-1,2-dihydrobenzene-1,2-diol dehydrogenase; Testosterone 17-beta-dehydrogenase 5; Prostaglandin F synthase; PGFS; KIAA0119; Indanol dehydrogenase; HSD17B5; HA1753; Dihydrodiol dehydrogenase 3; DDH1; DD3; DD-3; Chlordecone reductase homolog HAKRb; Aldo-keto reductase family 1 member C3; 3-alpha-hydroxysteroid dehydrogenase type 2; 3-alpha-HSD type II, brain; 3-alpha-HSD type 2; 17-beta-hydroxysteroid dehydrogenase type 5; 17-beta-HSD 5 T60857 FUNCTION Catalyzes the conversion of aldehydes and ketones to alcohols. Catalyzes the reduction of prostaglandin (PG) D2, PGH2 and phenanthrenequinone (PQ) and the oxidation of 9-alpha,11-beta-PGF2 to PGD2. Functions as a bi-directional 3-alpha-, 17-beta- and 20-alpha HSD. Can interconvert active androgens, estrogens and progestins with their cognate inactive metabolites. Preferentially transforms androstenedione (4-dione) to testosterone. T60857 PDBSTRUC 6GXK; 6F78; 6F2U; 5JM5; 5HNU T60857 BIOCLASS Short-chain dehydrogenases reductase T60857 ECNUMBER EC 1.-.-.- T60857 SEQUENCE MDSKHQCVKLNDGHFMPVLGFGTYAPPEVPRSKALEVTKLAIEAGFRHIDSAHLYNNEEQVGLAIRSKIADGSVKREDIFYTSKLWSTFHRPELVRPALENSLKKAQLDYVDLYLIHSPMSLKPGEELSPTDENGKVIFDIVDLCTTWEAMEKCKDAGLAKSIGVSNFNRRQLEMILNKPGLKYKPVCNQVECHPYFNRSKLLDFCKSKDIVLVAYSALGSQRDKRWVDPNSPVLLEDPVLCALAKKHKRTPALIALRYQLQRGVVVLAKSYNEQRIRQNVQVFEFQLTAEDMKAIDGLDRNLHYFNSDSFASHPNYPYSDEY T60857 DRUGINFO D0B2WJ Flufenamic Acid Approved T60857 DRUGINFO D0H7XJ ASP-9521 Phase 1/2 T60857 DRUGINFO D0G8VB Beta-naphthylacetic acids derivative 1 Patented T60857 DRUGINFO D0GY2Z Indomethacin analog 1 Patented T60857 DRUGINFO D0F0PK Indomethacin analog 2 Patented T60857 DRUGINFO D0E2TY Indomethacin analog 3 Patented T60857 DRUGINFO D0Y7XJ Isoquinolone derivative 1 Patented T60857 DRUGINFO D0S6TL N-(benzimidazole/indole) benzoic acid derivative 1 Patented T60857 DRUGINFO D02JPV N-(benzimidazole/indole) benzoic acid derivative 2 Patented T60857 DRUGINFO D0N3XY N-(benzimidazolylcarbonyl)-piperidine derivative 1 Patented T60857 DRUGINFO D0Q8RC N-(indolylcarbonyl)-piperidine derivative 1 Patented T60857 DRUGINFO D0M6LX N-(naphthylamino)-benzoate derivative 1 Patented T60857 DRUGINFO D05GKS N-(phenylamino)-benzoate derivative 1 Patented T60857 DRUGINFO D0SM2O N-(pyridinepyrroylylcarbonyl)-piperidine derivative 1 Patented T60857 DRUGINFO D0PI1W Nitrogen/sulfur-substituted estrene derivative 1 Patented T60857 DRUGINFO D0MC5H 2-(4-Chlorobenzylidene)cyclopentanone Investigative T60857 DRUGINFO D00XMO 2-(4-chlorobenzylidene)cyclopentyl ethyl ether Investigative T60857 DRUGINFO D0Q9RA 2-(4-chlorobenzylidene)cyclopentylmethyl ether Investigative T60857 DRUGINFO D0V5AQ 2,2-Dibenzylcyclopentanol Investigative T60857 DRUGINFO D03POE 2-[(2,2-diphenylacetyl)amino]benzoic acid Investigative T60857 DRUGINFO D06GOK 2-Methyl-2,4-Pentanediol Investigative T60857 DRUGINFO D0J2FY 2'-Monophosphoadenosine 5'-Diphosphoribose Investigative T60857 DRUGINFO D00DDO 3-Bromo-5-phenylsalicylc acid Investigative T60857 DRUGINFO D0Z0IR 3-Phenylcyclopentanecarboxylic acid Investigative T60857 DRUGINFO D0M8RO 4-ANDROSTENE-3-17-DIONE Investigative T60857 DRUGINFO D0F2ME Acetate Ion Investigative T60857 DRUGINFO D0K9YS EM1396 Investigative T60857 DRUGINFO D0ZR1V EM-1424 Investigative T60857 DRUGINFO D0DF1Z M-Phenoxybenzoic Acid For Cis-Isomer Investigative T60857 DRUGINFO D09ALJ Rutin Investigative T60857 KEGGPATH hsa00140:Steroid hormone biosynthesis T60857 KEGGPATH hsa00590:Arachidonic acid metabolism T60857 KEGGPATH hsa01100:Metabolic pathways T60857 KEGGPATH hsa04913:Ovarian steroidogenesis T60857 WIKIPATH WP2650:Arachidonic acid metabolism T60857 WIKIPATH WP696:Benzo(a)pyrene metabolism T60857 WIKIPATH WP702:Metapathway biotransformation T60857 WHIZPATH PW000044:Arachidonic Acid Metabolism T60857 REACPATH R-HSA-975634:Retinoid metabolism and transport T60857 NET_PATH NetPath_7:TGF_beta_Receptor Signaling Pathway T60857 BIOCPATH PWY66-378:Androgen biosynthesis T60857 BIOCPATH PWY-7305:Superpathway of steroid hormone biosynthesis T60857 BIOCPATH PWY-7455:Allopregnanolone biosynthesis T80276 TARGETID T80276 T80276 FORMERID TTDNC00388 T80276 UNIPROID PK3CA_HUMAN T80276 TARGNAME PI3-kinase alpha (PIK3CA) T80276 GENENAME PIK3CA T80276 TARGTYPE Successful target T80276 SYNONYMS p110alpha; Serine/threonine protein kinase PIK3CA; PtdIns3kinase subunit p110alpha; PtdIns3kinase subunit alpha; PtdIns-3-kinase subunit p110-alpha; PtdIns-3-kinase subunit alpha; Phosphoinositide3kinase catalytic alpha polypeptide; Phosphoinositide-3-kinase catalytic alpha polypeptide; Phosphatidylinositol 4,5bisphosphate 3kinase catalytic subunit alpha isoform; Phosphatidylinositol 4,5bisphosphate 3kinase 110 kDa catalytic subunit alpha; Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform; Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit alpha; PI3kinase subunit alpha; PI3Kalpha; PI3K-alpha; PI3-kinase subunit alpha T80276 FUNCTION Phosphoinositide-3-kinase (PI3K) that phosphorylates PtdIns (Phosphatidylinositol), PtdIns4P (Phosphatidylinositol 4-phosphate) and PtdIns(4,5)P2 (Phosphatidylinositol 4,5-bisphosphate) to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3). PIP3 plays a key role by recruiting PH domain-containing proteins to the membrane, including AKT1 and PDPK1, activating signaling cascades involved in cell growth, survival, proliferation, motility and morphology. Participates in cellular signaling in response to various growth factors. Involved in the activation of AKT1 upon stimulation by receptor tyrosine kinases ligands such as EGF, insulin, IGF1, VEGFA and PDGF. Involved in signaling via insulin-receptor substrate (IRS) proteins. Essential in endothelial cell migration during vascular development through VEGFA signaling, possibly by regulating RhoA activity. Required for lymphatic vasculature development, possibly by binding to RAS and by activation by EGF and FGF2, but not by PDGF. Regulates invadopodia formation through the PDPK1-AKT1 pathway. Participates in cardiomyogenesis in embryonic stem cells through a AKT1 pathway. Participates in vasculogenesis in embryonic stem cells through PDK1 and protein kinase C pathway. Also has serine-protein kinase activity: phosphorylates PIK3R1 (p85alpha regulatory subunit), EIF4EBP1 and HRAS. Plays a role in the positive regulation of phagocytosis and pinocytosis. T80276 PDBSTRUC 6NCT; 5XGJ; 5XGI; 5XGH; 5UL1 T80276 BIOCLASS Kinase T80276 ECNUMBER EC 2.7.1.153 T80276 SEQUENCE MPPRPSSGELWGIHLMPPRILVECLLPNGMIVTLECLREATLITIKHELFKEARKYPLHQLLQDESSYIFVSVTQEAEREEFFDETRRLCDLRLFQPFLKVIEPVGNREEKILNREIGFAIGMPVCEFDMVKDPEVQDFRRNILNVCKEAVDLRDLNSPHSRAMYVYPPNVESSPELPKHIYNKLDKGQIIVVIWVIVSPNNDKQKYTLKINHDCVPEQVIAEAIRKKTRSMLLSSEQLKLCVLEYQGKYILKVCGCDEYFLEKYPLSQYKYIRSCIMLGRMPNLMLMAKESLYSQLPMDCFTMPSYSRRISTATPYMNGETSTKSLWVINSALRIKILCATYVNVNIRDIDKIYVRTGIYHGGEPLCDNVNTQRVPCSNPRWNEWLNYDIYIPDLPRAARLCLSICSVKGRKGAKEEHCPLAWGNINLFDYTDTLVSGKMALNLWPVPHGLEDLLNPIGVTGSNPNKETPCLELEFDWFSSVVKFPDMSVIEEHANWSVSREAGFSYSHAGLSNRLARDNELRENDKEQLKAISTRDPLSEITEQEKDFLWSHRHYCVTIPEILPKLLLSVKWNSRDEVAQMYCLVKDWPPIKPEQAMELLDCNYPDPMVRGFAVRCLEKYLTDDKLSQYLIQLVQVLKYEQYLDNLLVRFLLKKALTNQRIGHFFFWHLKSEMHNKTVSQRFGLLLESYCRACGMYLKHLNRQVEAMEKLINLTDILKQEKKDETQKVQMKFLVEQMRRPDFMDALQGFLSPLNPAHQLGNLRLEECRIMSSAKRPLWLNWENPDIMSELLFQNNEIIFKNGDDLRQDMLTLQIIRIMENIWQNQGLDLRMLPYGCLSIGDCVGLIEVVRNSHTIMQIQCKGGLKGALQFNSHTLHQWLKDKNKGEIYDAAIDLFTRSCAGYCVATFILGIGDRHNSNIMVKDDGQLFHIDFGHFLDHKKKKFGYKRERVPFVLTQDFLIVISKGAQECTKTREFERFQEMCYKAYLAIRQHANLFINLFSMMLGSGMPELQSFDDIAYIRKTLALDKTEQEALEYFMKQMNDAHHGGWTTKMDWIFHTIKQHALN T80276 DRUGINFO D0W7HE Alpelisib Approved T80276 DRUGINFO D0S5LD BAY 80-6946 Approved T80276 DRUGINFO D01QSO Buparlisib Phase 3 T80276 DRUGINFO D0UP1Z GDC-0032 Phase 3 T80276 DRUGINFO D0H1WC LY3023414 Phase 2 T80276 DRUGINFO D0Y2NS MLN1117 Phase 1/2 T80276 DRUGINFO D05CBJ PA-799 Phase 1/2 T80276 DRUGINFO D01LMM BLY719 Phase 1 T80276 DRUGINFO DYF2N4 HHCYH33 Phase 1 T80276 DRUGINFO D0Y0FE PWT-33597 Phase 1 T80276 DRUGINFO DOR1I0 ETP-46321 Investigative T80276 KEGGPATH hsa00562:Inositol phosphate metabolism T80276 KEGGPATH hsa04012:ErbB signaling pathway T80276 KEGGPATH hsa04014:Ras signaling pathway T80276 KEGGPATH hsa04015:Rap1 signaling pathway T80276 KEGGPATH hsa04022:cGMP-PKG signaling pathway T80276 KEGGPATH hsa04024:cAMP signaling pathway T80276 KEGGPATH hsa04062:Chemokine signaling pathway T80276 KEGGPATH hsa04066:HIF-1 signaling pathway T80276 KEGGPATH hsa04068:FoxO signaling pathway T80276 KEGGPATH hsa04070:Phosphatidylinositol signaling system T80276 KEGGPATH hsa04071:Sphingolipid signaling pathway T80276 KEGGPATH hsa04150:mTOR signaling pathway T80276 KEGGPATH hsa04151:PI3K-Akt signaling pathway T80276 KEGGPATH hsa04152:AMPK signaling pathway T80276 KEGGPATH hsa04210:Apoptosis T80276 KEGGPATH hsa04261:Adrenergic signaling in cardiomyocytes T80276 KEGGPATH hsa04370:VEGF signaling pathway T80276 KEGGPATH hsa04380:Osteoclast differentiation T80276 KEGGPATH hsa04510:Focal adhesion T80276 KEGGPATH hsa04550:Signaling pathways regulating pluripotency of stem cells T80276 KEGGPATH hsa04611:Platelet activation T80276 KEGGPATH hsa04620:Toll-like receptor signaling pathway T80276 KEGGPATH hsa04630:Jak-STAT signaling pathway T80276 KEGGPATH hsa04650:Natural killer cell mediated cytotoxicity T80276 KEGGPATH hsa04660:T cell receptor signaling pathway T80276 KEGGPATH hsa04662:B cell receptor signaling pathway T80276 KEGGPATH hsa04664:Fc epsilon RI signaling pathway T80276 KEGGPATH hsa04666:Fc gamma R-mediated phagocytosis T80276 KEGGPATH hsa04668:TNF signaling pathway T80276 KEGGPATH hsa04670:Leukocyte transendothelial migration T80276 KEGGPATH hsa04722:Neurotrophin signaling pathway T80276 KEGGPATH hsa04725:Cholinergic synapse T80276 KEGGPATH hsa04750:Inflammatory mediator regulation of TRP channels T80276 KEGGPATH hsa04810:Regulation of actin cytoskeleton T80276 KEGGPATH hsa04910:Insulin signaling pathway T80276 KEGGPATH hsa04914:Progesterone-mediated oocyte maturation T80276 KEGGPATH hsa04915:Estrogen signaling pathway T80276 KEGGPATH hsa04917:Prolactin signaling pathway T80276 KEGGPATH hsa04919:Thyroid hormone signaling pathway T80276 KEGGPATH hsa04921:Oxytocin signaling pathway T80276 KEGGPATH hsa04923:Regulation of lipolysis in adipocytes T80276 KEGGPATH hsa04930:Type II diabetes mellitus T80276 KEGGPATH hsa04932:Non-alcoholic fatty liver disease (NAFLD) T80276 KEGGPATH hsa04960:Aldosterone-regulated sodium reabsorption T80276 KEGGPATH hsa04973:Carbohydrate digestion and absorption T80276 KEGGPATH hsa05100:Bacterial invasion of epithelial cells T80276 KEGGPATH hsa05142:Chagas disease (American trypanosomiasis) T80276 KEGGPATH hsa05145:Toxoplasmosis T80276 KEGGPATH hsa05146:Amoebiasis T80276 KEGGPATH hsa05160:Hepatitis C T80276 KEGGPATH hsa05161:Hepatitis B T80276 KEGGPATH hsa05162:Measles T80276 KEGGPATH hsa05164:Influenza A T80276 KEGGPATH hsa05166:HTLV-I infection T80276 KEGGPATH hsa05169:Epstein-Barr virus infection T80276 KEGGPATH hsa05200:Pathways in cancer T80276 KEGGPATH hsa05203:Viral carcinogenesis T80276 KEGGPATH hsa05205:Proteoglycans in cancer T80276 KEGGPATH hsa05206:MicroRNAs in cancer T80276 KEGGPATH hsa05210:Colorectal cancer T80276 KEGGPATH hsa05211:Renal cell carcinoma T80276 KEGGPATH hsa05212:Pancreatic cancer T80276 KEGGPATH hsa05213:Endometrial cancer T80276 KEGGPATH hsa05214:Glioma T80276 KEGGPATH hsa05215:Prostate cancer T80276 KEGGPATH hsa05218:Melanoma T80276 KEGGPATH hsa05220:Chronic myeloid leukemia T80276 KEGGPATH hsa05221:Acute myeloid leukemia T80276 KEGGPATH hsa05222:Small cell lung cancer T80276 KEGGPATH hsa05223:Non-small cell lung cancer T80276 KEGGPATH hsa05230:Central carbon metabolism in cancer T80276 KEGGPATH hsa05231:Choline metabolism in cancer T80276 WIKIPATH WP1403:AMPK Signaling T80276 WIKIPATH WP1449:Regulation of toll-like receptor signaling pathway T80276 WIKIPATH WP1539:Angiogenesis T80276 WIKIPATH WP1544:MicroRNAs in cardiomyocyte hypertrophy T80276 WIKIPATH WP1794:Cell surface interactions at the vascular wall T80276 WIKIPATH WP1799:Costimulation by the CD28 family T80276 WIKIPATH WP1824:GPCR downstream signaling T80276 WIKIPATH WP1826:GPVI-mediated activation cascade T80276 WIKIPATH WP1840:Interleukin-3, 5 and GM-CSF signaling T80276 WIKIPATH WP1867:Nephrin interactions T80276 WIKIPATH WP1873:NGF signalling via TRKA from the plasma membrane T80276 WIKIPATH WP1910:Signaling by EGFR T80276 WIKIPATH WP1911:Signaling by FGFR T80276 WIKIPATH WP1913:Signaling by Insulin receptor T80276 WIKIPATH WP1916:Signaling by PDGF T80276 WIKIPATH WP1927:TCR signaling T80276 WIKIPATH WP1982:SREBP signalling T80276 WIKIPATH WP2032:TSH signaling pathway T80276 WIKIPATH WP2038:Regulation of Microtubule Cytoskeleton T80276 WIKIPATH WP2203:TSLP Signaling Pathway T80276 WIKIPATH WP2261:Signaling Pathways in Glioblastoma T80276 WIKIPATH WP2263:Prostate Cancer T80276 WIKIPATH WP2377:Integrated Pancreatic Cancer Pathway T80276 WIKIPATH WP2653:PIP3 activates AKT signaling T80276 WIKIPATH WP2664:Gastrin-CREB signalling pathway via PKC and MAPK T80276 WIKIPATH WP2677:Signaling by Type 1 Insulin-like Growth Factor 1 Receptor (IGF1R) T80276 WIKIPATH WP2694:DAP12 interactions T80276 WIKIPATH WP2713:Signaling by SCF-KIT T80276 WIKIPATH WP2719:Fcgamma receptor (FCGR) dependent phagocytosis T80276 WIKIPATH WP2732:Interleukin-2 signaling T80276 WIKIPATH WP2747:PI Metabolism T80276 WIKIPATH WP2759:Fc epsilon receptor (FCERI) signaling T80276 WIKIPATH WP2780:Signaling by ERBB2 T80276 WIKIPATH WP2781:Signaling by ERBB4 T80276 WIKIPATH WP2865:IL1 and megakaryotyces in obesity T80276 WIKIPATH WP3:Transcriptional activation by NRF2 T80276 WIKIPATH WP313:Signaling of Hepatocyte Growth Factor Receptor T80276 WIKIPATH WP395:IL-4 Signaling Pathway T80276 WIKIPATH WP481:Insulin Signaling T80276 WIKIPATH WP51:Regulation of Actin Cytoskeleton T80276 WIKIPATH WP524:G13 Signaling Pathway T80276 WIKIPATH WP710:DNA Damage Response (only ATM dependent) T80276 WIKIPATH WP722:Serotonin HTR1 Group and FOS Pathway T80276 WIKIPATH WP75:Toll-like receptor signaling pathway T80276 WHIZPATH PW000143:Inositol Metabolism T80276 WHIZPATH PW000168:Phosphatidylinositol Phosphate Metabolism T80276 WHIZPATH PW000445:Intracellular Signalling Through Adenosine Receptor A2a and Adenosine T80276 WHIZPATH PW000446:Intracellular Signalling Through Adenosine Receptor A2b and Adenosine T80276 WHIZPATH PW000453:Fc Epsilon Receptor I Signaling in Mast Cells T80276 REACPATH R-HSA-109704:PI3K Cascade T80276 REACPATH R-HSA-114604:GPVI-mediated activation cascade T80276 REACPATH R-HSA-1236382:Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants T80276 REACPATH R-HSA-1250342:PI3K events in ERBB4 signaling T80276 REACPATH R-HSA-1257604:PIP3 activates AKT signaling T80276 REACPATH R-HSA-180292:GAB1 signalosome T80276 REACPATH R-HSA-1963642:PI3K events in ERBB2 signaling T80276 REACPATH R-HSA-198203:PI3K/AKT activation T80276 REACPATH R-HSA-2029485:Role of phospholipids in phagocytosis T80276 REACPATH R-HSA-210993:Tie2 Signaling T80276 REACPATH R-HSA-2219530:Constitutive Signaling by Aberrant PI3K in Cancer T80276 REACPATH R-HSA-2424491:DAP12 signaling T80276 REACPATH R-HSA-2730905:Role of LAT2/NTAL/LAB on calcium mobilization T80276 REACPATH R-HSA-373753:Nephrin interactions T80276 REACPATH R-HSA-388841:Costimulation by the CD28 family T80276 REACPATH R-HSA-389357:CD28 dependent PI3K/Akt signaling T80276 REACPATH R-HSA-392451:G beta:gamma signalling through PI3Kgamma T80276 REACPATH R-HSA-416476:G alpha (q) signalling events T80276 REACPATH R-HSA-416482:G alpha (12/13) signalling events T80276 REACPATH R-HSA-4420097:VEGFA-VEGFR2 Pathway T80276 REACPATH R-HSA-512988:Interleukin-3, 5 and GM-CSF signaling T80276 REACPATH R-HSA-5637810:Constitutive Signaling by EGFRvIII T80276 REACPATH R-HSA-5654689:PI-3K cascade:FGFR1 T80276 REACPATH R-HSA-5654695:PI-3K cascade:FGFR2 T80276 REACPATH R-HSA-5654710:PI-3K cascade:FGFR3 T80276 REACPATH R-HSA-5654720:PI-3K cascade:FGFR4 T80276 REACPATH R-HSA-912526:Interleukin receptor SHC signaling T80276 REACPATH R-HSA-912631:Regulation of signaling by CBL T80276 INTEPATH a6b1_a6b4_integrin_pathway:a6b1 and a6b4 Integrin signaling T80276 INTEPATH angiopoietinreceptor_pathway:Angiopoietin receptor Tie2-mediated signaling T80276 INTEPATH ar_nongenomic_pathway:Nongenotropic Androgen signaling T80276 INTEPATH avb3_integrin_pathway:Integrins in angiogenesis T80276 INTEPATH avb3_opn_pathway:Osteopontin-mediated events T80276 INTEPATH bcr_5pathway:BCR signaling pathway T80276 INTEPATH cdc42_pathway:CDC42 signaling events T80276 INTEPATH cxcr3pathway:CXCR3-mediated signaling events T80276 INTEPATH cxcr4_pathway:CXCR4-mediated signaling events T80276 INTEPATH ecadherin_keratinocyte_pathway:E-cadherin signaling in keratinocytes T80276 INTEPATH ecadherin_nascentaj_pathway:E-cadherin signaling in the nascent adherens junction T80276 INTEPATH epha2_fwdpathway:EPHA2 forward signaling T80276 INTEPATH ephbfwdpathway:EPHB forward signaling T80276 INTEPATH ephrinbrevpathway:Ephrin B reverse signaling T80276 INTEPATH er_nongenomic_pathway:Plasma membrane estrogen receptor signaling T80276 INTEPATH erbb1_downstream_pathway:ErbB1 downstream signaling T80276 INTEPATH erbb1_internalization_pathway:Internalization of ErbB1 T80276 INTEPATH erbb1_receptor_proximal_pathway:EGF receptor (ErbB1) signaling pathway T80276 INTEPATH erbb2erbb3pathway:ErbB2/ErbB3 signaling events T80276 INTEPATH erbb4_pathway:ErbB4 signaling events T80276 INTEPATH fak_pathway:Signaling events mediated by focal adhesion kinase T80276 INTEPATH faspathway:FAS (CD95) signaling pathway T80276 INTEPATH fcer1pathway:Fc-epsilon receptor I signaling in mast cells T80276 INTEPATH fgf_pathway:FGF signaling pathway T80276 INTEPATH gmcsf_pathway:GMCSF-mediated signaling events T80276 INTEPATH hedgehog_2pathway:Signaling events mediated by the Hedgehog family T80276 INTEPATH ifngpathway:IFN-gamma pathway T80276 INTEPATH igf1_pathway:IGF1 pathway T80276 INTEPATH il1pathway:IL1-mediated signaling events T80276 INTEPATH il2_1pathway:IL2-mediated signaling events T80276 INTEPATH il2_pi3kpathway:IL2 signaling events mediated by PI3K T80276 INTEPATH il2_stat5pathway:IL2 signaling events mediated by STAT5 T80276 INTEPATH il23pathway:IL23-mediated signaling events T80276 INTEPATH il3_pathway:IL3-mediated signaling events T80276 INTEPATH il4_2pathway:IL4-mediated signaling events T80276 INTEPATH il5_pathway:IL5-mediated signaling events T80276 INTEPATH il6_7pathway:IL6-mediated signaling events T80276 INTEPATH insulin_pathway:Insulin Pathway T80276 INTEPATH kitpathway:Signaling events mediated by Stem cell factor receptor (c-Kit) T80276 INTEPATH lymphangiogenesis_pathway:VEGFR3 signaling in lymphatic endothelium T80276 INTEPATH met_pathway:Signaling events mediated by Hepatocyte Growth Factor Receptor (c-Met) T80276 INTEPATH ncadherinpathway:N-cadherin signaling events T80276 INTEPATH nectin_pathway:Nectin adhesion pathway T80276 INTEPATH nephrin_neph1_pathway:Nephrin/Neph1 signaling in the kidney podocyte T80276 INTEPATH netrin_pathway:Netrin-mediated signaling events T80276 INTEPATH nfkappabatypicalpathway:Atypical NF-kappaB pathway T80276 INTEPATH p75ntrpathway:p75(NTR)-mediated signaling T80276 INTEPATH pdgfrapathway:PDGFR-alpha signaling pathway T80276 INTEPATH pdgfrbpathway:PDGFR-beta signaling pathway T80276 INTEPATH pi3kcipathway:Class I PI3K signaling events T80276 INTEPATH pi3kplctrkpathway:Trk receptor signaling mediated by PI3K and PLC-gamma T80276 INTEPATH ptp1bpathway:Signaling events mediated by PTP1B T80276 INTEPATH reelinpathway:Reelin signaling pathway T80276 INTEPATH ret_pathway:Signaling events regulated by Ret tyrosine kinase T80276 INTEPATH shp2_pathway:SHP2 signaling T80276 INTEPATH tcptp_pathway:Signaling events mediated by TCPTP T80276 INTEPATH thrombin_par1_pathway:PAR1-mediated thrombin signaling events T80276 INTEPATH trail_pathway:TRAIL signaling pathway T80276 INTEPATH trkrpathway:Neurotrophic factor-mediated Trk receptor signaling T80276 INTEPATH vegfr1_2_pathway:Signaling events mediated by VEGFR1 and VEGFR2 T80276 INTEPATH vegfr1_pathway:VEGFR1 specific signals T80276 PANTPATH P00005:Angiogenesis T80276 PANTPATH P00006:Apoptosis signaling pathway T80276 PANTPATH P00009:Axon guidance mediated by netrin T80276 PANTPATH P00010:B cell activation T80276 PANTPATH P00018:EGF receptor signaling pathway T80276 PANTPATH P00019:Endothelin signaling pathway T80276 PANTPATH P00021:FGF signaling pathway T80276 PANTPATH P00030:Hypoxia response via HIF activation T80276 PANTPATH P00031:Inflammation mediated by chemokine and cytokine signaling pathway T80276 PANTPATH P00033:Insulin/IGF pathway-protein kinase B signaling cascade T80276 PANTPATH P00034:Integrin signalling pathway T80276 PANTPATH P00036:Interleukin signaling pathway T80276 PANTPATH P00047:PDGF signaling pathway T80276 PANTPATH P00048:PI3 kinase pathway T80276 PANTPATH P00053:T cell activation T80276 PANTPATH P00056:VEGF signaling pathway T80276 PANTPATH P00059:p53 pathway T80276 PANTPATH P04393:Ras Pathway T80276 PANTPATH P04398:p53 pathway feedback loops 2 T80276 BIOCPATH PWY-6352:3-phosphoinositide biosynthesis T80276 BIOCPATH PWY-6371:Superpathway of inositol phosphate compounds T62431 TARGETID T62431 T62431 FORMERID TTDC00156 T62431 UNIPROID KSYK_HUMAN T62431 TARGNAME Tyrosine-protein kinase SYK (SYK) T62431 GENENAME SYK T62431 TARGTYPE Successful target T62431 SYNONYMS p72-Syk; Spleen tyrosine kinase T62431 FUNCTION Regulates several biological processes including innate and adaptive immunity, cell adhesion, osteoclast maturation, platelet activation and vascular development. Assembles into signaling complexes with activated receptors at the plasma membrane via interaction between its SH2 domains and the receptor tyrosine-phosphorylated ITAM domains. The association with the receptor can also be indirect and mediated by adapter proteins containing ITAM or partial hemITAM domains. The phosphorylation of the ITAM domains is generally mediated by SRC subfamily kinases upon engagement of the receptor. More rarely signal transduction via SYK could be ITAM-independent. Direct downstream effectors phosphorylated by SYK include VAV1, PLCG1, PI-3-kinase, LCP2 and BLNK. Initially identified as essential in B-cell receptor (BCR) signaling, it is necessary for the maturation of B-cells most probably at the pro-B to pre-B transition. Activated upon BCR engagement, it phosphorylates and activates BLNK an adapter linking the activated BCR to downstream signaling adapters and effectors. It also phosphorylates and activates PLCG1 and the PKC signaling pathway. It also phosphorylates BTK and regulates its activity in B-cell antigen receptor (BCR)-coupled signaling. In addition to its function downstream of BCR plays also a role in T-cell receptor signaling. Plays also a crucial role in the innate immune response to fungal, bacterial and viral pathogens. It is for instance activated by the membrane lectin CLEC7A. Upon stimulation by fungal proteins, CLEC7A together with SYK activates immune cells inducing the production of ROS. Also activates the inflammasome and NF-kappa-B-mediated transcription of chemokines and cytokines in presence of pathogens. Regulates neutrophil degranulation and phagocytosis through activation of the MAPK signaling cascade. Required for the stimulation of neutrophil phagocytosis by IL15. Also mediates the activation of dendritic cells by cell necrosis stimuli. Also involved in mast cells activation. Involved in interleukin-3/IL3-mediated signaling pathway in basophils. Also functions downstream of receptors mediating cell adhesion. Relays for instance, integrin-mediated neutrophils and macrophages activation and P-selectin receptor/SELPG-mediated recruitment of leukocytes to inflammatory loci. Plays also a role in non-immune processes. It is for instance involved in vascular development where it may regulate blood and lymphatic vascular separation. It is also required for osteoclast development and function. Functions in the activation of platelets by collagen, mediating PLCG2 phosphorylation and activation. May be coupled to the collagen receptor by the ITAM domain-containing FCER1G. Also activated by the membrane lectin CLEC1B that is required for activation of platelets by PDPN/podoplanin. Involved in platelet adhesion being activated by ITGB3 engaged by fibrinogen. Together with CEACAM20, enhances production of the cytokine CXCL8/IL-8 via the NFKB pathway and may thus have a role in the intestinal immune response. Non-receptor tyrosine kinase which mediates signal transduction downstream of a variety of transmembrane receptors including classical immunoreceptors like the B-cell receptor (BCR). T62431 PDBSTRUC 6HM7; 6HM6; 5Y5U; 5Y5T; 5TT7 T62431 BIOCLASS Kinase T62431 ECNUMBER EC 2.7.10.2 T62431 SEQUENCE MASSGMADSANHLPFFFGNITREEAEDYLVQGGMSDGLYLLRQSRNYLGGFALSVAHGRKAHHYTIERELNGTYAIAGGRTHASPADLCHYHSQESDGLVCLLKKPFNRPQGVQPKTGPFEDLKENLIREYVKQTWNLQGQALEQAIISQKPQLEKLIATTAHEKMPWFHGKISREESEQIVLIGSKTNGKFLIRARDNNGSYALCLLHEGKVLHYRIDKDKTGKLSIPEGKKFDTLWQLVEHYSYKADGLLRVLTVPCQKIGTQGNVNFGGRPQLPGSHPATWSAGGIISRIKSYSFPKPGHRKSSPAQGNRQESTVSFNPYEPELAPWAADKGPQREALPMDTEVYESPYADPEEIRPKEVYLDRKLLTLEDKELGSGNFGTVKKGYYQMKKVVKTVAVKILKNEANDPALKDELLAEANVMQQLDNPYIVRMIGICEAESWMLVMEMAELGPLNKYLQQNRHVKDKNIIELVHQVSMGMKYLEESNFVHRDLAARNVLLVTQHYAKISDFGLSKALRADENYYKAQTHGKWPVKWYAPECINYYKFSSKSDVWSFGVLMWEAFSYGQKPYRGMKGSEVTAMLEKGERMGCPAGCPREMYDLMNLCWTYDVENRPGFAAVELRLRNYYYDVVN T62431 DRUGINFO D0V8HJ Fostamatinib Approved T62431 DRUGINFO D00OPX Fostamatinib disodium Phase 3 T62431 DRUGINFO D0BI3N Cerdulatinib Phase 2 T62431 DRUGINFO D0BW6F GS-9876 Phase 2 T62431 DRUGINFO D0G9AW GS-9973 Phase 2 T62431 DRUGINFO D06KTJ TAK-659 Phase 2 T62431 DRUGINFO DI1VM3 HM43239 Phase 1/2 T62431 DRUGINFO D0H2HZ GSK2646264 Phase 1 T62431 DRUGINFO DODG42 HMPL-523 Phase 1 T62431 DRUGINFO D0R9IU PRT-062607 Phase 1 T62431 DRUGINFO D0C0SZ PRT6207 Phase 1 T62431 DRUGINFO D01IDW SKI-O-703 Phase 1 T62431 DRUGINFO D0S6TK tamatinib Clinical trial T62431 DRUGINFO D0CD6Y Pyrimidopyridazinone derivative 1 Patented T62431 DRUGINFO D0WA1V Pyrimidopyridazinone derivative 2 Patented T62431 DRUGINFO D0JU1R Pyrrolo-pyrazine derivative 3 Patented T62431 DRUGINFO D0Y6ON Pyrrolo-pyrazine derivative 4 Patented T62431 DRUGINFO D08DBE R-343 Discontinued in Phase 2 T62431 DRUGINFO D0Y2XQ PF-3526299 Discontinued in Phase 1 T62431 DRUGINFO D00EIL CG-103065 Investigative T62431 DRUGINFO D0J3FK DNX-2000 Investigative T62431 DRUGINFO D0A1CM ELLAGIC ACID Investigative T62431 DRUGINFO D0T4MJ K00592a Investigative T62431 DRUGINFO D0C7AS N-Benzyl-4-(2,5-dihydroxy-benzylamino)-benzamide Investigative T62431 DRUGINFO D04TLI PMID17600705C23 Investigative T62431 DRUGINFO D0O6OH PMID23312943C21 Investigative T62431 DRUGINFO D09KEB PRT-060318 Investigative T62431 DRUGINFO D03YUW SBB007833 Investigative T62431 DRUGINFO D04LGK VRT-750018 Investigative T62431 KEGGPATH hsa04064:NF-kappa B signaling pathway T62431 KEGGPATH hsa04151:PI3K-Akt signaling pathway T62431 KEGGPATH hsa04380:Osteoclast differentiation T62431 KEGGPATH hsa04611:Platelet activation T62431 KEGGPATH hsa04650:Natural killer cell mediated cytotoxicity T62431 KEGGPATH hsa04662:B cell receptor signaling pathway T62431 KEGGPATH hsa04664:Fc epsilon RI signaling pathway T62431 KEGGPATH hsa04666:Fc gamma R-mediated phagocytosis T62431 KEGGPATH hsa05152:Tuberculosis T62431 KEGGPATH hsa05169:Epstein-Barr virus infection T62431 KEGGPATH hsa05203:Viral carcinogenesis T62431 WIKIPATH WP127:IL-5 Signaling Pathway T62431 WIKIPATH WP1449:Regulation of toll-like receptor signaling pathway T62431 WIKIPATH WP1826:GPVI-mediated activation cascade T62431 WIKIPATH WP1832:Integrin alphaIIb beta3 signaling T62431 WIKIPATH WP2018:RANKL/RANK Signaling Pathway T62431 WIKIPATH WP23:B Cell Receptor Signaling Pathway T62431 WIKIPATH WP2694:DAP12 interactions T62431 WIKIPATH WP2719:Fcgamma receptor (FCGR) dependent phagocytosis T62431 WIKIPATH WP2732:Interleukin-2 signaling T62431 WIKIPATH WP2746:Signaling by the B Cell Receptor (BCR) T62431 WIKIPATH WP2759:Fc epsilon receptor (FCERI) signaling T62431 WIKIPATH WP286:IL-3 Signaling Pathway T62431 WIKIPATH WP49:IL-2 Signaling Pathway T62431 WHIZPATH PW000453:Fc Epsilon Receptor I Signaling in Mast Cells T62431 REACPATH R-HSA-114604:GPVI-mediated activation cascade T62431 REACPATH R-HSA-2029481:FCGR activation T62431 REACPATH R-HSA-2029482:Regulation of actin dynamics for phagocytic cup formation T62431 REACPATH R-HSA-2029485:Role of phospholipids in phagocytosis T62431 REACPATH R-HSA-2424491:DAP12 signaling T62431 REACPATH R-HSA-2454202:Fc epsilon receptor (FCERI) signaling T62431 REACPATH R-HSA-2730905:Role of LAT2/NTAL/LAB on calcium mobilization T62431 REACPATH R-HSA-2871796:FCERI mediated MAPK activation T62431 REACPATH R-HSA-2871809:FCERI mediated Ca+2 mobilization T62431 REACPATH R-HSA-354192:Integrin alphaIIb beta3 signaling T62431 REACPATH R-HSA-451927:Interleukin-2 signaling T62431 REACPATH R-HSA-5607764:CLEC7A (Dectin-1) signaling T62431 REACPATH R-HSA-5621480:Dectin-2 family T62431 REACPATH R-HSA-912631:Regulation of signaling by CBL T62431 REACPATH R-HSA-983695:Antigen activates B Cell Receptor (BCR) leading to generation of second messengers T62431 INTEPATH alphasynuclein_pathway:Alpha-synuclein signaling T62431 INTEPATH avb3_opn_pathway:Osteopontin-mediated events T62431 INTEPATH bcr_5pathway:BCR signaling pathway T62431 INTEPATH faspathway:FAS (CD95) signaling pathway T62431 INTEPATH fcer1pathway:Fc-epsilon receptor I signaling in mast cells T62431 INTEPATH gmcsf_pathway:GMCSF-mediated signaling events T62431 INTEPATH il2_1pathway:IL2-mediated signaling events T62431 INTEPATH nfkappabatypicalpathway:Atypical NF-kappaB pathway T62431 INTEPATH pi3kcipathway:Class I PI3K signaling events T62431 INTEPATH txa2pathway:Thromboxane A2 receptor signaling T62431 PANTPATH P00010:B cell activation T97613 TARGETID T97613 T97613 FORMERID TTDI01766 T97613 UNIPROID MTR1A_HUMAN T97613 TARGNAME Melatonin receptor type 1A (MTNR1A) T97613 GENENAME MTNR1A T97613 TARGTYPE Successful target T97613 SYNONYMS Mel1a receptor; Mel1AR; Mel-1A-R T97613 FUNCTION Likely to mediate the reproductive and circadian actions of melatonin. The activity of this receptor is mediated by pertussis toxin sensitive G proteins that inhibit adenylate cyclase activity. High affinity receptor for melatonin. T97613 PDBSTRUC 6ME5; 6ME4; 6ME3; 6ME2 T97613 BIOCLASS GPCR rhodopsin T97613 SEQUENCE MQGNGSALPNASQPVLRGDGARPSWLASALACVLIFTIVVDILGNLLVILSVYRNKKLRNAGNIFVVSLAVADLVVAIYPYPLVLMSIFNNGWNLGYLHCQVSGFLMGLSVIGSIFNITGIAINRYCYICHSLKYDKLYSSKNSLCYVLLIWLLTLAAVLPNLRAGTLQYDPRIYSCTFAQSVSSAYTIAVVVFHFLVPMIIVIFCYLRIWILVLQVRQRVKPDRKPKLKPQDFRNFVTMFVVFVLFAICWAPLNFIGLAVASDPASMVPRIPEWLFVASYYMAYFNSCLNAIIYGLLNQNFRKEYRRIIVSLCTARVFFVDSSNDVADRVKWKPSPLMTNNNVVKVDSV T97613 DRUGINFO D0AN7B Melatonin Approved T97613 DRUGINFO D0U0KW Ramelteon Approved T97613 DRUGINFO D0Q5MQ Tasimelteon Approved T97613 DRUGINFO D0D8FN LY-156735 Phase 2 T97613 DRUGINFO D00CVJ Neu-P11 Phase 2 T97613 DRUGINFO D0Y8UB Agomelatine Withdrawn from market T97613 DRUGINFO D0B2CQ GR-131663 Terminated T97613 DRUGINFO D0B1VQ GR-133347 Terminated T97613 DRUGINFO D01ESJ Luzindole Terminated T97613 DRUGINFO D05GOM S-20928 Terminated T97613 DRUGINFO D0T4XV SL-18.1616 Terminated T97613 DRUGINFO D07BKH (hydroxymethylphenyl)agomelatine Investigative T97613 DRUGINFO D0Q3WV [125I]DIV880 Investigative T97613 DRUGINFO D09HWZ [125I]S70254 Investigative T97613 DRUGINFO D01YDR [125I]SD6 Investigative T97613 DRUGINFO D0S3NS 2-(indolin-1yl)-melatonin Investigative T97613 DRUGINFO D08WOV 2-[125I]melatonin Investigative T97613 DRUGINFO D0H6YF 2-iodo-melatonin Investigative T97613 DRUGINFO D03OGA 2-methoxy-alpha,beta-didehydro-agomelatine Investigative T97613 DRUGINFO D0T2RY 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Investigative T97613 DRUGINFO D04VGL 4P-PDOT Investigative T97613 DRUGINFO D08SGV 5-HEAT Investigative T97613 DRUGINFO D01LAU 5-methoxycarbonylamino-N-acetyltryptamine Investigative T97613 DRUGINFO D0RF4L 5-methoxy-luzindole Investigative T97613 DRUGINFO D0B8PD 6-Cl-MLT Investigative T97613 DRUGINFO D0S6SN 6-hydroxymelatonin Investigative T97613 DRUGINFO D0I4DJ AAE-M-PBP-amine Investigative T97613 DRUGINFO D0Q6HT Beta,beta-dimethylmelatonin Investigative T97613 DRUGINFO D05EDR Beta-methylmelatonin Investigative T97613 DRUGINFO D08TBF BOMPPA Investigative T97613 DRUGINFO D07MFG CBOBNEA Investigative T97613 DRUGINFO D0Y2JY CIFEA Investigative T97613 DRUGINFO D0XX9Y DH97 Investigative T97613 DRUGINFO D04BLO difluoroagomelatine Investigative T97613 DRUGINFO D07YFL EFPPEA Investigative T97613 DRUGINFO D09LPG GR 128107 Investigative T97613 DRUGINFO D02VIZ GR 196429 Investigative T97613 DRUGINFO D01SNS IIK7 Investigative T97613 DRUGINFO D08ZJM isoamyl-agomelatine Investigative T97613 DRUGINFO D0WE4C K185 Investigative T97613 DRUGINFO D0O2GK N-(2-(5-methoxybenzofuran-3-yl)ethyl)acetamide Investigative T97613 DRUGINFO D01FVY N-(2,3,4,9-Tetrahydro-1H-carbazol-3-yl)-acetamide Investigative T97613 DRUGINFO D07FDL N-(2,3-Dihydro-1H-phenalen-2-yl)-acetamide Investigative T97613 DRUGINFO D0W7ZB N-(3-(2,5-dimethoxyphenyl)propyl)acetamide Investigative T97613 DRUGINFO D01UIY N-(3-(2-ethoxy-5-methoxyphenyl)propyl)acetamide Investigative T97613 DRUGINFO D0F6VI N-(3-(2-hydroxy-5-methoxyphenyl)propyl)acetamide Investigative T97613 DRUGINFO D0V7VF N-(3-(3-methoxyphenyl)-3-phenylallyl)acetamide Investigative T97613 DRUGINFO D0U8OS N-(3-(3-methoxyphenyl)propyl)acetamide Investigative T97613 DRUGINFO D0D6IK N-(3-(3-methoxyphenyl)propyl)propionamide Investigative T97613 DRUGINFO D07ZQU N-(3-(4-hydroxy-3-methoxyphenyl)propyl)acetamide Investigative T97613 DRUGINFO D09ETU N-(3-(5-methoxy-2-propoxyphenyl)propyl)acetamide Investigative T97613 DRUGINFO D0F9ZW N-acetylserotonin Investigative T97613 DRUGINFO D04YWX S22153 Investigative T97613 DRUGINFO D0Q0LH S24014 Investigative T97613 DRUGINFO D07EOD S24773 Investigative T97613 DRUGINFO D0R5JD S26131 Investigative T97613 DRUGINFO D06AUM S26284 Investigative T97613 DRUGINFO D0OY8Y UCM 549 Investigative T97613 DRUGINFO D0YN8Q UCM 724 Investigative T97613 DRUGINFO D0TM0N UCM 765 Investigative T97613 DRUGINFO D0K1HD UCM 793 Investigative T97613 DRUGINFO D05WKI UCM-454 Investigative T97613 KEGGPATH hsa04080:Neuroactive ligand-receptor interaction T97613 KEGGPATH hsa04713:Circadian entrainment T97613 WIKIPATH WP1824:GPCR downstream signaling T97613 WIKIPATH WP1825:GPCR ligand binding T97613 WIKIPATH WP247:Small Ligand GPCRs T97613 WIKIPATH WP455:GPCRs, Class A Rhodopsin-like T97613 REACPATH R-HSA-373076:Class A/1 (Rhodopsin-like receptors) T97613 REACPATH R-HSA-418594:G alpha (i) signalling events T95913 TARGETID T95913 T95913 FORMERID TTDR00356 T95913 UNIPROID PK3CG_HUMAN T95913 TARGNAME PI3-kinase gamma (PIK3CG) T95913 GENENAME PIK3CG T95913 TARGTYPE Successful target T95913 SYNONYMS p120-PI3K; p110gamma; Serine/threonine protein kinase PIK3CG; PtdIns-3-kinase subunit p110-gamma; PtdIns-3-kinase subunit gamma; PtdIns-3-kinase p110; Phosphoinositol-3 kinase; Phosphoinositide-3-kinase catalytic gamma polypeptide; Phosphoinositide 3-Kinase gamma; Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit, gamma isoform; Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform; Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit gamma; PI3Kgamma; PI3K-gamma; PI3K; PI3-kinase subunit gamma; PI3-kinase p110 subunit gamma T95913 FUNCTION Phosphoinositide-3-kinase (PI3K) that phosphorylates PtdIns(4,5)P2 (Phosphatidylinositol 4,5-bisphosphate) to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3). PIP3 plays a key role by recruiting PH domain-containing proteins to the membrane, including AKT1 and PDPK1, activating signaling cascades involved in cell growth, survival, proliferation, motility and morphology. Links G-protein coupled receptor activation to PIP3 production. Involved in immune, inflammatory and allergic responses. Modulates leukocyte chemotaxis to inflammatory sites and in response to chemoattractant agents. May control leukocyte polarization and migration by regulating the spatial accumulation of PIP3 and by regulating the organization of F-actin formation and integrin-based adhesion at the leading edge. Controls motility of dendritic cells. Together with PIK3CD is involved in natural killer (NK) cell development and migration towards the sites of inflammation. Participates in T-lymphocyte migration. Regulates T-lymphocyte proliferation and cytokine production. Together with PIK3CD participates in T-lymphocyte development. Required for B-lymphocyte development and signaling. Together with PIK3CD participates in neutrophil respiratory burst. Together with PIK3CD is involved in neutrophil chemotaxis and extravasation. Together with PIK3CB promotes platelet aggregation and thrombosis. Regulates alpha-IIb/beta-3 integrins (ITGA2B/ ITGB3) adhesive function in platelets downstream of P2Y12 through a lipid kinase activity-independent mechanism. May have also a lipid kinase activity-dependent function in platelet aggregation. Involved in endothelial progenitor cell migration. Negative regulator of cardiac contractility. Modulates cardiac contractility by anchoring protein kinase A (PKA) and PDE3B activation, reducing cAMP levels. Regulates cardiac contractility also by promoting beta-adrenergic receptor internalization by binding to GRK2 and by non-muscle tropomyosin phosphorylation. Also has serine/threonine protein kinase activity: both lipid and protein kinase activities are required for beta-adrenergic receptor endocytosis. May also have a scaffolding role in modulating cardiac contractility. Contributes to cardiac hypertrophy under pathological stress. Through simultaneous binding of PDE3B to RAPGEF3 and PIK3R6 is assembled in a signaling complex in which the PI3K gamma complex is activated by RAPGEF3 and which is involved in angiogenesis. T95913 PDBSTRUC 6GQ7; 6FH5; 6C1S; 6AUD; 5T23 T95913 BIOCLASS Kinase T95913 ECNUMBER EC 2.7.1.153 T95913 SEQUENCE MELENYKQPVVLREDNCRRRRRMKPRSAAASLSSMELIPIEFVLPTSQRKCKSPETALLHVAGHGNVEQMKAQVWLRALETSVAADFYHRLGPHHFLLLYQKKGQWYEIYDKYQVVQTLDCLRYWKATHRSPGQIHLVQRHPPSEESQAFQRQLTALIGYDVTDVSNVHDDELEFTRRGLVTPRMAEVASRDPKLYAMHPWVTSKPLPEYLWKKIANNCIFIVIHRSTTSQTIKVSPDDTPGAILQSFFTKMAKKKSLMDIPESQSEQDFVLRVCGRDEYLVGETPIKNFQWVRHCLKNGEEIHVVLDTPPDPALDEVRKEEWPLVDDCTGVTGYHEQLTIHGKDHESVFTVSLWDCDRKFRVKIRGIDIPVLPRNTDLTVFVEANIQHGQQVLCQRRTSPKPFTEEVLWNVWLEFSIKIKDLPKGALLNLQIYCGKAPALSSKASAESPSSESKGKVQLLYYVNLLLIDHRFLLRRGEYVLHMWQISGKGEDQGSFNADKLTSATNPDKENSMSISILLDNYCHPIALPKHQPTPDPEGDRVRAEMPNQLRKQLEAIIATDPLNPLTAEDKELLWHFRYESLKHPKAYPKLFSSVKWGQQEIVAKTYQLLARREVWDQSALDVGLTMQLLDCNFSDENVRAIAVQKLESLEDDDVLHYLLQLVQAVKFEPYHDSALARFLLKRGLRNKRIGHFLFWFLRSEIAQSRHYQQRFAVILEAYLRGCGTAMLHDFTQQVQVIEMLQKVTLDIKSLSAEKYDVSSQVISQLKQKLENLQNSQLPESFRVPYDPGLKAGALAIEKCKVMASKKKPLWLEFKCADPTALSNETIGIIFKHGDDLRQDMLILQILRIMESIWETESLDLCLLPYGCISTGDKIGMIEIVKDATTIAKIQQSTVGNTGAFKDEVLNHWLKEKSPTEEKFQAAVERFVYSCAGYCVATFVLGIGDRHNDNIMITETGNLFHIDFGHILGNYKSFLGINKERVPFVLTPDFLFVMGTSGKKTSPHFQKFQDICVKAYLALRHHTNLLIILFSMMLMTGMPQLTSKEDIEYIRDALTVGKNEEDAKKYFLDQIEVCRDKGWTVQFNWFLHLVLGIKQGEKHSA T95913 DRUGINFO D0S5LD BAY 80-6946 Approved T95913 DRUGINFO D0RU0O IPI-145 Approved T95913 DRUGINFO D01QSO Buparlisib Phase 3 T95913 DRUGINFO D0I6VU Enzastaurin Phase 3 T95913 DRUGINFO D0UP1Z GDC-0032 Phase 3 T95913 DRUGINFO D0KF9Q Rigosertib Phase 3 T95913 DRUGINFO D0VG0D BEZ235 Phase 2 T95913 DRUGINFO D03KHN CLR-1404 Phase 2 T95913 DRUGINFO D0GW8X GDC-0077 Phase 2 T95913 DRUGINFO D07BGC GDC-0084 Phase 2 T95913 DRUGINFO D08QGT GDC0941 Phase 2 T95913 DRUGINFO D0O6VZ GDC-0980/RG7422 Phase 2 T95913 DRUGINFO D0I3LO IPI-549 Phase 2 T95913 DRUGINFO D0N5JZ PF-04691502 Phase 2 T95913 DRUGINFO D0D8JB PF-05212384 Phase 2 T95913 DRUGINFO D0TU7B PQR309 Phase 2 T95913 DRUGINFO D0AW5T PX-866 Phase 2 T95913 DRUGINFO D01PGR SAR245409 Phase 2 T95913 DRUGINFO D03NJY SF1126 Phase 2 T95913 DRUGINFO D03KAC XL147 Phase 2 T95913 DRUGINFO D0X7IN BGT226 Phase 1/2 T95913 DRUGINFO D07MEX CLR-1401 Phase 1/2 T95913 DRUGINFO D07ACZ CLR457 Phase 1/2 T95913 DRUGINFO D0E6UZ CUDC-907 Phase 1/2 T95913 DRUGINFO D05CBJ PA-799 Phase 1/2 T95913 DRUGINFO D0C3ZR TG100-115 Phase 1/2 T95913 DRUGINFO D03BHZ AZD8186 Phase 1 T95913 DRUGINFO D0X4RT DS-7423 Phase 1 T95913 DRUGINFO D03EZE GSK2126458 Phase 1 T95913 DRUGINFO D0J8MA KA2237 Phase 1 T95913 DRUGINFO D09SFV LY294002 Phase 1 T95913 DRUGINFO D0R8ID P-7170 Phase 1 T95913 DRUGINFO D0R1VU Perifosine Phase 1 T95913 DRUGINFO D0U3DP VS-5584 Phase 1 T95913 DRUGINFO D0O1LD ZSTK474 Phase 1 T95913 DRUGINFO D02CQL Adyvia Discontinued in Phase 2 T95913 DRUGINFO D0L0ZC GSK1059615 Discontinued in Phase 1 T95913 DRUGINFO D0T5IN PX-867 Terminated T95913 DRUGINFO D05SXC SCR-44001 Terminated T95913 DRUGINFO D0P1JI Wortmannin Terminated T95913 DRUGINFO D05BPX 3-(4-morpholinothieno[3,2-d]pyrimidin-2-yl)phenol Investigative T95913 DRUGINFO D08NQM 5-QUINOXALIN-6-YLMETHYLENE-THIAZOLIDINE-2,4-DIONE Investigative T95913 DRUGINFO D03FIE AEZS-126 Investigative T95913 DRUGINFO D03DRM AS-604850 Investigative T95913 DRUGINFO D04DBA BAG956 Investigative T95913 DRUGINFO D0JD4S CU-906 Investigative T95913 DRUGINFO D06PWI CZC 24832 Investigative T95913 DRUGINFO D00LZO CZC-19091 Investigative T95913 DRUGINFO D0W1ST Ethyl 1-[(1H-benzimidazol-2(3H)one-5-yl)sulfonyl]-1H-pyrrole-2-carboxylate Investigative T95913 DRUGINFO D0J1CF Her2- and PSA-targeted TGX-D1 Investigative T95913 DRUGINFO D02ELN HM-5016699 Investigative T95913 DRUGINFO D0R2UG HS-173 Investigative T95913 DRUGINFO D0R0TW KU-0060648 Investigative T95913 DRUGINFO D02WGD LOR-220 Investigative T95913 DRUGINFO D07APP LY-292223 Investigative T95913 DRUGINFO D0O6JE Multiform PI3K inhibitors Investigative T95913 DRUGINFO D0T3PW Myricetin Investigative T95913 DRUGINFO D0QE9F P-6915 Investigative T95913 DRUGINFO D05RSS PF-03772304 Investigative T95913 DRUGINFO D00JIV PF-4989216 Investigative T95913 DRUGINFO D0W8XH PI-103 Investigative T95913 DRUGINFO D01SSI PI-3065 Investigative T95913 DRUGINFO D00HSJ PIK-75 Investigative T95913 DRUGINFO D07PMP PKI-402 Investigative T95913 DRUGINFO D03EHM PP121 Investigative T95913 DRUGINFO D06DNH TGX-221 Investigative T95913 DRUGINFO D08RBS WX-037 Investigative T95913 KEGGPATH hsa00562:Inositol phosphate metabolism T95913 KEGGPATH hsa04012:ErbB signaling pathway T95913 KEGGPATH hsa04014:Ras signaling pathway T95913 KEGGPATH hsa04015:Rap1 signaling pathway T95913 KEGGPATH hsa04022:cGMP-PKG signaling pathway T95913 KEGGPATH hsa04024:cAMP signaling pathway T95913 KEGGPATH hsa04062:Chemokine signaling pathway T95913 KEGGPATH hsa04066:HIF-1 signaling pathway T95913 KEGGPATH hsa04068:FoxO signaling pathway T95913 KEGGPATH hsa04070:Phosphatidylinositol signaling system T95913 KEGGPATH hsa04071:Sphingolipid signaling pathway T95913 KEGGPATH hsa04150:mTOR signaling pathway T95913 KEGGPATH hsa04151:PI3K-Akt signaling pathway T95913 KEGGPATH hsa04152:AMPK signaling pathway T95913 KEGGPATH hsa04210:Apoptosis T95913 KEGGPATH hsa04261:Adrenergic signaling in cardiomyocytes T95913 KEGGPATH hsa04370:VEGF signaling pathway T95913 KEGGPATH hsa04380:Osteoclast differentiation T95913 KEGGPATH hsa04510:Focal adhesion T95913 KEGGPATH hsa04550:Signaling pathways regulating pluripotency of stem cells T95913 KEGGPATH hsa04611:Platelet activation T95913 KEGGPATH hsa04620:Toll-like receptor signaling pathway T95913 KEGGPATH hsa04630:Jak-STAT signaling pathway T95913 KEGGPATH hsa04650:Natural killer cell mediated cytotoxicity T95913 KEGGPATH hsa04660:T cell receptor signaling pathway T95913 KEGGPATH hsa04662:B cell receptor signaling pathway T95913 KEGGPATH hsa04664:Fc epsilon RI signaling pathway T95913 KEGGPATH hsa04666:Fc gamma R-mediated phagocytosis T95913 KEGGPATH hsa04668:TNF signaling pathway T95913 KEGGPATH hsa04670:Leukocyte transendothelial migration T95913 KEGGPATH hsa04722:Neurotrophin signaling pathway T95913 KEGGPATH hsa04725:Cholinergic synapse T95913 KEGGPATH hsa04750:Inflammatory mediator regulation of TRP channels T95913 KEGGPATH hsa04810:Regulation of actin cytoskeleton T95913 KEGGPATH hsa04910:Insulin signaling pathway T95913 KEGGPATH hsa04914:Progesterone-mediated oocyte maturation T95913 KEGGPATH hsa04915:Estrogen signaling pathway T95913 KEGGPATH hsa04917:Prolactin signaling pathway T95913 KEGGPATH hsa04919:Thyroid hormone signaling pathway T95913 KEGGPATH hsa04921:Oxytocin signaling pathway T95913 KEGGPATH hsa04923:Regulation of lipolysis in adipocytes T95913 KEGGPATH hsa04930:Type II diabetes mellitus T95913 KEGGPATH hsa04932:Non-alcoholic fatty liver disease (NAFLD) T95913 KEGGPATH hsa04960:Aldosterone-regulated sodium reabsorption T95913 KEGGPATH hsa04973:Carbohydrate digestion and absorption T95913 KEGGPATH hsa05100:Bacterial invasion of epithelial cells T95913 KEGGPATH hsa05142:Chagas disease (American trypanosomiasis) T95913 KEGGPATH hsa05145:Toxoplasmosis T95913 KEGGPATH hsa05146:Amoebiasis T95913 KEGGPATH hsa05160:Hepatitis C T95913 KEGGPATH hsa05161:Hepatitis B T95913 KEGGPATH hsa05162:Measles T95913 KEGGPATH hsa05164:Influenza A T95913 KEGGPATH hsa05166:HTLV-I infection T95913 KEGGPATH hsa05169:Epstein-Barr virus infection T95913 KEGGPATH hsa05200:Pathways in cancer T95913 KEGGPATH hsa05203:Viral carcinogenesis T95913 KEGGPATH hsa05205:Proteoglycans in cancer T95913 KEGGPATH hsa05206:MicroRNAs in cancer T95913 KEGGPATH hsa05210:Colorectal cancer T95913 KEGGPATH hsa05211:Renal cell carcinoma T95913 KEGGPATH hsa05212:Pancreatic cancer T95913 KEGGPATH hsa05213:Endometrial cancer T95913 KEGGPATH hsa05214:Glioma T95913 KEGGPATH hsa05215:Prostate cancer T95913 KEGGPATH hsa05218:Melanoma T95913 KEGGPATH hsa05220:Chronic myeloid leukemia T95913 KEGGPATH hsa05221:Acute myeloid leukemia T95913 KEGGPATH hsa05222:Small cell lung cancer T95913 KEGGPATH hsa05223:Non-small cell lung cancer T95913 KEGGPATH hsa05230:Central carbon metabolism in cancer T95913 KEGGPATH hsa05231:Choline metabolism in cancer T95913 WIKIPATH WP1403:AMPK Signaling T95913 WIKIPATH WP1449:Regulation of toll-like receptor signaling pathway T95913 WIKIPATH WP1539:Angiogenesis T95913 WIKIPATH WP1544:MicroRNAs in cardiomyocyte hypertrophy T95913 WIKIPATH WP1794:Cell surface interactions at the vascular wall T95913 WIKIPATH WP1799:Costimulation by the CD28 family T95913 WIKIPATH WP1824:GPCR downstream signaling T95913 WIKIPATH WP1826:GPVI-mediated activation cascade T95913 WIKIPATH WP1840:Interleukin-3, 5 and GM-CSF signaling T95913 WIKIPATH WP1867:Nephrin interactions T95913 WIKIPATH WP1873:NGF signalling via TRKA from the plasma membrane T95913 WIKIPATH WP1910:Signaling by EGFR T95913 WIKIPATH WP1911:Signaling by FGFR T95913 WIKIPATH WP1913:Signaling by Insulin receptor T95913 WIKIPATH WP1916:Signaling by PDGF T95913 WIKIPATH WP1927:TCR signaling T95913 WIKIPATH WP1982:SREBP signalling T95913 WIKIPATH WP2032:TSH signaling pathway T95913 WIKIPATH WP2038:Regulation of Microtubule Cytoskeleton T95913 WIKIPATH WP2203:TSLP Signaling Pathway T95913 WIKIPATH WP2261:Signaling Pathways in Glioblastoma T95913 WIKIPATH WP2263:Prostate Cancer T95913 WIKIPATH WP2377:Integrated Pancreatic Cancer Pathway T95913 WIKIPATH WP2653:PIP3 activates AKT signaling T95913 WIKIPATH WP2664:Gastrin-CREB signalling pathway via PKC and MAPK T95913 WIKIPATH WP2677:Signaling by Type 1 Insulin-like Growth Factor 1 Receptor (IGF1R) T95913 WIKIPATH WP2694:DAP12 interactions T95913 WIKIPATH WP2713:Signaling by SCF-KIT T95913 WIKIPATH WP2719:Fcgamma receptor (FCGR) dependent phagocytosis T95913 WIKIPATH WP2732:Interleukin-2 signaling T95913 WIKIPATH WP2747:PI Metabolism T95913 WIKIPATH WP2759:Fc epsilon receptor (FCERI) signaling T95913 WIKIPATH WP2780:Signaling by ERBB2 T95913 WIKIPATH WP2781:Signaling by ERBB4 T95913 WIKIPATH WP2865:IL1 and megakaryotyces in obesity T95913 WIKIPATH WP3:Transcriptional activation by NRF2 T95913 WIKIPATH WP313:Signaling of Hepatocyte Growth Factor Receptor T95913 WIKIPATH WP3286:Copper homeostasis T95913 WIKIPATH WP395:IL-4 Signaling Pathway T95913 WIKIPATH WP481:Insulin Signaling T95913 WIKIPATH WP51:Regulation of Actin Cytoskeleton T95913 WIKIPATH WP524:G13 Signaling Pathway T95913 WIKIPATH WP710:DNA Damage Response (only ATM dependent) T95913 WIKIPATH WP722:Serotonin HTR1 Group and FOS Pathway T95913 WIKIPATH WP75:Toll-like receptor signaling pathway T95913 WHIZPATH PW000143:Inositol Metabolism T95913 WHIZPATH PW000168:Phosphatidylinositol Phosphate Metabolism T95913 WHIZPATH PW000445:Intracellular Signalling Through Adenosine Receptor A2a and Adenosine T95913 WHIZPATH PW000446:Intracellular Signalling Through Adenosine Receptor A2b and Adenosine T95913 WHIZPATH PW000453:Fc Epsilon Receptor I Signaling in Mast Cells T95913 REACPATH R-HSA-109704:PI3K Cascade T95913 REACPATH R-HSA-114604:GPVI-mediated activation cascade T95913 REACPATH R-HSA-1236382:Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants T95913 REACPATH R-HSA-1250342:PI3K events in ERBB4 signaling T95913 REACPATH R-HSA-1257604:PIP3 activates AKT signaling T95913 REACPATH R-HSA-180292:GAB1 signalosome T95913 REACPATH R-HSA-1963642:PI3K events in ERBB2 signaling T95913 REACPATH R-HSA-198203:PI3K/AKT activation T95913 REACPATH R-HSA-2029485:Role of phospholipids in phagocytosis T95913 REACPATH R-HSA-210993:Tie2 Signaling T95913 REACPATH R-HSA-2219530:Constitutive Signaling by Aberrant PI3K in Cancer T95913 REACPATH R-HSA-2424491:DAP12 signaling T95913 REACPATH R-HSA-2730905:Role of LAT2/NTAL/LAB on calcium mobilization T95913 REACPATH R-HSA-373753:Nephrin interactions T95913 REACPATH R-HSA-388841:Costimulation by the CD28 family T95913 REACPATH R-HSA-389357:CD28 dependent PI3K/Akt signaling T95913 REACPATH R-HSA-392451:G beta:gamma signalling through PI3Kgamma T95913 REACPATH R-HSA-416476:G alpha (q) signalling events T95913 REACPATH R-HSA-416482:G alpha (12/13) signalling events T95913 REACPATH R-HSA-4420097:VEGFA-VEGFR2 Pathway T95913 REACPATH R-HSA-512988:Interleukin-3, 5 and GM-CSF signaling T95913 REACPATH R-HSA-5637810:Constitutive Signaling by EGFRvIII T95913 REACPATH R-HSA-5654689:PI-3K cascade:FGFR1 T95913 REACPATH R-HSA-5654695:PI-3K cascade:FGFR2 T95913 REACPATH R-HSA-5654710:PI-3K cascade:FGFR3 T95913 REACPATH R-HSA-5654720:PI-3K cascade:FGFR4 T95913 REACPATH R-HSA-912526:Interleukin receptor SHC signaling T95913 REACPATH R-HSA-912631:Regulation of signaling by CBL T48268 TARGETID T48268 T48268 FORMERID TTDS00422 T48268 UNIPROID MTR1B_HUMAN T48268 TARGNAME Melatonin receptor type 1B (MTNR1B) T48268 GENENAME MTNR1B T48268 TARGTYPE Successful target T48268 SYNONYMS Mel1b receptor; Mel1b melatonin receptor; Mel-1B-R T48268 FUNCTION Likely to mediate the reproductive and circadian actions of melatonin. The activity of this receptor is mediated by pertussis toxin sensitive G proteins that inhibit adenylate cyclase activity. High affinity receptor for melatonin. T48268 PDBSTRUC 6ME9; 6ME8; 6ME7; 6ME6 T48268 BIOCLASS GPCR rhodopsin T48268 SEQUENCE MSENGSFANCCEAGGWAVRPGWSGAGSARPSRTPRPPWVAPALSAVLIVTTAVDVVGNLLVILSVLRNRKLRNAGNLFLVSLALADLVVAFYPYPLILVAIFYDGWALGEEHCKASAFVMGLSVIGSVFNITAIAINRYCYICHSMAYHRIYRRWHTPLHICLIWLLTVVALLPNFFVGSLEYDPRIYSCTFIQTASTQYTAAVVVIHFLLPIAVVSFCYLRIWVLVLQARRKAKPESRLCLKPSDLRSFLTMFVVFVIFAICWAPLNCIGLAVAINPQEMAPQIPEGLFVTSYLLAYFNSCLNAIVYGLLNQNFRREYKRILLALWNPRHCIQDASKGSHAEGLQSPAPPIIGVQHQADAL T48268 DRUGINFO D0U0KW Ramelteon Approved T48268 DRUGINFO D0Q5MQ Tasimelteon Approved T48268 DRUGINFO D0RL5B VLB-01 Phase 3 T48268 DRUGINFO D0H6YF 2-iodo-melatonin Investigative T48268 DRUGINFO D01LAU 5-methoxycarbonylamino-N-acetyltryptamine Investigative T48268 DRUGINFO D0Q6HT Beta,beta-dimethylmelatonin Investigative T48268 DRUGINFO D05EDR Beta-methylmelatonin Investigative T48268 DRUGINFO D0O2GK N-(2-(5-methoxybenzofuran-3-yl)ethyl)acetamide Investigative T48268 DRUGINFO D01FVY N-(2,3,4,9-Tetrahydro-1H-carbazol-3-yl)-acetamide Investigative T48268 DRUGINFO D0W7ZB N-(3-(2,5-dimethoxyphenyl)propyl)acetamide Investigative T48268 DRUGINFO D01UIY N-(3-(2-ethoxy-5-methoxyphenyl)propyl)acetamide Investigative T48268 DRUGINFO D0F6VI N-(3-(2-hydroxy-5-methoxyphenyl)propyl)acetamide Investigative T48268 DRUGINFO D0V7VF N-(3-(3-methoxyphenyl)-3-phenylallyl)acetamide Investigative T48268 DRUGINFO D0U8OS N-(3-(3-methoxyphenyl)propyl)acetamide Investigative T48268 DRUGINFO D0D6IK N-(3-(3-methoxyphenyl)propyl)propionamide Investigative T48268 DRUGINFO D07ZQU N-(3-(4-hydroxy-3-methoxyphenyl)propyl)acetamide Investigative T48268 DRUGINFO D09ETU N-(3-(5-methoxy-2-propoxyphenyl)propyl)acetamide Investigative T48268 DRUGINFO D0L9YA N-(3-Benzooxazol-7-yl-propyl)-acetamide Investigative T48268 DRUGINFO D03AJW N-(3-Benzooxazol-7-yl-propyl)-butyramide Investigative T48268 DRUGINFO D03NND N-(3-Benzooxazol-7-yl-propyl)-propionamide Investigative T48268 DRUGINFO D05TRX N-[3-(2-Ethyl-benzooxazol-7-yl)-propyl]-acetamide Investigative T48268 DRUGINFO D05WKI UCM-454 Investigative T48268 KEGGPATH hsa04080:Neuroactive ligand-receptor interaction T48268 KEGGPATH hsa04713:Circadian entrainment T48268 WIKIPATH WP1824:GPCR downstream signaling T48268 WIKIPATH WP1825:GPCR ligand binding T48268 WIKIPATH WP247:Small Ligand GPCRs T48268 WIKIPATH WP455:GPCRs, Class A Rhodopsin-like T48268 REACPATH R-HSA-373076:Class A/1 (Rhodopsin-like receptors) T48268 REACPATH R-HSA-418594:G alpha (i) signalling events T76910 TARGETID T76910 T76910 FORMERID TTDS00136 T76910 UNIPROID GSK3A_HUMAN T76910 TARGNAME Glycogen synthase kinase-3 alpha (GSK-3A) T76910 GENENAME GSK3A T76910 TARGTYPE Successful target T76910 SYNONYMS Serine/threonineprotein kinase GSK3A; Serine/threonine-protein kinase GSK3A; Glycogen synthase kinase3 alpha; Glycogen synthase kinase 3; GSK3 alpha; GSK-3 alpha; GSK-3 T76910 FUNCTION Requires primed phosphorylation of the majority of its substrates. Contributes to insulin regulation of glycogen synthesis by phosphorylating and inhibiting GYS1 activity and hence glycogen synthesis. Regulates glycogen metabolism in liver, but not in muscle. May also mediate the development of insulin resistance by regulating activation of transcription factors. In Wnt signaling, regulates the level and transcriptional activity of nuclear CTNNB1/beta-catenin. Facilitates amyloid precursor protein (APP) processing and the generation of APP-derived amyloid plaques found in Alzheimer disease. May be involved in the regulation of replication in pancreatic beta-cells. Is necessary for the establishment of neuronal polarity and axon outgrowth. Through phosphorylation of the anti-apoptotic protein MCL1, may control cell apoptosis in response to growth factors deprivation. Acts as a regulator of autophagy by mediating phosphorylation of KAT5/TIP60 under starvation conditions, leading to activate KAT5/TIP60 acetyltransferase activity and promote acetylation of key autophagy regulators, such as ULK1 and RUBCNL/Pacer. Constitutively active protein kinase that acts as a negative regulator in the hormonal control of glucose homeostasis, Wnt signaling and regulation of transcription factors and microtubules, by phosphorylating and inactivating glycogen synthase (GYS1 or GYS2), CTNNB1/beta-catenin, APC and AXIN1. T76910 PDBSTRUC 2DFM T76910 BIOCLASS Kinase T76910 ECNUMBER EC 2.7.11.26 T76910 SEQUENCE MSGGGPSGGGPGGSGRARTSSFAEPGGGGGGGGGGPGGSASGPGGTGGGKASVGAMGGGVGASSSGGGPGGSGGGGSGGPGAGTSFPPPGVKLGRDSGKVTTVVATLGQGPERSQEVAYTDIKVIGNGSFGVVYQARLAETRELVAIKKVLQDKRFKNRELQIMRKLDHCNIVRLRYFFYSSGEKKDELYLNLVLEYVPETVYRVARHFTKAKLTIPILYVKVYMYQLFRSLAYIHSQGVCHRDIKPQNLLVDPDTAVLKLCDFGSAKQLVRGEPNVSYICSRYYRAPELIFGATDYTSSIDVWSAGCVLAELLLGQPIFPGDSGVDQLVEIIKVLGTPTREQIREMNPNYTEFKFPQIKAHPWTKVFKSRTPPEAIALCSSLLEYTPSSRLSPLEACAHSFFDELRCLGTQLPNNRPLPPLFNFSAGELSIQPSLNAILIPPHLRSPAGTTTLTPSSQALTETPTSSDWQSTDATPTLTNSS T76910 DRUGINFO D0Y3KG Valproate Approved T76910 DRUGINFO D5MF8Y Lithium Phase 2 T76910 DRUGINFO D0Z1DH LY2090314 Phase 2 T76910 DRUGINFO D0A3MV AR-A014418 Patented T76910 DRUGINFO D0YK9D CHIR-99021 Patented T76910 DRUGINFO D0WX0K Indazole derivative 6 Patented T76910 DRUGINFO D0I2RF Indirubin derivative 2 Patented T76910 DRUGINFO D00PWQ KENPAULLONE Patented T76910 DRUGINFO D0NG2F Maleimides derivative 1 Patented T76910 DRUGINFO D0QW6B Maleimides derivative 2 Patented T76910 DRUGINFO D0J6UW Maleimides derivative 3 Patented T76910 DRUGINFO D0UZ7I N-naphtyl-N-benzylurea derivative 1 Patented T76910 DRUGINFO D0UL2V PMID27828716-Compound-15 Patented T76910 DRUGINFO D0P8RK PMID27828716-Compound-16 Patented T76910 DRUGINFO D0J9YX PMID27828716-Compound-17 Patented T76910 DRUGINFO D03ETN PMID27828716-Compound-18 Patented T76910 DRUGINFO D08CWE PMID27828716-Compound-19 Patented T76910 DRUGINFO D0NO7V PMID27828716-Compound-20 Patented T76910 DRUGINFO D01WAJ PMID27828716-Compound-21 Patented T76910 DRUGINFO D03SNE PMID27828716-Compound-BIO-acetoxime Patented T76910 DRUGINFO D0M9JE Pyrazole and benzimidazole derivative 1 Patented T76910 DRUGINFO D0FV9Z Pyrazolodihydropyridine derivative 1 Patented T76910 DRUGINFO D0A4QD Quinoline derivative 14 Patented T76910 DRUGINFO D04RDR Quinoline derivative 15 Patented T76910 DRUGINFO D06ZRL Quinolinyl pyrazinyl urea derivative 1 Patented T76910 DRUGINFO D0RD9V Quinolinyl pyrazinyl urea derivative 2 Patented T76910 DRUGINFO D09PGW Spiroquinolone derivative 1 Patented T76910 DRUGINFO D06KNK TDZD-8 Patented T76910 DRUGINFO D0QE2H Thiadiazolidindione derivative 1 Patented T76910 DRUGINFO D02OGA Thiadiazolidindione derivative 2 Patented T76910 DRUGINFO D0CR2E Thiadiazolidindione derivative 3 Patented T76910 DRUGINFO D0XR7S Tricyclic 5-quinolone derivative 1 Patented T76910 DRUGINFO D06OAH 6-bromoindirubin-3-oxime Investigative T76910 DRUGINFO D02BIK AR-534 Investigative T76910 DRUGINFO D0S7ZZ Benzofuran-3-yl-(indol-3-yl)maleimides Investigative T76910 DRUGINFO D07WXT Lithium chloride Investigative T76910 DRUGINFO D0A1YQ SB216763 Investigative T76910 REACPATH R-HSA-198323:AKT phosphorylates targets in the cytosol T76910 REACPATH R-HSA-381038:XBP1(S) activates chaperone genes T76910 REACPATH R-HSA-5674400:Constitutive Signaling by AKT1 E17K in Cancer T76910 NET_PATH NetPath_7:TGF_beta_Receptor Signaling Pathway T76910 INTEPATH betacatenin_deg_pathway:Degradation of beta catenin T76910 INTEPATH foxm1pathway:FOXM1 transcription factor network T76910 INTEPATH pi3kciaktpathway:Class I PI3K signaling events mediated by Akt T76910 INTEPATH wnt_canonical_pathway:Canonical Wnt signaling pathway T76910 PANTPATH P00026:Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway T76910 PANTPATH P00033:Insulin/IGF pathway-protein kinase B signaling cascade T76910 PANTPATH P00047:PDGF signaling pathway T76910 PANTPATH P04393:Ras Pathway T09960 TARGETID T09960 T09960 FORMERID TTDS00326 T09960 UNIPROID CCR5_HUMAN T09960 TARGNAME C-C chemokine receptor type 5 (CCR5) T09960 GENENAME CCR5 T09960 TARGTYPE Successful target T09960 SYNONYMS HIV-1 fusion coreceptor; HIV-1 fusion co-receptor; Chemokine receptor CCR5; CMKBR5; CHEMR13; CD195 antigen; CD195; CCR-5; CC-CKR-5; C-C CKR-5 T09960 FUNCTION May play a role in the control of granulocytic lineage proliferation or differentiation. Receptor for a number of inflammatory CC-chemokines including CCL3/MIP-1-alpha, CCL4/MIP-1-beta and RANTES and subsequently transduces a signal by increasing the intracellular calcium ion level. T09960 PDBSTRUC 6MET; 6MEO; 6FGP; 5YY4; 5YD5 T09960 BIOCLASS GPCR rhodopsin T09960 SEQUENCE MDYQVSSPIYDINYYTSEPCQKINVKQIAARLLPPLYSLVFIFGFVGNMLVILILINCKRLKSMTDIYLLNLAISDLFFLLTVPFWAHYAAAQWDFGNTMCQLLTGLYFIGFFSGIFFIILLTIDRYLAVVHAVFALKARTVTFGVVTSVITWVVAVFASLPGIIFTRSQKEGLHYTCSSHFPYSQYQFWKNFQTLKIVILGLVLPLLVMVICYSGILKTLLRCRNEKKRHRAVRLIFTIMIVYFLFWAPYNIVLLLNTFQEFFGLNNCSSSNRLDQAMQVTETLGMTHCCINPIIYAFVGEKFRNYLLVFFQKHIAKRFCKCCSIFQQEAPERASSVYTRSTGEQEISVGL T09960 DRUGINFO D0NR6S Maraviroc Approved T09960 DRUGINFO D0J7QU E-913 Phase 3 T09960 DRUGINFO D0CG0N PRO-140 Phase 3 T09960 DRUGINFO D09JLI Vicriviroc Phase 3 T09960 DRUGINFO D1M8GC PRO 140 Phase 2/3 T09960 DRUGINFO D0Y7NA INCB9471 Phase 2a T09960 DRUGINFO D0B1SG BMS-813160 Phase 2 T09960 DRUGINFO D0YQ7U Cenicriviroc Phase 2 T09960 DRUGINFO D0UV4H GSK-706769 Phase 2 T09960 DRUGINFO D0F7PZ PF-232798 Phase 2 T09960 DRUGINFO D06FIT SB-728-T Phase 2 T09960 DRUGINFO D0A0BK Cal-1 Phase 1/2 T09960 DRUGINFO D0K1OK CCR5 mab Phase 1 T09960 DRUGINFO D06KNE INCB15050 Phase 1 T09960 DRUGINFO D0O9UC Tak-220 Phase 1 T09960 DRUGINFO D09XXH VCH-286 Phase 1 T09960 DRUGINFO D0G6SZ GW873140 Discontinued in Phase 3 T09960 DRUGINFO D06EMW AZD8566 Discontinued in Phase 1 T09960 DRUGINFO D0G6JE SCH-C Discontinued in Phase 1 T09960 DRUGINFO D07GIB AZD5672 Terminated T09960 DRUGINFO D0O9AZ CCR5Qb Terminated T09960 DRUGINFO D0W0LS TAK-779 Terminated T09960 DRUGINFO D0I3IZ (2-(4-chlorobenzyloxy)-5-bromophenyl)methanamine Investigative T09960 DRUGINFO D0BD3G 4-(2-(4-chlorobenzyloxy)-5-bromobenzyl)morpholine Investigative T09960 DRUGINFO D01LRC ANIBAMINE Investigative T09960 DRUGINFO D06TQD CMPD-167 Investigative T09960 DRUGINFO D0BD6A GT-1282 Investigative T09960 DRUGINFO D06XRS N-(2-(4-chlorobenzyloxy)-5-bromobenzyl)ethanamine Investigative T09960 DRUGINFO D0J3BT NIFEVIROC Investigative T09960 DRUGINFO D01TYO SCH-210971 Investigative T09960 DRUGINFO D06XIC VARIECOLIN Investigative T09960 KEGGPATH hsa04060:Cytokine-cytokine receptor interaction T09960 KEGGPATH hsa04062:Chemokine signaling pathway T09960 KEGGPATH hsa04144:Endocytosis T09960 KEGGPATH hsa05145:Toxoplasmosis T09960 KEGGPATH hsa05203:Viral carcinogenesis T09960 WIKIPATH WP117:GPCRs, Other T09960 WIKIPATH WP1824:GPCR downstream signaling T09960 WIKIPATH WP1825:GPCR ligand binding T09960 WIKIPATH WP24:Peptide GPCRs T09960 WIKIPATH WP2658:HIV Life Cycle T09960 WIKIPATH WP455:GPCRs, Class A Rhodopsin-like T09960 WIKIPATH WP69:TCR Signaling Pathway T09960 REACPATH R-HSA-173107:Binding and entry of HIV virion T09960 REACPATH R-HSA-380108:Chemokine receptors bind chemokines T09960 REACPATH R-HSA-418594:G alpha (i) signalling events T09960 NET_PATH NetPath_11:TCR Signaling Pathway T09960 NET_PATH NetPath_14:IL2 Signaling Pathway T09960 NET_PATH NetPath_24:TSLP Signaling Pathway T09960 INTEPATH il12_2pathway:IL12-mediated signaling events T09960 PANTPATH P00031:Inflammation mediated by chemokine and cytokine signaling pathway T23172 TARGETID T23172 T23172 FORMERID TTDC00084 T23172 UNIPROID JAK3_HUMAN T23172 TARGNAME Janus kinase 3 (JAK-3) T23172 GENENAME JAK3 T23172 TARGTYPE Successful target T23172 SYNONYMS Tyrosine-protein kinase JAK3; Leukocyte janus kinase; L-JAK T23172 FUNCTION Mediates essential signaling events in both innate and adaptive immunity and plays a crucial role in hematopoiesis during T-cells development. In the cytoplasm, plays a pivotal role in signal transduction via its association with type I receptors sharing the common subunit gamma such as IL2R, IL4R, IL7R, IL9R, IL15R and IL21R. Following ligand binding to cell surface receptors, phosphorylates specific tyrosine residues on the cytoplasmic tails of the receptor, creating docking sites for STATs proteins. Subsequently, phosphorylates the STATs proteins once they are recruited to the receptor. Phosphorylated STATs then form homodimer or heterodimers and translocate to the nucleus to activate gene transcription. For example, upon IL2R activation by IL2, JAK1 and JAK3 molecules bind to IL2R beta (IL2RB) and gamma chain (IL2RG) subunits inducing the tyrosine phosphorylation of both receptor subunits on their cytoplasmic domain. Then, STAT5A AND STAT5B are recruited, phosphorylated and activated by JAK1 and JAK3. Once activated, dimerized STAT5 translocates to the nucleus and promotes the transcription of specific target genes in a cytokine-specific fashion. Non-receptor tyrosine kinase involved in various processes such as cell growth, development, or differentiation. T23172 PDBSTRUC 6NY4; 6GLB; 6GLA; 6GL9; 6DUD T23172 BIOCLASS Kinase T23172 ECNUMBER EC 2.7.10.2 T23172 SEQUENCE MAPPSEETPLIPQRSCSLLSTEAGALHVLLPARGPGPPQRLSFSFGDHLAEDLCVQAAKASGILPVYHSLFALATEDLSCWFPPSHIFSVEDASTQVLLYRIRFYFPNWFGLEKCHRFGLRKDLASAILDLPVLEHLFAQHRSDLVSGRLPVGLSLKEQGECLSLAVLDLARMAREQAQRPGELLKTVSYKACLPPSLRDLIQGLSFVTRRRIRRTVRRALRRVAACQADRHSLMAKYIMDLERLDPAGAAETFHVGLPGALGGHDGLGLLRVAGDGGIAWTQGEQEVLQPFCDFPEIVDISIKQAPRVGPAGEHRLVTVTRTDNQILEAEFPGLPEALSFVALVDGYFRLTTDSQHFFCKEVAPPRLLEEVAEQCHGPITLDFAINKLKTGGSRPGSYVLRRSPQDFDSFLLTVCVQNPLGPDYKGCLIRRSPTGTFLLVGLSRPHSSLRELLATCWDGGLHVDGVAVTLTSCCIPRPKEKSNLIVVQRGHSPPTSSLVQPQSQYQLSQMTFHKIPADSLEWHENLGHGSFTKIYRGCRHEVVDGEARKTEVLLKVMDAKHKNCMESFLEAASLMSQVSYRHLVLLHGVCMAGDSTMVQEFVHLGAIDMYLRKRGHLVPASWKLQVVKQLAYALNYLEDKGLPHGNVSARKVLLAREGADGSPPFIKLSDPGVSPAVLSLEMLTDRIPWVAPECLREAQTLSLEADKWGFGATVWEVFSGVTMPISALDPAKKLQFYEDRQQLPAPKWTELALLIQQCMAYEPVQRPSFRAVIRDLNSLISSDYELLSDPTPGALAPRDGLWNGAQLYACQDPTIFEERHLKYISQLGKGNFGSVELCRYDPLGDNTGALVAVKQLQHSGPDQQRDFQREIQILKALHSDFIVKYRGVSYGPGRQSLRLVMEYLPSGCLRDFLQRHRARLDASRLLLYSSQICKGMEYLGSRRCVHRDLAARNILVESEAHVKIADFGLAKLLPLDKDYYVVREPGQSPIFWYAPESLSDNIFSRQSDVWSFGVVLYELFTYCDKSCSPSAEFLRMMGCERDVPALCRLLELLEEGQRLPAPPACPAEVHELMKLCWAPSPQDRPSFSALGPQLDMLWSGSRGCETHAFTAHPEGKHHSLSFS T23172 DRUGINFO D0EG1I Tofacitinib Approved T23172 DRUGINFO D06EIC ASP-015K Phase 3 T23172 DRUGINFO D02TUL PF-06651600 Phase 2/3 T23172 DRUGINFO D04QWQ VX-509 Phase 2/3 T23172 DRUGINFO D6INZ9 ATI-501 Phase 2 T23172 DRUGINFO D6N5UC ATI-502 Phase 2 T23172 DRUGINFO D0BI3N Cerdulatinib Phase 2 T23172 DRUGINFO D0Q0IM SNA-125 Phase 1 T23172 DRUGINFO D07XYI 1,2,4-triazolo[1,5a]pyridine derivative 1 Patented T23172 DRUGINFO D05AXE Aminooxazole carboxamide derivative 1 Patented T23172 DRUGINFO D09ALF Aminotriazolopyridine derivative 1 Patented T23172 DRUGINFO D0SX1B Benzimidazole derivative 5 Patented T23172 DRUGINFO D01CRX Benzimidazole derivative 7 Patented T23172 DRUGINFO D01FVC Bis-aminopyrimidine derivative 1 Patented T23172 DRUGINFO D0LR6J Bis-aminopyrimidine derivative 2 Patented T23172 DRUGINFO D0S6XT Bis-aminopyrimidine derivative 3 Patented T23172 DRUGINFO D0SJ1Q Bis-aminopyrimidine derivative 4 Patented T23172 DRUGINFO D08WPB Five-and-six-membered heterocyclic compound 1 Patented T23172 DRUGINFO D07PTU Imidazo[4,5-c]pyridine derivative 1 Patented T23172 DRUGINFO D0VJ1R Imidazo[4,5-c]pyridine derivative 2 Patented T23172 DRUGINFO D07BND Imidazopyridazine derivative 1 Patented T23172 DRUGINFO D00PTE Imidazopyridazine derivative 2 Patented T23172 DRUGINFO D0P3UH Imidazopyridine derivative 4 Patented T23172 DRUGINFO D0G9MM Isoxazole derivative 1 Patented T23172 DRUGINFO D0TX2G Isoxazole derivative 2 Patented T23172 DRUGINFO D0Y2IM N-(cyanomethyl)-4-(2-(phenylamino)pyrimidin-4-yl)benzamide derivative 1 Patented T23172 DRUGINFO D0XH7H N-methylmethanesulfonamide derivative 1 Patented T23172 DRUGINFO D0GH8D PMID27774822-Compound-Figure10Example1 Patented T23172 DRUGINFO D0W8DN PMID27774822-Compound-Figure10Example19 Patented T23172 DRUGINFO D0RJ3W PMID27774822-Compound-Figure11Example5 Patented T23172 DRUGINFO D0M3CB PMID27774822-Compound-Figure1Example20 Patented T23172 DRUGINFO D0E2WK PMID27774822-Compound-Figure2Example1-1left Patented T23172 DRUGINFO D0IQ6G PMID27774822-Compound-Figure2Example1-1right Patented T23172 DRUGINFO D0WB5U PMID27774822-Compound-Figure2Example4-3 Patented T23172 DRUGINFO D0X6DL PMID27774822-Compound-Figure6Example2 Patented T23172 DRUGINFO D09JLL PMID27774822-Compound-Figure6Example3 Patented T23172 DRUGINFO D0B9TH PMID27774822-Compound-Figure8Example5 Patented T23172 DRUGINFO D0YR8S PMID27774824-Compound-Figure11Example1up Patented T23172 DRUGINFO D0NK1R PMID27774824-Compound-Figure12Example1 Patented T23172 DRUGINFO D0UH8J PMID27774824-Compound-Figure12Example10 Patented T23172 DRUGINFO D00BYK PMID27774824-Compound-Figure12Example61 Patented T23172 DRUGINFO D0A6RG PMID27774824-Compound-Figure2Example4 Patented T23172 DRUGINFO D0U1HA PMID27774824-Compound-Figure3Example18 Patented T23172 DRUGINFO D02IET PMID27774824-Compound-Figure3Example7 Patented T23172 DRUGINFO D0T5AF PMID27774824-Compound-Figure5Example13 Patented T23172 DRUGINFO D0GB7G PMID27774824-Compound-Figure6Example12 Patented T23172 DRUGINFO D01DBB PMID27774824-Compound-Figure9Example2down Patented T23172 DRUGINFO D0WZ8N PMID27774824-Compound-Figure9Example2up Patented T23172 DRUGINFO D09PIS Pyrazolo[4,3-c]pyridine derivative 2 Patented T23172 DRUGINFO D0VJ5M Pyrazolopyridine derivative 1 Patented T23172 DRUGINFO D00ZVY Pyrazolopyridine derivative 2 Patented T23172 DRUGINFO D03QAY Pyrazolopyridine derivative 3 Patented T23172 DRUGINFO D09RUN Pyrazolopyridine derivative 4 Patented T23172 DRUGINFO D02VGC Pyrazolopyridine derivative 6 Patented T23172 DRUGINFO D0D1QH Pyrazolopyridine derivative 7 Patented T23172 DRUGINFO D0WA1V Pyrimidopyridazinone derivative 2 Patented T23172 DRUGINFO D09UBE Pyrrole six-membered heteroaryl ring derivative 1 Patented T23172 DRUGINFO D0FQ4Z Pyrrolo[2,3-d]pyrimidine derivative 6 Patented T23172 DRUGINFO D0U5FZ Pyrrolo[2,3-d]pyrimidine derivative 7 Patented T23172 DRUGINFO D0KL3B Pyrrolo[2,3-d]pyrimidine derivative 8 Patented T23172 DRUGINFO D0EX5C Pyrrolo-pyrazine derivative 1 Patented T23172 DRUGINFO D0HL5C Pyrrolo-pyrazine derivative 2 Patented T23172 DRUGINFO D0JU1R Pyrrolo-pyrazine derivative 3 Patented T23172 DRUGINFO D0Y6ON Pyrrolo-pyrazine derivative 4 Patented T23172 DRUGINFO D0VR6E Pyrrolo-pyridine derivative 3 Patented T23172 DRUGINFO D01EYJ Ruxolitinib derivative 2 Patented T23172 DRUGINFO D0G0FK Tricyclic compound 1 Patented T23172 DRUGINFO D0LS1O Tricyclic compound 11 Patented T23172 DRUGINFO D0QL7J Tricyclic compound 2 Patented T23172 DRUGINFO D0X1FD Tricyclic heterocycle derivative 1 Patented T23172 DRUGINFO D03TEE Tricyclic heterocycle derivative 2 Patented T23172 DRUGINFO D0M2WA Tricyclic heterocycle derivative 5 Patented T23172 DRUGINFO D04BOW Tricyclic pyrrolopyridine compound 1 Patented T23172 DRUGINFO D0GZ7B AG490 Terminated T23172 DRUGINFO D0Z1HQ PNU156804 Terminated T23172 DRUGINFO D01XEQ R348 Terminated T23172 DRUGINFO D09HXU 6-o-tolylquinazolin-2-amine Investigative T23172 DRUGINFO D0M2AN AD-412 Investigative T23172 DRUGINFO D05MHL Atropisomer 1 Investigative T23172 DRUGINFO D0IR6U CMP-6 Investigative T23172 DRUGINFO D0P1BK NC1153 Investigative T23172 DRUGINFO D0V6VQ PF-956980 Investigative T23172 DRUGINFO D08RZB PMID15546730C2 Investigative T23172 DRUGINFO D02NNT PMID21493067C1d Investigative T23172 DRUGINFO D0US9O PMID24359159C19a Investigative T23172 DRUGINFO D0G7YF VX-467 Investigative T23172 DRUGINFO D0E5IP WHI-P154 Investigative T23172 DRUGINFO D0YX5U ZM-39923 Investigative T23172 KEGGPATH hsa04062:Chemokine signaling pathway T23172 KEGGPATH hsa04151:PI3K-Akt signaling pathway T23172 KEGGPATH hsa04550:Signaling pathways regulating pluripotency of stem cells T23172 KEGGPATH hsa04630:Jak-STAT signaling pathway T23172 KEGGPATH hsa05162:Measles T23172 KEGGPATH hsa05166:HTLV-I infection T23172 KEGGPATH hsa05169:Epstein-Barr virus infection T23172 KEGGPATH hsa05203:Viral carcinogenesis T23172 KEGGPATH hsa05340:Primary immunodeficiency T23172 WIKIPATH WP1840:Interleukin-3, 5 and GM-CSF signaling T23172 WIKIPATH WP205:IL-7 Signaling Pathway T23172 WIKIPATH WP22:IL-9 Signaling Pathway T23172 WIKIPATH WP2374:Oncostatin M Signaling Pathway T23172 WIKIPATH WP2673:Interleukin-7 signaling T23172 WIKIPATH WP2732:Interleukin-2 signaling T23172 WIKIPATH WP395:IL-4 Signaling Pathway T23172 WIKIPATH WP49:IL-2 Signaling Pathway T23172 REACPATH R-HSA-114604:GPVI-mediated activation cascade T23172 REACPATH R-HSA-1266695:Interleukin-7 signaling T23172 REACPATH R-HSA-392451:G beta:gamma signalling through PI3Kgamma T23172 REACPATH R-HSA-451927:Interleukin-2 signaling T23172 REACPATH R-HSA-5673001:RAF/MAP kinase cascade T23172 REACPATH R-HSA-912526:Interleukin receptor SHC signaling T23172 INTEPATH cd40_pathway:CD40/CD40L signaling T23172 INTEPATH il2_1pathway:IL2-mediated signaling events T23172 INTEPATH il2_pi3kpathway:IL2 signaling events mediated by PI3K T23172 INTEPATH il2_stat5pathway:IL2 signaling events mediated by STAT5 T23172 INTEPATH il4_2pathway:IL4-mediated signaling events T23172 INTEPATH shp2_pathway:SHP2 signaling T23172 INTEPATH tcptp_pathway:Signaling events mediated by TCPTP T23172 PANTPATH P00036:Interleukin signaling pathway T23172 PANTPATH P00038:JAK/STAT signaling pathway T23172 PANTPATH P00047:PDGF signaling pathway T89361 TARGETID T89361 T89361 FORMERID TTDC00169 T89361 UNIPROID CDK6_HUMAN T89361 TARGNAME Cyclin-dependent kinase 6 (CDK6) T89361 GENENAME CDK6 T89361 TARGTYPE Successful target T89361 SYNONYMS Serine/threonine-protein kinase PLSTIRE; Serine/threonine protein kinase PLSTIRE; Cell division protein kinase 6; CDKN6 T89361 FUNCTION Phosphorylates pRB/RB1 and NPM1. Interacts with D-type G1 cyclins during interphase at G1 to form a pRB/RB1 kinase and controls the entrance into the cell cycle. Involved in initiation and maintenance of cell cycle exit during cell differentiation; prevents cell proliferation and regulates negatively cell differentiation, but is required for the proliferation of specific cell types (e. g. erythroid and hematopoietic cells). Essential for cell proliferation within the dentate gyrus of the hippocampus and the subventricular zone of the lateral ventricles. Required during thymocyte development. Promotes the production of newborn neurons, probably by modulating G1 length. Promotes, at least in astrocytes, changes in patterns of gene expression, changes in the actin cytoskeleton including loss of stress fibers, and enhanced motility during cell differentiation. Prevents myeloid differentiation by interfering with RUNX1 and reducing its transcription transactivation activity, but promotes proliferation of normal myeloid progenitors. Delays senescence. Promotes the proliferation of beta-cells in pancreatic islets of Langerhans. May play a role in the centrosome organization during the cell cycle phases. Serine/threonine-protein kinase involved in the control of the cell cycle and differentiation; promotes G1/S transition. T89361 PDBSTRUC 5L2T; 5L2S; 5L2I; 4TTH; 4EZ5 T89361 BIOCLASS Kinase T89361 ECNUMBER EC 2.7.11.22 T89361 SEQUENCE MEKDGLCRADQQYECVAEIGEGAYGKVFKARDLKNGGRFVALKRVRVQTGEEGMPLSTIREVAVLRHLETFEHPNVVRLFDVCTVSRTDRETKLTLVFEHVDQDLTTYLDKVPEPGVPTETIKDMMFQLLRGLDFLHSHRVVHRDLKPQNILVTSSGQIKLADFGLARIYSFQMALTSVVVTLWYRAPEVLLQSSYATPVDLWSVGCIFAEMFRRKPLFRGSSDVDQLGKILDVIGLPGEEDWPRDVALPRQAFHSKSAQPIEKFVTDIDELGKDLLLKCLTFNPAKRISAYSALSHPYFQDLERCKENLDSHLPPSQNTSELNTA T89361 DRUGINFO D07ESC Apremilast Approved T89361 DRUGINFO D05SBO LY2835219 Approved T89361 DRUGINFO D00UZR Palbociclib Approved T89361 DRUGINFO D01HVT Ribociclib Succinate Approved T89361 DRUGINFO D0AP9E Trilaciclib Approved T89361 DRUGINFO D08MXP LEE011 Phase 3 T89361 DRUGINFO D0WU1O G1T38 Phase 2 T89361 DRUGINFO D8ZV2Q FCN-437 Phase 1/2 T89361 DRUGINFO D4IS0G GLR2007 Phase 1/2 T89361 DRUGINFO DKCU40 FN-1501 Phase 1 T89361 DRUGINFO D01XZG G1T28-1 Phase 1 T89361 DRUGINFO D0W4MN Isoquinoline 1,3-dione derivative 1 Patented T89361 DRUGINFO D0M5DX Oxazolyl methylthiothiazole derivative 1 Patented T89361 DRUGINFO D0X5VI PMID25726713-Compound-47 Patented T89361 DRUGINFO D0WJ3W PMID25726713-Compound-48 Patented T89361 DRUGINFO D07TVO PMID25726713-Compound-49 Patented T89361 DRUGINFO D0Y8JF PMID25726713-Compound-50 Patented T89361 DRUGINFO D0KH7Q PMID25726713-Compound-51 Patented T89361 DRUGINFO D07ZJC INOC-005 Preclinical T89361 DRUGINFO D0Y6HA CYC-103 Terminated T89361 DRUGINFO D0Z0KD PD-0183812 Terminated T89361 DRUGINFO D0EK0G 3-(4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione Investigative T89361 DRUGINFO D00NYT 3,4-di-(4-methoxyphenyl)-1H-pyrrole-2,5-dione Investigative T89361 DRUGINFO D0C3WY 3,4-diphenyl-1H-pyrrole-2,5-dione Investigative T89361 DRUGINFO D0MF5Y 3,7,3',4'-TETRAHYDROXYFLAVONE Investigative T89361 DRUGINFO D00RIX APIGENIN Investigative T89361 DRUGINFO D01UYI Chrysin Investigative T89361 DRUGINFO D0CI3C Deschloroflavopiridol Investigative T89361 DRUGINFO D09OAH Fascaplysin Investigative T89361 DRUGINFO D0J4ON RGB-286147 Investigative T89361 KEGGPATH hsa04110:Cell cycle T89361 KEGGPATH hsa04115:p53 signaling pathway T89361 KEGGPATH hsa04151:PI3K-Akt signaling pathway T89361 KEGGPATH hsa05161:Hepatitis B T89361 KEGGPATH hsa05162:Measles T89361 KEGGPATH hsa05200:Pathways in cancer T89361 KEGGPATH hsa05203:Viral carcinogenesis T89361 KEGGPATH hsa05206:MicroRNAs in cancer T89361 KEGGPATH hsa05212:Pancreatic cancer T89361 KEGGPATH hsa05214:Glioma T89361 KEGGPATH hsa05218:Melanoma T89361 KEGGPATH hsa05220:Chronic myeloid leukemia T89361 KEGGPATH hsa05222:Small cell lung cancer T89361 KEGGPATH hsa05223:Non-small cell lung cancer T89361 WIKIPATH WP1530:miRNA Regulation of DNA Damage Response T89361 WIKIPATH WP1545:miRNAs involved in DNA damage response T89361 WIKIPATH WP179:Cell Cycle T89361 WIKIPATH WP1858:Mitotic G1-G1/S phases T89361 WIKIPATH WP2002:miR-targeted genes in epithelium - TarBase T89361 WIKIPATH WP2003:miR-targeted genes in leukocytes - TarBase T89361 WIKIPATH WP2004:miR-targeted genes in lymphocytes - TarBase T89361 WIKIPATH WP2005:miR-targeted genes in muscle cell - TarBase T89361 WIKIPATH WP2249:Metastatic brain tumor T89361 WIKIPATH WP2261:Signaling Pathways in Glioblastoma T89361 WIKIPATH WP2446:Retinoblastoma (RB) in Cancer T89361 WIKIPATH WP363:Wnt Signaling Pathway Netpath T89361 WIKIPATH WP45:G1 to S cell cycle control T89361 WIKIPATH WP707:DNA Damage Response T89361 REACPATH R-HSA-2559580:Oxidative Stress Induced Senescence T89361 REACPATH R-HSA-2559582:Senescence-Associated Secretory Phenotype (SASP) T89361 REACPATH R-HSA-2559585:Oncogene Induced Senescence T89361 REACPATH R-HSA-69231:Cyclin D associated events in G1 T89361 NET_PATH NetPath_7:TGF_beta_Receptor Signaling Pathway T89361 INTEPATH ar_pathway:Coregulation of Androgen receptor activity T89361 INTEPATH cmyb_pathway:C-MYB transcription factor network T89361 INTEPATH il2_stat5pathway:IL2 signaling events mediated by STAT5 T89361 INTEPATH p73pathway:p73 transcription factor network T89361 INTEPATH rb_1pathway:Regulation of retinoblastoma protein T38338 TARGETID T38338 T38338 FORMERID TTDS00529 T38338 UNIPROID CAC1B_HUMAN T38338 TARGNAME Voltage-gated calcium channel alpha Cav2.2 (CACNA1B) T38338 GENENAME CACNA1B T38338 TARGTYPE Successful target T38338 SYNONYMS Voltage-gated calcium channel alpha subunit Cav2.2; Voltage-dependent N-type calcium channel alpha-1B subunit; N-type Ca2+ channel; Calcium channel, L type, alpha-1 polypeptide isoform 5; CACNA1B; Brain calcium channel III; BIII T38338 FUNCTION Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1B gives rise to N-type calcium currents. N-type calcium channels belong to the 'high-voltage activated' (HVA) group and are blocked by omega-conotoxin-GVIA (omega-CTx-GVIA) and by omega-agatoxin- IIIA (omega-Aga-IIIA). They are however insensitive to dihydropyridines (DHP), and omega-agatoxin-IVA (omega-Aga-IVA). Calcium channels containing alpha-1B subunit may play a role in directed migration of immature neurons. T38338 PDBSTRUC 2LCM T38338 BIOCLASS Voltage-gated ion channel T38338 SEQUENCE MVRFGDELGGRYGGPGGGERARGGGAGGAGGPGPGGLQPGQRVLYKQSIAQRARTMALYNPIPVKQNCFTVNRSLFVFSEDNVVRKYAKRITEWPPFEYMILATIIANCIVLALEQHLPDGDKTPMSERLDDTEPYFIGIFCFEAGIKIIALGFVFHKGSYLRNGWNVMDFVVVLTGILATAGTDFDLRTLRAVRVLRPLKLVSGIPSLQVVLKSIMKAMVPLLQIGLLLFFAILMFAIIGLEFYMGKFHKACFPNSTDAEPVGDFPCGKEAPARLCEGDTECREYWPGPNFGITNFDNILFAILTVFQCITMEGWTDILYNTNDAAGNTWNWLYFIPLIIIGSFFMLNLVLGVLSGEFAKERERVENRRAFLKLRRQQQIERELNGYLEWIFKAEEVMLAEEDRNAEEKSPLDVLKRAATKKSRNDLIHAEEGEDRFADLCAVGSPFARASLKSGKTESSSYFRRKEKMFRFFIRRMVKAQSFYWVVLCVVALNTLCVAMVHYNQPRRLTTTLYFAEFVFLGLFLTEMSLKMYGLGPRSYFRSSFNCFDFGVIVGSVFEVVWAAIKPGSSFGISVLRALRLLRIFKVTKYWSSLRNLVVSLLNSMKSIISLLFLLFLFIVVFALLGMQLFGGQFNFQDETPTTNFDTFPAAILTVFQILTGEDWNAVMYHGIESQGGVSKGMFSSFYFIVLTLFGNYTLLNVFLAIAVDNLANAQELTKDEEEMEEAANQKLALQKAKEVAEVSPMSAANISIAARQQNSAKARSVWEQRASQLRLQNLRASCEALYSEMDPEERLRFATTRHLRPDMKTHLDRPLVVELGRDGARGPVGGKARPEAAEAPEGVDPPRRHHRHRDKDKTPAAGDQDRAEAPKAESGEPGAREERPRPHRSHSKEAAGPPEARSERGRGPGPEGGRRHHRRGSPEEAAEREPRRHRAHRHQDPSKECAGAKGERRARHRGGPRAGPREAESGEEPARRHRARHKAQPAHEAVEKETTEKEATEKEAEIVEADKEKELRNHQPREPHCDLETSGTVTVGPMHTLPSTCLQKVEEQPEDADNQRNVTRMGSQPPDPNTIVHIPVMLTGPLGEATVVPSGNVDLESQAEGKKEVEADDVMRSGPRPIVPYSSMFCLSPTNLLRRFCHYIVTMRYFEVVILVVIALSSIALAAEDPVRTDSPRNNALKYLDYIFTGVFTFEMVIKMIDLGLLLHPGAYFRDLWNILDFIVVSGALVAFAFSGSKGKDINTIKSLRVLRVLRPLKTIKRLPKLKAVFDCVVNSLKNVLNILIVYMLFMFIFAVIAVQLFKGKFFYCTDESKELERDCRGQYLDYEKEEVEAQPRQWKKYDFHYDNVLWALLTLFTVSTGEGWPMVLKHSVDATYEEQGPSPGYRMELSIFYVVYFVVFPFFFVNIFVALIIITFQEQGDKVMSECSLEKNERACIDFAISAKPLTRYMPQNRQSFQYKTWTFVVSPPFEYFIMAMIALNTVVLMMKFYDAPYEYELMLKCLNIVFTSMFSMECVLKIIAFGVLNYFRDAWNVFDFVTVLGSITDILVTEIAETNNFINLSFLRLFRAARLIKLLRQGYTIRILLWTFVQSFKALPYVCLLIAMLFFIYAIIGMQVFGNIALDDDTSINRHNNFRTFLQALMLLFRSATGEAWHEIMLSCLSNQACDEQANATECGSDFAYFYFVSFIFLCSFLMLNLFVAVIMDNFEYLTRDSSILGPHHLDEFIRVWAEYDPAACGRISYNDMFEMLKHMSPPLGLGKKCPARVAYKRLVRMNMPISNEDMTVHFTSTLMALIRTALEIKLAPAGTKQHQCDAELRKEISVVWANLPQKTLDLLVPPHKPDEMTVGKVYAALMIFDFYKQNKTTRDQMQQAPGGLSQMGPVSLFHPLKATLEQTQPAVLRGARVFLRQKSSTSLSNGGAIQNQESGIKESVSWGTQRTQDAPHEARPPLERGHSTEIPVGRSGALAVDVQMQSITRRGPDGEPQPGLESQGRAASMPRLAAETQPVTDASPMKRSISTLAQRPRGTHLCSTTPDRPPPSQASSHHHHHRCHRRRDRKQRSLEKGPSLSADMDGAPSSAVGPGLPPGEGPTGCRRERERRQERGRSQERRQPSSSSSEKQRFYSCDRFGGREPPKPKPSLSSHPTSPTAGQEPGPHPQGSGSVNGSPLLSTSGASTPGRGGRRQLPQTPLTPRPSITYKTANSSPIHFAGAQTSLPAFSPGRLSRGLSEHNALLQRDPLSQPLAPGSRIGSDPYLGQRLDSEASVHALPEDTLTFEEAVATNSGRSSRTSYVSSLTSQSHPLRRVPNGYHCTLGLSSGGRARHSYHHPDQDHWC T38338 DRUGINFO D0I9HF Hesperidin Approved T38338 DRUGINFO D0N3ZJ LOMERIZINE Approved T38338 DRUGINFO D01NLB Ziconotide Approved T38338 DRUGINFO D0N3SR Cilnidipine Phase 3 T38338 DRUGINFO D00GEG Ralfinamide Phase 3 T38338 DRUGINFO D01UDS CNV-2197944 Phase 2 T38338 DRUGINFO D0K8NW Ritanserin Discontinued in Phase 3 T38338 DRUGINFO D0T4YZ CNSB-004 Preclinical T38338 DRUGINFO D04BSZ PD-0204318 Terminated T38338 DRUGINFO D03QMS PD-157667 Terminated T38338 DRUGINFO D0G6HZ PD-29361 Terminated T38338 DRUGINFO D0QQ7N TH-9229 Terminated T38338 DRUGINFO D0K4ZX Conotoxin Investigative T38338 DRUGINFO D09YTH CPU-228 Investigative T38338 DRUGINFO D00PVO GNF-PF-3464 Investigative T38338 DRUGINFO D0X7VM KYS-05090 Investigative T38338 DRUGINFO D0WN7V NSC-180246 Investigative T38338 DRUGINFO D0GX2A NSC-87509 Investigative T38338 DRUGINFO D09LRA omega-conotoxin GVIA Investigative T38338 DRUGINFO D07BDQ PD-151307 Investigative T38338 DRUGINFO D0C3VI PD-167341 Investigative T38338 DRUGINFO D08RJC PD-32577 Investigative T38338 DRUGINFO D06NHS TROX-1 Investigative T38338 KEGGPATH hsa04010:MAPK signaling pathway T38338 KEGGPATH hsa04020:Calcium signaling pathway T38338 KEGGPATH hsa04721:Synaptic vesicle cycle T38338 KEGGPATH hsa04723:Retrograde endocannabinoid signaling T38338 KEGGPATH hsa04725:Cholinergic synapse T38338 KEGGPATH hsa04726:Serotonergic synapse T38338 KEGGPATH hsa04727:GABAergic synapse T38338 KEGGPATH hsa04728:Dopaminergic synapse T38338 KEGGPATH hsa04742:Taste transduction T38338 KEGGPATH hsa04930:Type II diabetes mellitus T38338 KEGGPATH hsa05032:Morphine addiction T38338 KEGGPATH hsa05033:Nicotine addiction T38338 WIKIPATH WP2267:Synaptic Vesicle Pathway T38338 WIKIPATH WP536:Calcium Regulation in the Cardiac Cell T38338 REACPATH R-HSA-112308:Depolarization of the Presynaptic Terminal Triggers the Opening of Calcium Channels T38338 PANTPATH P00027:Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway T38338 PANTPATH P00037:Ionotropic glutamate receptor pathway T38338 PANTPATH P00039:Metabotropic glutamate receptor group III pathway T38338 PANTPATH P00040:Metabotropic glutamate receptor group II pathway T38338 PANTPATH P04394:Thyrotropin-releasing hormone receptor signaling pathway T38338 PANTPATH P05730:Endogenous cannabinoid signaling T38338 PANTPATH P05731:GABA-B receptor II signaling T00895 TARGETID T00895 T00895 FORMERID TTDC00066 T00895 UNIPROID KPCE_HUMAN T00895 TARGNAME Protein kinase C epsilon (PRKCE) T00895 GENENAME PRKCE T00895 TARGTYPE Successful target T00895 SYNONYMS Protein kinase C epsilon type; PKCE; PKC epsilon; NPKC-epsilon T00895 FUNCTION Mediates cell adhesion to the extracellular matrix via integrin-dependent signaling, by mediating angiotensin-2-induced activation of integrin beta-1 (ITGB1) in cardiac fibroblasts. Phosphorylates MARCKS, which phosphorylates and activates PTK2/FAK, leading to the spread of cardiomyocytes. Involved in the control of the directional transport of ITGB1 in mesenchymal cells by phosphorylating vimentin (VIM), an intermediate filament (IF) protein. In epithelial cells, associates with and phosphorylates keratin-8 (KRT8), which induces targeting of desmoplakin at desmosomes and regulates cell-cell contact. Phosphorylates IQGAP1, which binds to CDC42, mediating epithelial cell-cell detachment prior to migration. In HeLa cells, contributes to hepatocyte growth factor (HGF)-induced cell migration, and in human corneal epithelial cells, plays a critical role in wound healing after activation by HGF. During cytokinesis, forms a complex with YWHAB, which is crucial for daughter cell separation, and facilitates abscission by a mechanism which may implicate the regulation of RHOA. In cardiac myocytes, regulates myofilament function and excitation coupling at the Z-lines, where it is indirectly associated with F-actin via interaction with COPB1. During endothelin-induced cardiomyocyte hypertrophy, mediates activation of PTK2/FAK, which is critical for cardiomyocyte survival and regulation of sarcomere length. Plays a role in the pathogenesis of dilated cardiomyopathy via persistent phosphorylation of troponin I (TNNI3). Involved in nerve growth factor (NFG)-induced neurite outgrowth and neuron morphological change independently of its kinase activity, by inhibition of RHOA pathway, activation of CDC42 and cytoskeletal rearrangement. May be involved in presynaptic facilitation by mediating phorbol ester-induced synaptic potentiation. Phosphorylates gamma-aminobutyric acid receptor subunit gamma-2 (GABRG2), which reduces the response of GABA receptors to ethanol and benzodiazepines and may mediate acute tolerance to the intoxicating effects of ethanol. Upon PMA treatment, phosphorylates the capsaicin- and heat-activated cation channel TRPV1, which is required for bradykinin-induced sensitization of the heat response in nociceptive neurons. Is able to form a complex with PDLIM5 and N-type calcium channel, and may enhance channel activities and potentiates fast synaptic transmission by phosphorylating the pore-forming alpha subunit CACNA1B (CaV2. 2). In prostate cancer cells, interacts with and phosphorylates STAT3, which increases DNA-binding and transcriptional activity of STAT3 and seems to be essential for prostate cancer cell invasion. Downstream of TLR4, plays an important role in the lipopolysaccharide (LPS)-induced immune response by phosphorylating and activating TICAM2/TRAM, which in turn activates the transcription factor IRF3 and subsequent cytokines production. In differentiating erythroid progenitors, is regulated by EPO and controls the protection against the TNFSF10/TRAIL-mediated apoptosis, via BCL2. May be involved in the regulation of the insulin-induced phosphorylation and activation of AKT1. Calcium-independent, phospholipid- and diacylglycerol (DAG)-dependent serine/threonine-protein kinase that plays essential roles in the regulation of multiple cellular processes linked to cytoskeletal proteins, such as cell adhesion, motility, migration and cell cycle, functions in neuron growth and ion channel regulation, and is involved in immune response, cancer cell invasion and regulation of apoptosis. T00895 PDBSTRUC 5LIH; 2WH0 T00895 BIOCLASS Kinase T00895 ECNUMBER EC 2.7.11.13 T00895 SEQUENCE MVVFNGLLKIKICEAVSLKPTAWSLRHAVGPRPQTFLLDPYIALNVDDSRIGQTATKQKTNSPAWHDEFVTDVCNGRKIELAVFHDAPIGYDDFVANCTIQFEELLQNGSRHFEDWIDLEPEGRVYVIIDLSGSSGEAPKDNEERVFRERMRPRKRQGAVRRRVHQVNGHKFMATYLRQPTYCSHCRDFIWGVIGKQGYQCQVCTCVVHKRCHELIITKCAGLKKQETPDQVGSQRFSVNMPHKFGIHNYKVPTFCDHCGSLLWGLLRQGLQCKVCKMNVHRRCETNVAPNCGVDARGIAKVLADLGVTPDKITNSGQRRKKLIAGAESPQPASGSSPSEEDRSKSAPTSPCDQEIKELENNIRKALSFDNRGEEHRAASSPDGQLMSPGENGEVRQGQAKRLGLDEFNFIKVLGKGSFGKVMLAELKGKDEVYAVKVLKKDVILQDDDVDCTMTEKRILALARKHPYLTQLYCCFQTKDRLFFVMEYVNGGDLMFQIQRSRKFDEPRSRFYAAEVTSALMFLHQHGVIYRDLKLDNILLDAEGHCKLADFGMCKEGILNGVTTTTFCGTPDYIAPEILQELEYGPSVDWWALGVLMYEMMAGQPPFEADNEDDLFESILHDDVLYPVWLSKEAVSILKAFMTKNPHKRLGCVASQNGEDAIKQHPFFKEIDWVLLEQKKIKPPFKPRIKTKRDVNNFDQDFTREEPVLTLVDEAIVKQINQEEFKGFSYFGEDLMP T00895 DRUGINFO D0Y4AW Meprobamate Approved T00895 DRUGINFO D0E6AH Bryostatin-1 Phase 2 T00895 DRUGINFO D0J7CE CDE-6960 Terminated T00895 DRUGINFO D0X0HN LY-317644 Terminated T00895 DRUGINFO D0R5ZR RO-320432 Terminated T00895 DRUGINFO D00TWA [2,2':5',2'']Terthiophen-4-yl-methanol Investigative T00895 DRUGINFO D05LRV [2,2':5',2'']Terthiophene-4,5''-dicarbaldehyde Investigative T00895 DRUGINFO D0D3MR [2,2':5',2'']Terthiophene-4-carbaldehyde Investigative T00895 DRUGINFO D02QME 2-(4-Hydroxy-phenyl)-3,3-diphenyl-acrylonitrile Investigative T00895 DRUGINFO D0S9UK 2,3,3-Triphenyl-acrylonitrile Investigative T00895 DRUGINFO D09XIE 3-(4-Hydroxy-phenyl)-2,3-diphenyl-acrylonitrile Investigative T00895 DRUGINFO D0EK0G 3-(4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione Investigative T00895 DRUGINFO D06AOY 3-(indole-3-yl)-4-phenyl-1H-pyrrole-2,5-dione Investigative T00895 DRUGINFO D0T0UH 3,3-Bis-(4-hydroxy-phenyl)-2-phenyl-acrylonitrile Investigative T00895 DRUGINFO D0A8MN 3,3-Bis-(4-methoxy-phenyl)-2-phenyl-acrylonitrile Investigative T00895 DRUGINFO D00NYT 3,4-di-(4-methoxyphenyl)-1H-pyrrole-2,5-dione Investigative T00895 DRUGINFO D0C3WY 3,4-diphenyl-1H-pyrrole-2,5-dione Investigative T00895 DRUGINFO D02PUV 4-[1-(4-hydroxyphenyl)-3-methyl-1-butenyl]phenol Investigative T00895 DRUGINFO D0Q3GQ 4-cycloheptyliden(4-hydroxyphenyl)methylphenol Investigative T00895 DRUGINFO D0V9SW 4-cyclohexyliden(4-hydroxyphenyl)methylphenol Investigative T00895 DRUGINFO D06ZCX LY-326449 Investigative T00895 DRUGINFO D0D4ZL Phorbol 12-myristate Investigative T00895 DRUGINFO D0L8HO RO-316233 Investigative T00895 DRUGINFO D09TSC Ro-32-0557 Investigative T00895 KEGGPATH hsa04022:cGMP-PKG signaling pathway T00895 KEGGPATH hsa04071:Sphingolipid signaling pathway T00895 KEGGPATH hsa04270:Vascular smooth muscle contraction T00895 KEGGPATH hsa04530:Tight junction T00895 KEGGPATH hsa04664:Fc epsilon RI signaling pathway T00895 KEGGPATH hsa04666:Fc gamma R-mediated phagocytosis T00895 KEGGPATH hsa04750:Inflammatory mediator regulation of TRP channels T00895 KEGGPATH hsa04930:Type II diabetes mellitus T00895 KEGGPATH hsa05206:MicroRNAs in cancer T00895 WIKIPATH WP1528:Physiological and Pathological Hypertrophy of the Heart T00895 WIKIPATH WP1809:Effects of PIP2 hydrolysis T00895 WIKIPATH WP1824:GPCR downstream signaling T00895 WIKIPATH WP2012:miRs in Muscle Cell Differentiation T00895 WIKIPATH WP2374:Oncostatin M Signaling Pathway T00895 WIKIPATH WP289:Myometrial Relaxation and Contraction Pathways T00895 WIKIPATH WP35:G Protein Signaling Pathways T00895 WIKIPATH WP399:Wnt Signaling Pathway and Pluripotency T00895 WIKIPATH WP428:Wnt Signaling Pathway T00895 WIKIPATH WP536:Calcium Regulation in the Cardiac Cell T00895 WIKIPATH WP666:Hypothetical Network for Drug Addiction T00895 REACPATH R-HSA-114508:Effects of PIP2 hydrolysis T00895 REACPATH R-HSA-1489509:DAG and IP3 signaling T00895 REACPATH R-HSA-2029485:Role of phospholipids in phagocytosis T00895 REACPATH R-HSA-418597:G alpha (z) signalling events T00895 NET_PATH NetPath_14:IL2 Signaling Pathway T00895 INTEPATH cd8tcrdownstreampathway:Downstream signaling in naïve CD8+ T cells T00895 INTEPATH cd8tcrpathway:TCR signaling in naïve CD8+ T cells T00895 INTEPATH cdc42_pathway:CDC42 signaling events T00895 INTEPATH endothelinpathway:Endothelins T00895 INTEPATH il2_1pathway:IL2-mediated signaling events T00895 INTEPATH il8cxcr1_pathway:IL8- and CXCR1-mediated signaling events T00895 INTEPATH lpa4_pathway:LPA4-mediated signaling events T00895 INTEPATH lysophospholipid_pathway:LPA receptor mediated events T00895 INTEPATH nfat_3pathway:Role of Calcineurin-dependent NFAT signaling in lymphocytes T00895 INTEPATH pdgfrbpathway:PDGFR-beta signaling pathway T00895 INTEPATH ras_pathway:Regulation of Ras family activation T00895 INTEPATH tcr_pathway:TCR signaling in naïve CD4+ T cells T00895 INTEPATH txa2pathway:Thromboxane A2 receptor signaling T00895 PANTPATH P00002:Alpha adrenergic receptor signaling pathway T00895 PANTPATH P00003:Alzheimer disease-amyloid secretase pathway T00895 PANTPATH P00005:Angiogenesis T00895 PANTPATH P00006:Apoptosis signaling pathway T00895 PANTPATH P00018:EGF receptor signaling pathway T00895 PANTPATH P00019:Endothelin signaling pathway T00895 PANTPATH P00021:FGF signaling pathway T00895 PANTPATH P00027:Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway T00895 PANTPATH P00031:Inflammation mediated by chemokine and cytokine signaling pathway T00895 PANTPATH P00042:Muscarinic acetylcholine receptor 1 and 3 signaling pathway T00895 PANTPATH P00056:VEGF signaling pathway T00895 PANTPATH P00057:Wnt signaling pathway T00895 PANTPATH P04374:5HT2 type receptor mediated signaling pathway T00895 PANTPATH P04385:Histamine H1 receptor mediated signaling pathway T00895 PANTPATH P04391:Oxytocin receptor mediated signaling pathway T00895 PANTPATH P04394:Thyrotropin-releasing hormone receptor signaling pathway T00895 PANTPATH P06959:CCKR signaling map ST T97071 TARGETID T97071 T97071 FORMERID TTDS00441 T97071 UNIPROID FOLH1_HUMAN T97071 TARGNAME Glutamate carboxypeptidase II (GCPII) T97071 GENENAME FOLH1 T97071 TARGTYPE Successful target T97071 SYNONYMS Pteroylpoly-gamma-glutamate carboxypeptidase; Prostate-specific membrane antigen; PSMA; PSM; NAALADase I; NAALAD1; N-acetylated-alpha-linked acidic dipeptidase I; Membrane glutamate carboxypeptidase; MGCP; Glutamate carboxypeptidase 2; GIG27; Folylpoly-gamma-glutamate carboxypeptidase; Folate hydrolase 1; FOLH; FGCP; Cell growth-inhibiting gene 27 protein T97071 FUNCTION Has a preference for tri-alpha-glutamate peptides. In the intestine, required for the uptake of folate. In the brain, modulates excitatory neurotransmission through the hydrolysis of the neuropeptide, N-aceylaspartylglutamate (NAAG), thereby releasing glutamate. Involved in prostate tumor progression. Has both folate hydrolase and N-acetylated-alpha-linked-acidic dipeptidase (NAALADase) activity. T97071 PDBSTRUC 6HKZ; 6HKJ; 6H7Z; 6H7Y; 6FE5 T97071 BIOCLASS Peptidase T97071 ECNUMBER EC 3.4.17.21 T97071 SEQUENCE MWNLLHETDSAVATARRPRWLCAGALVLAGGFFLLGFLFGWFIKSSNEATNITPKHNMKAFLDELKAENIKKFLYNFTQIPHLAGTEQNFQLAKQIQSQWKEFGLDSVELAHYDVLLSYPNKTHPNYISIINEDGNEIFNTSLFEPPPPGYENVSDIVPPFSAFSPQGMPEGDLVYVNYARTEDFFKLERDMKINCSGKIVIARYGKVFRGNKVKNAQLAGAKGVILYSDPADYFAPGVKSYPDGWNLPGGGVQRGNILNLNGAGDPLTPGYPANEYAYRRGIAEAVGLPSIPVHPIGYYDAQKLLEKMGGSAPPDSSWRGSLKVPYNVGPGFTGNFSTQKVKMHIHSTNEVTRIYNVIGTLRGAVEPDRYVILGGHRDSWVFGGIDPQSGAAVVHEIVRSFGTLKKEGWRPRRTILFASWDAEEFGLLGSTEWAEENSRLLQERGVAYINADSSIEGNYTLRVDCTPLMYSLVHNLTKELKSPDEGFEGKSLYESWTKKSPSPEFSGMPRISKLGSGNDFEVFFQRLGIASGRARYTKNWETNKFSGYPLYHSVYETYELVEKFYDPMFKYHLTVAQVRGGMVFELANSIVLPFDCRDYAVVLRKYADKIYSISMKHPQEMKTYSVSFDSLFSAVKNFTEIASKFSERLQDFDKSNPIVLRMMNDQLMFLERAFIDPLGLPDRPFYRHVIYAPSSHNKYAGESFPGIYDALFDIESKVDPSKAWGEVKRQIYVAAFTVQAAAETLSEVA T97071 DRUGINFO D09PGL Capromab Approved T97071 DRUGINFO DBG46D PSMA-11 Ga-68 Approved T97071 DRUGINFO DGQW52 177Lu-labelled PSMA-617 Phase 3 T97071 DRUGINFO DSM5X9 177-Lu-PSMA-617 Phase 3 T97071 DRUGINFO D08FTP 99mTc-MIP-1404 Phase 2 T97071 DRUGINFO D06URI ATL101 Phase 2 T97071 DRUGINFO D05MOZ G-202 Phase 2 T97071 DRUGINFO D02EEK J 591 Lu-177 Phase 2 T97071 DRUGINFO D0H5ER MLN-591RL Phase 2 T97071 DRUGINFO DP6J5K 177Lu-labelled PSMA-R2 Phase 1/2 T97071 DRUGINFO D1CZ8K 177-Lu-PSMA-R2 Phase 1/2 T97071 DRUGINFO D0VI8T 4SCAR-PSMA Phase 1/2 T97071 DRUGINFO D0RO2L CAR-T cells targeting PSMA Phase 1/2 T97071 DRUGINFO D0W7FC MLN-2704 Phase 1/2 T97071 DRUGINFO D8UZM7 REGN5678 Phase 1/2 T97071 DRUGINFO DM6CE2 177Lu-labelled CTT-1403 Phase 1 T97071 DRUGINFO DXV67Q 227Th-labelled PSMA-TTC Phase 1 T97071 DRUGINFO D0F5KN 99mTc-MIP-1405 Phase 1 T97071 DRUGINFO DOY4E6 AMG 160 Phase 1 T97071 DRUGINFO D03JTL APVO414 Phase 1 T97071 DRUGINFO D04UWG Autologous T-cell therapy Phase 1 T97071 DRUGINFO D0TN7S BAY-1075553 Phase 1 T97071 DRUGINFO DY4X5W CCW702 Phase 1 T97071 DRUGINFO DH5S6Z CTT1403 Phase 1 T97071 DRUGINFO D0H4IU GPI-16072 Phase 1 T97071 DRUGINFO D48MDS HPN424 Phase 1 T97071 DRUGINFO D04KRV Iofolastat I-124 Phase 1 T97071 DRUGINFO D2Y9IG JNJ-63898081 Phase 1 T97071 DRUGINFO D0N6QB MT-112 Phase 1 T97071 DRUGINFO DAS4D6 PSMA CAR-T cell therapy Phase 1 T97071 DRUGINFO D08JYV PSMA subunit vaccine Phase 1 T97071 DRUGINFO D0O0JB PSMA-targeted tubulysin B conjugates Phase 1 T97071 DRUGINFO D07KHR PSMA-VRP Phase 1 T97071 DRUGINFO D03ZHE MDX-070 Discontinued in Phase 2 T97071 DRUGINFO D0M8PM IRX-4 Preclinical T97071 DRUGINFO D06DUE [3H]quisqualate Investigative T97071 DRUGINFO D0QA5U 2-(2-carboxy-5-mercaptopentyl)benzoic acid Investigative T97071 DRUGINFO D03JFL 2-(2-carboxy-7-mercaptoheptyl)benzoic acid Investigative T97071 DRUGINFO D05SNS 2-(2-Hydroxycarbamoyl-ethyl)-pentanedioic acid Investigative T97071 DRUGINFO D0C2FS 2-(2-Mercapto-ethyl)-pentanedioic acid Investigative T97071 DRUGINFO D0Z5VI 2-(2-Phosphonooxy-ethyl)-pentanedioic acid Investigative T97071 DRUGINFO D0D8NM 2-(3-carbamoylbenzyl)-5-mercaptopentanoic acid Investigative T97071 DRUGINFO D05VWZ 2-(3-carboxybenzyl)succinic acid Investigative T97071 DRUGINFO D0E3OH 2-(3-cyanobenzyl)-5-mercaptopentanoic acid Investigative T97071 DRUGINFO D0ZJ9S 2-(3-Hydroxycarbamoyl-propyl)-pentanedioic acid Investigative T97071 DRUGINFO D0Y7AN 2-(3-Mercapto-propyl)-pentanedioic acid Investigative T97071 DRUGINFO D0Q2OH 2-(3-Methylsulfanyl-propyl)-pentanedioic acid Investigative T97071 DRUGINFO D08TDE 2-(4-Mercapto-butyl)-pentanedioic acid Investigative T97071 DRUGINFO D0Q3KD 2-(5-Mercapto-pentyl)-pentanedioic acid Investigative T97071 DRUGINFO D0B9YO 2-benzyl-5-mercaptopentanoic acid Investigative T97071 DRUGINFO D0FU7Y 2-Hydroxycarbamoylmethyl-pentanedioic acid Investigative T97071 DRUGINFO D02CYQ 2-Hydroxycarbamoyl-pentanedioic acid Investigative T97071 DRUGINFO D0E0HK 2-Mercaptomethyl-pentanedioic acid Investigative T97071 DRUGINFO D08CYU 2-Mercapto-pentanedioic acid Investigative T97071 DRUGINFO D0A1FL 2-Phosphonooxy-pentanedioic acid Investigative T97071 DRUGINFO D0Y6UB 2-PMPA Investigative T97071 DRUGINFO D0ND1C 3-(1-carboxy-4-mercaptobutoxy)benzoic acid Investigative T97071 DRUGINFO D0JX2S 3-(2-carbamoyl-5-mercaptopentyl)benzoic acid Investigative T97071 DRUGINFO D0T8ZL 3-(2-carboxy-3-mercaptopropyl)benzoic acid Investigative T97071 DRUGINFO D0C5JP 3-(2-carboxy-3-phosphonopropyl)benzoic acid Investigative T97071 DRUGINFO D04VFS 3-(2-carboxy-4-mercaptobutyl)benzoic acid Investigative T97071 DRUGINFO D0F8TZ 3-(2-carboxy-5-mercaptopentyl)benzoic acid Investigative T97071 DRUGINFO D03RMT 3-(2-carboxy-6-mercaptohexyl)benzoic acid Investigative T97071 DRUGINFO D0X1DO 3-[(1-carboxy-4-mercaptobutyl)thio]benzoic acid Investigative T97071 DRUGINFO D04SZR 4-(2-carboxy-5-mercaptopentyl)benzoic acid Investigative T97071 DRUGINFO D0Z0UQ 5-Mercapto-pentanoic acid Investigative T97071 DRUGINFO D0Z9BU 99mTc-EC-0652 Investigative T97071 DRUGINFO D0K3GB 99mTc-MIP-1340 Investigative T97071 DRUGINFO D0M1NS CTT-54 Investigative T97071 DRUGINFO D05UAO J591-Ac-225 Investigative T97071 DRUGINFO D0IW9Q MDX-1147 Investigative T97071 DRUGINFO D0Z5UD MIP-1375 Investigative T97071 DRUGINFO D06LAX PGI-02749 Investigative T97071 DRUGINFO D06JOJ PMID15027864C8d Investigative T97071 KEGGPATH hsa00250:Alanine, aspartate and glutamate metabolism T97071 KEGGPATH hsa01100:Metabolic pathways T97071 KEGGPATH hsa04977:Vitamin digestion and absorption T97071 WIKIPATH WP241:One Carbon Metabolism T97071 REACPATH R-HSA-70614:Amino acid synthesis and interconversion (transamination) T97071 NET_PATH NetPath_11:TCR Signaling Pathway T97071 NET_PATH NetPath_9:TNFalpha Signaling Pathway T86591 TARGETID T86591 T86591 FORMERID TTDS00340 T86591 UNIPROID PPARA_HUMAN T86591 TARGNAME Peroxisome proliferator-activated receptor alpha (PPARA) T86591 GENENAME PPARA T86591 TARGTYPE Successful target T86591 SYNONYMS Peroxisome proliferater-activated receptor alpha; PPARalpha; PPAR-alpha; PPAR; Nuclear receptor subfamily 1 group C member 1; NR1C1 T86591 FUNCTION Key regulator of lipid metabolism. Activated by the endogenous ligand 1-palmitoyl-2-oleoyl-sn-glycerol-3-phosphocholine (16:0/18:1-GPC). Activated by oleylethanolamide, a naturally occurring lipid that regulates satiety. Receptor for peroxisome proliferators such as hypolipidemic drugs and fatty acids. Regulates the peroxisomal beta-oxidation pathway of fatty acids. Functions as transcription activator for the ACOX1 and P450 genes. Transactivation activity requires heterodimerization with RXRA and is antagonized by NR2C2. May be required for the propagation of clock information to metabolic pathways regulated by PER2. Ligand-activated transcription factor. T86591 PDBSTRUC 5HYK; 5AZT; 4CI4; 4BCR; 3VI8 T86591 BIOCLASS Nuclear hormone receptor T86591 SEQUENCE MVDTESPLCPLSPLEAGDLESPLSEEFLQEMGNIQEISQSIGEDSSGSFGFTEYQYLGSCPGSDGSVITDTLSPASSPSSVTYPVVPGSVDESPSGALNIECRICGDKASGYHYGVHACEGCKGFFRRTIRLKLVYDKCDRSCKIQKKNRNKCQYCRFHKCLSVGMSHNAIRFGRMPRSEKAKLKAEILTCEHDIEDSETADLKSLAKRIYEAYLKNFNMNKVKARVILSGKASNNPPFVIHDMETLCMAEKTLVAKLVANGIQNKEAEVRIFHCCQCTSVETVTELTEFAKAIPGFANLDLNDQVTLLKYGVYEAIFAMLSSVMNKDGMLVAYGNGFITREFLKSLRKPFCDIMEPKFDFAMKFNALELDDSDISLFVAAIICCGDRPGLLNVGHIEKMQEGIVHVLRLHLQSNHPDDIFLFPKLLQKMADLRQLVTEHAQLVQIIKKTESDAALHPLLQEIYRDMY T86591 DRUGINFO D00WCX Bezafibrate Approved T86591 DRUGINFO D0EJ6O Ciprofibrate Approved T86591 DRUGINFO D07XGR Fenofibrate Approved T86591 DRUGINFO D04BCB Lobeglitazone Approved T86591 DRUGINFO D04QIE Pemafibrate Approved T86591 DRUGINFO D0F5JH CS-038 Phase 3 T86591 DRUGINFO D0LW1Y GFT-505 Phase 3 T86591 DRUGINFO D0VU5M Imiglitazar Phase 3 T86591 DRUGINFO D0M3UT MURAGLITAZAR Phase 3 T86591 DRUGINFO D02NHD Ragaglitazar Phase 3 T86591 DRUGINFO D0H1NL TESAGLITAZAR Phase 3 T86591 DRUGINFO D0T7MN ZYH-1 Phase 3 T86591 DRUGINFO D0RJ0V GFT14 Phase 2 T86591 DRUGINFO D0I5IM LY-518674 Phase 2 T86591 DRUGINFO D04BPS Naveglitazar Phase 2 T86591 DRUGINFO D0PP8G ONO-5129 Phase 2 T86591 DRUGINFO DE6GF4 ZYH7 Phase 2 T86591 DRUGINFO D01UJK AVE0897 Phase 1 T86591 DRUGINFO D00HYD CDT-fenofibrate Phase 1 T86591 DRUGINFO D0AX9S GW-409544 Phase 1 T86591 DRUGINFO D03RJZ Oxeglitazar Phase 1 T86591 DRUGINFO DF8M1T TPST-1120 Phase 1 T86591 DRUGINFO D0HW6Y Flavonoid derivative 8 Patented T86591 DRUGINFO D0O5IN PMID25416646-Compound-Figure5-A Patented T86591 DRUGINFO D05AUY PMID25416646-Compound-Figure5-H Patented T86591 DRUGINFO D0B9EN Aleglitazar Discontinued in Phase 3 T86591 DRUGINFO D0W2IU AVE-0847 Discontinued in Phase 2 T86591 DRUGINFO D0R5QQ AVE-8134 Discontinued in Phase 2 T86591 DRUGINFO D0Q8UU BM-17.0744 Discontinued in Phase 2 T86591 DRUGINFO D0S6KX GSK-677954 Discontinued in Phase 2 T86591 DRUGINFO D09OHP Indeglitazar Discontinued in Phase 2 T86591 DRUGINFO D0B8JQ KRP-101 Discontinued in Phase 2 T86591 DRUGINFO D02RAU KRP-297 Discontinued in Phase 2 T86591 DRUGINFO D08LZI NS-220 Discontinued in Phase 2 T86591 DRUGINFO D02ZKL Reglixane Discontinued in Phase 2 T86591 DRUGINFO D01JGG Sodelglitazar Discontinued in Phase 2 T86591 DRUGINFO D04FTB AR-H049020 Discontinued in Phase 1 T86591 DRUGINFO D0W3YW DRF 10945 Discontinued in Phase 1 T86591 DRUGINFO D06PHO E-3030 Discontinued in Phase 1 T86591 DRUGINFO D09SLU LG-101280 Discontinued in Phase 1 T86591 DRUGINFO D0B0EB LY-929 Discontinued in Phase 1 T86591 DRUGINFO D0Z3XO MP-136 Discontinued in Phase 1 T86591 DRUGINFO D04PBS MC-3001 Preclinical T86591 DRUGINFO D08WOE MC-3002 Preclinical T86591 DRUGINFO D09XCX PIRINIXIC ACID Preclinical T86591 DRUGINFO D0U2FN Romazarit Preclinical T86591 DRUGINFO D0I0RF BVT-142 Terminated T86591 DRUGINFO D0V0TT CS-204 Terminated T86591 DRUGINFO D03CUS CS-207 Terminated T86591 DRUGINFO D0BB1X KRP-105 Terminated T86591 DRUGINFO D0OW6Z Sipoglitazar Terminated T86591 DRUGINFO D06GYO (9Z,12E)-12-nitrooctadeca-9,12-dienoic acid Investigative T86591 DRUGINFO D0M9LL (E)-12-Nitrooctadec-12-enoic Acid Investigative T86591 DRUGINFO D0P5QM (E)-13-Nitrooctadec-12-enoic Acid Investigative T86591 DRUGINFO D00AII (E)-4-(3,5-dimethoxystyryl)phenol Investigative T86591 DRUGINFO D0K6TI 8S-HETE Investigative T86591 DRUGINFO D00EOP AD-5061 Investigative T86591 DRUGINFO D08UWZ BMS-687453 Investigative T86591 DRUGINFO D01KPN CP-775146 Investigative T86591 DRUGINFO D01ARG DB-900 Investigative T86591 DRUGINFO D0S4GK Deoxy-Bigchap Investigative T86591 DRUGINFO D0M8VN DRF 2519 Investigative T86591 DRUGINFO D0G9IP eicosatetranoic acid Investigative T86591 DRUGINFO D06RRD Fibrates Investigative T86591 DRUGINFO D05CLM GSK-9578 Investigative T86591 DRUGINFO D01POG GW-2331 Investigative T86591 DRUGINFO D00TFA GW7647 Investigative T86591 DRUGINFO D0F0MP L-165461 Investigative T86591 DRUGINFO D09JII L-796449 Investigative T86591 DRUGINFO D0K8HA LL-6531 Investigative T86591 DRUGINFO D0Z7OX LY-465608 Investigative T86591 DRUGINFO D07MBC N-oleoylethanolamide Investigative T86591 DRUGINFO D0EN7T pristanic acid Investigative T86591 DRUGINFO D08XGH reglitazar Investigative T86591 DRUGINFO D04JOG TZD18 Investigative T86591 DRUGINFO D0Z4MH ZY H2 Investigative T86591 KEGGPATH hsa03320:PPAR signaling pathway T86591 KEGGPATH hsa04024:cAMP signaling pathway T86591 KEGGPATH hsa04920:Adipocytokine signaling pathway T86591 KEGGPATH hsa04922:Glucagon signaling pathway T86591 KEGGPATH hsa04932:Non-alcoholic fatty liver disease (NAFLD) T86591 KEGGPATH hsa05160:Hepatitis C T86591 WIKIPATH WP170:Nuclear Receptors T86591 WIKIPATH WP1797:Circadian Clock T86591 WIKIPATH WP2011:SREBF and miR33 in cholesterol and lipid homeostasis T86591 WIKIPATH WP236:Adipogenesis T86591 WIKIPATH WP2706:Activation of Gene Expression by SREBP (SREBF) T86591 WIKIPATH WP2738:YAP1- and WWTR1 (TAZ)-stimulated gene expression T86591 WIKIPATH WP2751:Transcriptional Regulation of White Adipocyte Differentiation T86591 WIKIPATH WP2797:Regulation of Lipid Metabolism by Peroxisome proliferator-activated receptor alpha (PPARalpha) T86591 WIKIPATH WP2878:PPAR Alpha Pathway T86591 WIKIPATH WP2881:Estrogen Receptor Pathway T86591 WIKIPATH WP2882:Nuclear Receptors Meta-Pathway T86591 WIKIPATH WP299:Nuclear Receptors in Lipid Metabolism and Toxicity T86591 REACPATH R-HSA-1368082:RORA activates gene expression T86591 REACPATH R-HSA-1368108:BMAL1:CLOCK,NPAS2 activates circadian gene expression T86591 REACPATH R-HSA-1989781:PPARA activates gene expression T86591 REACPATH R-HSA-2032785:YAP1- and WWTR1 (TAZ)-stimulated gene expression T86591 REACPATH R-HSA-2151201:Transcriptional activation of mitochondrial biogenesis T86591 REACPATH R-HSA-2426168:Activation of gene expression by SREBF (SREBP) T86591 REACPATH R-HSA-381340:Transcriptional regulation of white adipocyte differentiation T86591 REACPATH R-HSA-383280:Nuclear Receptor transcription pathway T86591 REACPATH R-HSA-400206:Regulation of lipid metabolism by Peroxisome proliferator-activated receptor alpha (PPARalpha) T86591 REACPATH R-HSA-400253:Circadian Clock T86591 INTEPATH rxr_vdr_pathway:RXR and RAR heterodimerization with other nuclear receptor T25464 TARGETID T25464 T25464 FORMERID TTDS00363 T25464 UNIPROID PP2BA_HUMAN T25464 TARGNAME Calcineurin (PPP3CA) T25464 GENENAME PPP3CA T25464 TARGTYPE Successful target T25464 SYNONYMS Serine/threonine-protein phosphatase 2B catalytic subunit alpha isoform; Calmodulin-dependent calcineurin A subunit alpha isoform; CNA; CAM-PRP catalytic subunit; CALNA T25464 FUNCTION Many of the substrates contain a PxIxIT motif and/or a LxVP motif. In response to increased Ca(2+) levels, dephosphorylates and activates phosphatase SSH1 which results in cofilin dephosphorylation. In response to increased Ca(2+) levels following mitochondrial depolarization, dephosphorylates DNM1L inducing DNM1L translocation to the mitochondrion. Dephosphorylates heat shock protein HSPB1. Dephosphorylates and activates transcription factor NFATC1. In response to increased Ca(2+) levels, regulates NFAT-mediated transcription probably by dephosphorylating NFAT and promoting its nuclear translocation. Dephosphorylates and inactivates transcription factor ELK1. Dephosphorylates DARPP32. May dephosphorylate CRTC2 at 'Ser-171' resulting in CRTC2 dissociation from 14-3-3 proteins. Calcium-dependent, calmodulin-stimulated protein phosphatase which plays an essential role in the transduction of intracellular Ca(2+)-mediated signals. T25464 PDBSTRUC 5SVE; 5C1V; 4Q5U; 4F0Z; 3LL8 T25464 BIOCLASS Phosphoric monoester hydrolase T25464 ECNUMBER EC 3.1.3.16 T25464 SEQUENCE MSEPKAIDPKLSTTDRVVKAVPFPPSHRLTAKEVFDNDGKPRVDILKAHLMKEGRLEESVALRIITEGASILRQEKNLLDIDAPVTVCGDIHGQFFDLMKLFEVGGSPANTRYLFLGDYVDRGYFSIECVLYLWALKILYPKTLFLLRGNHECRHLTEYFTFKQECKIKYSERVYDACMDAFDCLPLAALMNQQFLCVHGGLSPEINTLDDIRKLDRFKEPPAYGPMCDILWSDPLEDFGNEKTQEHFTHNTVRGCSYFYSYPAVCEFLQHNNLLSILRAHEAQDAGYRMYRKSQTTGFPSLITIFSAPNYLDVYNNKAAVLKYENNVMNIRQFNCSPHPYWLPNFMDVFTWSLPFVGEKVTEMLVNVLNICSDDELGSEEDGFDGATAAARKEVIRNKIRAIGKMARVFSVLREESESVLTLKGLTPTGMLPSGVLSGGKQTLQSATVEAIEADEAIKGFSPQHKITSFEEAKGLDRINERMPPRRDAMPSDANLNSINKALTSETNGTDSNGSNSSNIQ T25464 DRUGINFO D0O3YF Ciclosporin Approved T25464 DRUGINFO D0Z4UN Pimecrolimus Approved T25464 DRUGINFO D06OMK Tacrolimus Approved T25464 DRUGINFO D0L9HX Voclosporin Approved T25464 DRUGINFO D08IGF L-685,818 Investigative T25464 KEGGPATH hsa04010:MAPK signaling pathway T25464 KEGGPATH hsa04020:Calcium signaling pathway T25464 KEGGPATH hsa04022:cGMP-PKG signaling pathway T25464 KEGGPATH hsa04114:Oocyte meiosis T25464 KEGGPATH hsa04210:Apoptosis T25464 KEGGPATH hsa04310:Wnt signaling pathway T25464 KEGGPATH hsa04360:Axon guidance T25464 KEGGPATH hsa04370:VEGF signaling pathway T25464 KEGGPATH hsa04380:Osteoclast differentiation T25464 KEGGPATH hsa04650:Natural killer cell mediated cytotoxicity T25464 KEGGPATH hsa04660:T cell receptor signaling pathway T25464 KEGGPATH hsa04662:B cell receptor signaling pathway T25464 KEGGPATH hsa04720:Long-term potentiation T25464 KEGGPATH hsa04724:Glutamatergic synapse T25464 KEGGPATH hsa04728:Dopaminergic synapse T25464 KEGGPATH hsa04921:Oxytocin signaling pathway T25464 KEGGPATH hsa04922:Glucagon signaling pathway T25464 KEGGPATH hsa05010:Alzheimer's disease T25464 KEGGPATH hsa05014:Amyotrophic lateral sclerosis (ALS) T25464 KEGGPATH hsa05031:Amphetamine addiction T25464 KEGGPATH hsa05152:Tuberculosis T25464 KEGGPATH hsa05166:HTLV-I infection T25464 WIKIPATH WP1528:Physiological and Pathological Hypertrophy of the Heart T25464 WIKIPATH WP1544:MicroRNAs in cardiomyocyte hypertrophy T25464 WIKIPATH WP1978:Opioid Signalling T25464 WIKIPATH WP2004:miR-targeted genes in lymphocytes - TarBase T25464 WIKIPATH WP2005:miR-targeted genes in muscle cell - TarBase T25464 WIKIPATH WP2059:Alzheimers Disease T25464 WIKIPATH WP2431:Spinal Cord Injury T25464 WIKIPATH WP2447:Amyotrophic lateral sclerosis (ALS) T25464 WIKIPATH WP2583:T-Cell Receptor and Co-stimulatory Signaling T25464 WIKIPATH WP2746:Signaling by the B Cell Receptor (BCR) T25464 WIKIPATH WP2759:Fc epsilon receptor (FCERI) signaling T25464 WIKIPATH WP2795:Cardiac Hypertrophic Response T25464 WIKIPATH WP35:G Protein Signaling Pathways T25464 WIKIPATH WP382:MAPK Signaling Pathway T25464 WIKIPATH WP391:Mitochondrial Gene Expression T25464 REACPATH R-HSA-180024:DARPP-32 events T25464 REACPATH R-HSA-2871809:FCERI mediated Ca+2 mobilization T25464 REACPATH R-HSA-4086398:Ca2+ pathway T88975 TARGETID T88975 T88975 FORMERID TTDS00390 T88975 UNIPROID PDE3A_HUMAN T88975 TARGNAME Phosphodiesterase 3A (PDE3A) T88975 GENENAME PDE3A T88975 TARGTYPE Successful target T88975 SYNONYMS cGMP-inhibited 3',5'-cyclic phosphodiesterase A; Phosphodiesterase 3A; Cyclic GMP-inhibited phosphodiesterase A; Cyclic GMP inhibited phosphodiesterase A; CGI-PDE A T88975 FUNCTION Cyclic nucleotide phosphodiesterase with a dual-specificity for the second messengers cAMP and cGMP, which are key regulators of many important physiological processes. T88975 PDBSTRUC 1LRC T88975 BIOCLASS Phosphoric diester hydrolase T88975 ECNUMBER EC 3.1.4.17 T88975 SEQUENCE MAVPGDAARVRDKPVHSGVSQAPTAGRDCHHRADPASPRDSGCRGCWGDLVLQPLRSSRKLSSALCAGSLSFLLALLVRLVRGEVGCDLEQCKEAAAAEEEEAAPGAEGGVFPGPRGGAPGGGARLSPWLQPSALLFSLLCAFFWMGLYLLRAGVRLPLAVALLAACCGGEALVQIGLGVGEDHLLSLPAAGVVLSCLAAATWLVLRLRLGVLMIALTSAVRTVSLISLERFKVAWRPYLAYLAGVLGILLARYVEQILPQSAEAAPREHLGSQLIAGTKEDIPVFKRRRRSSSVVSAEMSGCSSKSHRRTSLPCIPREQLMGHSEWDHKRGPRGSQSSGTSITVDIAVMGEAHGLITDLLADPSLPPNVCTSLRAVSNLLSTQLTFQAIHKPRVNPVTSLSENYTCSDSEESSEKDKLAIPKRLRRSLPPGLLRRVSSTWTTTTSATGLPTLEPAPVRRDRSTSIKLQEAPSSSPDSWNNPVMMTLTKSRSFTSSYAISAANHVKAKKQSRPGALAKISPLSSPCSSPLQGTPASSLVSKISAVQFPESADTTAKQSLGSHRALTYTQSAPDLSPQILTPPVICSSCGRPYSQGNPADEPLERSGVATRTPSRTDDTAQVTSDYETNNNSDSSDIVQNEDETECLREPLRKASACSTYAPETMMFLDKPILAPEPLVMDNLDSIMEQLNTWNFPIFDLVENIGRKCGRILSQVSYRLFEDMGLFEAFKIPIREFMNYFHALEIGYRDIPYHNRIHATDVLHAVWYLTTQPIPGLSTVINDHGSTSDSDSDSGFTHGHMGYVFSKTYNVTDDKYGCLSGNIPALELMALYVAAAMHDYDHPGRTNAFLVATSAPQAVLYNDRSVLENHHAAAAWNLFMSRPEYNFLINLDHVEFKHFRFLVIEAILATDLKKHFDFVAKFNGKVNDDVGIDWTNENDRLLVCQMCIKLADINGPAKCKELHLQWTDGIVNEFYEQGDEEASLGLPISPFMDRSAPQLANLQESFISHIVGPLCNSYDSAGLMPGKWVEDSDESGDTDDPEEEEEEAPAPNEEETCENNESPKKKTFKRRKIYCQITQHLLQNHKMWKKVIEEEQRLAGIENQSLDQTPQSHSSEQIQAIKEEEEEKGKPRGEEIPTQKPDQ T88975 DRUGINFO D03TYI Aminophylline Approved T88975 DRUGINFO D0D1HW Anagrelide Approved T88975 DRUGINFO D03VPC Cilostazol Approved T88975 DRUGINFO D0E0SW Enoximone Approved T88975 DRUGINFO D0L0ZF VESNARINONE Approved T88975 DRUGINFO D08HKT BEMORADAN Phase 2 T88975 DRUGINFO D0BK6B CI-930 Discontinued in Phase 2 T88975 DRUGINFO D0Y6HV EMD-53998 Discontinued in Phase 1 T88975 DRUGINFO D08NXX BMY-20844 Terminated T88975 DRUGINFO D09UMA IMAZODAN Terminated T88975 DRUGINFO D01OFY LAS-31180 Terminated T88975 DRUGINFO D07LCE 1,3,9,9a-Tetrahydro-imidazo[4,5-b]quinolin-2-one Investigative T88975 DRUGINFO D0N6MR 1,3-Dihydro-imidazo[4,5-b]quinolin-2-one Investigative T88975 DRUGINFO D0T3UP 1,3-Dihydro-naphtho[2,3-d]imidazol-2-one Investigative T88975 DRUGINFO D0TE6A 1,5-Dihydro-imidazo[2,1-b]quinazolin-2-one Investigative T88975 DRUGINFO D0W3RR 2-Morpholin-4-yl-8-phenylethynyl-chromen-4-one Investigative T88975 DRUGINFO D04BXL 2-morpholino-7-(2-phenylethynyl)-4H-chromen-4-one Investigative T88975 DRUGINFO D0MJ1L 2-morpholino-7-phenyl-4H-chromen-4-one Investigative T88975 DRUGINFO D0J7NR 5-Methyl-1,3-dihydro-imidazo[4,5-b]quinolin-2-one Investigative T88975 DRUGINFO D0TZ8C 6-(2-Imidazol-1-yl-vinyl)-1H-quinolin-2-one Investigative T88975 DRUGINFO D04KDB 6-Imidazol-1-yl-3,4-dihydro-1H-quinolin-2-one Investigative T88975 DRUGINFO D09CPC 6-Pyridin-3-yl-3,4-dihydro-1H-quinolin-2-one Investigative T88975 DRUGINFO D0NI4Z 7-Chloro-1,3-dihydro-imidazo[4,5-b]quinolin-2-one Investigative T88975 DRUGINFO D0DX3V 7-Ethoxy-1,3-dihydro-imidazo[4,5-b]quinolin-2-one Investigative T88975 DRUGINFO D09GTN 7-Fluoro-1,3-dihydro-imidazo[4,5-b]quinolin-2-one Investigative T88975 DRUGINFO D0E3ID 7-Iodo-1,5-dihydro-imidazo[2,1-b]quinazolin-2-one Investigative T88975 DRUGINFO D05HFD 7-Methyl-1,3-dihydro-imidazo[4,5-b]quinolin-2-one Investigative T88975 DRUGINFO D08XKO 8-Chloro-1,3-dihydro-imidazo[4,5-b]quinolin-2-one Investigative T88975 DRUGINFO D03GAQ 8-Methyl-1,3-dihydro-imidazo[4,5-b]quinolin-2-one Investigative T88975 DRUGINFO D08WIJ 8-methyl-2-morpholino-7-phenoxy-4H-chromen-4-one Investigative T88975 DRUGINFO D07BFF 8-methyl-2-morpholino-7-phenyl-4H-chromen-4-one Investigative T88975 DRUGINFO D06XVV BENZOYLENUREA Investigative T88975 DRUGINFO D0R6MT isobutylmethylxanthine Investigative T88975 DRUGINFO D06GUJ KURAIDIN Investigative T88975 DRUGINFO D0W4ZU KURARINOL Investigative T88975 DRUGINFO D00QCL SOPHOFLAVESCENOL Investigative T88975 DRUGINFO D00YPO TETRAHYDROBENXIMIDAZOLE Investigative T88975 KEGGPATH hsa00230:Purine metabolism T88975 KEGGPATH hsa04022:cGMP-PKG signaling pathway T88975 KEGGPATH hsa04024:cAMP signaling pathway T88975 KEGGPATH hsa05032:Morphine addiction T88975 WIKIPATH WP2004:miR-targeted genes in lymphocytes - TarBase T88975 WIKIPATH WP2005:miR-targeted genes in muscle cell - TarBase T88975 REACPATH R-HSA-418457:cGMP effects T88975 REACPATH R-HSA-418555:G alpha (s) signalling events T14558 TARGETID T14558 T14558 FORMERID TTDS00130 T14558 UNIPROID TRYB1_HUMAN T14558 TARGNAME Tryptase alpha/beta-1 (Tryptase) T14558 GENENAME TPSAB1 T14558 TARGTYPE Successful target T14558 SYNONYMS Tryptase-1; Tryptase alpha-1; Tryptase I; TPSB1; TPS2; TPS1 T14558 FUNCTION May play a role in innate immunity. Isoform 2 cleaves large substrates, such as fibronectin, more efficiently than isoform 1, but seems less efficient toward small substrates. Tryptase is the major neutral protease present in mast cells and is secreted upon the coupled activation-degranulation response of this cell type. T14558 PDBSTRUC 5WI6; 5F03; 4MQA; 4MPX; 4MPW T14558 BIOCLASS Peptidase T14558 ECNUMBER EC 3.4.21.59 T14558 SEQUENCE MLNLLLLALPVLASRAYAAPAPGQALQRVGIVGGQEAPRSKWPWQVSLRVHGPYWMHFCGGSLIHPQWVLTAAHCVGPDVKDLAALRVQLREQHLYYQDQLLPVSRIIVHPQFYTAQIGADIALLELEEPVNVSSHVHTVTLPPASETFPPGMPCWVTGWGDVDNDERLPPPFPLKQVKVPIMENHICDAKYHLGAYTGDDVRIVRDDMLCAGNTRRDSCQGDSGGPLVCKVNGTWLQAGVVSWGEGCAQPNRPGIYTRVTYYLDWIHHYVPKKP T14558 DRUGINFO D0O5WD Lactoferrin Approved T14558 DRUGINFO D05EAM Pentamidine Approved T14558 DRUGINFO D08RMH APC-2059 Discontinued in Phase 2 T14558 DRUGINFO D0N9WB APC-366 Discontinued in Phase 2 T14558 DRUGINFO D02INZ BABIM Terminated T14558 DRUGINFO D0L7ZX BAY-17-1998 Terminated T14558 DRUGINFO D0W7DD BAY-44-3428 Terminated T14558 DRUGINFO D07IZR AMG-126737 Investigative T14558 DRUGINFO D09YQM BMS-262084 Investigative T14558 DRUGINFO D0Y5IQ Grassystatin a Investigative T14558 DRUGINFO D0NZ3Q Lactoferrin Investigative T14558 DRUGINFO D0Q4PB MOL 6131 Investigative T14558 REACPATH R-HSA-1592389:Activation of Matrix Metalloproteinases T51076 TARGETID T51076 T51076 FORMERID TTDI01807 T51076 UNIPROID NTRK3_HUMAN T51076 TARGNAME NT-3 growth factor receptor (TrkC) T51076 GENENAME NTRK3 T51076 TARGTYPE Successful target T51076 SYNONYMS TrkC tyrosine kinase; Trk-C; TRKC; Neurotrophic tyrosine kinase receptor type 3; NT3 growth factor receptor; GP145TrkC; GP145-TrkC T51076 FUNCTION Upon binding of its ligand NTF3/neurotrophin-3, NTRK3 autophosphorylates and activates different signaling pathways, including the phosphatidylinositol 3-kinase/AKT and the MAPK pathways, that control cell survival and differentiation. Receptor tyrosine kinase involved in nervous system and probably heart development. T51076 PDBSTRUC 4YMJ; 3V5Q; 1WWC T51076 BIOCLASS Kinase T51076 ECNUMBER EC 2.7.10.1 T51076 SEQUENCE MDVSLCPAKCSFWRIFLLGSVWLDYVGSVLACPANCVCSKTEINCRRPDDGNLFPLLEGQDSGNSNGNASINITDISRNITSIHIENWRSLHTLNAVDMELYTGLQKLTIKNSGLRSIQPRAFAKNPHLRYINLSSNRLTTLSWQLFQTLSLRELQLEQNFFNCSCDIRWMQLWQEQGEAKLNSQNLYCINADGSQLPLFRMNISQCDLPEISVSHVNLTVREGDNAVITCNGSGSPLPDVDWIVTGLQSINTHQTNLNWTNVHAINLTLVNVTSEDNGFTLTCIAENVVGMSNASVALTVYYPPRVVSLEEPELRLEHCIEFVVRGNPPPTLHWLHNGQPLRESKIIHVEYYQEGEISEGCLLFNKPTHYNNGNYTLIAKNPLGTANQTINGHFLKEPFPESTDNFILFDEVSPTPPITVTHKPEEDTFGVSIAVGLAAFACVLLVVLFVMINKYGRRSKFGMKGPVAVISGEEDSASPLHHINHGITTPSSLDAGPDTVVIGMTRIPVIENPQYFRQGHNCHKPDTYVQHIKRRDIVLKRELGEGAFGKVFLAECYNLSPTKDKMLVAVKALKDPTLAARKDFQREAELLTNLQHEHIVKFYGVCGDGDPLIMVFEYMKHGDLNKFLRAHGPDAMILVDGQPRQAKGELGLSQMLHIASQIASGMVYLASQHFVHRDLATRNCLVGANLLVKIGDFGMSRDVYSTDYYRLFNPSGNDFCIWCEVGGHTMLPIRWMPPESIMYRKFTTESDVWSFGVILWEIFTYGKQPWFQLSNTEVIECITQGRVLERPRVCPKEVYDVMLGCWQREPQQRLNIKEIYKILHALGKATPIYLDILG T51076 DRUGINFO D0O0LS Entrectinib Approved T51076 DRUGINFO D07TOK Larotrectinib Approved T51076 DRUGINFO D00DRL MK-2461 Phase 1/2 T51076 DRUGINFO D0FA6S Altiratinib Phase 1 T51076 DRUGINFO D0AU4G 3-amino-5-benzyl-substituted indazole derivative 1 Patented T51076 DRUGINFO D0Y1NH Azaindazole amide derivative 1 Patented T51076 DRUGINFO D0NS6S Cyclopenta[d]pyrimidine derivative 1 Patented T51076 DRUGINFO D07RLB PMID28270010-Compound-Figure24-b Patented T51076 DRUGINFO D0J9ZG PMID28270010-Compound-Figure5-1 Patented T51076 DRUGINFO D0T2OX PMID28270010-Compound-Figure5-2 Patented T51076 DRUGINFO D0V5AG PMID28270010-Compound-Figure5-3 Patented T51076 DRUGINFO D0M8VS PMID28270021-Compound-WO2015042088Example4 Patented T51076 DRUGINFO D00MGO PMID28270021-Compound-WO2016054807Example1 Patented T51076 DRUGINFO D0AG2A Pyrrolo[2,3-d]pyrimidine derivative 4 Patented T51076 DRUGINFO D0KX1E CEP-2563 Discontinued in Phase 1 T51076 DRUGINFO D0MH1X AZD1332 Investigative T51076 DRUGINFO D02RWC GNF-5837 Investigative T51076 DRUGINFO D0Y4BL JNJ-28312141 Investigative T51076 DRUGINFO D02NNT PMID21493067C1d Investigative T51076 DRUGINFO D0E7VO PMID24900538C2c Investigative T51076 WIKIPATH WP1873:NGF signalling via TRKA from the plasma membrane T51076 WIKIPATH WP2377:Integrated Pancreatic Cancer Pathway T51076 WIKIPATH WP2380:BDNF signaling pathway T51076 WIKIPATH WP382:MAPK Signaling Pathway T51076 REACPATH R-HSA-170984:ARMS-mediated activation T51076 REACPATH R-HSA-187024:NGF-independant TRKA activation T51076 REACPATH R-HSA-198203:PI3K/AKT activation T80896 TARGETID T80896 T80896 FORMERID TTDS00250 T80896 UNIPROID ESR2_HUMAN T80896 TARGNAME Estrogen receptor beta (ESR2) T80896 GENENAME ESR2 T80896 TARGTYPE Successful target T80896 SYNONYMS Oestrogen receptor beta; Nuclear receptor subfamily 3 group A member 2; NR3A2; Erbeta; ESTRB; ER-beta; Beta-1 T80896 FUNCTION Binds estrogens with an affinity similar to that of ESR1, and activates expression of reporter genes containing estrogen response elements (ERE) in an estrogen-dependent manner. Isoform beta-cx lacks ligand binding ability and has no or only very low ere binding activity resulting in the loss of ligand-dependent transactivation ability. DNA-binding by ESR1 and ESR2 is rapidly lost at 37 degrees Celsius in the absence of ligand while in the presence of 17 beta-estradiol and 4-hydroxy-tamoxifen loss in DNA-binding at elevated temperature is more gradual. Nuclear hormone receptor. T80896 PDBSTRUC 5TOA; 4ZI1; 4J26; 4J24; 3OMQ T80896 BIOCLASS Nuclear hormone receptor T80896 SEQUENCE MDIKNSPSSLNSPSSYNCSQSILPLEHGSIYIPSSYVDSHHEYPAMTFYSPAVMNYSIPSNVTNLEGGPGRQTTSPNVLWPTPGHLSPLVVHRQLSHLYAEPQKSPWCEARSLEHTLPVNRETLKRKVSGNRCASPVTGPGSKRDAHFCAVCSDYASGYHYGVWSCEGCKAFFKRSIQGHNDYICPATNQCTIDKNRRKSCQACRLRKCYEVGMVKCGSRRERCGYRLVRRQRSADEQLHCAGKAKRSGGHAPRVRELLLDALSPEQLVLTLLEAEPPHVLISRPSAPFTEASMMMSLTKLADKELVHMISWAKKIPGFVELSLFDQVRLLESCWMEVLMMGLMWRSIDHPGKLIFAPDLVLDRDEGKCVEGILEIFDMLLATTSRFRELKLQHKEYLCVKAMILLNSSMYPLVTATQDADSSRKLAHLLNAVTDALVWVIAKSGISSQQQSMRLANLLMLLSHVRHASNKGMEHLLNMKCKNVVPVYDLLLEMLNAHVLRGCKSSITGSECSPAEDSKSKEGSQNPQSQ T80896 DRUGINFO D06LOQ ARZOXIFENE Approved T80896 DRUGINFO D0T0LU Conjugated Estrogens Approved T80896 DRUGINFO D0M8PD Estrogen Approved T80896 DRUGINFO D03XOC Trilostane Approved T80896 DRUGINFO D02GLD MF-101 Phase 3 T80896 DRUGINFO D0G7IV Premarin/Pravachol Phase 3 T80896 DRUGINFO D0L4FS Genistein Phase 2/3 T80896 DRUGINFO D01HXA AUS-131 Phase 2 T80896 DRUGINFO D07LZH ERB-041 Phase 2 T80896 DRUGINFO D0R2SK Erteberel Phase 2 T80896 DRUGINFO D01PTS VG-101 Phase 1/2 T80896 DRUGINFO D05KUP ERB-257 Phase 1 T80896 DRUGINFO D02ABO NARINGENIN Phase 1 T80896 DRUGINFO D0QQ1J BITHIONOL Withdrawn from market T80896 DRUGINFO D0C4FT HEXESTROL Withdrawn from market T80896 DRUGINFO D0MU0S EM-800 Discontinued in Phase 3 T80896 DRUGINFO D0R8TB ERA-923 Discontinued in Phase 2 T80896 DRUGINFO D08HIH ERB-196 Discontinued in Phase 1 T80896 DRUGINFO D08DZZ HE2100 Discontinued in Phase 1 T80896 DRUGINFO D09AAM ICI-164384 Terminated T80896 DRUGINFO D0SM0J LY-117018 Terminated T80896 DRUGINFO D0H5CV ZK-119010 Terminated T80896 DRUGINFO D00HUB [1,1':2',1'']Terphenyl-4'-carbaldehyde oxime Investigative T80896 DRUGINFO D0Z0UC 1,2-Bis-(4-hydroxy-phenyl)-3H-inden-5-ol Investigative T80896 DRUGINFO D05FUY 1,8-Dichloro-6-(4-hydroxy-phenyl)-naphthalen-2-ol Investigative T80896 DRUGINFO D0S6NV 1-Bromo-6-(4-hydroxy-phenyl)-naphthalen-2-ol Investigative T80896 DRUGINFO D01KJU 1-CHLORO-6-(4-HYDROXYPHENYL)-2-NAPHTHOL Investigative T80896 DRUGINFO D0ZT4U 1-Fluoro-6-(4-hydroxy-phenyl)-naphthalen-2-ol Investigative T80896 DRUGINFO D0V7QZ 2-(2-Chloro-4-hydroxy-phenyl)-benzooxazol-5-ol Investigative T80896 DRUGINFO D0DK9S 2-(3-Butoxy-4-hydroxy-phenyl)-benzooxazol-6-ol Investigative T80896 DRUGINFO D0K1TW 2-(3-Chloro-4-hydroxy-phenyl)-benzooxazol-5-ol Investigative T80896 DRUGINFO D08HCF 2-(3-Chloro-4-hydroxy-phenyl)-benzooxazol-6-ol Investigative T80896 DRUGINFO D09TQE 2-(3-Fluoro-4-hydroxy-phenyl)-benzooxazol-5-ol Investigative T80896 DRUGINFO D0AD3U 2-(3-Fluoro-4-hydroxy-phenyl)-benzooxazol-6-ol Investigative T80896 DRUGINFO D01SWO 2-(3-hydroxyphenyl)-1,2'-spirobi[1H-indene]-5-ol Investigative T80896 DRUGINFO D03DVM 2-(3-hydroxyphenyl)-1,2'-spirobi[1H-indene]-6-ol Investigative T80896 DRUGINFO D0W3FF 2-(4-Hydroxy-naphthalen-1-yl)-benzooxazol-6-ol Investigative T80896 DRUGINFO D0X2VK 2-(4-hydroxyphenyl)-1,2'-spirobi[1H-indene]-5-ol Investigative T80896 DRUGINFO D0P4SR 2-(4-Hydroxy-phenyl)-1-p-tolyl-3H-inden-5-ol Investigative T80896 DRUGINFO D0L6IQ 2-(4-Hydroxy-phenyl)-4-methoxy-quinolin-6-ol Investigative T80896 DRUGINFO D0K7HR 2-(4-Hydroxy-phenyl)-4-vinyl-quinolin-6-ol Investigative T80896 DRUGINFO D02LCC 2-(4-Hydroxy-phenyl)-7-isopropyl-benzooxazol-5-ol Investigative T80896 DRUGINFO D03XEU 2-(4-Hydroxy-phenyl)-7-methoxy-benzofuran-5-ol Investigative T80896 DRUGINFO D05JPW 2-(4-Hydroxy-phenyl)-7-methoxy-benzooxazol-5-ol Investigative T80896 DRUGINFO D0C6AP 2-(4-Hydroxy-phenyl)-7-methyl-benzofuran-5-ol Investigative T80896 DRUGINFO D07VPM 2-(4-Hydroxy-phenyl)-7-phenyl-benzooxazol-5-ol Investigative T80896 DRUGINFO D02EJM 2-(4-Hydroxy-phenyl)-7-propenyl-benzooxazol-5-ol Investigative T80896 DRUGINFO D04WHH 2-(4-Hydroxy-phenyl)-7-propyl-benzooxazol-5-ol Investigative T80896 DRUGINFO D0YW4C 2-(4-Hydroxy-phenyl)-7-vinyl-benzooxazol-5-ol Investigative T80896 DRUGINFO D01WCA 2-(4-HYDROXY-PHENYL)BENZOFURAN-5-OL Investigative T80896 DRUGINFO D0N0OY 2-(4-Hydroxy-phenyl)-benzooxazol-5-ol Investigative T80896 DRUGINFO D09CQC 2-(4-Hydroxy-phenyl)-benzooxazol-6-ol Investigative T80896 DRUGINFO D00CWN 2-(4-Hydroxy-phenyl)-quinolin-6-ol Investigative T80896 DRUGINFO D0U2VA 2-(5-Hydroxy-naphthalen-1-yl)-benzooxazol-6-ol Investigative T80896 DRUGINFO D01QXL 2-(6-Hydroxy-naphthalen-1-yl)-benzooxazol-5-ol Investigative T80896 DRUGINFO D0YH4T 2-(6-Hydroxy-naphthalen-1-yl)-benzooxazol-6-ol Investigative T80896 DRUGINFO D02JJU 2-(6-Hydroxy-naphthalen-2-yl)-benzooxazol-5-ol Investigative T80896 DRUGINFO D00HZT 2-(6-Hydroxy-naphthalen-2-yl)-benzooxazol-6-ol Investigative T80896 DRUGINFO D0P7PK 2,3-diphenyl-1H-indole Investigative T80896 DRUGINFO D0H1CO 2-Naphthalen-1-yl-benzooxazol-6-ol Investigative T80896 DRUGINFO D0O2KP 2-phenyl-1,2'-spirobi[1H-indene]-5'-ol Investigative T80896 DRUGINFO D04EAY 3-(2-Hydroxy-phenyl)-benzo[d]isoxazol-6-ol Investigative T80896 DRUGINFO D0K0TR 3-(4-Hydroxy-phenyl)-4H-chromen-7-ol Investigative T80896 DRUGINFO D08FLV 3-(4-Hydroxy-phenyl)-benzo[d]isoxazol-5-ol Investigative T80896 DRUGINFO D0B1HP 3-(4-Hydroxy-phenyl)-benzo[d]isoxazol-6-ol Investigative T80896 DRUGINFO D0W2YR 3-(5-Hydroxy-benzooxazol-2-yl)-benzene-1,2-diol Investigative T80896 DRUGINFO D0S2ZJ 3-(6-Hydroxy-benzooxazol-2-yl)-benzene-1,2-diol Investigative T80896 DRUGINFO D00FPJ 3,4,6-Trihydroxy-2-(4-hydroxy-phenyl)-inden-1-one Investigative T80896 DRUGINFO D0V3OR 3,6-Dihydroxy-2-(4-hydroxy-phenyl)-inden-1-one Investigative T80896 DRUGINFO D0C5FY 3,8-dihydroxy-4-methyl-6H-benzo[c]chromen-6-one Investigative T80896 DRUGINFO D0HM8Y 3,8-dihydroxy-7-methyl-6H-benzo[c]chromen-6-one Investigative T80896 DRUGINFO D00AAU 3-[1-ethyl-2-(3-hydroxyphenyl)butyl]phenol Investigative T80896 DRUGINFO D01UAO 3-chloro-4-(4-hydroxyphenyl)salicylaldoxime Investigative T80896 DRUGINFO D05LQD 3-hydroxy-4,10-dimethyl-6H-benzo[c]chromen-6-one Investigative T80896 DRUGINFO D02XVV 3-hydroxy-4,7-dimethyl-6H-benzo[c]chromen-6-one Investigative T80896 DRUGINFO D0WP6A 3-hydroxy-4-methyl-6H-benzo[c]chromen-6-one Investigative T80896 DRUGINFO D0U0ZE 3-hydroxy-8,10-dimethyl-6H-benzo[c]chromen-6-one Investigative T80896 DRUGINFO D0A1JP 3'-Methoxy-4'Hydroxyclomiphene Investigative T80896 DRUGINFO D0I5HZ 4-(2-phenyl-1H-benzo[d]imidazol-1-yl)phenol Investigative T80896 DRUGINFO D0K0IC 4-(2-phenyl-1H-indol-3-yl)phenol Investigative T80896 DRUGINFO D0U7KV 4-(3-(4-hydroxyphenyl)-1H-indol-2-yl)phenol Investigative T80896 DRUGINFO D00NEK 4-(3-phenyl-1H-indol-2-yl)phenol Investigative T80896 DRUGINFO D01IRO 4-(4-HYDROXYPHENYL)-1-NAPHTHALDEHYDE OXIME Investigative T80896 DRUGINFO D0R7AG 4-(5-Hydroxy-benzooxazol-2-yl)-benzene-1,3-diol Investigative T80896 DRUGINFO D0C9XK 4-(6-Hydroxy-benzooxazol-2-yl)-benzene-1,2-diol Investigative T80896 DRUGINFO D03RYU 4-(6-Hydroxy-benzooxazol-2-yl)-benzene-1,3-diol Investigative T80896 DRUGINFO D00URP 4,10-dimethyl-6H-benzo[c]chromene-3,8-diol Investigative T80896 DRUGINFO D0NN0V 4',5,7-trihydroxy-6,8-dimethylisoflavone Investigative T80896 DRUGINFO D0S8EB 4,6,10-trimethyl-6H-benzo[c]chromene-3,8-diol Investigative T80896 DRUGINFO D0H5HI 4,6,6,7-tetramethyl-6H-benzo[c]chromene-3,8-diol Investigative T80896 DRUGINFO D0O6FX 4,6,7,10-tetramethyl-6H-benzo[c]chromene-3,8-diol Investigative T80896 DRUGINFO D0O5KR 4,6,7-trimethyl-6H-benzo[c]chromene-3,8-diol Investigative T80896 DRUGINFO D09PXU 4,7-dimethyl-6H-benzo[c]chromene-3,8-diol Investigative T80896 DRUGINFO D0I1NX 4-[1,2-bis(4-hydroxyphenyl)but-1-enyl]phenol Investigative T80896 DRUGINFO D06DNN 4-[1,2-bis(4-hydroxyphenyl)hex-1-enyl]phenol Investigative T80896 DRUGINFO D02DVT 4-[1,2-bis(4-hydroxyphenyl)pent-1-enyl]phenol Investigative T80896 DRUGINFO D00OLH 4-[1,2-bis(4-hydroxyphenyl)vinyl]phenol Investigative T80896 DRUGINFO D03EOD 4-[2,2-bis(4-hydroxyphenyl)-1-methylvinyl]phenol Investigative T80896 DRUGINFO D08WDN 4-Benzo[d]isoxazol-3-yl-benzene-1,3-diol Investigative T80896 DRUGINFO D03CBX 4-Bromo-2-(4-hydroxy-phenyl)-quinolin-6-ol Investigative T80896 DRUGINFO D01TUB 4-Chloro-2-(4-hydroxy-phenyl)-quinolin-6-ol Investigative T80896 DRUGINFO D09FWS 4-Ethyl-2-(4-hydroxy-phenyl)-quinolin-6-ol Investigative T80896 DRUGINFO D08SJL 4-Ethynyl-2-(4-hydroxy-phenyl)-quinolin-6-ol Investigative T80896 DRUGINFO D0L3AX 4-Naphthalen-2-yl-phenol Investigative T80896 DRUGINFO D02WSA 5,7-dihydroxy-3-phenyl-3H-quinazolin-4-one Investigative T80896 DRUGINFO D0J0AG 5-Bromo-2-(4-hydroxy-phenyl)-quinolin-6-ol Investigative T80896 DRUGINFO D01KSR 5-Chloro-2-(4-hydroxy-phenyl)-benzooxazol-6-ol Investigative T80896 DRUGINFO D02HGS 5-Chloro-2-(4-hydroxy-phenyl)-quinolin-6-ol Investigative T80896 DRUGINFO D0X7DJ 6-(2,5-Difluoro-4-hydroxy-phenyl)-naphthalen-2-ol Investigative T80896 DRUGINFO D0V6KJ 6-(2,6-Difluoro-4-hydroxy-phenyl)-naphthalen-2-ol Investigative T80896 DRUGINFO D02OKF 6-(2-Chloro-4-hydroxy-phenyl)-naphthalen-2-ol Investigative T80896 DRUGINFO D0CC6R 6-(2-Fluoro-4-hydroxy-phenyl)-naphthalen-2-ol Investigative T80896 DRUGINFO D09FWP 6-(2-Hydroxy-phenyl)-naphthalen-2-ol Investigative T80896 DRUGINFO D0MY8V 6-(3,5-Difluoro-4-hydroxy-phenyl)-naphthalen-2-ol Investigative T80896 DRUGINFO D0K6TE 6-(3-Chloro-4-hydroxy-phenyl)-naphthalen-2-ol Investigative T80896 DRUGINFO D0X4VN 6-(3-Fluoro-4-hydroxy-phenyl)-naphthalen-2-ol Investigative T80896 DRUGINFO D0HR8L 6-(3-Hydroxy-phenyl)-naphthalen-1-ol Investigative T80896 DRUGINFO D0P8PK 6-(3-Hydroxy-phenyl)-naphthalen-2-ol Investigative T80896 DRUGINFO D0P6FN 6-(4-Hydroxy-2-methoxy-phenyl)-naphthalen-2-ol Investigative T80896 DRUGINFO D01GPY 6-(4-Hydroxy-2-methyl-phenyl)-naphthalen-2-ol Investigative T80896 DRUGINFO D0M0XL 6-(4-Hydroxy-phenyl)-1-methoxy-naphthalen-2-ol Investigative T80896 DRUGINFO D07XBD 6-(4-Hydroxy-phenyl)-1-methyl-naphthalen-2-ol Investigative T80896 DRUGINFO D0H2FI 6-(4-Hydroxy-phenyl)-1-nitro-naphthalen-2-ol Investigative T80896 DRUGINFO D0VN2R 6-(4-Hydroxy-phenyl)-1-phenyl-naphthalen-2-ol Investigative T80896 DRUGINFO D0H8PI 6-(4-Hydroxy-phenyl)-naphthalen-1-ol Investigative T80896 DRUGINFO D07LUI 6-(4-Hydroxy-phenyl)-naphthalen-2-ol Investigative T80896 DRUGINFO D05JKC 6-Chloro-2-(4-hydroxy-phenyl)-benzooxazol-5-ol Investigative T80896 DRUGINFO D00IXB 6-ethyl-4,7-dimethyl-6H-benzo[c]chromene-3,8-diol Investigative T80896 DRUGINFO D0UV9G 6-Phenyl-naphthalen-2-ol Investigative T80896 DRUGINFO D01IAT 7-(3-Hydroxy-phenyl)-naphthalen-2-ol Investigative T80896 DRUGINFO D09DEK 7-(4-Hydroxy-phenyl)-naphthalen-2-ol Investigative T80896 DRUGINFO D00ZBL 7-Allyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol Investigative T80896 DRUGINFO D0L2MU 7-Bromo-2-(4-hydroxy-phenyl)-benzofuran-5-ol Investigative T80896 DRUGINFO D03GYS 7-Butyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol Investigative T80896 DRUGINFO D05YIU 7-Chloro-2-(4-hydroxy-phenyl)-benzofuran-5-ol Investigative T80896 DRUGINFO D06OAL 7-Ethyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol Investigative T80896 DRUGINFO D0S0SZ 7-Ethynyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol Investigative T80896 DRUGINFO D01AHL 7-hydroxy-1,2,9,9a-tetrahydrofluoren-3-one Investigative T80896 DRUGINFO D01CYI 7-hydroxy-3-(4-hydroxyphenyl)-3H-quinazolin-4-one Investigative T80896 DRUGINFO D0SR8Q 7-Phenyl-naphthalen-2-ol Investigative T80896 DRUGINFO D03QHG 8-(2,2-dimethylpropyl)naringenin Investigative T80896 DRUGINFO D0Y2LJ 8-(2-methylpropyl)naringenin Investigative T80896 DRUGINFO D09NOH 8-(3-methylbutyl)naringenin Investigative T80896 DRUGINFO D0D1LB 8-benzylnaringenin Investigative T80896 DRUGINFO D08VDX 8-Chloro-6-(4-hydroxy-phenyl)-naphthalen-2-ol Investigative T80896 DRUGINFO D0FD6Z 8-Fluoro-6-(4-hydroxy-phenyl)-naphthalen-2-ol Investigative T80896 DRUGINFO D07XUY 8-methylnaringenin Investigative T80896 DRUGINFO D0J2NG 8-n-heptylnaringenin Investigative T80896 DRUGINFO D0W5HT 8-n-nonylnaringenin Investigative T80896 DRUGINFO D0LI0M 8-n-pentylnaringenin Investigative T80896 DRUGINFO D0W0LG 8-n-propylnaringenin Investigative T80896 DRUGINFO D05KXP 8-n-undecylnaringenin Investigative T80896 DRUGINFO D0F2ME Acetate Ion Investigative T80896 DRUGINFO D02RQP bisphenol A Investigative T80896 DRUGINFO D06DDT BROUSSONIN A Investigative T80896 DRUGINFO D02DML COUMESTROL Investigative T80896 DRUGINFO D0L5IC CP-394531 Investigative T80896 DRUGINFO D0J7XZ CP-409069 Investigative T80896 DRUGINFO D0SY2M daidzein Investigative T80896 DRUGINFO D05EOW diarylpropionitril Investigative T80896 DRUGINFO D02VIW DIHYDRORALOXIFENE Investigative T80896 DRUGINFO D0RI6O Doxorubicin-Formaldehyde Conjugate Investigative T80896 DRUGINFO D0W4WF EFFUSOL Investigative T80896 DRUGINFO D0XD4N ERB-002 Investigative T80896 DRUGINFO D0H6OS Geldanamycin-estradiol hybrid Investigative T80896 DRUGINFO D0P8XE GNF-PF-3037 Investigative T80896 DRUGINFO D05QIZ GTx-822 Investigative T80896 DRUGINFO D01MWF GTx-878 Investigative T80896 DRUGINFO D0Z3NC HPTE Investigative T80896 DRUGINFO D0OX6I KB-9520 Investigative T80896 DRUGINFO D0NJ4H MORIN Investigative T80896 DRUGINFO D00FUO Nafoxidine Investigative T80896 DRUGINFO D0H4RV NDC-1022 Investigative T80896 DRUGINFO D02EIK Para-Mercury-Benzenesulfonic Acid Investigative T80896 DRUGINFO D02WRU PHTPP Investigative T80896 DRUGINFO D04SEX R,R-THC Investigative T80896 DRUGINFO D0S8AV SOPHORAFLAVANONE B Investigative T80896 DRUGINFO D0I5VJ THIOGENISTEIN Investigative T80896 DRUGINFO D0B4VV Trans-hydroxytamoxifen Investigative T80896 DRUGINFO D05PNP TUPICHINOL C Investigative T80896 DRUGINFO D0Y9BO WAY-169916 Investigative T80896 DRUGINFO D06SCS WAY200070 Investigative T80896 DRUGINFO D0P0FN ZK-164015 Investigative T80896 KEGGPATH hsa04915:Estrogen signaling pathway T80896 KEGGPATH hsa04917:Prolactin signaling pathway T80896 WIKIPATH WP170:Nuclear Receptors T80896 WIKIPATH WP2377:Integrated Pancreatic Cancer Pathway T80896 WIKIPATH WP34:Ovarian Infertility Genes T80896 WIKIPATH WP706:SIDS Susceptibility Pathways T80896 REACPATH R-HSA-383280:Nuclear Receptor transcription pathway T80896 INTEPATH er_nongenomic_pathway:Plasma membrane estrogen receptor signaling T80896 INTEPATH era_genomic_pathway:Validated nuclear estrogen receptor alpha network T80896 INTEPATH erb_genomic_pathway:Validated nuclear estrogen receptor beta network T46360 TARGETID T46360 T46360 FORMERID TTDS00129 T46360 UNIPROID SGMR1_HUMAN T46360 TARGNAME Opioid receptor sigma 1 (OPRS1) T46360 GENENAME SIGMAR1 T46360 TARGTYPE Successful target T46360 SYNONYMS hSigmaR1; Sigma1R; Sigma1-receptor; Sigma non-opioid intracellular receptor 1; Sigma 1-type opioid receptor; SRBP; SR31747-binding protein; SR31747 binding protein 1; SR-BP; SIG-1R; Opioid receptor, sigma 1, isoform 1; OPRS1 protein; Aging-associated gene 8 protein; AAG8 T46360 FUNCTION Involved in the regulation of different receptors it plays a role in BDNF signaling and EGF signaling. Also regulates ion channels like the potassium channel and could modulate neurotransmitter release. Plays a role in calcium signaling through modulation together with ANK2 of the ITP3R-dependent calcium efflux at the endoplasmic reticulum. Plays a role in several other cell functions including proliferation, survival and death. Originally identified for its ability to bind various psychoactive drugs it is involved in learning processes, memory and mood alteration. Necessary for proper mitochondrial axonal transport in motor neurons, in particular the retrograde movement of mitochondria. Plays a role in protecting cells against oxidative stress-induced cell death via its interaction with RNF112. Functions in lipid transport from the endoplasmic reticulum and is involved in a wide array of cellular functions probably through regulation of the biogenesis of lipid microdomains at the plasma membrane. T46360 PDBSTRUC 6DK1; 6DK0; 6DJZ; 5HK2; 5HK1 T46360 BIOCLASS GPCR rhodopsin T46360 SEQUENCE MQWAVGRRWAWAALLLAVAAVLTQVVWLWLGTQSFVFQREEIAQLARQYAGLDHELAFSRLIVELRRLHPGHVLPDEELQWVFVNAGGWMGAMCLLHASLSEYVLLFGTALGSRGHSGRYWAEISDTIISGTFHQWREGTTKSEVFYPGETVVHGPGEATAVEWGPNTWMVEYGRGVIPSTLAFALADTVFSTQDFLTLFYTLRSYARGLRLELTTYLFGQDP T46360 DRUGINFO D09OBB Dextromethorphan Approved T46360 DRUGINFO D00KFB Dextromethorphan Polistirex Approved T46360 DRUGINFO D0GW6K ADX N05 Phase 3 T46360 DRUGINFO D0Z6IB AVP-786 Phase 3 T46360 DRUGINFO D0X6XH CM-2395 Phase 3 T46360 DRUGINFO D0N5LJ Igmesine Phase 2 T46360 DRUGINFO D0R8GR OPC-14523 Phase 2 T46360 DRUGINFO D09AOO ANAVEX 2-73 Phase 1 T46360 DRUGINFO D0G9SH SA-5845 Phase 1 T46360 DRUGINFO D0Q7QY SSR-125047 Phase 1 T46360 DRUGINFO D0T6ES SSR-125329A Phase 1 T46360 DRUGINFO D0MD6P 1,2,4-triazole derivative 3 Patented T46360 DRUGINFO D08RUG 1,2,4-triazole derivative 4 Patented T46360 DRUGINFO D0E9CK Aryl alkanolamine derivative 1 Patented T46360 DRUGINFO D07XVQ Aryl alkanolamine derivative 2 Patented T46360 DRUGINFO D05YFF Benzamide derivative 10 Patented T46360 DRUGINFO D0W3TS Benzamide derivative 11 Patented T46360 DRUGINFO D0RS2J Benzamide derivative 7 Patented T46360 DRUGINFO D0H2SE Benzamide derivative 8 Patented T46360 DRUGINFO D03MKY Benzamide derivative 9 Patented T46360 DRUGINFO D0S3ON Isoindoline derivative 1 Patented T46360 DRUGINFO D0F8XU Isoindoline derivative 2 Patented T46360 DRUGINFO D06FNA Isoindoline derivative 3 Patented T46360 DRUGINFO D0EK3Z Isoindoline derivative 4 Patented T46360 DRUGINFO D02NPB Isoindoline derivative 5 Patented T46360 DRUGINFO D0G4GT Phenylpropylamine derivative 1 Patented T46360 DRUGINFO D0L0CD Phenylpropylamine derivative 2 Patented T46360 DRUGINFO D0C1YW Phenylpropylamine derivative 3 Patented T46360 DRUGINFO D0A0DV Phenylpropylamine derivative 4 Patented T46360 DRUGINFO D0G7GN Phenylpropylamine derivative 5 Patented T46360 DRUGINFO D0J9SL Piperazine derivative 7 Patented T46360 DRUGINFO D0X5FS Piperidine derivative 4 Patented T46360 DRUGINFO D0X9RA Piperidine derivative 5 Patented T46360 DRUGINFO D0T5SO Piperidine derivative 6 Patented T46360 DRUGINFO D0EO9Z PMID28051882-Compound-XIV Patented T46360 DRUGINFO D0DW1D PMID30185082-Compound-57 Patented T46360 DRUGINFO D0SG9W PMID30185082-Compound-64 Patented T46360 DRUGINFO D04PCA Pyrazole derivative 86 Patented T46360 DRUGINFO D01YOC BMS-181100 Discontinued in Phase 3 T46360 DRUGINFO D0L4PY KB-5492 Discontinued in Phase 2 T46360 DRUGINFO D02JNX OxycoDex Discontinued in Phase 2 T46360 DRUGINFO D00EZE Panamesine Discontinued in Phase 2 T46360 DRUGINFO D0Z4QV DUP-734 Discontinued in Phase 1 T46360 DRUGINFO D0L7BV Gevotroline Discontinued in Phase 1 T46360 DRUGINFO D0M6OW ANAVEX 1007 Preclinical T46360 DRUGINFO D0T0UC ANAVEX 1-41 Preclinical T46360 DRUGINFO D00KVE Cutamesine Preclinical T46360 DRUGINFO D0T8BP AH-9700 Terminated T46360 DRUGINFO D0U7VO CNS-1307 Terminated T46360 DRUGINFO D00IRU E-5842 Terminated T46360 DRUGINFO D0B7BX E-6276 Terminated T46360 DRUGINFO D0Z5HB FH-510 Terminated T46360 DRUGINFO D0Q7OA HydrocoDex Terminated T46360 DRUGINFO D0T8HU LU-29252 Terminated T46360 DRUGINFO D09OTG MS-377 Terminated T46360 DRUGINFO D0L1YS NE-033 Terminated T46360 DRUGINFO D09DRG NE-100 Terminated T46360 DRUGINFO D0B1PD NPC-16377 Terminated T46360 DRUGINFO D01KIU PRE-084 Terminated T46360 DRUGINFO D0M9GE Rimcazole Terminated T46360 DRUGINFO D0MK2C SR-31742A Terminated T46360 DRUGINFO D0IZ1X (+)-SK&F10047 Investigative T46360 DRUGINFO D07LVT (RS)-PPCC Investigative T46360 DRUGINFO D0G4KB [3H]pentazocine Investigative T46360 DRUGINFO D02WJT 1,3-ditolylguanidine Investigative T46360 DRUGINFO D03DLZ 2-(1H-indol-3-yl)-N,N-dimethylethanamine Investigative T46360 DRUGINFO D09CGH BD-1047 Investigative T46360 DRUGINFO D0F1WD C-10068 Investigative T46360 DRUGINFO D0J9VK CM-156 Investigative T46360 DRUGINFO D0A3XA CNS-1169 Investigative T46360 DRUGINFO D09AUU Dimemorfan Investigative T46360 DRUGINFO D0G5RT MC-113 Investigative T46360 DRUGINFO D05BLG MC-116 Investigative T46360 WIKIPATH WP2004:miR-targeted genes in lymphocytes - TarBase T46360 WIKIPATH WP2006:miR-targeted genes in squamous cell - TarBase T66505 TARGETID T66505 T66505 FORMERID TTDNS00536 T66505 UNIPROID SMO_HUMAN T66505 TARGNAME Smoothened homolog (SMO) T66505 GENENAME SMO T66505 TARGTYPE Successful target T66505 SYNONYMS Smo-D473H; SMOH; Protein Gx T66505 FUNCTION Binding of sonic hedgehog (SHH) to its receptor patched is thought to prevent normal inhibition by patched of smoothened (SMO). Required for the accumulation of KIF7, GLI2 and GLI3 in the cilia. Interacts with DLG5 at the ciliary base to induce the accumulation of KIF7 and GLI2 at the ciliary tip for GLI2 activation. G protein-coupled receptor that probably associates with the patched protein (PTCH) to transduce the hedgehog's proteins signal. T66505 PDBSTRUC 5V57; 5V56; 5L7I; 5L7D; 4QIN T66505 BIOCLASS GPCR frizzled T66505 SEQUENCE MAAARPARGPELPLLGLLLLLLLGDPGRGAASSGNATGPGPRSAGGSARRSAAVTGPPPPLSHCGRAAPCEPLRYNVCLGSVLPYGATSTLLAGDSDSQEEAHGKLVLWSGLRNAPRCWAVIQPLLCAVYMPKCENDRVELPSRTLCQATRGPCAIVERERGWPDFLRCTPDRFPEGCTNEVQNIKFNSSGQCEVPLVRTDNPKSWYEDVEGCGIQCQNPLFTEAEHQDMHSYIAAFGAVTGLCTLFTLATFVADWRNSNRYPAVILFYVNACFFVGSIGWLAQFMDGARREIVCRADGTMRLGEPTSNETLSCVIIFVIVYYALMAGVVWFVVLTYAWHTSFKALGTTYQPLSGKTSYFHLLTWSLPFVLTVAILAVAQVDGDSVSGICFVGYKNYRYRAGFVLAPIGLVLIVGGYFLIRGVMTLFSIKSNHPGLLSEKAASKINETMLRLGIFGFLAFGFVLITFSCHFYDFFNQAEWERSFRDYVLCQANVTIGLPTKQPIPDCEIKNRPSLLVEKINLFAMFGTGIAMSTWVWTKATLLIWRRTWCRLTGQSDDEPKRIKKSKMIAKAFSKRHELLQNPGQELSFSMHTVSHDGPVAGLAFDLNEPSADVSSAWAQHVTKMVARRGAILPQDISVTPVATPVPPEEQANLWLVEAEISPELQKRLGRKKKRRKRKKEVCPLAPPPELHPPAPAPSTIPRLPQLPRQKCLVAAGAWGAGDSCRQGAWTLVSNPFCPEPSPPQDPFLPSAPAPVAWAHGRRQGLGPIHSRTNLMDTELMDADSDF T66505 DRUGINFO D0S5LO PF-04449913 Approved T66505 DRUGINFO D03EDQ Vismodegib Approved T66505 DRUGINFO D09BNZ LDE225 Phase 2 T66505 DRUGINFO D0W0SL LY2940680 Phase 1/2 T66505 DRUGINFO D03DUY BMS-833923 Phase 1b T66505 DRUGINFO D09UMN LEQ-506 Phase 1 T66505 DRUGINFO D0Q4JM TAK-441 Phase 1 T66505 DRUGINFO D0P8IR Bicyclic hexapeptide derivative 1 Patented T66505 DRUGINFO D0I8RK Bicyclic hexapeptide derivative 2 Patented T66505 DRUGINFO D0IW7A Cyclic sulfonamide derivative 1 Patented T66505 DRUGINFO D0B3XW Cyclic sulfonamide derivative 2 Patented T66505 DRUGINFO D0K2FK Cyclic sulfonamide derivative 3 Patented T66505 DRUGINFO D0V9AB Cyclic sulfonamide derivative 4 Patented T66505 DRUGINFO D0VR8N Imidazo bicyclic iminium derivative 3 Patented T66505 DRUGINFO D0FS1J Imidazo bicyclic iminium derivative 4 Patented T66505 DRUGINFO D0AB3D Imidazo bicyclic iminium derivative 5 Patented T66505 DRUGINFO D0LH6R Imidazo bicyclic iminium derivative 6 Patented T66505 DRUGINFO D0XH5O Imidazo bicyclic iminium derivative 7 Patented T66505 DRUGINFO D0KX5G Imidazo bicyclic iminium derivative 8 Patented T66505 DRUGINFO D01AJO Imidazo bicyclic iminium derivative 9 Patented T66505 DRUGINFO D00RRB Isoflavone derivative 1 Patented T66505 DRUGINFO D0WI1G Isoflavone derivative 2 Patented T66505 DRUGINFO D0TP0S Isoflavone derivative 3 Patented T66505 DRUGINFO D0Z6IS Isoflavone derivative 4 Patented T66505 DRUGINFO D01BGG Isoflavone derivative 5 Patented T66505 DRUGINFO D0J1RB Isoflavone derivative 6 Patented T66505 DRUGINFO D04IFL Isoflavone derivative 7 Patented T66505 DRUGINFO D05NRG Isoflavone derivative 8 Patented T66505 DRUGINFO D09VIE Isoflavone derivative 9 Patented T66505 DRUGINFO D0TK2O PMID25726713-Compound-10 Patented T66505 DRUGINFO D0ZF1N PMID25726713-Compound-11 Patented T66505 DRUGINFO D05CWM PMID25726713-Compound-12 Patented T66505 DRUGINFO D0E4TO PMID25726713-Compound-13 Patented T66505 DRUGINFO D0QA9Q PMID25726713-Compound-14 Patented T66505 DRUGINFO D05QYN PMID25726713-Compound-15 Patented T66505 DRUGINFO D0C4VR PMID25726713-Compound-16 Patented T66505 DRUGINFO D07BIQ PMID25726713-Compound-17 Patented T66505 DRUGINFO D0Y6EY PMID25726713-Compound-18 Patented T66505 DRUGINFO D0CD8G PMID25726713-Compound-19 Patented T66505 DRUGINFO D0RV9D PMID25726713-Compound-20 Patented T66505 DRUGINFO D0KC6Y PMID25726713-Compound-21 Patented T66505 DRUGINFO D0QO1Y PMID25726713-Compound-22 Patented T66505 DRUGINFO D06NBL PMID25726713-Compound-23 Patented T66505 DRUGINFO D0B9ML PMID25726713-Compound-24 Patented T66505 DRUGINFO D0J0AT PMID25726713-Compound-25 Patented T66505 DRUGINFO D0R8UO PMID25726713-Compound-26 Patented T66505 DRUGINFO D0RH3O PMID25726713-Compound-27 Patented T66505 DRUGINFO D07ZUO PMID25726713-Compound-28 Patented T66505 DRUGINFO D0K6XL PMID25726713-Compound-29 Patented T66505 DRUGINFO D0DH0O PMID25726713-Compound-30 Patented T66505 DRUGINFO D05MIG PMID25726713-Compound-31 Patented T66505 DRUGINFO D06ELK PMID25726713-Compound-32 Patented T66505 DRUGINFO D0IS8B PMID25726713-Compound-33 Patented T66505 DRUGINFO D0Y8SC PMID25726713-Compound-34 Patented T66505 DRUGINFO D0B3FN PMID25726713-Compound-35 Patented T66505 DRUGINFO D00GMI PMID25726713-Compound-36 Patented T66505 DRUGINFO D0B6GA PMID25726713-Compound-37 Patented T66505 DRUGINFO D0C4PD PMID25726713-Compound-38 Patented T66505 DRUGINFO D0K8HU PMID25726713-Compound-39 Patented T66505 DRUGINFO D03QAU PMID25726713-Compound-42 Patented T66505 DRUGINFO D00ITT PMID25726713-Compound-43 Patented T66505 DRUGINFO D0SO6T PMID25726713-Compound-44 Patented T66505 DRUGINFO D01AWH PMID25726713-Compound-45 Patented T66505 DRUGINFO D0O7BH PMID25726713-Compound-46 Patented T66505 DRUGINFO D0X5VI PMID25726713-Compound-47 Patented T66505 DRUGINFO D0WJ3W PMID25726713-Compound-48 Patented T66505 DRUGINFO D07TVO PMID25726713-Compound-49 Patented T66505 DRUGINFO D0Y8JF PMID25726713-Compound-50 Patented T66505 DRUGINFO D0KH7Q PMID25726713-Compound-51 Patented T66505 DRUGINFO D08LBZ PMID25726713-Compound-56 Patented T66505 DRUGINFO D0PG1G PMID25726713-Compound-57 Patented T66505 DRUGINFO D02JSW PMID25726713-Compound-58 Patented T66505 DRUGINFO D0FT1X PMID25726713-Compound-59 Patented T66505 DRUGINFO D05QCM PMID25726713-Compound-60 Patented T66505 DRUGINFO D0R3UI PMID25726713-Compound-61 Patented T66505 DRUGINFO D03SCM PMID25726713-Compound-62 Patented T66505 DRUGINFO D06MXI PMID25726713-Compound-63 Patented T66505 DRUGINFO D0KS3J PMID25726713-Compound-64 Patented T66505 DRUGINFO D0WB2S Pyrimidine derivative 19 Patented T66505 DRUGINFO D03HMW Pyrimidine derivative 20 Patented T66505 DRUGINFO D0K0IO Pyrimidine derivative 21 Patented T66505 DRUGINFO D0J9JS Pyrimidine derivative 22 Patented T66505 DRUGINFO D0R8DO 1-Benzyl-4-(4-phenylpiperazin-1-yl)phthalazine Investigative T66505 DRUGINFO D0V8GX AZD8542 Investigative T66505 DRUGINFO D05UKJ CYCLOPAMINE Investigative T66505 DRUGINFO D06MUB SMOi2-17 Investigative T66505 KEGGPATH hsa04340:Hedgehog signaling pathway T66505 KEGGPATH hsa05200:Pathways in cancer T66505 KEGGPATH hsa05205:Proteoglycans in cancer T66505 KEGGPATH hsa05217:Basal cell carcinoma T66505 WIKIPATH WP117:GPCRs, Other T66505 WIKIPATH WP1825:GPCR ligand binding T66505 WIKIPATH WP2377:Integrated Pancreatic Cancer Pathway T66505 WIKIPATH WP2804:Hair Follicle Development: Induction (Part 1 of 3) T66505 WIKIPATH WP2839:Hair Follicle Development: Organogenesis (Part 2 of 3) T66505 WIKIPATH WP47:Hedgehog Signaling Pathway T66505 REACPATH R-HSA-373080:Class B/2 (Secretin family receptors) T66505 REACPATH R-HSA-5610787:Hedgehog 'off' state T66505 REACPATH R-HSA-5635838:Activation of SMO T66505 INTEPATH hedgehog_2pathway:Signaling events mediated by the Hedgehog family T66505 INTEPATH hedgehog_glipathway:Hedgehog signaling events mediated by Gli proteins T66505 PANTPATH P00025:Hedgehog signaling pathway T31992 TARGETID T31992 T31992 FORMERID TTDR00213 T31992 UNIPROID CAH14_HUMAN T31992 TARGNAME Carbonic anhydrase XIV (CA-XIV) T31992 GENENAME CA14 T31992 TARGTYPE Successful target T31992 SYNONYMS UNQ690/PRO1335; Carbonic anhydrase 14; Carbonate dehydratase XIV T31992 FUNCTION Reversible hydration of carbon dioxide. T31992 PDBSTRUC 5CJF; 4LU3 T31992 BIOCLASS Alpha-carbonic anhydrase T31992 ECNUMBER EC 4.2.1.1 T31992 SEQUENCE MLFSALLLEVIWILAADGGQHWTYEGPHGQDHWPASYPECGNNAQSPIDIQTDSVTFDPDLPALQPHGYDQPGTEPLDLHNNGHTVQLSLPSTLYLGGLPRKYVAAQLHLHWGQKGSPGGSEHQINSEATFAELHIVHYDSDSYDSLSEAAERPQGLAVLGILIEVGETKNIAYEHILSHLHEVRHKDQKTSVPPFNLRELLPKQLGQYFRYNGSLTTPPCYQSVLWTVFYRRSQISMEQLEKLQGTLFSTEEEPSKLLVQNYRALQPLNQRMVFASFIQAGSSYTTGEMLSLGVGILVGCLCLLLAVYFIARKIRKKRLENRKSVVFTSAQATTEA T31992 DRUGINFO D0K1QD Sulfamylon Approved T31992 DRUGINFO D09VAZ TRIENTINE Approved T31992 DRUGINFO D07SDQ Curcumin Phase 3 T31992 DRUGINFO D0A8JP PARABEN Phase 3 T31992 DRUGINFO D0L6HN PHENOL Phase 2/3 T31992 DRUGINFO D0Y6OA Coumate Phase 2 T31992 DRUGINFO D03SLR FERULIC ACID Patented T31992 DRUGINFO D0LD9S SPERMINE Terminated T31992 DRUGINFO D0LC0F 2,3-dihydro-1H-indene-5-sulfonamide Investigative T31992 DRUGINFO D0M3PO 2,4-Disulfamyltrifluoromethylaniline Investigative T31992 DRUGINFO D09TES 2-acetamido-2,3-dihydro-1H-indene-5-sulfonic acid Investigative T31992 DRUGINFO D07CYN 2-amino-2,3-dihydro-1H-indene-5-sulfonamide Investigative T31992 DRUGINFO D0OI1H 2-Amino-benzenesulfonamide Investigative T31992 DRUGINFO D0C4QB 2-Amino-indan-5-sulfonic acid Investigative T31992 DRUGINFO D0H3NS 2-oxo-2H-chromene-3-carboxylic acid Investigative T31992 DRUGINFO D0D6UR 2-oxo-2H-thiochromene-3-carboxylic acid Investigative T31992 DRUGINFO D0J2AE 3-Amino-benzenesulfonamide Investigative T31992 DRUGINFO D04NSN 4-(2-AMINOETHYL)BENZENESULFONAMIDE Investigative T31992 DRUGINFO D04VLI 4-(2-Hydroxy-ethyl)-benzenesulfonamide Investigative T31992 DRUGINFO D05ETN 4-(2-Methyl-8-quinolinoxy)-3-pyridinesulfonamide Investigative T31992 DRUGINFO D02BMV 4-(2-Propynylthio)pyridine-3-sulfonamide Investigative T31992 DRUGINFO D0R4KQ 4-(5-Methyl-2-pirazolino)-3-pyridinesulfonamide Investigative T31992 DRUGINFO D09TKG 4-(Allylamino)-3-pyridinesulfonamide Investigative T31992 DRUGINFO D0V5OW 4-(Carbamolymethylthio)pyridine-3-sulfonamide Investigative T31992 DRUGINFO D01OTW 4-(Cyanomethylthio)pyridine-3-sulfonamide Investigative T31992 DRUGINFO D05XZM 4-(hydroxymethyl)benzenesulfonamide Investigative T31992 DRUGINFO D0Q5VB 4-(Methylhydrazino)-3-pyridinesulfonamide Investigative T31992 DRUGINFO D05JAJ 4-(Quinolinoxy)-3-pyridinesulfonamide Investigative T31992 DRUGINFO D03KRB 4,4'-thiodipyridine-3-sulfonamide Investigative T31992 DRUGINFO D0P6AM 4-Amino-3-bromo-benzenesulfonamide Investigative T31992 DRUGINFO D0YU8J 4-Amino-3-chloro-benzenesulfonamide Investigative T31992 DRUGINFO D04CVC 4-Amino-3-fluoro-benzenesulfonamide Investigative T31992 DRUGINFO D01STY 4-Amino-3-iodo-benzenesulfonamide Investigative T31992 DRUGINFO D07MTM 4-AMINOPHENOL Investigative T31992 DRUGINFO D06IOI 4-Benzythiopyridine-3-sulfonamide Investigative T31992 DRUGINFO D04VSP 4-Ethoxy-3-pyridinesulfonamide Investigative T31992 DRUGINFO D0UM1I 4-Hydrazino-3-pyridinesulfonamide Investigative T31992 DRUGINFO D0NN3Q 4-Hydrazino-benzenesulfonamide Investigative T31992 DRUGINFO D0J7GU 4-Methylthiopyridine-3-sulfonamide Investigative T31992 DRUGINFO D0N1AW 6-(aminomethyl)-2H-chromen-2-one Investigative T31992 DRUGINFO D0L5TZ 6-(hydroxymethyl)-2H-chromen-2-one Investigative T31992 DRUGINFO D0Q2LL 6-Hydroxy-benzothiazole-2-sulfonic acid amide Investigative T31992 DRUGINFO D00XJA 6-methoxy-2-oxo-2H-chromene-3-carboxylic acid Investigative T31992 DRUGINFO D0G3BI 6-methyl-2-oxo-2H-chromene-3-carboxylic acid Investigative T31992 DRUGINFO D00RNZ 7-(benzyloxy)-2H-chromen-2-one Investigative T31992 DRUGINFO D0LU4S 7-butoxy-2H-chromen-2-one Investigative T31992 DRUGINFO D0RB0D 7-methoxy-2-oxo-2H-chromene-4-carboxylic acid Investigative T31992 DRUGINFO D05QUG 7-phenethoxy-2H-chromen-2-one Investigative T31992 DRUGINFO D0OT5L 7-propoxy-2H-chromen-2-one Investigative T31992 DRUGINFO D06DYP 8-methoxy-2-oxo-2H-chromene-3-carboxylic acid Investigative T31992 DRUGINFO D0E8CC BENZOLAMIDE Investigative T31992 DRUGINFO D0SD9H Beta-D-Mannose Investigative T31992 DRUGINFO D09PWX Carzenide Investigative T31992 DRUGINFO D0V7AA CATECHIN Investigative T31992 DRUGINFO D0VD7H CL-5343 Investigative T31992 DRUGINFO D03ZMQ COUMARIN Investigative T31992 DRUGINFO D00YEF Decane-1,10-diyl disulfamate Investigative T31992 DRUGINFO D09WSJ Decyl sulfamate Investigative T31992 DRUGINFO D0A1CM ELLAGIC ACID Investigative T31992 DRUGINFO D05VSK ETHOXYCOUMARIN Investigative T31992 DRUGINFO D07TAJ Ethyl 7-methoxy-2-oxo-2H-chromene-3-carboxylate Investigative T31992 DRUGINFO D0Y3TZ GALLICACID Investigative T31992 DRUGINFO D0U4BB HERNIARIN Investigative T31992 DRUGINFO D09JPC Hexane-1,6-diamine Investigative T31992 DRUGINFO D09WVV N1-(2-aminoethyl)ethane-1,2-diamine Investigative T31992 DRUGINFO D0X5HL N1-(naphthalen-1-yl)ethane-1,2-diamine Investigative T31992 DRUGINFO D01XFH N-propynyl amidebenzenesulphonide Investigative T31992 DRUGINFO D0D4OV Octane-1,8-diyl disulfamate Investigative T31992 DRUGINFO D05TLB Octyl sulfamate Investigative T31992 DRUGINFO D0AU0M P-Coumaric Acid Investigative T31992 DRUGINFO D02QGI Pentane-1,5-diamine Investigative T31992 DRUGINFO D00IAE Prop-2-ynyl 4-sulfamoylbenzoate Investigative T31992 DRUGINFO D02DBP RESORCINOL Investigative T31992 DRUGINFO D0Q7DJ Syringic Acid Investigative T31992 KEGGPATH hsa00910:Nitrogen metabolism T31992 WIKIPATH WP2770:Reversible Hydration of Carbon Dioxide T31992 REACPATH R-HSA-1475029:Reversible hydration of carbon dioxide T56418 TARGETID T56418 T56418 FORMERID TTDI02271 T56418 UNIPROID ALK_HUMAN T56418 TARGNAME ALK tyrosine kinase receptor (ALK) T56418 GENENAME ALK T56418 TARGTYPE Successful target T56418 SYNONYMS CD246; Anaplastic lymphoma kinase T56418 FUNCTION Transduces signals from ligands at the cell surface, through specific activation of the mitogen-activated protein kinase (MAPK) pathway. Phosphorylates almost exclusively at the first tyrosine of the Y-x-x-x-Y-Y motif. Following activation by ligand, ALK induces tyrosine phosphorylation of CBL, FRS2, IRS1 and SHC1, as well as of the MAP kinases MAPK1/ERK2 and MAPK3/ERK1. Acts as a receptor for ligands pleiotrophin (PTN), a secreted growth factor, and midkine (MDK), a PTN-related factor, thus participating in PTN and MDK signal transduction. PTN-binding induces MAPK pathway activation, which is important for the anti-apoptotic signaling of PTN and regulation of cell proliferation. MDK-binding induces phosphorylation of the ALK target insulin receptor substrate (IRS1), activates mitogen-activated protein kinases (MAPKs) and PI3-kinase, resulting also in cell proliferation induction. Drives NF-kappa-B activation, probably through IRS1 and the activation of the AKT serine/threonine kinase. Recruitment of IRS1 to activated ALK and the activation of NF-kappa-B are essential for the autocrine growth and survival signaling of MDK. Neuronal receptor tyrosine kinase that is essentially and transiently expressed in specific regions of the central and peripheral nervous systems and plays an important role in the genesis and differentiation of the nervous system. T56418 PDBSTRUC 6MX8; 6EDL; 6EBW; 6E0R; 6CDT T56418 BIOCLASS Kinase T56418 ECNUMBER EC 2.7.10.1 T56418 SEQUENCE MGAIGLLWLLPLLLSTAAVGSGMGTGQRAGSPAAGPPLQPREPLSYSRLQRKSLAVDFVVPSLFRVYARDLLLPPSSSELKAGRPEARGSLALDCAPLLRLLGPAPGVSWTAGSPAPAEARTLSRVLKGGSVRKLRRAKQLVLELGEEAILEGCVGPPGEAAVGLLQFNLSELFSWWIRQGEGRLRIRLMPEKKASEVGREGRLSAAIRASQPRLLFQIFGTGHSSLESPTNMPSPSPDYFTWNLTWIMKDSFPFLSHRSRYGLECSFDFPCELEYSPPLHDLRNQSWSWRRIPSEEASQMDLLDGPGAERSKEMPRGSFLLLNTSADSKHTILSPWMRSSSEHCTLAVSVHRHLQPSGRYIAQLLPHNEAAREILLMPTPGKHGWTVLQGRIGRPDNPFRVALEYISSGNRSLSAVDFFALKNCSEGTSPGSKMALQSSFTCWNGTVLQLGQACDFHQDCAQGEDESQMCRKLPVGFYCNFEDGFCGWTQGTLSPHTPQWQVRTLKDARFQDHQDHALLLSTTDVPASESATVTSATFPAPIKSSPCELRMSWLIRGVLRGNVSLVLVENKTGKEQGRMVWHVAAYEGLSLWQWMVLPLLDVSDRFWLQMVAWWGQGSRAIVAFDNISISLDCYLTISGEDKILQNTAPKSRNLFERNPNKELKPGENSPRQTPIFDPTVHWLFTTCGASGPHGPTQAQCNNAYQNSNLSVEVGSEGPLKGIQIWKVPATDTYSISGYGAAGGKGGKNTMMRSHGVSVLGIFNLEKDDMLYILVGQQGEDACPSTNQLIQKVCIGENNVIEEEIRVNRSVHEWAGGGGGGGGATYVFKMKDGVPVPLIIAAGGGGRAYGAKTDTFHPERLENNSSVLGLNGNSGAAGGGGGWNDNTSLLWAGKSLQEGATGGHSCPQAMKKWGWETRGGFGGGGGGCSSGGGGGGYIGGNAASNNDPEMDGEDGVSFISPLGILYTPALKVMEGHGEVNIKHYLNCSHCEVDECHMDPESHKVICFCDHGTVLAEDGVSCIVSPTPEPHLPLSLILSVVTSALVAALVLAFSGIMIVYRRKHQELQAMQMELQSPEYKLSKLRTSTIMTDYNPNYCFAGKTSSISDLKEVPRKNITLIRGLGHGAFGEVYEGQVSGMPNDPSPLQVAVKTLPEVCSEQDELDFLMEALIISKFNHQNIVRCIGVSLQSLPRFILLELMAGGDLKSFLRETRPRPSQPSSLAMLDLLHVARDIACGCQYLEENHFIHRDIAARNCLLTCPGPGRVAKIGDFGMARDIYRASYYRKGGCAMLPVKWMPPEAFMEGIFTSKTDTWSFGVLLWEIFSLGYMPYPSKSNQEVLEFVTSGGRMDPPKNCPGPVYRIMTQCWQHQPEDRPNFAIILERIEYCTQDPDVINTALPIEYGPLVEEEEKVPVRPKDPEGVPPLLVSQQAKREEERSPAAPPPLPTTSSGKAAKKPTAAEISVRVPRGPAVEGGHVNMAFSQSNPPSELHKVHGSRNKPTSLWNPTYGSWFTEKPTKKNNPIAKKEPHDRGNLGLEGSCTVPPNVATGRLPGASLLLEPSSLTANMKEVPLFRLRHFPCGNVNYGYQQQGLPLEAATAPGAGHYEDTILKSKNSMNQPGP T56418 DRUGINFO D0U3SY Alectinib Approved T56418 DRUGINFO D08PIE Brigatinib Approved T56418 DRUGINFO D04LVK Ceritinib Approved T56418 DRUGINFO D03ZBT Crizotinib Approved T56418 DRUGINFO D0O0LS Entrectinib Approved T56418 DRUGINFO D0AF6O Lorlatinib Approved T56418 DRUGINFO D0KX7I Ensartinib Phase 3 T56418 DRUGINFO D0O9PQ AP26113 Phase 2 T56418 DRUGINFO D04DYC PF-06463922 Phase 2 T56418 DRUGINFO D05NFR TPX-0005 Phase 1/2 T56418 DRUGINFO D01HKZ TSR-011 Phase 1/2 T56418 DRUGINFO D0L9PA X-396 Phase 1/2 T56418 DRUGINFO D09GEK ASP3026 Phase 1 T56418 DRUGINFO D0NP2W 1,2,4-triazolo[1,5a]pyridine derivative 2 Patented T56418 DRUGINFO D0T3TZ Benzimidazole derivative 6 Patented T56418 DRUGINFO D0MX7B Carboxamide derivative 4 Patented T56418 DRUGINFO D0N8YJ PMID28270010-Compound-Figure21-b Patented T56418 DRUGINFO D0O7LU AZD3463 Investigative T56418 DRUGINFO D03IDK CEP-18050 Investigative T56418 DRUGINFO D09PTP CEP-28122 Investigative T56418 DRUGINFO D0I3TD CRL-37212 Investigative T56418 DRUGINFO D0D2SU DLX-521 Investigative T56418 DRUGINFO D06PJW GSK-1838705A Investigative T56418 DRUGINFO D0H0LP PMID20483621C5g Investigative T56418 DRUGINFO D02NZE PMID20483621C5m Investigative T56418 DRUGINFO D08TVU PMID20483621C5n Investigative T56418 DRUGINFO D09AID PMID22564207C25b Investigative T56418 DRUGINFO D0K5UF PMID24432909C8e Investigative T56418 DRUGINFO D0G4CS PMID24900237C15 Investigative T56418 KEGGPATH hsa05223:Non-small cell lung cancer T56418 WIKIPATH WP2848:Differentiation Pathway T47623 TARGETID T47623 T47623 FORMERID TTDC00060 T47623 UNIPROID HPSE_HUMAN T47623 TARGNAME Heparanase (HPSE) T47623 GENENAME HPSE T47623 TARGTYPE Successful target T47623 SYNONYMS Hpa1; Heparanase-1; Heparanase 8 kDa subunit; Heparanase 50 kDa subunit; HSE1; HPSE1; HPR1; HPA; HEP protein; Endo-glucoronidase T47623 FUNCTION Participates in extracellular matrix (ECM) degradation and remodeling. Selectively cleaves the linkage between a glucuronic acid unit and an N-sulfo glucosamine unit carrying either a 3-O-sulfo or a 6-O-sulfo group. Can also cleave the linkage between a glucuronic acid unit and an N-sulfo glucosamine unit carrying a 2-O-sulfo group, but not linkages between a glucuronic acid unit and a 2-O-sulfated iduronic acid moiety. It is essentially inactive at neutral pH but becomes active under acidic conditions such as during tumor invasion and in inflammatory processes. Facilitates cell migration associated with metastasis, wound healing and inflammation. Enhances shedding of syndecans, and increases endothelial invasion and angiogenesis in myelomas. Acts as procoagulant by increasing the generation of activation factor X in the presence of tissue factor and activation factor VII. Increases cell adhesion to the extracellular matrix (ECM), independent of its enzymatic activity. Induces AKT1/PKB phosphorylation via lipid rafts increasing cell mobility and invasion. Heparin increases this AKT1/PKB activation. Regulates osteogenesis. Enhances angiogenesis through up-regulation of SRC-mediated activation of VEGF. Implicated in hair follicle inner root sheath differentiation and hair homeostasis. Endoglycosidase that cleaves heparan sulfate proteoglycans (HSPGs) into heparan sulfate side chains and core proteoglycans. T47623 PDBSTRUC 5LA7; 5LA4; 5L9Z; 5L9Y; 5E9C T47623 BIOCLASS Glycosylase T47623 ECNUMBER EC 3.2.1.166 T47623 SEQUENCE MLLRSKPALPPPLMLLLLGPLGPLSPGALPRPAQAQDVVDLDFFTQEPLHLVSPSFLSVTIDANLATDPRFLILLGSPKLRTLARGLSPAYLRFGGTKTDFLIFDPKKESTFEERSYWQSQVNQDICKYGSIPPDVEEKLRLEWPYQEQLLLREHYQKKFKNSTYSRSSVDVLYTFANCSGLDLIFGLNALLRTADLQWNSSNAQLLLDYCSSKGYNISWELGNEPNSFLKKADIFINGSQLGEDFIQLHKLLRKSTFKNAKLYGPDVGQPRRKTAKMLKSFLKAGGEVIDSVTWHHYYLNGRTATKEDFLNPDVLDIFISSVQKVFQVVESTRPGKKVWLGETSSAYGGGAPLLSDTFAAGFMWLDKLGLSARMGIEVVMRQVFFGAGNYHLVDENFDPLPDYWLSLLFKKLVGTKVLMASVQGSKRRKLRVYLHCTNTDNPRYKEGDLTLYAINLHNVTKYLRLPYPFSNKQVDKYLLRPLGPHGLLSKSVQLNGLTLKMVDDQTLPPLMEKPLRPGSSLGLPAFSYSFFVIRNAKVAACI T47623 DRUGINFO D04KNL PG-545 Phase 1 T47623 DRUGINFO D0H2UB Suramin Phase 1 T47623 DRUGINFO D0G9LP Neutralase Discontinued in Phase 3 T47623 KEGGPATH hsa00531:Glycosaminoglycan degradation T47623 KEGGPATH hsa01100:Metabolic pathways T47623 KEGGPATH hsa05205:Proteoglycans in cancer T47623 WIKIPATH WP2743:Glycosaminoglycan metabolism T47623 REACPATH R-HSA-2024096:HS-GAG degradation T47623 INTEPATH syndecan_1_pathway:Syndecan-1-mediated signaling events T80782 TARGETID T80782 T80782 FORMERID TTDC00334 T80782 UNIPROID VGFR1_HUMAN T80782 TARGNAME VEGFR1 messenger RNA (VEGFR1 mRNA) T80782 GENENAME FLT1 T80782 TARGTYPE Successful target T80782 SYNONYMS Vascular permeability factor receptor (mRNA); VEGFR1 (mRNA); VEGFR-1 (mRNA); VEGF-1 receptor (mRNA); Tyrosine-protein kinase receptor FLT (mRNA); Tyrosine-protein kinase FRT (mRNA); Fms-like tyrosine kinase 1 (mRNA); FRT (mRNA); FLT (mRNA) T80782 FUNCTION May play an essential role as a negative regulator of embryonic angiogenesis by inhibiting excessive proliferation of endothelial cells. Can promote endothelial cell proliferation, survival and angiogenesis in adulthood. Its function in promoting cell proliferation seems to be cell-type specific. Promotes PGF-mediated proliferation of endothelial cells, proliferation of some types of cancer cells, but does not promote proliferation of normal fibroblasts (in vitro). Has very high affinity for VEGFA and relatively low protein kinase activity; may function as a negative regulator of VEGFA signaling by limiting the amount of free VEGFA and preventing its binding to KDR. Likewise, isoforms lacking a transmembrane domain, such as isoform 2, isoform 3 and isoform 4, may function as decoy receptors for VEGFA. Modulates KDR signaling by forming heterodimers with KDR. Ligand binding leads to the activation of several signaling cascades. Activation of PLCG leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate and the activation of protein kinase C. Mediates phosphorylation of PIK3R1, the regulatory subunit of phosphatidylinositol 3-kinase, leading to activation of phosphatidylinositol kinase and the downstream signaling pathway. Mediates activation of MAPK1/ERK2, MAPK3/ERK1 and the MAP kinase signaling pathway, as well as of the AKT1 signaling pathway. Phosphorylates SRC and YES1, and may also phosphorylate CBL. Isoform 1 phosphorylates PLCG. Promotes phosphorylation of AKT1 at 'Ser-473'. Promotes phosphorylation of PTK2/FAK1. Isoform 7 has a truncated kinase domain; it increases phosphorylation of SRC at 'Tyr-418' by unknown means and promotes tumor cell invasion. Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFA, VEGFB and PGF, and plays an essential role in the development of embryonic vasculature, the regulation of angiogenesis, cell survival, cell migration, macrophage function, chemotaxis, and cancer cell invasion. T80782 PDBSTRUC 5T89; 5EX3; 5ABD; 4CL7; 4CKV T80782 BIOCLASS mRNA target T80782 ECNUMBER EC 2.7.10.1 T80782 SEQUENCE MVSYWDTGVLLCALLSCLLLTGSSSGSKLKDPELSLKGTQHIMQAGQTLHLQCRGEAAHKWSLPEMVSKESERLSITKSACGRNGKQFCSTLTLNTAQANHTGFYSCKYLAVPTSKKKETESAIYIFISDTGRPFVEMYSEIPEIIHMTEGRELVIPCRVTSPNITVTLKKFPLDTLIPDGKRIIWDSRKGFIISNATYKEIGLLTCEATVNGHLYKTNYLTHRQTNTIIDVQISTPRPVKLLRGHTLVLNCTATTPLNTRVQMTWSYPDEKNKRASVRRRIDQSNSHANIFYSVLTIDKMQNKDKGLYTCRVRSGPSFKSVNTSVHIYDKAFITVKHRKQQVLETVAGKRSYRLSMKVKAFPSPEVVWLKDGLPATEKSARYLTRGYSLIIKDVTEEDAGNYTILLSIKQSNVFKNLTATLIVNVKPQIYEKAVSSFPDPALYPLGSRQILTCTAYGIPQPTIKWFWHPCNHNHSEARCDFCSNNEESFILDADSNMGNRIESITQRMAIIEGKNKMASTLVVADSRISGIYICIASNKVGTVGRNISFYITDVPNGFHVNLEKMPTEGEDLKLSCTVNKFLYRDVTWILLRTVNNRTMHYSISKQKMAITKEHSITLNLTIMNVSLQDSGTYACRARNVYTGEEILQKKEITIRDQEAPYLLRNLSDHTVAISSSTTLDCHANGVPEPQITWFKNNHKIQQEPGIILGPGSSTLFIERVTEEDEGVYHCKATNQKGSVESSAYLTVQGTSDKSNLELITLTCTCVAATLFWLLLTLFIRKMKRSSSEIKTDYLSIIMDPDEVPLDEQCERLPYDASKWEFARERLKLGKSLGRGAFGKVVQASAFGIKKSPTCRTVAVKMLKEGATASEYKALMTELKILTHIGHHLNVVNLLGACTKQGGPLMVIVEYCKYGNLSNYLKSKRDLFFLNKDAALHMEPKKEKMEPGLEQGKKPRLDSVTSSESFASSGFQEDKSLSDVEEEEDSDGFYKEPITMEDLISYSFQVARGMEFLSSRKCIHRDLAARNILLSENNVVKICDFGLARDIYKNPDYVRKGDTRLPLKWMAPESIFDKIYSTKSDVWSYGVLLWEIFSLGGSPYPGVQMDEDFCSRLREGMRMRAPEYSTPEIYQIMLDCWHRDPKERPRFAELVEKLGDLLQANVQQDGKDYIPINAILTGNSGFTYSTPAFSEDFFKESISAPKFNSGSSDDVRYVNAFKFMSLERIKTFEELLPNATSMFDDYQGDSSTLLASPMLKRFTWTDSKPKASLKIDLRVTSKSKESGLSDVSRPSFCHSSCGHVSEGKRRFTYDHAELERKIACCSPPPDYNSVVLYSTPPI T80782 DRUGINFO D01PZD Romiplostim Approved T80782 DRUGINFO D0P6DJ VATALANIB Phase 2 T80782 DRUGINFO D00DRL MK-2461 Phase 1/2 T80782 DRUGINFO D04WIE Sirna-027 Phase 1/2 T80782 DRUGINFO D06GJO (2-Methoxy-phenyl)-(5-phenyl-oxazol-2-yl)-amine Investigative T80782 DRUGINFO D0D3YL (5-Phenyl-oxazol-2-yl)-m-tolyl-amine Investigative T80782 DRUGINFO D0V9DQ [3-(5-Phenyl-oxazol-2-ylamino)-phenyl]-methanol Investigative T80782 DRUGINFO D0XC6G 2-(1H-indazol-3-yl)-1H-benzo[d]imidazole Investigative T80782 DRUGINFO D03HQK 2-(5-Phenyl-oxazol-2-ylamino)-benzonitrile Investigative T80782 DRUGINFO D0J2XD 3-(5-Phenyl-oxazol-2-ylamino)-benzonitrile Investigative T80782 DRUGINFO D0YN1E 3,6-Di-pyridin-4-yl-pyrazolo[1,5-a]pyrimidine Investigative T80782 DRUGINFO D09LEK 4-(5-Phenyl-oxazol-2-ylamino)-benzenesulfonamide Investigative T80782 DRUGINFO D0D3QA 4-(isoquinolin-5-yl)-N-m-tolylphthalazin-1-amine Investigative T80782 DRUGINFO D03HTT 4-(isoquinolin-5-yl)-N-o-tolylphthalazin-1-amine Investigative T80782 DRUGINFO D0UZ5W 4-Chloro-N-(2-chloro-benzoyl)-benzenesulfonamide Investigative T80782 DRUGINFO D0V4BR 4-Chloro-N-(2-methyl-benzoyl)-benzenesulfonamide Investigative T80782 DRUGINFO D05THI 4-Chloro-N-(3-chloro-benzoyl)-benzenesulfonamide Investigative T80782 DRUGINFO D09MSA 4-Chloro-N-(4-chloro-benzoyl)-benzenesulfonamide Investigative T80782 DRUGINFO D0C6OD 4-Chloro-N-(4-nitro-benzoyl)-benzenesulfonamide Investigative T80782 DRUGINFO D0EE6A AAL-993 Investigative T80782 DRUGINFO D02MFX C[homoPhe-Hca-Glu-Gly-Leu-Glu-Glu]-NH2 Investigative T80782 DRUGINFO D0K7FA C[YYAEGLEE]-NH2 Investigative T80782 DRUGINFO D0R0XY C[YYDEGLEE]-NH2 Investigative T80782 DRUGINFO D02NZG C[YYDEKLEE]-NH2 Investigative T80782 DRUGINFO D0C6KI CB-676475 Investigative T80782 DRUGINFO D07OCA Cdk1/2 inhibitor III Investigative T80782 DRUGINFO D0Z8TR IM-094261 Investigative T80782 DRUGINFO D0A9ZP IM-094882 Investigative T80782 DRUGINFO D03ZHK LYCOGARUBIN B Investigative T80782 DRUGINFO D07XBW N-(2,4-Dichloro-benzoyl)-benzenesulfonamide Investigative T80782 DRUGINFO D0M2QA N-(3-Bromo-benzoyl)-4-chloro-benzenesulfonamide Investigative T80782 DRUGINFO D04NYQ N3-GHQMFYYPra-NH2 Investigative T80782 DRUGINFO D0BM4F Phenyl-(5-phenyl-oxazol-2-yl)-amine Investigative T80782 DRUGINFO D00ERW PMID17935989C25 Investigative T80782 DRUGINFO D0C2GE PMID22765894C8h Investigative T80782 KEGGPATH hsa04014:Ras signaling pathway T80782 KEGGPATH hsa04015:Rap1 signaling pathway T80782 KEGGPATH hsa04060:Cytokine-cytokine receptor interaction T80782 KEGGPATH hsa04066:HIF-1 signaling pathway T80782 KEGGPATH hsa04144:Endocytosis T80782 KEGGPATH hsa04151:PI3K-Akt signaling pathway T80782 KEGGPATH hsa04510:Focal adhesion T80782 KEGGPATH hsa05202:Transcriptional misregulation in cancer T80782 KEGGPATH hsa05323:Rheumatoid arthritis T80782 WIKIPATH WP1539:Angiogenesis T80782 WIKIPATH WP1919:Signaling by VEGF T80782 WIKIPATH WP306:Focal Adhesion T80782 REACPATH R-HSA-194306:Neurophilin interactions with VEGF and VEGFR T80782 REACPATH R-HSA-195399:VEGF binds to VEGFR leading to receptor dimerization T80782 INTEPATH glypican_1pathway:Glypican 1 network T80782 INTEPATH hif2pathway:HIF-2-alpha transcription factor network T80782 INTEPATH s1p_s1p3_pathway:S1P3 pathway T80782 INTEPATH vegf_vegfr_pathway:VEGF and VEGFR signaling network T80782 INTEPATH vegfr1_2_pathway:Signaling events mediated by VEGFR1 and VEGFR2 T80782 INTEPATH vegfr1_pathway:VEGFR1 specific signals T89529 TARGETID T89529 T89529 FORMERID TTDR01437 T89529 UNIPROID PTN1_HUMAN T89529 TARGNAME PTPN1 messenger RNA (PTPN1 mRNA) T89529 GENENAME PTPN1 T89529 TARGTYPE Successful target T89529 SYNONYMS Tyrosine-protein phosphatase non-receptor type 1 (mRNA); PTP-1B (mRNA) T89529 FUNCTION Mediates dephosphorylation of EIF2AK3/PERK; inactivating the protein kinase activity of EIF2AK3/PERK. May play an important role in CKII- and p60c-src-induced signal transduction cascades. May regulate the EFNA5-EPHA3 signaling pathway which modulates cell reorganization and cell-cell repulsion. May also regulate the hepatocyte growth factor receptor signaling pathway through dephosphorylation of MET. Tyrosine-protein phosphatase which acts as a regulator of endoplasmic reticulum unfolded protein response. T89529 PDBSTRUC 6CWV; 6CWU; 6BAI; 6B95; 6B90 T89529 BIOCLASS mRNA target T89529 ECNUMBER EC 3.1.3.48 T89529 SEQUENCE MEMEKEFEQIDKSGSWAAIYQDIRHEASDFPCRVAKLPKNKNRNRYRDVSPFDHSRIKLHQEDNDYINASLIKMEEAQRSYILTQGPLPNTCGHFWEMVWEQKSRGVVMLNRVMEKGSLKCAQYWPQKEEKEMIFEDTNLKLTLISEDIKSYYTVRQLELENLTTQETREILHFHYTTWPDFGVPESPASFLNFLFKVRESGSLSPEHGPVVVHCSAGIGRSGTFCLADTCLLLMDKRKDPSSVDIKKVLLEMRKFRMGLIQTADQLRFSYLAVIEGAKFIMGDSSVQDQWKELSHEDLEPPPEHIPPPPRPPKRILEPHNGKCREFFPNHQWVKEETQEDKDCPIKEEKGSPLNAAPYGIESMSQDTEVRSRVVGGSLRGAQAASPAKGEPSLPEKDEDHALSYWKPFLVNMCVATVLTAGAYLCYRFLFNSNT T89529 DRUGINFO D03IDU Hydrogen peroxide Approved T89529 DRUGINFO D03TTQ TRYPAN BLUE Approved T89529 DRUGINFO D0J1WO ISIS 113715 Phase 2 T89529 DRUGINFO D0SM6N ISIS-PTP1Brx Phase 2 T89529 DRUGINFO D07LUJ URSOLIC ACID Phase 2 T89529 DRUGINFO D06WBE ERTIPROTAFIB Terminated T89529 DRUGINFO D0O8PQ [[4-(Aminomethyl)Phenyl]Amino]Oxo-Acetic Acid, Investigative T89529 DRUGINFO D00BLD 1,2,3,4,6-penta-O-galloyl-D-glucopyranose Investigative T89529 DRUGINFO D06NGA 1,2,5-THIADIAZOLIDIN-3-ONE-1,1-DIOXIDE Investigative T89529 DRUGINFO D0W9VA 1,2-NAPHTHOQUINONE Investigative T89529 DRUGINFO D0OJ1V 16-alphaH,17-isovaleryloxy-ent-kauran-19-oic acid Investigative T89529 DRUGINFO D08ABU 18alpha-Glycyrrhetic acid Investigative T89529 DRUGINFO D0X2OD 18beta-Glycyrrhetic acid Investigative T89529 DRUGINFO D0K0PR 19alpha,24-dihydroxyurs-12-en-3-on-28-oic acid Investigative T89529 DRUGINFO D05AOH 1-Iodyl-3-nitro-benzene Investigative T89529 DRUGINFO D03KJL 1-Iodyl-4-nitro-benzene Investigative T89529 DRUGINFO D0OK8N 1-METHYL-3-PHENYL-1H-PYRAZOL-5-YLSULFAMIC ACID Investigative T89529 DRUGINFO D0Y5SB 2-(Oxalyl-Amino)-Benzoic Acid Investigative T89529 DRUGINFO D0D4SI 24-hydroxyursolic acid Investigative T89529 DRUGINFO D06GOK 2-Methyl-2,4-Pentanediol Investigative T89529 DRUGINFO D05SEV 3-(4,5-Bis-biphenyl-4-yl-1H-imidazol-2-yl)-phenol Investigative T89529 DRUGINFO D07DNK 3-(Oxalyl-Amino)-Naphthalene-2-Carboxylic Acid Investigative T89529 DRUGINFO D0OY2V 3,9-Dihydroxy-4-prenyl-[6aR,11aR]pterocarpan Investigative T89529 DRUGINFO D04TTB 3alpha,24-dihydroxyolean-12-en-27-oic acid Investigative T89529 DRUGINFO D06BFB 3beta,6beta-dihydroxyolean-12-en-27-oic acid Investigative T89529 DRUGINFO D0M0XS 3beta-acetoxyolean-12-en-27-oic acid Investigative T89529 DRUGINFO D00VNC 3beta-hydroxyolean-12-en-27-oic acid Investigative T89529 DRUGINFO D0J1GM 3beta-hydroxyurs-12-en-27-oic acid Investigative T89529 DRUGINFO D0Q8AT 3-epi-masilinic acid Investigative T89529 DRUGINFO D0U2WU 3-Iodyl-benzoic acid Investigative T89529 DRUGINFO D08GWQ 3-isopropyl-4-(phenylthio)naphthalene-1,2-dione Investigative T89529 DRUGINFO D08NUF 3-oxoolean-12-en-27-oic acid Investigative T89529 DRUGINFO D0Q3KF 4'-((2-butylbenzofuran-3-yl)methyl)biphenyl-4-ol Investigative T89529 DRUGINFO D0A4ML 4'-(2-butylbenzofuran-3-yl)biphenyl-4-ol Investigative T89529 DRUGINFO D0N7YT 4-(p-toluidino)-3-isopropylnaphthalene-1,2-dione Investigative T89529 DRUGINFO D0G7HN 4-Iodyl-benzoic acid Investigative T89529 DRUGINFO D0DU3J 5-deoxyabyssinin II Investigative T89529 DRUGINFO D0E0BU 6-(Oxalyl-Amino)-1h-Indole-5-Carboxylic Acid Investigative T89529 DRUGINFO D0M6KC Abyssinin I Investigative T89529 DRUGINFO D00RZN Abyssinin II Investigative T89529 DRUGINFO D05YZE Abyssinoflavanone VI Investigative T89529 DRUGINFO D0S9GU Abyssinoflavanone VII Investigative T89529 DRUGINFO D00MNE Abyssinone-IV Investigative T89529 DRUGINFO D0QQ7A Abyssinone-VI-4-O-methyl ether Investigative T89529 DRUGINFO D0F2ME Acetate Ion Investigative T89529 DRUGINFO D0E1ZS ALBAFURAN A Investigative T89529 DRUGINFO D0O7ZL Augustic acid Investigative T89529 DRUGINFO D02UVH B-Octylglucoside Investigative T89529 DRUGINFO D09YKH BURTTINONE Investigative T89529 DRUGINFO D06AWX CAULERPIN Investigative T89529 DRUGINFO D0JB4G CHROMOTROPATE Investigative T89529 DRUGINFO D0V6UC Cysteine Sulfenic Acid Investigative T89529 DRUGINFO D05AMX Cysteinesulfonic Acid Investigative T89529 DRUGINFO D0H1GU Double Oxidized Cysteine Investigative T89529 DRUGINFO D0U9HN DYSIDINE Investigative T89529 DRUGINFO D0ZS7M Erybreadin b Investigative T89529 DRUGINFO D00KZO Erybreadin C Investigative T89529 DRUGINFO D0P9SW Erybreadin D Investigative T89529 DRUGINFO D0M7ZZ Erysubin E Investigative T89529 DRUGINFO D0JL8I ERYTHRIBYSSIN A Investigative T89529 DRUGINFO D0Q5PQ FOLITENOL Investigative T89529 DRUGINFO D03BHQ FORMYLCHROMONE Investigative T89529 DRUGINFO D06LNL Iodyl-benzene Investigative T89529 DRUGINFO D0AL8P ISIS 107772 Investigative T89529 DRUGINFO D0P2TB ISIS 107773 Investigative T89529 DRUGINFO D0Q0XJ ISIS 107774 Investigative T89529 DRUGINFO D0S0XV ISIS 107775 Investigative T89529 DRUGINFO D0QV8M ISIS 107776 Investigative T89529 DRUGINFO D0L1ZD ISIS 107791 Investigative T89529 DRUGINFO D05WJI ISIS 107792 Investigative T89529 DRUGINFO D0A1QK Isochroman mono-carboxylic acid Investigative T89529 DRUGINFO D08GDJ ISOTHIAZOLIDINONE ANALOG Investigative T89529 DRUGINFO D03CBD Isoxazolecarboxylic acid Investigative T89529 DRUGINFO D0J7EN KR61639 Investigative T89529 DRUGINFO D0D8QO Kuwanon J Investigative T89529 DRUGINFO D0A8WJ Kuwanon L Investigative T89529 DRUGINFO D09WED Kuwanon R Investigative T89529 DRUGINFO D08VRV Kuwanon V Investigative T89529 DRUGINFO D08GEN LICOAGROCHACONE A Investigative T89529 DRUGINFO D09TUB LICOAGROCHALCONE A Investigative T89529 DRUGINFO D01BZE MASLINIC ACID Investigative T89529 DRUGINFO D0J5KG Methyl 3beta-hydroxyolean-12-en-28-oate Investigative T89529 DRUGINFO D0E1UG Methyl3beta-hydroxyolean-12-en-27-oate Investigative T89529 DRUGINFO D0VA9F Mulberrofuran C Investigative T89529 DRUGINFO D01NUT Mulberrofuran D Investigative T89529 DRUGINFO D0H1WV Mulberrofuran W Investigative T89529 DRUGINFO D01EJH NEORAUTENOL Investigative T89529 DRUGINFO D0Y1RO Novo Nordisk a/S Compound Investigative T89529 DRUGINFO D03EGZ OHIOENSIN A Investigative T89529 DRUGINFO D0V0LU Ohioensin C Investigative T89529 DRUGINFO D08SAG Ohioensin F Investigative T89529 DRUGINFO D0ZE8C Ohioensin G Investigative T89529 DRUGINFO D0SJ2Q OLEANOLIC_ACID Investigative T89529 DRUGINFO D02KKU Oleanonic acid Investigative T89529 DRUGINFO D03ZIH Oxalylaminobenzoic acid Investigative T89529 DRUGINFO D08AHA PARA-(BENZOYL)-PHENYLALANINE Investigative T89529 DRUGINFO D0MG9O PHELLIGRIDIN I Investigative T89529 DRUGINFO D0XB7H PNU177836 Investigative T89529 DRUGINFO D0Z1HV Pomolic acid Investigative T89529 DRUGINFO D08BSQ RK-682 Investigative T89529 DRUGINFO D03KGX Rotungenic acid Investigative T89529 DRUGINFO D0M7IA Sanggenon C Investigative T89529 DRUGINFO D01TNT Sanggenon G Investigative T89529 DRUGINFO D0K3TS SIGMOIDIN A Investigative T89529 DRUGINFO D09HAX SIGMOIDIN B Investigative T89529 DRUGINFO D0N8OO Sigmoidin F Investigative T89529 DRUGINFO D03NTG Sp7343-Sp7964 Investigative T89529 DRUGINFO D09GPV Spathodic acid Investigative T89529 DRUGINFO D07VEP USIMINE A Investigative T89529 DRUGINFO D09JSD USNIC ACID Investigative T89529 DRUGINFO D09OWE UVAOL Investigative T89529 KEGGPATH hsa04520:Adherens junction T89529 KEGGPATH hsa04910:Insulin signaling pathway T89529 WIKIPATH WP1832:Integrin alphaIIb beta3 signaling T89529 WIKIPATH WP1835:Interferon alpha/beta signaling T89529 WIKIPATH WP1836:Interferon gamma signaling T89529 WIKIPATH WP2034:Leptin signaling pathway T89529 WIKIPATH WP2657:Growth hormone receptor signaling T89529 WIKIPATH WP481:Insulin Signaling T89529 REACPATH R-HSA-354192:Integrin alphaIIb beta3 signaling T89529 REACPATH R-HSA-877312:Regulation of IFNG signaling T89529 REACPATH R-HSA-912694:Regulation of IFNA signaling T89529 REACPATH R-HSA-982772:Growth hormone receptor signaling T89529 NET_PATH NetPath_25:FSH Signaling Pathway T89529 INTEPATH ajdiss_2pathway:Posttranslational regulation of adherens junction stability and dissassembly T89529 INTEPATH erbb1_receptor_proximal_pathway:EGF receptor (ErbB1) signaling pathway T89529 INTEPATH igf1_pathway:IGF1 pathway T89529 INTEPATH insulin_pathway:Insulin Pathway T89529 INTEPATH met_pathway:Signaling events mediated by Hepatocyte Growth Factor Receptor (c-Met) T89529 INTEPATH ncadherinpathway:N-cadherin signaling events T89529 INTEPATH nfat_tfpathway:Calcineurin-regulated NFAT-dependent transcription in lymphocytes T89529 INTEPATH pdgfrbpathway:PDGFR-beta signaling pathway T89529 INTEPATH ptp1bpathway:Signaling events mediated by PTP1B T89529 INTEPATH tcptp_pathway:Signaling events mediated by TCPTP T89529 PANTPATH P00012:Cadherin signaling pathway T08922 TARGETID T08922 T08922 FORMERID TTDS00357 T08922 UNIPROID ACACB_HUMAN T08922 TARGNAME Acetyl-CoA carboxylase 2 (ACACB) T08922 GENENAME ACACB T08922 TARGTYPE Successful target T08922 SYNONYMS Acetyl-Coenzyme A carboxylase beta; Acetyl CoA carboxylase beta; ACCbeta; ACC2; ACC-beta; ACACB T08922 FUNCTION Catalyzes the ATP-dependent carboxylation of acetyl-CoA to malonyl-CoA. Carries out three functions: biotin carboxyl carrier protein, biotin carboxylase and carboxyltransferase. Involved in inhibition of fatty acid and glucose oxidation and enhancement of fat storage. May play a role in regulation of mitochondrial fatty acid oxidation through malonyl- CoA-dependent inhibition of carnitine palmitoyltransferase 1. T08922 PDBSTRUC 5KKN; 4HQ6; 3TDC; 3JRX; 3JRW T08922 BIOCLASS Carbon-carbon ligase T08922 ECNUMBER EC 6.4.1.2 T08922 SEQUENCE MVLLLCLSCLIFSCLTFSWLKIWGKMTDSKPITKSKSEANLIPSQEPFPASDNSGETPQRNGEGHTLPKTPSQAEPASHKGPKDAGRRRNSLPPSHQKPPRNPLSSSDAAPSPELQANGTGTQGLEATDTNGLSSSARPQGQQAGSPSKEDKKQANIKRQLMTNFILGSFDDYSSDEDSVAGSSRESTRKGSRASLGALSLEAYLTTGEAETRVPTMRPSMSGLHLVKRGREHKKLDLHRDFTVASPAEFVTRFGGDRVIEKVLIANNGIAAVKCMRSIRRWAYEMFRNERAIRFVVMVTPEDLKANAEYIKMADHYVPVPGGPNNNNYANVELIVDIAKRIPVQAVWAGWGHASENPKLPELLCKNGVAFLGPPSEAMWALGDKIASTVVAQTLQVPTLPWSGSGLTVEWTEDDLQQGKRISVPEDVYDKGCVKDVDEGLEAAERIGFPLMIKASEGGGGKGIRKAESAEDFPILFRQVQSEIPGSPIFLMKLAQHARHLEVQILADQYGNAVSLFGRDCSIQRRHQKIVEEAPATIAPLAIFEFMEQCAIRLAKTVGYVSAGTVEYLYSQDGSFHFLELNPRLQVEHPCTEMIADVNLPAAQLQIAMGVPLHRLKDIRLLYGESPWGVTPISFETPSNPPLARGHVIAARITSENPDEGFKPSSGTVQELNFRSSKNVWGYFSVAATGGLHEFADSQFGHCFSWGENREEAISNMVVALKELSIRGDFRTTVEYLINLLETESFQNNDIDTGWLDYLIAEKVQAEKPDIMLGVVCGALNVADAMFRTCMTDFLHSLERGQVLPADSLLNLVDVELIYGGVKYILKVARQSLTMFVLIMNGCHIEIDAHRLNDGGLLLSYNGNSYTTYMKEEVDSYRITIGNKTCVFEKENDPTVLRSPSAGKLTQYTVEDGGHVEAGSSYAEMEVMKMIMTLNVQERGRVKYIKRPGAVLEAGCVVARLELDDPSKVHPAEPFTGELPAQQTLPILGEKLHQVFHSVLENLTNVMSGFCLPEPVFSIKLKEWVQKLMMTLRHPSLPLLELQEIMTSVAGRIPAPVEKSVRRVMAQYASNITSVLCQFPSQQIATILDCHAATLQRKADREVFFINTQSIVQLVQRYRSGIRGYMKTVVLDLLRRYLRVEHHFQQAHYDKCVINLREQFKPDMSQVLDCIFSHAQVAKKNQLVIMLIDELCGPDPSLSDELISILNELTQLSKSEHCKVALRARQILIASHLPSYELRHNQVESIFLSAIDMYGHQFCPENLKKLILSETTIFDVLPTFFYHANKVVCMASLEVYVRRGYIAYELNSLQHRQLPDGTCVVEFQFMLPSSHPNRMTVPISITNPDLLRHSTELFMDSGFSPLCQRMGAMVAFRRFEDFTRNFDEVISCFANVPKDTPLFSEARTSLYSEDDCKSLREEPIHILNVSIQCADHLEDEALVPILRTFVQSKKNILVDYGLRRITFLIAQEKEFPKFFTFRARDEFAEDRIYRHLEPALAFQLELNRMRNFDLTAVPCANHKMHLYLGAAKVKEGVEVTDHRFFIRAIIRHSDLITKEASFEYLQNEGERLLLEAMDELEVAFNNTSVRTDCNHIFLNFVPTVIMDPFKIEESVRYMVMRYGSRLWKLRVLQAEVKINIRQTTTGSAVPIRLFITNESGYYLDISLYKEVTDSRSGNIMFHSFGNKQGPQHGMLINTPYVTKDLLQAKRFQAQTLGTTYIYDFPEMFRQALFKLWGSPDKYPKDILTYTELVLDSQGQLVEMNRLPGGNEVGMVAFKMRFKTQEYPEGRDVIVIGNDITFRIGSFGPGEDLLYLRASEMARAEGIPKIYVAANSGARIGMAEEIKHMFHVAWVDPEDPHKGFKYLYLTPQDYTRISSLNSVHCKHIEEGGESRYMITDIIGKDDGLGVENLRGSGMIAGESSLAYEEIVTISLVTCRAIGIGAYLVRLGQRVIQVENSHIILTGASALNKVLGREVYTSNNQLGGVQIMHYNGVSHITVPDDFEGVYTILEWLSYMPKDNHSPVPIITPTDPIDREIEFLPSRAPYDPRWMLAGRPHPTLKGTWQSGFFDHGSFKEIMAPWAQTVVTGRARLGGIPVGVIAVETRTVEVAVPADPANLDSEAKIIQQAGQVWFPDSAYKTAQAVKDFNREKLPLMIFANWRGFSGGMKDMYDQVLKFGAYIVDGLRQYKQPILIYIPPYAELRGGSWVVIDATINPLCIEMYADKESRGGVLEPEGTVEIKFRKKDLIKSMRRIDPAYKKLMEQLGEPDLSDKDRKDLEGRLKAREDLLLPIYHQVAVQFADFHDTPGRMLEKGVISDILEWKTARTFLYWRLRRLLLEDQVKQEILQASGELSHVHIQSMLRRWFVETEGAVKAYLWDNNQVVVQWLEQHWQAGDGPRSTIRENITYLKHDSVLKTIRGLVEENPEVAVDCVIYLSQHISPAERAQVVHLLSTMDSPAST T08922 DRUGINFO D0D7LA Metformin Approved T08922 DRUGINFO D03KHO PF-05175157 Phase 2 T08922 DRUGINFO D01OKS Axokine Discontinued in Phase 3 T08922 DRUGINFO D0K4WI 2-[4-(2,4-Dichlorophenoxy)Phenoxy]Propanoic Acid Investigative T08922 DRUGINFO D0IY5Y A-80040 Investigative T08922 DRUGINFO D0P7HI AC-8632 Investigative T08922 DRUGINFO D07WIC CP-640186 Investigative T08922 DRUGINFO D08FSR QLT-091382 Investigative T08922 DRUGINFO D0WD1E Soraphen A Investigative T08922 KEGGPATH hsa00061:Fatty acid biosynthesis T08922 KEGGPATH hsa00620:Pyruvate metabolism T08922 KEGGPATH hsa00640:Propanoate metabolism T08922 KEGGPATH hsa01100:Metabolic pathways T08922 KEGGPATH hsa01212:Fatty acid metabolism T08922 KEGGPATH hsa04152:AMPK signaling pathway T08922 KEGGPATH hsa04910:Insulin signaling pathway T08922 KEGGPATH hsa04920:Adipocytokine signaling pathway T08922 KEGGPATH hsa04922:Glucagon signaling pathway T08922 WIKIPATH WP1403:AMPK Signaling T08922 WIKIPATH WP1817:Fatty acid, triacylglycerol, and ketone body metabolism T08922 WIKIPATH WP2034:Leptin signaling pathway T08922 WIKIPATH WP2380:BDNF signaling pathway T08922 WIKIPATH WP2706:Activation of Gene Expression by SREBP (SREBF) T08922 WIKIPATH WP357:Fatty Acid Biosynthesis T08922 REACPATH R-HSA-163765:ChREBP activates metabolic gene expression T08922 REACPATH R-HSA-200425:Import of palmitoyl-CoA into the mitochondrial matrix T08922 REACPATH R-HSA-2426168:Activation of gene expression by SREBF (SREBP) T08922 NET_PATH NetPath_7:TGF_beta_Receptor Signaling Pathway T08922 BIOCPATH PWY0-1264:Biotin-carboxyl carrier protein assembly T08922 BIOCPATH PWY-5966-1:Fatty acid biosynthesis initiation T21334 TARGETID T21334 T21334 FORMERID TTDC00224 T21334 UNIPROID TNF11_HUMAN T21334 TARGNAME Osteoclast differentiation factor (ODF) T21334 GENENAME TNFSF11 T21334 TARGTYPE Successful target T21334 SYNONYMS Tumor necrosis factor ligand superfamily member 11; TRANCE; TNF-related activation-induced cytokine; Receptor activatorof nuclear factor kappa B ligand; Receptor activator of nuclear factor kappa-B ligand; RANKL; Osteoprotegerin ligand; OPGL; CD254 T21334 FUNCTION Osteoclast differentiation and activation factor. Augments the ability of dendritic cells to stimulate naive T-cell proliferation. May be an important regulator of interactions between T-cells and dendritic cells and may play a role in the regulation of the T-cell-dependent immune response. May also play an important role in enhanced bone-resorption in humoral hypercalcemia of malignancy. Induces osteoclastogenesis by activating multiple signaling pathways in osteoclast precursor cells, chief among which is induction of long lasting oscillations in the intracellular concentration of Ca (2+) resulting in the activation of NFATC1, which translocates to the nucleus and induces osteoclast-specific gene transcription to allow differentiation of osteoclasts. During osteoclast differentiation, in a TMEM64 and ATP2A2-dependent manner induces activation of CREB1 and mitochondrial ROS generation necessary for proper osteoclast generation. Cytokine that binds to TNFRSF11B/OPG and to TNFRSF11A/RANK. T21334 PDBSTRUC 5BNQ; 3URF T21334 BIOCLASS Cytokine: tumor necrosis factor T21334 SEQUENCE MRRASRDYTKYLRGSEEMGGGPGAPHEGPLHAPPPPAPHQPPAASRSMFVALLGLGLGQVVCSVALFFYFRAQMDPNRISEDGTHCIYRILRLHENADFQDTTLESQDTKLIPDSCRRIKQAFQGAVQKELQHIVGSQHIRAEKAMVDGSWLDLAKRSKLEAQPFAHLTINATDIPSGSHKVSLSSWYHDRGWAKISNMTFSNGKLIVNQDGFYYLYANICFRHHETSGDLATEYLQLMVYVTKTSIKIPSSHTLMKGGSTKYWSGNSEFHFYSINVGGFFKLRSGEEISIEVSNPSLLDPDQDATYFGAFKVRDID T21334 DRUGINFO D08WSY Denosumab Approved T21334 DRUGINFO D0MG2R ALX-0141 Phase 1 T21334 DRUGINFO D09QWD CEP-37251 Phase 1 T21334 KEGGPATH hsa04060:Cytokine-cytokine receptor interaction T21334 KEGGPATH hsa04064:NF-kappa B signaling pathway T21334 KEGGPATH hsa04380:Osteoclast differentiation T21334 KEGGPATH hsa04917:Prolactin signaling pathway T21334 KEGGPATH hsa05323:Rheumatoid arthritis T21334 WIKIPATH WP12:Osteoclast Signaling T21334 WIKIPATH WP2018:RANKL/RANK Signaling Pathway T21334 WIKIPATH WP2848:Differentiation Pathway T21334 WIKIPATH WP2877:Vitamin D Receptor Pathway T21334 WIKIPATH WP322:Osteoblast Signaling T21334 REACPATH R-HSA-5668541:TNFR2 non-canonical NF-kB pathway T21334 REACPATH R-HSA-5669034:TNFs bind their physiological receptors T21334 REACPATH R-HSA-5676594:TNF receptor superfamily (TNFSF) members mediating non-canonical NF-kB pathway T21334 NET_PATH NetPath_22:Leptin Signaling Pathway T21334 NET_PATH NetPath_26:TWEAK Signaling Pathway T21334 INTEPATH il6_7pathway:IL6-mediated signaling events T92777 TARGETID T92777 T92777 FORMERID TTDS00291 T92777 UNIPROID MGA_HUMAN T92777 TARGNAME Intestinal maltase-glucoamylase (MGAM) T92777 GENENAME MGAM T92777 TARGTYPE Successful target T92777 SYNONYMS MGAM T92777 FUNCTION May serve as an alternate pathway for starch digestion when luminal alpha-amylase activity is reduced because of immaturity or malnutrition. May play a unique role in the digestion of malted dietary oligosaccharides used in food manufacturing. T92777 PDBSTRUC 3TOP; 3TON; 3L4Z; 3L4Y; 3L4X T92777 BIOCLASS Glycosylase T92777 SEQUENCE MARKKLKKFTTLEIVLSVLLLVLFIISIVLIVLLAKESLKSTAPDPGTTGTPDPGTTGTPDPGTTGTTHARTTGPPDPGTTGTTPVSAECPVVNELERINCIPDQPPTKATCDQRGCCWNPQGAVSVPWCYYSKNHSYHVEGNLVNTNAGFTARLKNLPSSPVFGSNVDNVLLTAEYQTSNRFHFKLTDQTNNRFEVPHEHVQSFSGNAAASLTYQVEISRQPFSIKVTRRSNNRVLFDSSIGPLLFADQFLQLSTRLPSTNVYGLGEHVHQQYRHDMNWKTWPIFNRDTTPNGNGTNLYGAQTFFLCLEDASGLSFGVFLMNSNAMEVVLQPAPAITYRTIGGILDFYVFLGNTPEQVVQEYLELIGRPALPSYWALGFHLSRYEYGTLDNMREVVERNRAAQLPYDVQHADIDYMDERRDFTYDSVDFKGFPEFVNELHNNGQKLVIIVDPAISNNSSSSKPYGPYDRGSDMKIWVNSSDGVTPLIGEVWPGQTVFPDYTNPNCAVWWTKEFELFHNQVEFDGIWIDMNEVSNFVDGSVSGCSTNNLNNPPFTPRILDGYLFCKTLCMDAVQHWGKQYDIHNLYGYSMAVATAEAAKTVFPNKRSFILTRSTFAGSGKFAAHWLGDNTATWDDLRWSIPGVLEFNLFGIPMVGPDICGFALDTPEELCRRWMQLGAFYPFSRNHNGQGYKDQDPASFGADSLLLNSSRHYLNIRYTLLPYLYTLFFRAHSRGDTVARPLLHEFYEDNSTWDVHQQFLWGPGLLITPVLDEGAEKVMAYVPDAVWYDYETGSQVRWRKQKVEMELPGDKIGLHLRGGYIFPTQQPNTTTLASRKNPLGLIIALDENKEAKGELFWDNGETKDTVANKVYLLCEFSVTQNRLEVNISQSTYKDPNNLAFNEIKILGTEEPSNVTVKHNGVPSQTSPTVTYDSNLKVAIITDIDLLLGEAYTVEWSIKIRDEEKIDCYPDENGASAENCTARGCIWEASNSSGVPFCYFVNDLYSVSDVQYNSHGATADISLKSSVYANAFPSTPVNPLRLDVTYHKNEMLQFKIYDPNKNRYEVPVPLNIPSMPSSTPEGQLYDVLIKKNPFGIEIRRKSTGTIIWDSQLLGFTFSDMFIRISTRLPSKYLYGFGETEHRSYRRDLEWHTWGMFSRDQPPGYKKNSYGVHPYYMGLEEDGSAHGVLLLNSNAMDVTFQPLPALTYRTTGGVLDFYVFLGPTPELVTQQYTELIGRPVMVPYWSLGFQLCRYGYQNDSEIASLYDEMVAAQIPYDVQYSDIDYMERQLDFTLSPKFAGFPALINRMKADGMRVILILDPAISGNETQPYPAFTRGVEDDVFIKYPNDGDIVWGKVWPDFPDVVVNGSLDWDSQVELYRAYVAFPDFFRNSTAKWWKREIEELYNNPQNPERSLKFDGMWIDMNEPSSFVNGAVSPGCRDASLNHPPYMPHLESRDRGLSSKTLCMESQQILPDGSLVQHYNVHNLYGWSQTRPTYEAVQEVTGQRGVVITRSTFPSSGRWAGHWLGDNTAAWDQLKKSIIGMMEFSLFGISYTGADICGFFQDAEYEMCVRWMQLGAFYPFSRNHNTIGTRRQDPVSWDVAFVNISRTVLQTRYTLLPYLYTLMHKAHTEGVTVVRPLLHEFVSDQVTWDIDSQFLLGPAFLVSPVLERNARNVTAYFPRARWYDYYTGVDINARGEWKTLPAPLDHINLHVRGGYILPWQEPALNTHLSRQKFMGFKIALDDEGTAGGWLFWDDGQSIDTYGKGLYYLASFSASQNTMQSHIIFNNYITGTNPLKLGYIEIWGVGSVPVTSVSISVSGMVITPSFNNDPTTQVLSIDVTDRNISLHNFTSLTWISTL T92777 DRUGINFO D0AD5C Acarbose Approved T92777 DRUGINFO D0D0ZD Miglitol Approved T92777 DRUGINFO D0M1CZ Rh-alphaglucosidase Approved T92777 DRUGINFO D04ZTY Voglibose Approved T92777 DRUGINFO D0Y2SE Alpha-glucosidase Phase 3 T92777 DRUGINFO D0S5LT Deoxynojirimycin Phase 3 T92777 DRUGINFO D0H9WY PAZ-320 Phase 2 T92777 DRUGINFO D0O1HL SC-49483 Phase 2 T92777 DRUGINFO D08CDE Celgosivir Phase 1/2 T92777 DRUGINFO D04RYY Maltose Phase 1/2 T92777 DRUGINFO D07TSW SALACINOL Phase 1/2 T92777 DRUGINFO D0H9SF A-76202M Terminated T92777 DRUGINFO D0GS0O 1,4-dideoxy-1,4-imino-D-arabinito Investigative T92777 DRUGINFO D0R5HV 2,5-Dideoxy-2,5-imino-D-mannitol Investigative T92777 DRUGINFO D0Z2RR 2-Aminomethyl-pyrrolidine-3,4-diol Investigative T92777 DRUGINFO D0T0EJ 2-Cyclopentylamin