Target General Infomation
Target ID
T85943
Former ID
TTDS00247
Target Name
Proto-oncogene tyrosine-protein kinase SRC
Gene Name
SRC
Synonyms
C-SRC tyrosine kinase; C-Src; C-src TK; P60-Src; Pp60(src); Src tyrosine kinase; Tyrosine kinase; Tyrosine kinase (pp60(src)); SRC
Target Type
Successful
Disease Advanced breast cancer [ICD9: 174, 175; ICD10: C50]
Brain cancer [ICD9: 191, 225.0; ICD10: C71, D33]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Chronic myelogenous leukaemia [ICD9: 205.1; ICD10: C92.1]
Glioblastoma multiforme [ICD9: 191; ICD10: C71]
Ischemia [ICD9: 459.89; ICD10: I99.8]
Multiple myeloma [ICD9: 203; ICD10: C90]
Osteoporosis [ICD9: 733.0, V07.4; ICD10: M80-M81, Z79.890]
Osteosarcoma; Hematological malignancies; Solid tumours [ICD9: 140-199, 140-239, 170, 200-209, 210-229; ICD10: C40-C41, C81-C86, D10-D36, D3A]
Function
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.
BioChemical Class
Kinase
Target Validation
T85943
UniProt ID
EC Number
EC 2.7.10.2
Sequence
MGSNKSKPKDASQRRRSLEPAENVHGAGGGAFPASQTPSKPASADGHRGPSAAFAPAAAE
PKLFGGFNSSDTVTSPQRAGPLAGGVTTFVALYDYESRTETDLSFKKGERLQIVNNTEGD
WWLAHSLSTGQTGYIPSNYVAPSDSIQAEEWYFGKITRRESERLLLNAENPRGTFLVRES
ETTKGAYCLSVSDFDNAKGLNVKHYKIRKLDSGGFYITSRTQFNSLQQLVAYYSKHADGL
CHRLTTVCPTSKPQTQGLAKDAWEIPRESLRLEVKLGQGCFGEVWMGTWNGTTRVAIKTL
KPGTMSPEAFLQEAQVMKKLRHEKLVQLYAVVSEEPIYIVTEYMSKGSLLDFLKGETGKY
LRLPQLVDMAAQIASGMAYVERMNYVHRDLRAANILVGENLVCKVADFGLARLIEDNEYT
ARQGAKFPIKWTAPEAALYGRFTIKSDVWSFGILLTELTTKGRVPYPGMVNREVLDQVER
GYRMPCPPECPESLHDLMCQCWRKEPEERPTFEYLQAFLEDYFTSTEPQYQPGENL
Structure
1A07; 1A08; 1A09; 1A1A; 1A1B; 1A1C; 1A1E; 1FMK; 1HCS; 1HCT; 1KSW; 1O41; 1O42; 1O43; 1O44; 1O45; 1O46; 1O47; 1O48; 1O49; 1O4A; 1O4B; 1O4C; 1O4D; 1O4E; 1O4F; 1O4G; 1O4H; 1O4I; 1O4J; 1O4K; 1O4L; 1O4M; 1O4N; 1O4O; 1O4P; 1O4Q; 1O4R; 1SHD; 1Y57; 1YI6; 1YOJ; 1YOL; 1YOM;2BDF; 2BDJ; 2H8H; 2SRC; 3VRO; 3ZMP; 3ZMQ; 4F59; 4F5A; 4F5B; 4HXJ; 4K11; 4MXO; 4MXX; 4MXY; 4MXZ; 1A07; 1A08; 1A09; 1A1A; 1A1B; 1A1C; 1A1E; 1FMK; 1HCS; 1HCT; 1KSW; 1O41; 1O42; 1O43; 1O44; 1O45; 1O46; 1O47; 1O48; 1O49; 1O4A; 1O4B; 1O4C; 1O4D; 1O4E; 1O4F; 1O4G; 1O4H; 1O4I; 1O4J; 1O4K; 1O4L; 1O4M; 1O4N; 1O4O; 1O4P; 1O4Q; 1O4R;1SHD; 1Y57; 1YI6; 1YOJ; 1YOL; 1YOM; 2BDF; 2BDJ; 2H8H; 2SRC; 3VRO; 3ZMP; 3ZMQ; 4F59; 4F5A; 4F5B; 4HXJ; 4K11; 4MXO; 4MXX; 4MXY; 4MXZ
Drugs and Mode of Action
Drug(s) Bosutinib Drug Info Approved Advanced breast cancer [525021], [541049]
Dasatinib Drug Info Approved Chronic myelogenous leukaemia [528715], [536577], [541021], [551871]
Herbimycin A Drug Info Approved Cancer [537902], [541254]
SKI-758 Drug Info Approved Ischemia [532210], [551871]
AZD0530 Drug Info Phase 2 Osteosarcoma; Hematological malignancies; Solid tumours [536957], [542701]
Dasatinib Drug Info Phase 2 Multiple myeloma [536957], [541021]
PD173074 Drug Info Phase 2 Discovery agent [468136], [523642]
KX-02 Drug Info Phase 1 Brain cancer [549581]
KX2-361 Drug Info Phase 1 Glioblastoma multiforme [525042]
AP22408 Drug Info Terminated Osteoporosis [546858]
PD166285 Drug Info Terminated Discovery agent [542988], [546594]
Inhibitor 2-(4-CARCOXY-5-ISOPROPYLTHIAZOLYL)BENZOPIPERIDINE Drug Info [551374]
3-(3-aminobenzo[e][1,2,4]triazin-7-yl)phenol Drug Info [528392]
4-Chloro-5,7-diphenyl-7H-pyrrolo[2,3-d]pyrimidine Drug Info [525793]
5,7-Diphenyl-7H-pyrrolo[2,3-d]pyrimidin-4-ol Drug Info [525793]
7-(naphthalen-2-yl)benzo[e][1,2,4]triazin-3-amine Drug Info [528392]
A-420983 Drug Info [527057]
A-770041 Drug Info [527790]
Ac-Cys-Ile-cyclo[Phe-Lys]-Tyr-Tyr Drug Info [528214]
Ac-Cys-Ile-Phe(4-NO2)-Lys-Phe(4-NO2)-Tyr Drug Info [528214]
Ac-Cys-Ile-Phe(4-NO2)-Lys-Tyr-Phe(4-NO2) Drug Info [528214]
Ac-Cys-Ile-Phe(4-NO2)-Lys-Tyr-Tyr Drug Info [528214]
Ac-Cys-Ile-Tyr-Lys-Phe(4-Cl)-Tyr Drug Info [528214]
Ac-Cys-Ile-Tyr-Lys-Phe(4-CN)-Tyr Drug Info [528214]
Ac-Cys-Ile-Tyr-Lys-Phe(4-I)-Tyr Drug Info [528214]
Ac-Cys-Ile-Tyr-Lys-Phe(4-N3)-Tyr Drug Info [528214]
Ac-Cys-Ile-Tyr-Lys-Phe(4-NO2)-Phe(4-NO2) Drug Info [528214]
Ac-Cys-Ile-Tyr-Lys-Phe(4-NO2)-Tyr-Phe Drug Info [528214]
Ac-Cys-Ile-Tyr-Lys-Tyr-Phe(4-NO2) Drug Info [528214]
AG-1879 Drug Info [529039]
AP-24163 Drug Info [530244]
AP-24226 Drug Info [530244]
AP22408 Drug Info [535031]
BAS-00387275 Drug Info [528211]
BAS-00387328 Drug Info [528211]
BAS-00387347 Drug Info [528211]
BAS-00672722 Drug Info [528211]
BAS-01047341 Drug Info [528211]
BAS-01047655 Drug Info [528211]
BAS-01373578 Drug Info [528211]
BAS-0338868 Drug Info [529217]
BAS-0338872 Drug Info [529217]
BAS-09534324 Drug Info [528211]
BAS-450225 Drug Info [528211]
BAS-4844343 Drug Info [528211]
BMS-279700 Drug Info [528520]
Bosutinib Drug Info [536474]
CGP 77675 Drug Info [534864]
CGP-191 Drug Info [525793]
CGP-62464 Drug Info [525793]
compound 2 Drug Info [527295]
compound 8h Drug Info [531959]
Cyclo[Ac-Cys-Ile-Phe]-Lys-Tyr-Tyr Drug Info [528214]
Cyclo[Ac-Cys-Ile-Tyr-Lys-Tyr-Phe] Drug Info [528214]
Cyclo[Ac-Cys-Ile-Tyr-Lys-Tyr-Tyr] Drug Info [528214]
Cysteine Sulfenic Acid Drug Info [551391]
Dasatinib Drug Info [536331], [536474], [536797]
DPI59 Drug Info [551374]
Glu-Pro-Gln-F2Pmp-Glu-Glu-Ile-Pro-Ile-Tyr-Leu Drug Info [551322]
Glu-Pro-Gln-pTyr-Glu-Glu-Ile-Pro-Ile-Tyr-Leu Drug Info [551322]
Herbimycin A Drug Info [537902]
ISO24 Drug Info [551374]
JNJ-10198409 Drug Info [527932]
K00244 Drug Info [530144]
KX-02 Drug Info [551070]
KX2-361 Drug Info [543576]
N-(4-PHENYLAMINO-QUINAZOLIN-6-YL)-ACRYLAMIDE Drug Info [551374]
N-Phenyl-5-phenylimidazo[1,5-a]pyrazin-8-amine Drug Info [528520]
N6-Benzyl Adenosine-5'-Diphosphate Drug Info [551393]
NG-25 Drug Info [532902]
NM-PP1 Drug Info [529039]
Oxalic Acid Drug Info [551393]
PAS219 Drug Info [551374]
PASBN Drug Info [551374]
PD-0166326 Drug Info [530497]
PD-0173952 Drug Info [525862]
PD-0173955 Drug Info [525862]
PD-0173956 Drug Info [530497]
PD-0173958 Drug Info [525862]
PD-0179483 Drug Info [525862]
PD-0180970 Drug Info [525862]
PD-174265 Drug Info [530156]
PD166285 Drug Info [534952]
PD173074 Drug Info [534952]
Phenylphosphate Drug Info [551391]
Phosphonotyrosine Drug Info [551393]
PP121 Drug Info [529744]
RU78191 Drug Info [551374]
RU78262 Drug Info [551374]
RU78299 Drug Info [551374]
RU78300 Drug Info [551374]
RU78783 Drug Info [551393]
RU79072 Drug Info [551374]
RU79073 Drug Info [551374]
RU79256 Drug Info [551374]
RU81843 Drug Info [551393]
RU82129 Drug Info [551393]
RU82197 Drug Info [551391]
RU82209 Drug Info [551393]
RU83876 Drug Info [551393]
RU84687 Drug Info [551374]
RU85053 Drug Info [551393]
RU85493 Drug Info [551393]
RU90395 Drug Info [551393]
SBB007833 Drug Info [528930]
SKI-758 Drug Info [528584]
SKS-927 Drug Info [528592]
SU 6656 Drug Info [529039]
TG-100435 Drug Info [528527]
WH-4-023 Drug Info [528352]
Y-c[D-Pen-(2')Nal-GSFC]KR-NH2 Drug Info [534651]
Y-c[D-Pen-(2R,3R)-2-Me-(2')Nal-GSFC]KR-NH2 Drug Info [534651]
Y-c[D-Pen-(2R,3S)-2-Me-(2')Nal-GSFC]KR-NH2 Drug Info [534651]
Y-c[D-Pen-(2S,3R)-2-Me-(2')Nal-GSFC]KR-NH2 Drug Info [534651]
Y-c[D-Pen-(2S,3S)-2-Me-(2')Nal-GSFC]KR-NH2 Drug Info [534651]
Y-c[D-Pen-(3,5-diI)Tyr-GSFC]KR-NH2 Drug Info [534651]
Y-c[D-Pen-(3-I)Tyr-GSFC]KR-NH2 Drug Info [534651]
Y-c[D-Pen-D-(2')Nal-GSFC]KR-NH2 Drug Info [534651]
Modulator AZD0530 Drug Info
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway ErbB signaling pathway
Rap1 signaling pathway
Chemokine signaling pathway
Endocytosis
VEGF signaling pathway
Focal adhesion
Adherens junction
Tight junction
Gap junction
Platelet activation
GABAergic synapse
Inflammatory mediator regulation of TRP channels
Regulation of actin cytoskeleton
GnRH signaling pathway
Estrogen signaling pathway
Prolactin signaling pathway
Thyroid hormone signaling pathway
Oxytocin signaling pathway
Bacterial invasion of epithelial cells
Epithelial cell signaling in Helicobacter pylori infection
Shigellosis
Tuberculosis
Hepatitis B
Viral carcinogenesis
Proteoglycans in cancer
NetPath Pathway IL2 Signaling Pathway
PANTHER Pathway Angiogenesis
Cadherin signaling pathway
Integrin signalling pathway
Parkinson disease
CCKR signaling map ST
Pathway Interaction Database Endothelins
Signaling events mediated by PRL
LPA receptor mediated events
Atypical NF-kappaB pathway
Glypican 1 network
Plasma membrane estrogen receptor signaling
Signaling events mediated by Hepatocyte Growth Factor Receptor (c-Met)
Signaling events mediated by PTP1B
S1P3 pathway
EPHB forward signaling
Nectin adhesion pathway
Regulation of p38-alpha and p38-beta
CDC42 signaling events
Signaling events regulated by Ret tyrosine kinase
Arf6 signaling events
Signaling events mediated by TCPTP
FAS (CD95) signaling pathway
Thromboxane A2 receptor signaling
Netrin-mediated signaling events
Alpha9 beta1 integrin signaling events
CXCR4-mediated signaling events
EGF receptor (ErbB1) signaling pathway
Class I PI3K signaling events
Posttranslational regulation of adherens junction stability and dissassembly
Regulation of Androgen receptor activity
E-cadherin signaling in the nascent adherens junction
amb2 Integrin signaling
Integrins in angiogenesis
ErbB1 downstream signaling
Urokinase-type plasminogen activator (uPA) and uPAR-mediated signaling
ErbB2/ErbB3 signaling events
EPHA forward signaling
E-cadherin signaling in keratinocytes
PDGFR-beta signaling pathway
Nongenotropic Androgen signaling
Internalization of ErbB1
CXCR3-mediated signaling events
Signaling events mediated by VEGFR1 and VEGFR2
Syndecan-2-mediated signaling events
Class I PI3K signaling events mediated by Akt
Syndecan-3-mediated signaling events
Ephrin B reverse signaling
Trk receptor signaling mediated by PI3K and PLC-gamma
EPHA2 forward signaling
Alpha-synuclein signaling
FGF signaling pathway
Alpha4 beta1 integrin signaling events
Signaling events mediated by focal adhesion kinase
WikiPathways ErbB Signaling Pathway
Senescence and Autophagy in Cancer
Notch Signaling Pathway
EPO Receptor Signaling
EGF/EGFR Signaling Pathway
TGF beta Signaling Pathway
Signaling of Hepatocyte Growth Factor Receptor
Kit receptor signaling pathway
Pregnane X Receptor pathway
Aryl Hydrocarbon Receptor Pathway
IL-3 Signaling Pathway
Nanoparticle-mediated activation of receptor signaling
Polycystic Kidney Disease Pathway
Alpha 6 Beta 4 signaling pathway
BDNF signaling pathway
Integrated Pancreatic Cancer Pathway
Oncostatin M Signaling Pathway
Interleukin-11 Signaling Pathway
AGE/RAGE pathway
Signaling Pathways in Glioblastoma
TSLP Signaling Pathway
Arylhydrocarbon receptor (AhR) signaling pathway
Regulation of Microtubule Cytoskeleton
FSH signaling pathway
Leptin signaling pathway
RANKL/RANK Signaling Pathway
Integrin-mediated Cell Adhesion
Angiogenesis
Androgen receptor signaling pathway
References
Ref 468136(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5037).
Ref 523642ClinicalTrials.gov (NCT01441297) BIBF 1120 as Second Line Treatment for Small Cell Lung Cancer. U.S. National Institutes of Health.
Ref 525021ClinicalTrials.gov (NCT02311998) Phase I/II Study of Bosutinib in Combination With Inotuzumab Ozogamicin in CD22-positive Philadelphia-Chromosome (PC) Positive Acute Lymphoblastic Leukemia (ALL) and Chronic Myeloid Leukemia (CML). U.S. National Institutes of Health.
Ref 525042ClinicalTrials.gov (NCT02326441) Safety, Tolerability & PK of KX2-361 in Subjects w Adv. Malignancies Refractory to Conventional Therapies. U.S. National Institutes of Health.
Ref 5287152006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
Ref 532210Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
Ref 536577Dasatinib: a tyrosine kinase inhibitor for the treatment of chronic myelogenous leukemia and philadelphia chromosome-positive acute lymphoblastic leukemia. Clin Ther. 2007 Nov;29(11):2289-308.
Ref 536957Current and future treatments of bone metastases. Expert Opin Emerg Drugs. 2008 Dec;13(4):609-27.
Ref 537902In vivo antitumor activity of herbimycin A, a tyrosine kinase inhibitor, targeted against BCR/ABL oncoprotein in mice bearing BCR/ABL-transfected cells. Leuk Res. 1994 Nov;18(11):867-73.
Ref 541021(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5678).
Ref 541049(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5710).
Ref 541254(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5984).
Ref 542701(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7731).
Ref 542988(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8183).
Ref 546594Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009107)
Ref 546858Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010691)
Ref 549581Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800041844)
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 525793Bioorg Med Chem Lett. 2000 May 1;10(9):945-9.Substituted 5,7-diphenyl-pyrrolo[2,3d]pyrimidines: potent inhibitors of the tyrosine kinase c-Src.
Ref 525862Biochem Pharmacol. 2000 Oct 1;60(7):885-98.Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors.
Ref 527057Bioorg Med Chem Lett. 2004 May 17;14(10):2613-6.A-420983: a potent, orally active inhibitor of lck with efficacy in a model of transplant rejection.
Ref 527295Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors. Bioorg Med Chem Lett. 2004 Dec 20;14(24):6061-6.
Ref 527790Bioorg Med Chem Lett. 2006 Jan 1;16(1):118-22. Epub 2005 Oct 10.Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.
Ref 527932J Med Chem. 2005 Dec 29;48(26):8163-73.(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells.
Ref 528211J Med Chem. 2006 Jun 1;49(11):3278-86.A combination of docking/dynamics simulations and pharmacophoric modeling to discover new dual c-Src/Abl kinase inhibitors.
Ref 528214J Med Chem. 2006 Jun 1;49(11):3395-401.Synthesis and structure-activity relationships of linear and conformationally constrained peptide analogues of CIYKYY as Src tyrosine kinase inhibitors.
Ref 528352Novel 2-aminopyrimidine carbamates as potent and orally active inhibitors of Lck: synthesis, SAR, and in vivo antiinflammatory activity. J Med Chem. 2006 Aug 10;49(16):4981-91.
Ref 528392Bioorg Med Chem Lett. 2006 Nov 1;16(21):5546-50. Epub 2006 Aug 22.Discovery and preliminary structure-activity relationship studies of novel benzotriazine based compounds as Src inhibitors.
Ref 528520Bioorg Med Chem. 2007 Jan 15;15(2):868-85. Epub 2006 Oct 24.Synthesis and c-Src inhibitory activity of imidazo[1,5-a]pyrazine derivatives as an agent for treatment of acute ischemic stroke.
Ref 528527Bioorg Med Chem Lett. 2007 Feb 1;17(3):602-8. Epub 2006 Nov 7.Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays.
Ref 528584J Med Chem. 2006 Dec 28;49(26):7868-76.Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles.
Ref 528592Bioorg Med Chem Lett. 2007 Mar 1;17(5):1358-61. Epub 2006 Dec 3.Inhibition of Src kinase activity by 7-ethynyl-4-phenylamino-3-quinolinecarbonitriles: identification of SKS-927.
Ref 528930Synthesis and pharmacological evaluation of novel beta-nitrostyrene derivatives as tyrosine kinase inhibitors with potent antiplatelet activity. Biochem Pharmacol. 2007 Aug 15;74(4):601-11. Epub 2007 Jun 3.
Ref 529039Biochem J. 2007 Dec 15;408(3):297-315.The selectivity of protein kinase inhibitors: a further update.
Ref 529217Bioorg Med Chem Lett. 2008 Feb 1;18(3):1207-11. Epub 2007 Dec 4.Discovery and SAR of 1,3,4-thiadiazole derivatives as potent Abl tyrosine kinase inhibitors and cytodifferentiating agents.
Ref 529744Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol. 2008 Nov;4(11):691-9.
Ref 530144The discovery of the potent aurora inhibitor MK-0457 (VX-680). Bioorg Med Chem Lett. 2009 Jul 1;19(13):3586-92.
Ref 530156J Med Chem. 2009 Jul 9;52(13):3915-26.Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc.
Ref 530244J Med Chem. 2009 Aug 13;52(15):4743-56.9-(Arenethenyl)purines as dual Src/Abl kinase inhibitors targeting the inactive conformation: design, synthesis, and biological evaluation.
Ref 530497Bioorg Med Chem Lett. 2009 Dec 15;19(24):6872-6. Epub 2009 Oct 23.Structure-activity relationships of 6-(2,6-dichlorophenyl)-8-methyl-2-(phenylamino)pyrido[2,3-d]pyrimidin-7-ones: toward selective Abl inhibitors.
Ref 531959The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2012 Aug 1;22(15):4979-85.
Ref 532902Discovery of type II inhibitors of TGFbeta-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2). J Med Chem. 2015 Jan 8;58(1):183-96.
Ref 534651J Med Chem. 1998 Jun 18;41(13):2252-60.Discovery of a novel series of potent and selective substrate-based inhibitors of p60c-src protein tyrosine kinase: conformational and topographical constraintsin peptide design.
Ref 534864A novel inhibitor of the tyrosine kinase Src suppresses phosphorylation of its major cellular substrates and reduces bone resorption in vitro and in rodent models in vivo. Bone. 1999 May;24(5):437-49.
Ref 534952Anti-angiogenic activity of selected receptor tyrosine kinase inhibitors, PD166285 and PD173074: implications for combination treatment with photodynamic therapy. Invest New Drugs. 1999;17(2):121-35.
Ref 535031Structure-based design of an osteoclast-selective, nonpeptide src homology 2 inhibitor with in vivo antiresorptive activity. Proc Natl Acad Sci U S A. 2000 Aug 15;97(17):9373-8.
Ref 536331Multi-target therapeutics: when the whole is greater than the sum of the parts. Drug Discov Today. 2007 Jan;12(1-2):34-42. Epub 2006 Nov 28.
Ref 536474A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
Ref 536797In vitro and clinical investigation of the relationship between CCR5 receptor occupancy and anti-HIV activity of Aplaviroc. J Clin Pharmacol. 2008 Oct;48(10):1179-88. Epub 2008 Aug 1.
Ref 537902In vivo antitumor activity of herbimycin A, a tyrosine kinase inhibitor, targeted against BCR/ABL oncoprotein in mice bearing BCR/ABL-transfected cells. Leuk Res. 1994 Nov;18(11):867-73.
Ref 543576(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2206).
Ref 551070Clinical pipeline report, company report or official report of Kinex Pharmaceuticals.
Ref 551322The Role of 4-phosphonodifluoromethyl- and 4-phosphono-phenylalanine in the selectivity and cellular uptake of SH2 domain ligands, Bioorg. Med. Chem. Lett. 7(14):1909-1914 (1997).
Ref 551374The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
Ref 551391DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Nucleic Acids Res. 2011 Jan;39(Database issue):D1035-4. Nucleic Acids Res. 2011 January
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
Ref 1587926URL: https://www.ebi.ac.uk/chembl/ The ChEMBL database in 2017

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