Target Information
| Target General Information | Top | |||||
|---|---|---|---|---|---|---|
| Target ID |
T59328
(Former ID: TTDS00355)
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| Target Name |
Epidermal growth factor receptor (EGFR)
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| Synonyms |
Receptor tyrosine-protein kinase erbB-1; Proto-oncogene c-ErbB-1; HER1; ERBB1; ERBB
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| Gene Name |
EGFR
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| Target Type |
Successful target
|
[1] | ||||
| Disease | [+] 9 Target-related Diseases | + | ||||
| 1 | Angina pectoris [ICD-11: BA40] | |||||
| 2 | Breast cancer [ICD-11: 2C60-2C6Y] | |||||
| 3 | Colorectal cancer [ICD-11: 2B91] | |||||
| 4 | Diabetic foot ulcer [ICD-11: BD54] | |||||
| 5 | Ischemia [ICD-11: 8B10-8B11] | |||||
| 6 | Lung cancer [ICD-11: 2C25] | |||||
| 7 | Renal cell carcinoma [ICD-11: 2C90] | |||||
| 8 | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||||
| 9 | Unspecific body region injury [ICD-11: ND56] | |||||
| 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).
Click to Show/Hide
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| BioChemical Class |
Kinase
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| UniProt ID | ||||||
| EC Number |
EC 2.7.10.1
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| Sequence |
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEV
VLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALA VLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDF QNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGC TGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYV VTDHGSCVRACGADSYEMEEDGVRKCKKCEGPCRKVCNGIGIGEFKDSLSINATNIKHFK NCTSISGDLHILPVAFRGDSFTHTPPLDPQELDILKTVKEITGFLLIQAWPENRTDLHAF ENLEIIRGRTKQHGQFSLAVVSLNITSLGLRSLKEISDGDVIISGNKNLCYANTINWKKL FGTSGQKTKIISNRGENSCKATGQVCHALCSPEGCWGPEPRDCVSCRNVSRGRECVDKCN LLEGEPREFVENSECIQCHPECLPQAMNITCTGRGPDNCIQCAHYIDGPHCVKTCPAGVM GENNTLVWKYADAGHVCHLCHPNCTYGCTGPGLEGCPTNGPKIPSIATGMVGALLLLLVV ALGIGLFMRRRHIVRKRTLRRLLQERELVEPLTPSGEAPNQALLRILKETEFKKIKVLGS GAFGTVYKGLWIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDNPHVCRLLGI CLTSTVQLITQLMPFGCLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAA RNVLVKTPQHVKITDFGLAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSY GVTVWELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPK FRELIIEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQ QGFFSSPSTSRTPLLSSLSATSNNSTVACIDRNGLQSCPIKEDSFLQRYSSDPTGALTED SIDDTFLPVPEYINQSVPKRPAGSVQNPVYHNQPLNPAPSRDPHYQDPHSTAVGNPEYLN TVQPTCVNSTFDSPAHWAQKGSHQISLDNPDYQQDFFPKEAKPNGIFKGSTAENAEYLRV APQSSEFIGA Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| ADReCS ID | BADD_A00924 ; BADD_A01146 ; BADD_A01626 ; BADD_A02005 ; BADD_A05675 ; BADD_A06535 | |||||
| HIT2.0 ID | T43N2D | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 18 Approved Drugs | + | ||||
| 1 | BIBW 2992 | Drug Info | Approved | Non-small-cell lung cancer | [2], [3] | |
| 2 | Cetuximab | Drug Info | Approved | Colorectal cancer | [4], [5] | |
| 3 | Dacomitinib | Drug Info | Approved | Non-small-cell lung cancer | [6] | |
| 4 | Epidermal growth factor | Drug Info | Approved | Vulnerary | [7] | |
| 5 | Erlotinib | Drug Info | Approved | Non-small-cell lung cancer | [5], [8] | |
| 6 | Gefitinib | Drug Info | Approved | Solid tumour/cancer | [9], [10] | |
| 7 | HEGF | Drug Info | Approved | Diabetic foot ulcer | [11] | |
| 8 | Lapatinib | Drug Info | Approved | Breast cancer | [12], [13] | |
| 9 | Merimepodib | Drug Info | Approved | Breast cancer | [14] | |
| 10 | Necitumumab | Drug Info | Approved | Colorectal cancer | [15], [16] | |
| 11 | NERATINIB MALEATE | Drug Info | Approved | HER2/NEU overexpressing breast cancer | [17] | |
| 12 | Nitroglycerin | Drug Info | Approved | Diabetic foot ulcer | [11] | |
| 13 | Osimertinib | Drug Info | Approved | Non-small-cell lung cancer | [18] | |
| 14 | Panitumumab | Drug Info | Approved | Colorectal cancer | [19], [20] | |
| 15 | SKI-758 | Drug Info | Approved | Ischemia | [7], [21] | |
| 16 | Sorafenib | Drug Info | Approved | Renal cell carcinoma | [22], [23] | |
| 17 | Vandetanib | Drug Info | Approved | Solid tumour/cancer | [24], [25] | |
| 18 | Icotinib hydrochloride | Drug Info | Registered | Non-small-cell lung cancer | [26], [27], [28] | |
| Clinical Trial Drug(s) | [+] 63 Clinical Trial Drugs | + | ||||
| 1 | Almonertinib | Drug Info | Phase 3 | Non-small-cell lung cancer | [29] | |
| 2 | Amivantamab | Drug Info | Phase 3 | Non-small-cell lung cancer | [30] | |
| 3 | ASP1929 | Drug Info | Phase 3 | Head and neck cancer | [31] | |
| 4 | Bevacizumab + Erlotinib | Drug Info | Phase 3 | Metastatic colorectal cancer | [32], [33] | |
| 5 | CO-1686 | Drug Info | Phase 3 | Lung cancer | [34] | |
| 6 | DE-766 | Drug Info | Phase 3 | Non-small-cell lung cancer | [35], [36] | |
| 7 | EGF816 | Drug Info | Phase 3 | Non-small-cell lung cancer | [37] | |
| 8 | HKI-272 | Drug Info | Phase 3 | Breast cancer | [38], [37] | |
| 9 | Rindopepimut | Drug Info | Phase 3 | Glioblastoma multiforme | [39] | |
| 10 | SYM-004 | Drug Info | Phase 3 | Metastatic colorectal cancer | [37] | |
| 11 | Zalutumumab | Drug Info | Phase 3 | Head and neck cancer | [40] | |
| 12 | Indium-111 | Drug Info | Phase 2/3 | Solid tumour/cancer | [41] | |
| 13 | Varlitinib | Drug Info | Phase 2/3 | Metastatic biliary tract neoplasms | [37] | |
| 14 | ABT-414 | Drug Info | Phase 2 | Glioblastoma multiforme | [42], [43] | |
| 15 | ASP8273 | Drug Info | Phase 2 | Non-small-cell lung cancer | [44] | |
| 16 | BMS-599626 | Drug Info | Phase 2 | Solid tumour/cancer | [45], [46] | |
| 17 | BMS-690514 | Drug Info | Phase 2 | Chronic pain | [47] | |
| 18 | CetuGEX | Drug Info | Phase 2 | Solid tumour/cancer | [48] | |
| 19 | CI-1033 | Drug Info | Phase 2 | Lymphoma | [49], [50] | |
| 20 | Depatuxizumab | Drug Info | Phase 2 | Glioblastoma of brain | [51] | |
| 21 | HER1-VSSP vaccine | Drug Info | Phase 2 | Solid tumour/cancer | [52], [53] | |
| 22 | HM-78136B | Drug Info | Phase 2 | Solid tumour/cancer | [54], [55] | |
| 23 | Matuzumab | Drug Info | Phase 2 | Gastric adenocarcinoma | [56] | |
| 24 | MEHD-7945A | Drug Info | Phase 2 | Colorectal cancer | [57], [58] | |
| 25 | Pazopanib + Tyverb/Tykerb | Drug Info | Phase 2 | Inflammatory breast cancer | [59] | |
| 26 | Pelitinib | Drug Info | Phase 2 | Lymphoma | [60], [61] | |
| 27 | RM-1929 | Drug Info | Phase 2 | Head and neck cancer | [37], [62] | |
| 28 | Tarloxotinib | Drug Info | Phase 2 | Non-small-cell lung cancer | [63] | |
| 29 | TT-100 | Drug Info | Phase 2 | Non-small-cell lung cancer | [64] | |
| 30 | VATALANIB | Drug Info | Phase 2 | Solid tumour/cancer | [65], [66] | |
| 31 | AFM24 | Drug Info | Phase 1/2 | Solid tumour/cancer | [67] | |
| 32 | BDTX-189 | Drug Info | Phase 1/2 | Solid tumour/cancer | [68] | |
| 33 | CART-EGFR | Drug Info | Phase 1/2 | Solid tumour/cancer | [69] | |
| 34 | EGFR CART | Drug Info | Phase 1/2 | Colorectal cancer | [70] | |
| 35 | EMB-01 | Drug Info | Phase 1/2 | Neoplasm | [71] | |
| 36 | EMD 55900 | Drug Info | Phase 1/2 | Glioma | [72] | |
| 37 | SN-32793 | Drug Info | Phase 1/2 | Non-small-cell lung cancer | [73] | |
| 38 | Sym013 | Drug Info | Phase 1/2 | Epithelial ovarian cancer | [37] | |
| 39 | Sym015 | Drug Info | Phase 1/2 | Solid tumour/cancer | [62], [37] | |
| 40 | ZN-e4 | Drug Info | Phase 1/2 | Non-small-cell lung cancer | [74] | |
| 41 | S-222611 | Drug Info | Phase 1b | Malignant solid tumour | [75] | |
| 42 | AMG 595 | Drug Info | Phase 1 | Glioblastoma multiforme | [76] | |
| 43 | Anti-EGFR CAR T | Drug Info | Phase 1 | Glioma | [77] | |
| 44 | Anti-HER3/EGFR DAF | Drug Info | Phase 1 | Metastatic epithelial tumour | [78] | |
| 45 | AP32788 | Drug Info | Phase 1 | Non-small-cell lung cancer | [37] | |
| 46 | AST-1306 | Drug Info | Phase 1 | Solid tumour/cancer | [79] | |
| 47 | BCA101 | Drug Info | Phase 1 | Solid tumour/cancer | [80] | |
| 48 | BIBX-1382 | Drug Info | Phase 1 | Chronic lymphocytic leukaemia | [81], [82] | |
| 49 | Cipatinib | Drug Info | Phase 1 | Solid tumour/cancer | [83] | |
| 50 | CLN-081 | Drug Info | Phase 1 | Non-small-cell lung cancer | [84] | |
| 51 | CUDC-101 | Drug Info | Phase 1 | Solid tumour/cancer | [85] | |
| 52 | D2C7 | Drug Info | Phase 1 | Glioblastoma of brain | [86] | |
| 53 | EGFR806-specific CAR T cell | Drug Info | Phase 1 | Atypical teratoid/rhabdoid tumour | [87] | |
| 54 | HER-2/HER-1 vaccine | Drug Info | Phase 1 | Solid tumour/cancer | [88] | |
| 55 | IMGN289 | Drug Info | Phase 1 | Solid tumour/cancer | [89] | |
| 56 | JNJ-26483327 | Drug Info | Phase 1 | Solid tumour/cancer | [90] | |
| 57 | LY3164530 | Drug Info | Phase 1 | Advanced cancer | [91] | |
| 58 | MCLA-158 | Drug Info | Phase 1 | Solid tumour/cancer | [92] | |
| 59 | MM-151 | Drug Info | Phase 1 | Solid tumour/cancer | [93] | |
| 60 | MR1-1 | Drug Info | Phase 1 | Brain cancer | [94] | |
| 61 | PF-05230907 | Drug Info | Phase 1 | Nontraumatic intracerebral hemorrhage | [95] | |
| 62 | SI-B001 | Drug Info | Phase 1 | Metastatic epithelial tumour | [96] | |
| 63 | SYN004 | Drug Info | Phase 1 | Solid tumour/cancer | [62], [37] | |
| Discontinued Drug(s) | [+] 8 Discontinued Drugs | + | ||||
| 1 | PKI166 | Drug Info | Discontinued in Phase 2 | Esophageal cancer | [97], [98] | |
| 2 | RG7160 | Drug Info | Discontinued in Phase 2 | Metastatic colorectal cancer | [99] | |
| 3 | AZD4769 | Drug Info | Discontinued in Phase 1 | Solid tumour/cancer | [100] | |
| 4 | PD-153035 | Drug Info | Discontinued in Phase 1 | Psoriasis vulgaris | [101] | |
| 5 | TAK165 | Drug Info | Discontinued in Phase 1 | Solid tumour/cancer | [102], [103] | |
| 6 | AZD-9935 | Drug Info | Terminated | Solid tumour/cancer | [107] | |
| 7 | CGP-52411 | Drug Info | Terminated | Solid tumour/cancer | [108] | |
| 8 | Heparin-EGF-like factor | Drug Info | Terminated | Gastrointestinal disease | [109], [110] | |
| Preclinical Drug(s) | [+] 2 Preclinical Drugs | + | ||||
| 1 | 111In-hEGF | Drug Info | Preclinical | Breast cancer | [104], [105] | |
| 2 | EGFR/IGFR tandem adnectin | Drug Info | Preclinical | Solid tumour/cancer | [106] | |
| Mode of Action | [+] 6 Modes of Action | + | ||||
| Inhibitor | [+] 127 Inhibitor drugs | + | ||||
| 1 | BIBW 2992 | Drug Info | [111] | |||
| 2 | Erlotinib | Drug Info | [115] | |||
| 3 | Gefitinib | Drug Info | [116], [117] | |||
| 4 | Lapatinib | Drug Info | [118], [119] | |||
| 5 | Merimepodib | Drug Info | [120] | |||
| 6 | Osimertinib | Drug Info | [122] | |||
| 7 | SKI-758 | Drug Info | [124] | |||
| 8 | Sorafenib | Drug Info | [125] | |||
| 9 | Vandetanib | Drug Info | [126], [127] | |||
| 10 | Almonertinib | Drug Info | [129] | |||
| 11 | Amivantamab | Drug Info | [130] | |||
| 12 | ASP1929 | Drug Info | [131] | |||
| 13 | Bevacizumab + Erlotinib | Drug Info | [132] | |||
| 14 | EGF816 | Drug Info | [134] | |||
| 15 | HKI-272 | Drug Info | [135] | |||
| 16 | ASP8273 | Drug Info | [141] | |||
| 17 | BMS-599626 | Drug Info | [142], [126] | |||
| 18 | BMS-690514 | Drug Info | [143] | |||
| 19 | CI-1033 | Drug Info | [126] | |||
| 20 | HM-78136B | Drug Info | [37], [144] | |||
| 21 | Pazopanib + Tyverb/Tykerb | Drug Info | [120] | |||
| 22 | Tarloxotinib | Drug Info | [148] | |||
| 23 | TT-100 | Drug Info | [149] | |||
| 24 | VATALANIB | Drug Info | [135] | |||
| 25 | BDTX-189 | Drug Info | [151] | |||
| 26 | EMB-01 | Drug Info | [152] | |||
| 27 | SN-32793 | Drug Info | [114] | |||
| 28 | ZN-e4 | Drug Info | [153] | |||
| 29 | S-222611 | Drug Info | [75] | |||
| 30 | AP32788 | Drug Info | [37] | |||
| 31 | BCA101 | Drug Info | [80] | |||
| 32 | CLN-081 | Drug Info | [160] | |||
| 33 | IMGN289 | Drug Info | [162] | |||
| 34 | JNJ-26483327 | Drug Info | [163] | |||
| 35 | MCLA-158 | Drug Info | [164] | |||
| 36 | PF-05230907 | Drug Info | [166] | |||
| 37 | SYN004 | Drug Info | [62] | |||
| 38 | Pyrrolo[2,3-d]pyrimidine derivative 24 | Drug Info | [168] | |||
| 39 | AZD4769 | Drug Info | [127] | |||
| 40 | TAK165 | Drug Info | [126] | |||
| 41 | EGFR/IGFR tandem adnectin | Drug Info | [173] | |||
| 42 | CGP-52411 | Drug Info | [175] | |||
| 43 | CGP-53353 | Drug Info | [176] | |||
| 44 | (3-Bromo-phenyl)-(5-nitro-quinazolin-4-yl)-amine | Drug Info | [177] | |||
| 45 | (3-Bromo-phenyl)-quinazolin-4-yl-amine | Drug Info | [178] | |||
| 46 | (E)-5-(4-Hydroxybenzylidene)-1-phenethylhydantoin | Drug Info | [179] | |||
| 47 | (S)-benzyl 4-chloro-3-oxobutan-2-ylcarbamate | Drug Info | [180] | |||
| 48 | 10-hydroxy-18-methoxybetaenone | Drug Info | [181] | |||
| 49 | 2-(4,5-Dihydroxy-indan-1-ylidene)-malononitrile | Drug Info | [182] | |||
| 50 | 2-(5,6-Dihydroxy-indan-1-ylidene)-malononitrile | Drug Info | [182] | |||
| 51 | 2-benzoyl-3-(3,4-dihydroxyphenyl)acrylonitrile | Drug Info | [180] | |||
| 52 | 2-cyano-3-(3,4-dihydroxyphenyl)acrylamide | Drug Info | [180] | |||
| 53 | 2-methoxy-4-(2-nitrovinyl)phenol | Drug Info | [180] | |||
| 54 | 3,4-di-(4-methoxyphenyl)-1H-pyrrole-2,5-dione | Drug Info | [183] | |||
| 55 | 3,4-diphenyl-1H-pyrrole-2,5-dione | Drug Info | [183] | |||
| 56 | 3-(3-Chloro-phenyl)-5,7-dihydroxy-chromen-4-one | Drug Info | [184] | |||
| 57 | 3-(4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione | Drug Info | [183] | |||
| 58 | 3-(indole-3-yl)-4-phenyl-1H-pyrrole-2,5-dione | Drug Info | [183] | |||
| 59 | 3-Pyridin-4-yl-quinoline-6,7-diol | Drug Info | [185] | |||
| 60 | 4-(2-nitroprop-1-enyl)benzene-1,2-diol | Drug Info | [180] | |||
| 61 | 4-(2-nitrovinyl)benzene-1,2-diol | Drug Info | [180] | |||
| 62 | 4-(2-nitrovinyl)phenol | Drug Info | [180] | |||
| 63 | 4-(3-Bromo-phenoxy)-6,7-dimethoxy-quinazoline | Drug Info | [186] | |||
| 64 | 4-(3-Bromo-phenoxy)-6,7-dimethoxy-quinoline | Drug Info | [186] | |||
| 65 | 4-(3-Bromo-phenylamino)-quinazoline-6,7-diol | Drug Info | [178] | |||
| 66 | 4-(4-(2-nitrovinyl)phenoxysulfonyl)benzoic acid | Drug Info | [180] | |||
| 67 | 4-(5-Bromoindole-3-yl)-6,7-dimethoxyquinazoline | Drug Info | [187] | |||
| 68 | 4-acrylamido-N-(3-bromophenyl)-2-hydroxybenzamide | Drug Info | [188] | |||
| 69 | 4-biphenyl-2-ylethynyl-6,7-dimethoxy-quinazoline | Drug Info | [189] | |||
| 70 | 4557W | Drug Info | [190] | |||
| 71 | 5,6-Bis-p-tolylamino-isoindole-1,3-dione | Drug Info | [176] | |||
| 72 | 5-acrylamido-N-(3-bromophenyl)-2-hydroxybenzamide | Drug Info | [188] | |||
| 73 | 6,7-diethoxy-4-(4-phenylbut-1-enyl)quinazoline | Drug Info | [189] | |||
| 74 | 6,7-diethoxy-4-(5-phenylpent-1-enyl)quinazoline | Drug Info | [189] | |||
| 75 | 6,7-diethoxy-4-styrylquinazoline | Drug Info | [189] | |||
| 76 | 6,7-dimethoxy-4-(2-phenylethynyl)quinazoline | Drug Info | [189] | |||
| 77 | 6,7-dimethoxy-4-(3-phenoxyprop-1-ynyl)quinazoline | Drug Info | [189] | |||
| 78 | 6,7-dimethoxy-4-(4-phenylbut-1-ynyl)quinazoline | Drug Info | [189] | |||
| 79 | 6,7-dimethoxy-N-m-tolylquinazolin-4-amine | Drug Info | [191] | |||
| 80 | 6-chloro-N-(3-chlorophenyl)quinazolin-4-amine | Drug Info | [192] | |||
| 81 | AG 112 | Drug Info | [193] | |||
| 82 | AG 9 | Drug Info | [193] | |||
| 83 | AG-213 | Drug Info | [187] | |||
| 84 | AG-538 | Drug Info | [180] | |||
| 85 | Benzo[g]quinazolin-4-yl-(3-bromo-phenyl)-amine | Drug Info | [178] | |||
| 86 | Benzyl-quinazolin-4-yl-amine | Drug Info | [177] | |||
| 87 | BPIQ-I | Drug Info | [178] | |||
| 88 | CL-387785 | Drug Info | [191] | |||
| 89 | Cochliobolic acid | Drug Info | [194] | |||
| 90 | EGFR inhibitor | Drug Info | [195] | |||
| 91 | Epitinib | Drug Info | [114] | |||
| 92 | HDS-029 | Drug Info | [196] | |||
| 93 | HKI-9924129 | Drug Info | [197] | |||
| 94 | HM-61713B | Drug Info | [114] | |||
| 95 | HTS-00213 | Drug Info | [191] | |||
| 96 | HTS-02876 | Drug Info | [191] | |||
| 97 | HTS-05058 | Drug Info | [195] | |||
| 98 | LAVENDUSTIN A | Drug Info | [198] | |||
| 99 | MDP-01 | Drug Info | [114] | |||
| 100 | MT-062 | Drug Info | [114] | |||
| 101 | N*4*-(3-Bromo-phenyl)-quinazoline-4,6,7-triamine | Drug Info | [178] | |||
| 102 | N*4*-(3-Bromo-phenyl)-quinazoline-4,6-diamine | Drug Info | [200] | |||
| 103 | N*4*-(3-Bromo-phenyl)-quinazoline-4,7-diamine | Drug Info | [177] | |||
| 104 | N*4*-Benzyl-pyrido[4,3-d]pyrimidine-4,7-diamine | Drug Info | [201] | |||
| 105 | N-(4-(phenylamino)quinazolin-6-yl)acrylamide | Drug Info | [202] | |||
| 106 | N-(4-m-Tolylamino-quinazolin-6-yl)-acrylamide | Drug Info | [203] | |||
| 107 | N-(4-m-Tolylamino-quinazolin-7-yl)-acrylamide | Drug Info | [203] | |||
| 108 | N4-(3-chlorophenyl)quinazoline-4,6-diamine | Drug Info | [204] | |||
| 109 | N4-(3-methylphenyl)-4,6-quinazolinediamine | Drug Info | [205] | |||
| 110 | NRC-2694 | Drug Info | [114] | |||
| 111 | ON-128 | Drug Info | [114] | |||
| 112 | OSI-75 | Drug Info | [206] | |||
| 113 | PD-0166326 | Drug Info | [197] | |||
| 114 | PD-0173956 | Drug Info | [197] | |||
| 115 | PD-158780 | Drug Info | [201] | |||
| 116 | PD-168393 | Drug Info | [202] | |||
| 117 | PD182905 | Drug Info | [207] | |||
| 118 | PMID24915291C38 | Drug Info | [209] | |||
| 119 | PMID8568816C56 | Drug Info | [210] | |||
| 120 | PP121 | Drug Info | [211] | |||
| 121 | RG-50810 | Drug Info | [180] | |||
| 122 | RM-6427 | Drug Info | [114] | |||
| 123 | Ro-4396686 | Drug Info | [212] | |||
| 124 | Theliatinib | Drug Info | [114] | |||
| 125 | Tyrphostin ag-1478 | Drug Info | [184] | |||
| 126 | WHI-P154 | Drug Info | [213] | |||
| 127 | WZ-3146 | Drug Info | [114] | |||
| Antagonist | [+] 13 Antagonist drugs | + | ||||
| 1 | Dacomitinib | Drug Info | [114] | |||
| 2 | NERATINIB MALEATE | Drug Info | [17] | |||
| 3 | Icotinib hydrochloride | Drug Info | [128] | |||
| 4 | Depatuxizumab | Drug Info | [62] | |||
| 5 | RM-1929 | Drug Info | [37] | |||
| 6 | Sym013 | Drug Info | [62], [37] | |||
| 7 | Sym015 | Drug Info | [62] | |||
| 8 | BIBX-1382 | Drug Info | [159] | |||
| 9 | MM-151 | Drug Info | [62] | |||
| 10 | AZD-9935 | Drug Info | [174] | |||
| 11 | EDP-13 | Drug Info | [114] | |||
| 12 | IPS-01003 | Drug Info | [114] | |||
| 13 | RX-1792 | Drug Info | [114] | |||
| Modulator | [+] 27 Modulator drugs | + | ||||
| 1 | Epidermal growth factor | Drug Info | [114] | |||
| 2 | Necitumumab | Drug Info | [121] | |||
| 3 | CO-1686 | Drug Info | [133] | |||
| 4 | DE-766 | Drug Info | [114] | |||
| 5 | Rindopepimut | Drug Info | [121] | |||
| 6 | Varlitinib | Drug Info | [138] | |||
| 7 | MEHD-7945A | Drug Info | [138], [146] | |||
| 8 | Pelitinib | Drug Info | [147] | |||
| 9 | AMG 595 | Drug Info | [154] | |||
| 10 | Anti-HER3/EGFR DAF | Drug Info | [155] | |||
| 11 | AST-1306 | Drug Info | [156], [157], [158] | |||
| 12 | Cipatinib | Drug Info | [138] | |||
| 13 | CUDC-101 | Drug Info | [85] | |||
| 14 | LY3164530 | Drug Info | [146] | |||
| 15 | MR1-1 | Drug Info | [165] | |||
| 16 | PKI166 | Drug Info | [169] | |||
| 17 | RG7160 | Drug Info | [170] | |||
| 18 | PD-153035 | Drug Info | [171] | |||
| 19 | 111In-hEGF | Drug Info | [172] | |||
| 20 | Heparin-EGF-like factor | Drug Info | [109], [110] | |||
| 21 | AGT-2000 | Drug Info | [114] | |||
| 22 | AL-6802 | Drug Info | [114] | |||
| 23 | LA22-radioimmunoconjugates | Drug Info | [114] | |||
| 24 | MG-111 | Drug Info | [199] | |||
| 25 | PF 5208766 | Drug Info | [208] | |||
| 26 | SYM-011 | Drug Info | [114] | |||
| 27 | TGF alpha | Drug Info | [114] | |||
| Activator | [+] 2 Activator drugs | + | ||||
| 1 | HEGF | Drug Info | [11] | |||
| 2 | Nitroglycerin | Drug Info | [11] | |||
| Suppressor | [+] 1 Suppressor drugs | + | ||||
| 1 | Panitumumab | Drug Info | [123] | |||
| CAR-T-Cell-Therapy | [+] 4 CAR-T-Cell-Therapy drugs | + | ||||
| 1 | CART-EGFR | Drug Info | [69] | |||
| 2 | EGFR CART | Drug Info | [70] | |||
| 3 | Anti-EGFR CAR T | Drug Info | [77] | |||
| 4 | EGFR806-specific CAR T cell | Drug Info | [87] | |||
| Chemical Structure based Activity Landscape of Target | Top |
|---|---|
| Drug Property Profile of Target | Top | |
|---|---|---|
| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
|
|
||
| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
|
|
||
| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
|
|
||
| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
|---|---|---|---|---|---|---|
| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
|---|---|---|---|---|---|---|
| Target-regulating microRNAs | ||||||
| Target-regulating Transcription Factors | ||||||
| Target-interacting Proteins | ||||||
| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| Drug Resistance Mutation (DRM) | ||||||
| Target-Related Models and Studies | Top | |||||
|---|---|---|---|---|---|---|
| Target Validation | ||||||
| Target QSAR Model | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Molecular inhibition of angiogenesis and metastatic potential in human squamous cell carcinomas after epidermal growth factor receptor blockade. Mol Cancer Ther. 2002 May;1(7):507-14. | |||||
| REF 2 | URL: 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: 5667). | |||||
| REF 3 | BIBW-2992, a dual receptor tyrosine kinase inhibitor for the treatment of solid tumors. Curr Opin Investig Drugs. 2008 Dec;9(12):1336-46. | |||||
| REF 4 | URL: 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: 6882). | |||||
| REF 5 | 2004 approvals: the demise of the blockbuster. Nat Rev Drug Discov. 2005 Feb;4(2):93-4. | |||||
| REF 6 | 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89. | |||||
| REF 7 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 8 | URL: 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: 4920). | |||||
| REF 9 | URL: 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: 4941). | |||||
| REF 10 | Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91. | |||||
| REF 11 | Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24. | |||||
| REF 12 | URL: 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: 5692). | |||||
| REF 13 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 022059. | |||||
| REF 14 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 022059. | |||||
| REF 15 | URL: 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: 8090). | |||||
| REF 16 | ClinicalTrials.gov (NCT00981058) First-line Treatment of Participants With Stage IV Squamous Non-Small Cell Lung Cancer With Necitumumab and Gemcitabine-Cisplatin. U.S. National Institutes of Health. | |||||
| REF 17 | 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85. | |||||
| REF 18 | The ChEMBL database in 2017. Nucleic Acids Res. 2017 Jan 4;45(D1):D945-D954. | |||||
| REF 19 | URL: 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: 6883). | |||||
| REF 20 | 2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101. | |||||
| REF 21 | Nat Rev Drug Discov. 2013 Feb;12(2):87-90. | |||||
| REF 22 | URL: 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: 5711). | |||||
| REF 23 | Sorafenib (BAY 43-9006, Nexavar), a dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature. Methods Enzymol. 2006;407:597-612. | |||||
| REF 24 | URL: 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: 5717). | |||||
| REF 25 | 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4. | |||||
| REF 26 | URL: 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: 7641). | |||||
| REF 27 | Clinical pipeline report, company report or official report of Beta Pharma. | |||||
| REF 28 | ClinicalTrials.gov (NCT02404675) High Dose Icotinib in Advanced Non-small Cell Lung Cancer Patients With EGFR 21 Exon Positive. U.S. National Institutes of Health. | |||||
| REF 29 | ClinicalTrials.gov (NCT04870190) Almonertinib Versus Osimertinib in the Patients With EGFR Mutations in Advanced NSCLC With Brain Metastases (ATTACK). U.S. National Institutes of Health. | |||||
| REF 30 | ClinicalTrials.gov (NCT04538664) A Study of Combination Amivantamab and Carboplatin-Pemetrexed Therapy, Compared With Carboplatin-Pemetrexed, in Participants With Advanced or Metastatic Non-Small Cell Lung Cancer Characterized by Epidermal Growth Factor Receptor (EGFR) Exon 20 Insertions (PAPILLON). U.S. National Institutes of Health. | |||||
| REF 31 | ClinicalTrials.gov (NCT03769506) ASP-1929 Photoimmunotherapy (PIT) Study in Recurrent Head/Neck Cancer for Patients Who Have Failed at Least Two Lines of Therapy. U.S. National Institutes of Health. | |||||
| REF 32 | ClinicalTrials.gov (NCT00130728) A Study to Evaluate the Efficacy of Bevacizumab in Combination With Tarceva for Advanced Non-Small Cell Lung Cancer | |||||
| REF 33 | ClinicalTrials.gov (NCT00598156) Chemotherapy and Avastin Followed by Maintenance Treatment With Avastin +/- Tarceva | |||||
| REF 34 | ClinicalTrials.gov (NCT02322281) TIGER-3: Open Label, Multicenter Study of Rociletinib (CO-1686) Mono Therapy Versus Single-agent Cytotoxic Chemotherapy in Patients With Mutant EGFR NSCLC Who Have Failed at Least One Previous EGFR-Directed TKI and Platinum-doublet Chemotherapy | |||||
| REF 35 | Clinical pipeline report, company report or official report of Daiichi Sankyo. | |||||
| REF 36 | Clinical pipeline report, company report or official report of Daiichi Sankyo. | |||||
| REF 37 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 38 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021154) | |||||
| REF 39 | ClinicalTrials.gov (NCT01480479) Phase III Study of Rindopepimut/GM-CSF in Patients With Newly Diagnosed Glioblastoma. U.S. National Institutes of Health. | |||||
| REF 40 | ClinicalTrials.gov (NCT00382031) Zalutumumab in Patients With Non-curable Head and Neck Cancer. U.S. National Institutes of Health. | |||||
| REF 41 | ClinicalTrials.gov (NCT00442533) Safety and Efficacy Study of In-111 Pentetreotide to Treat Neuroendocrine Tumors. U.S. National Institutes of Health. | |||||
| REF 42 | URL: 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: 7970). | |||||
| REF 43 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800035129) | |||||
| REF 44 | ClinicalTrials.gov (NCT02500927) A Study of ASP8273 in Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase Inhibitor-Naive Patients With Non-Small Cell Lung Cancer Harboring EGFR Mutations. | |||||
| REF 45 | URL: 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: 7647). | |||||
| REF 46 | ClinicalTrials.gov (NCT01614522) A Clinical Trial Evaluating the Effect of ASLAN001 in Patients With Recurrent/Metastatic Gastric Cancer Whose Tumors Are Either HER-2 Amplified or Co-expressing HER-1and HER-2. U.S. National Institutes of Health. | |||||
| REF 47 | A novel epidermal growth factor receptor inhibitor promotes apoptosis in non-small cell lung cancer cells resistant to erlotinib. Cancer Res. 2007 Jul 1;67(13):6253-62. | |||||
| REF 48 | Molecular mechanisms of resistance to the EGFR monoclonal antibody cetuximab. Cancer Biol Ther. 2011 May 1;11(9):777-92. | |||||
| REF 49 | URL: 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: 5675). | |||||
| REF 50 | Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions. J Med Chem. 2000 Apr 6;43(7):1380-97. | |||||
| REF 51 | ClinicalTrials.gov (NCT02343406) Adult Study: ABT-414 Alone or ABT-414 Plus Temozolomide vs. Lomustine or Temozolomide for Recurrent Glioblastoma Pediatric Study: Evaluation of ABT-414 in Children With High Grade Gliomas (INTELLANCE-2). U.S. National Institutes of Health. | |||||
| REF 52 | Active antimetastatic immunotherapy in Lewis lung carcinoma with self EGFR extracellular domain protein in VSSP adjuvant. Int J Cancer. 2006 Nov 1;119(9):2190-9. | |||||
| REF 53 | HER1-ECD vaccination dispenses with emulsification to elicit HER1-specific anti-proliferative effects. Hum Vaccin. 2009 Mar;5(3):158-65. | |||||
| REF 54 | URL: 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: 7903). | |||||
| REF 55 | ClinicalTrials.gov (NCT02216916) Phase II Trial of HM781-36B in Patients With Metastatic/Recurrent Head and Neck Squamous Cell Carcinoma (HNSCC) After Failure of or Unfit for Platinum-containing Therapy. U.S. National Institutes of Health. | |||||
| REF 56 | ClinicalTrials.gov (NCT00073541) A Study of the Safety and Effects of EMD 72000 in Subjects With Recurrent Ovarian Cancer. U.S. National Institutes of Health. | |||||
| REF 57 | ClinicalTrials.gov (NCT01577173) A Study of MEHD7945A Versus Cetuximab in Patients With Recurrent/Metastatic Squamous Cell Carcinoma of The Head And Neck | |||||
| REF 58 | ClinicalTrials.gov (NCT01652482) A Study of MEHD7945A + FOLFIRI Versus Cetuximab + FOLFIRI in Second Line in Patients With KRAS Wild-Type Metastatic Colorectal Cancer. U.S. National Institutes of Health. | |||||
| REF 59 | A randomized phase II study of lapatinib + pazopanib versus lapatinib in patients with HER2+ inflammatory breast cancer. Breast Cancer Res Treat. 2013 Jan;137(2):471-82. | |||||
| REF 60 | URL: 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: 7644). | |||||
| REF 61 | ClinicalTrials.gov (NCT00067548) Study Evaluating EKB-569 in Advanced Non-Small Cell Lung Cancer. U.S. National Institutes of Health. | |||||
| REF 62 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 63 | ClinicalTrials.gov (NCT02454842) Study for Treatment of Patients With EGFR Mutant, T790M-negative NSCLC (TH-4000). U.S. National Institutes of Health. | |||||
| REF 64 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021633) | |||||
| REF 65 | URL: 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: 5705). | |||||
| REF 66 | ClinicalTrials.gov (NCT00348790) Vatalanib in Treating Patients With Recurrent or Progressive Meningioma. U.S. National Institutes of Health. | |||||
| REF 67 | ClinicalTrials.gov (NCT04259450) Study to Assess AFM24 in Advanced Solid Cancers. U.S. National Institutes of Health. | |||||
| REF 68 | ClinicalTrials.gov (NCT04209465) A Study of BDTX-189, an Orally Available Allosteric ErbB Inhibitor, in Patients With Advanced Solid Tumors. (MasterKey-01). U.S. National Institutes of Health. | |||||
| REF 69 | ClinicalTrials.gov (NCT01869166) Treatment of Chemotherapy Refractory EGFR(Epidermal Growth Factor Receptor) Positive Advanced Solid Tumors (CART-EGFR) | |||||
| REF 70 | ClinicalTrials.gov (NCT03152435) EGFR CART Cells for Patients With Metastatic Colorectal Cancer | |||||
| REF 71 | ClinicalTrials.gov (NCT03797391) A Dose Escalation Study of EMB-01 in Participants With Advanced/Metastatic Solid Tumors. U.S. National Institutes of Health. | |||||
| REF 72 | Multiple infusions of anti-epidermal growth factor receptor (EGFR) monoclonal antibody (EMD 55,900) in patients with recurrent malignant gliomas. Eur J Cancer. 1996 Apr;32A(4):636-40. | |||||
| REF 73 | ClinicalTrials.gov (NCT01631279) A Dose Escalation Trial of PR610 Treating Patients With Solid Tumors. U.S. National Institutes of Health. | |||||
| REF 74 | ClinicalTrials.gov (NCT03446417) A Study of ZN-e4 in Subjects With Epidermal Growth Factor Receptor Mutated Non-Small Cell Lung Cancer. U.S. National Institutes of Health. | |||||
| REF 75 | Clinical pipeline report, company report or official report of Shionogi (2011). | |||||
| REF 76 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020588) | |||||
| REF 77 | ClinicalTrials.gov (NCT02331693) CAR T Cells in Treating Patients With Malignant Gliomas Overexpressing EGFR | |||||
| REF 78 | Clinical pipeline report, company report or official report of Genentech (2011). | |||||
| REF 79 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032292) | |||||
| REF 80 | ClinicalTrials.gov (NCT04429542) Study of Safety and Tolerability of BCA101 Alone and in Combination With Pembrolizumab in Patients With EGFR-driven Advanced Solid Tumors. U.S. National Institutes of Health. | |||||
| REF 81 | URL: 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: 7646). | |||||
| REF 82 | ClinicalTrials.gov (NCT00003980) BIBX 1382 in Treating Patients With Solid Tumors. U.S. National Institutes of Health. | |||||
| REF 83 | ClinicalTrials.gov (NCT01301911) Study of Cipatinib in Patients With HER2 Positive or Uncertain Advanced Breast Cancer. U.S. National Institutes of Health. | |||||
| REF 84 | ClinicalTrials.gov (NCT04036682) A Phase 1/2a Trial of CLN-081 in Patients With Non-Small Cell Lung Cancer. U.S. National Institutes of Health. | |||||
| REF 85 | A Phase I Study of CUDC-101, a Multitarget Inhibitor of HDACs, EGFR, and HER2, in Combination with Chemoradiation in Patients with Head and Neck Squamous Cell Carcinoma. Clin Cancer Res. 2015 Apr 1;21(7):1566-73. | |||||
| REF 86 | ClinicalTrials.gov (NCT02303678) D2C7 for Adult Patients With Recurrent Malignant Glioma. U.S. National Institutes of Health. | |||||
| REF 87 | ClinicalTrials.gov (NCT03638167) EGFR806-specific CAR T Cell Locoregional Immunotherapy for EGFR-positive Recurrent or Refractory Pediatric CNS Tumors | |||||
| REF 88 | Anti-Tumor Effects of Peptide Therapeutic and Peptide Vaccine Antibody Co-targeting HER-1 and HER-2 in Esophageal Cancer (EC) and HER-1 and IGF-1R in Triple-Negative Breast Cancer (TNBC). Vaccines (Basel). 2015 Jul 6;3(3):519-43. | |||||
| REF 89 | ClinicalTrials.gov (NCT01963715) A Phase 1 Study of IMGN289 in Adult Patients With EGFR-positive Solid Tumors. U.S. National Institutes of Health. | |||||
| REF 90 | ClinicalTrials.gov (NCT00676299) A Safety and Dose-finding Study of JNJ-26483327, a Drug in Development for Cancer, for Patients With Advanced and/or Refractory Solid Malignancies.. U.S. National Institutes of Health. | |||||
| REF 91 | ClinicalTrials.gov (NCT02221882) A Study of LY3164530 in Participants With Cancer | |||||
| REF 92 | ClinicalTrials.gov (NCT03526835) A Study of Bispecific Antibody MCLA-158 in Patients With Advanced Solid Tumors. U.S. National Institutes of Health. | |||||
| REF 93 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800035447) | |||||
| REF 94 | ClinicalTrials.gov (NCT01009866) Study of Immunotoxin, MR1-1. U.S. National Institutes of Health. | |||||
| REF 95 | ClinicalTrials.gov (NCT02537002) Single Dose Study of PF-05230907 in Healthy Japanese Subjects. | |||||
| REF 96 | ClinicalTrials.gov (NCT04603287) A Study of SI-B001, an EGFR/HER3 Bispecific Antibody, in Locally Advanced or Metastatic Epithelial Tumors. U.S. National Institutes of Health. | |||||
| REF 97 | URL: 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: 7642). | |||||
| REF 98 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013689) | |||||
| REF 99 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029052) | |||||
| REF 100 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024847) | |||||
| REF 101 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005268) | |||||
| REF 102 | URL: 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: 6011). | |||||
| REF 103 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019257) | |||||
| REF 104 | A comparison of non-biologically active truncated EGF (EGFt) and full-length hEGF for delivery of Auger electron-emitting 111In to EGFR-positive br... Nucl Med Biol. 2015 Dec;42(12):931-8. | |||||
| REF 105 | Preclinical pharmacokinetic, biodistribution, toxicology, and dosimetry studies of 111In-DTPA-human epidermal growth factor: an auger electron-emitting radiotherapeutic agent for epidermal growth factor receptor-positive breast cancer. J Nucl Med. 2006 Jun;47(6):1023-31. | |||||
| REF 106 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026610) | |||||
| REF 107 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018392) | |||||
| REF 108 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004971) | |||||
| REF 109 | The heparin-binding domain of heparin-binding EGF-like growth factor can target Pseudomonas exotoxin to kill cells exclusively through heparan sulfate proteoglycans. J Cell Sci. 1994 Sep;107 ( Pt 9):2599-608. | |||||
| REF 110 | Heparin-binding epidermal growth factor-like growth factor is an autocrine growth factor for human keratinocytes. J Biol Chem. 1994 Aug 5;269(31):20060-6. | |||||
| REF 111 | Boehringer Ingelheim. Product Development Pipeline. June 2 2009. | |||||
| REF 112 | Epidermal growth factor receptor-targeted therapy for pancreatic cancer. Semin Oncol. 2002 Oct;29(5 Suppl 14):31-7. | |||||
| REF 113 | Epidermal growth factor receptors as a target for cancer treatment: the emerging role of IMC-C225 in the treatment of lung and head and neck cancers. Semin Oncol. 2002 Feb;29(1 Suppl 4):27-36. | |||||
| REF 114 | URL: 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: 1797). | |||||
| REF 115 | Quantitative prediction of fold resistance for inhibitors of EGFR. Biochemistry. 2009 Sep 8;48(35):8435-48. | |||||
| REF 116 | Gefitinib ('Iressa', ZD1839) and new epidermal growth factor receptor inhibitors. Br J Cancer. 2004 Feb 9;90(3):566-72. | |||||
| REF 117 | Targeting' the epidermal growth factor receptor tyrosine kinase with gefitinib (Iressa) in non-small cell lung cancer (NSCLC). Semin Cancer Biol. 2004 Feb;14(1):33-40. | |||||
| REF 118 | Triple negative breast cancer--current status and prospective targeted treatment based on HER1 (EGFR), TOP2A and C-MYC gene assessment. Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2009 Mar;153(1):13-7. | |||||
| REF 119 | Multi-target therapeutics: when the whole is greater than the sum of the parts. Drug Discov Today. 2007 Jan;12(1-2):34-42. | |||||
| REF 120 | Clinical pipeline report, company report or official report of GlaxoSmithKline (2009). | |||||
| REF 121 | Rindopepimut, a 14-mer injectable peptide vaccine against EGFRvIII for the potential treatment of glioblastoma multiforme. Curr Opin Mol Ther. 2010 Dec;12(6):741-54. | |||||
| REF 122 | AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014 Sep;4(9):1046-61. | |||||
| REF 123 | Integration of panitumumab into the treatment of colorectal cancer. Crit Rev Oncol Hematol. 2010 Apr;74(1):16-26. | |||||
| REF 124 | Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles. J Med Chem. 2006 Dec 28;49(26):7868-76. | |||||
| REF 125 | Nasopharyngeal carcinoma: Current treatment options and future directions. J Nasopharyng Carcinoma, 2014, 1(16): e16. | |||||
| REF 126 | A 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 127 | Clinical pipeline report, company report or official report of AstraZeneca (2009). | |||||
| REF 128 | Phase I study of icotinib hydrochloride (BPI-2009H), an oral EGFR tyrosine kinase inhibitor, in patients with advanced NSCLC and other solid tumors. Lung Cancer. 2011 Aug;73(2):195-202. | |||||
| REF 129 | Safety, Efficacy, and Pharmacokinetics of Almonertinib (HS-10296) in Pretreated Patients With EGFR-Mutated Advanced NSCLC: A Multicenter, Open-label, Phase 1 Trial. J Thorac Oncol. 2020 Dec;15(12):1907-1918. | |||||
| REF 130 | Antitumor Activity of Amivantamab (JNJ-61186372), an EGFR-MET Bispecific Antibody, in Diverse Models of EGFR Exon 20 Insertion-Driven NSCLC. Cancer Discov. 2020 Aug;10(8):1194-1209. | |||||
| REF 131 | ClinicalTrials.gov (NCT04305795) An Open-label Study Using ASP-1929 Photoimmunotherapy in Combination With Anti-PD1 Therapy in EGFR Expressing Advanced Solid Tumors. U.S. National Institutes of Health. | |||||
| REF 132 | Clinical pipeline report, company report or official report of Roche (2009). | |||||
| REF 133 | Rociletinib in EGFR-mutated non-small-cell lung cancer. N Engl J Med. 2015 Apr 30;372(18):1700-9. | |||||
| REF 134 | Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC. Cancer Discov. 2013 Dec;3(12):1404-15. | |||||
| REF 135 | Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cyst... Bioorg Med Chem. 2007 Jun 1;15(11):3635-48. | |||||
| REF 136 | Sym004, a novel EGFR antibody mixture, can overcome acquired resistance to cetuximab. Neoplasia. 2013 Oct;15(10):1196-206. | |||||
| REF 137 | Characterization of ABT-806, a Humanized Tumor-Specific Anti-EGFR Monoclonal Antibody. Mol Cancer Ther. 2015 May;14(5):1141-51. | |||||
| REF 138 | Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41. | |||||
| REF 139 | Marine-Sourced Anti-Cancer and Cancer Pain Control Agents in Clinical and Late Preclinical Development. Mar Drugs. 2014 January; 12(1): 255-278. | |||||
| REF 140 | Monoclonal antibodies to target epidermal growth factor receptor-positive tumors: a new paradigm for cancer therapy. Cancer. 2002 Mar 1;94(5):1593-611. | |||||
| REF 141 | Phase I dose escalation study of ASP8273, a mutant-selective irreversible EGFR inhibitor, in subjects with EGFR mutation positive NSCLC, Journal of Clinical Oncology, Vol 33, No 15_suppl (May 20 Supplement), 2015: 8083. | |||||
| REF 142 | AC480, formerly BMS-599626, a pan Her inhibitor, enhances radiosensitivity and radioresponse of head and neck squamous cell carcinoma cells in vitro and in vivo. Invest New Drugs. 2011 Aug;29(4):554-61. | |||||
| REF 143 | Preclinical pharmacokinetics and in vitro metabolism of BMS-690514, a potent inhibitor of EGFR and VEGFR2. J Pharm Sci. 2010 Aug;99(8):3579-93. | |||||
| REF 144 | Antitumor activity of HM781-36B, a highly effective pan-HER inhibitor in erlotinib-resistant NSCLC and other EGFR-dependent cancer models. Int J Cancer. 2012 May 15;130(10):2445-54. | |||||
| REF 145 | Matuzumab binding to EGFR prevents the conformational rearrangement required for dimerization. Cancer Cell. 2008 Apr;13(4):365-73. | |||||
| REF 146 | Bispecific antibodies rise again. Nat Rev Drug Discov. 2014 Nov;13(11):799-801. | |||||
| REF 147 | EGFR tyrosine kinase inhibitor pelitinib regulates radiation-induced p65-dependent telomerase activation in squamous cell carcinoma.Radiat Res.2013 Mar;179(3):304-12. | |||||
| REF 148 | Tarloxotinib Is a Hypoxia-Activated Pan-HER Kinase Inhibitor Active Against a Broad Range of HER-Family Oncogenes. Clin Cancer Res. 2021 Mar 1;27(5):1463-1475. | |||||
| REF 149 | BiPar Sciences Co-founder Reunites Management Team At TriAct Therapeutics to Advance Clinical Stage Cancer Programs. TriAct Therapeutics. Sept. 10, 2009. | |||||
| REF 150 | Clinical pipeline report, company report or official report of Affimed Therapeutics. | |||||
| REF 151 | Clinical pipeline report, company report or official report of Black Diamond Therapeutics. | |||||
| REF 152 | Clinical pipeline report, company report or official report of EpimAb Biotherapeutics. | |||||
| REF 153 | Clinical pipeline report, company report or official report of Zentalis Pharmaceuticals. | |||||
| REF 154 | AMG 595, an Anti-EGFRvIII Antibody-Drug Conjugate, Induces Potent Antitumor Activity against EGFRvIII-Expressing Glioblastoma. Mol Cancer Ther. 2015 Jul;14(7):1614-24. | |||||
| REF 155 | Company report (Biooncology) | |||||
| REF 156 | AST1306, a novel irreversible inhibitor of the epidermal growth factor receptor 1 and 2, exhibits antitumor activity both in vitro and in vivo. PLoS One. 2011;6(7):e21487. | |||||
| REF 157 | Development and validation of a sensitive LC-MS/MS assay for the simultaneous quantification of allitinib and its two metabolites in human plasma.J Pharm Biomed Anal.2013 Dec;86:49-55. | |||||
| REF 158 | Metabolism and pharmacokinetics of allitinib in cancer patients: the roles of cytochrome P450s and epoxide hydrolase in its biotransformation.Drug Metab Dispos.2014 May;42(5):872-84. | |||||
| REF 159 | Phase I and pharmacokinetic study of BIBX 1382 BS, an epidermal growth factor receptor (EGFR) inhibitor, given in a continuous daily oral administration. Eur J Cancer. 2002 May;38(8):1072-80. | |||||
| REF 160 | TAS6417, A Novel EGFR Inhibitor Targeting Exon 20 Insertion Mutations. Mol Cancer Ther. 2018 Aug;17(8):1648-1658. | |||||
| REF 161 | Improved efficacy against malignant brain tumors with EGFRwt/EGFRvIII targeting immunotoxin and checkpoint inhibitor combinations. J Immunother Cancer. 2019 May 29;7(1):142. | |||||
| REF 162 | World Antibody-Drug Conjugate Summit, October 15-16, 2013, San Francisco, CA. MAbs. 2014 January 1; 6(1): 18-29. | |||||
| REF 163 | National Cancer Institute Drug Dictionary (drug id 596693). | |||||
| REF 164 | Clinical pipeline report, company report or official report of Merus. | |||||
| REF 165 | A Phase I Study of Immunotoxin, MR1-1. Duke University report. | |||||
| REF 166 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 167 | Clinical pipeline report, company report or official report of SystImmune. | |||||
| REF 168 | Pyrrolo[2,3-d]pyrimidines active as Btk inhibitors.Expert Opin Ther Pat. 2017 Dec;27(12):1305-1318. | |||||
| REF 169 | Epidermal growth factor receptor inhibitor PKI-166 governs cardiovascular protection without beneficial effects on the kidney in hypertensive 5/6 nephrectomized rats.J Pharmacol Exp Ther.2013 Jun;345(3):393-403. | |||||
| REF 170 | GA201 (RG7160): a novel, humanized, glycoengineered anti-EGFR antibody with enhanced ADCC and superior in vivo efficacy compared with cetuximab. Clin Cancer Res. 2013 Mar 1;19(5):1126-38. | |||||
| REF 171 | EGFR tyrosine kinase inhibitor (PD153035) improves glucose tolerance and insulin action in high-fat diet-fed mice.Diabetes.2009 Dec;58(12):2910-9. | |||||
| REF 172 | A comparison of EGF and MAb 528 labeled with 111In for imaging human breast cancer. J Nucl Med. 2000 May;41(5):903-11. | |||||
| REF 173 | Clinical pipeline report, company report or official report of Bristol-Myers Squibb. | |||||
| REF 174 | WO patent application no. 2009,0582,67, Benzomorpholine derivatives and methods of use. | |||||
| REF 175 | Retinoic acid-induced RB (retinoblastoma) hypophosphorylation enhanced by CGP 52411 (4,5-dianilinophthalimide), an EGF family tyrosine kinase receptor inhibitor. Eur J Cell Biol. 1996 Apr;69(4):327-34. | |||||
| REF 176 | Dianilinophthalimides: potent and selective, ATP-competitive inhibitors of the EGF-receptor protein tyrosine kinase. J Med Chem. 1994 Apr 1;37(7):1015-27. | |||||
| REF 177 | Tyrosine kinase inhibitors. 5. Synthesis and structure-activity relationships for 4-[(phenylmethyl)amino]- and 4-(phenylamino)quinazolines as poten... J Med Chem. 1995 Sep 1;38(18):3482-7. | |||||
| REF 178 | Tyrosine kinase inhibitors. 9. Synthesis and evaluation of fused tricyclic quinazoline analogues as ATP site inhibitors of the tyrosine kinase acti... J Med Chem. 1996 Feb 16;39(4):918-28. | |||||
| REF 179 | 5-Benzylidene-hydantoins: synthesis and antiproliferative activity on A549 lung cancer cell line. Eur J Med Chem. 2009 Sep;44(9):3471-9. | |||||
| REF 180 | Protein-tyrosine kinase inhibition: mechanism-based discovery of antitumor agents. J Nat Prod. 1992 Nov;55(11):1529-60. | |||||
| REF 181 | Anthraquinones and betaenone derivatives from the sponge-associated fungus Microsphaeropsis species: novel inhibitors of protein kinases. J Nat Prod. 2000 Jun;63(6):739-45. | |||||
| REF 182 | Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine... J Med Chem. 1991 Jun;34(6):1896-907. | |||||
| REF 183 | Design, synthesis, and biological evaluation of 3,4-diarylmaleimides as angiogenesis inhibitors. J Med Chem. 2006 Feb 23;49(4):1271-81. | |||||
| REF 184 | Use of a pharmacophore model for the design of EGFR tyrosine kinase inhibitors: isoflavones and 3-phenyl-4(1H)-quinolones. J Med Chem. 1999 Mar 25;42(6):1018-26. | |||||
| REF 185 | 5,7-Dimethoxy-3-(4-pyridinyl)quinoline is a potent and selective inhibitor of human vascular beta-type platelet-derived growth factor receptor tyro... J Med Chem. 1994 Aug 19;37(17):2627-9. | |||||
| REF 186 | A novel series of 4-phenoxyquinolines: potent and highly selective inhibitors of PDGF receptor autophosphorylation, Bioorg. Med. Chem. Lett. 7(23):2935-2940 (1997). | |||||
| REF 187 | Syntheses of 4-(indole-3-yl)quinazolines: a new class of epidermal growth factor receptor tyrosine kinase inhibitors. Eur J Med Chem. 2008 Jul;43(7):1478-88. | |||||
| REF 188 | Acryloylamino-salicylanilides as EGFR PTK inhibitors. Bioorg Med Chem Lett. 2006 Jan 15;16(2):469-72. | |||||
| REF 189 | Synthesis and inhibitory activity of 4-alkynyl and 4-alkenylquinazolines: identification of new scaffolds for potent EGFR tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5863-7. | |||||
| REF 190 | Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2. Bioorg Med Chem Lett. 2001 Jun 4;11(11):1401-5. | |||||
| REF 191 | Computational studies of epidermal growth factor receptor: docking reliability, three-dimensional quantitative structure-activity relationship anal... J Med Chem. 2009 Feb 26;52(4):964-75. | |||||
| REF 192 | Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6623-6. | |||||
| REF 193 | Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors. J Med Chem. 1989 Oct;32(10):2344-52. | |||||
| REF 194 | Cochliobolic acid, a novel metabolite produced by Cochliobolus lunatus, inhibits binding of TGF-alpha to the EGF receptor in a SPA assay. J Nat Prod. 1997 Jan;60(1):6-8. | |||||
| REF 195 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proc Natl Acad Sci U S A. 2007 Dec 18;104(51):20523-8. | |||||
| REF 196 | Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB... J Med Chem. 2006 Feb 23;49(4):1475-85. | |||||
| REF 197 | Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors. Biochem Pharmacol. 2000 Oct 1;60(7):885-98. | |||||
| REF 198 | Novel antiproliferative agents derived from lavendustin A. J Med Chem. 1994 Nov 25;37(24):4079-84. | |||||
| REF 199 | Effects of hEGF (MG111) on gastric mucosal potential difference in rats. Scand J Gastroenterol Suppl. 1989;162:198-201. | |||||
| REF 200 | Synthesis of a prodrug designed to release multiple inhibitors of the epidermal growth factor receptor tyrosine kinase and an alkylating agent: a n... J Med Chem. 2003 Dec 4;46(25):5546-51. | |||||
| REF 201 | Tyrosine kinase inhibitors. 10. Isomeric 4-[(3-bromophenyl)amino]pyrido[d]-pyrimidines are potent ATP binding site inhibitors of the tyrosine kinas... J Med Chem. 1996 Apr 26;39(9):1823-35. | |||||
| REF 202 | Structure-guided development of affinity probes for tyrosine kinases using chemical genetics. Nat Chem Biol. 2007 Apr;3(4):229-38. | |||||
| REF 203 | Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP... J Med Chem. 1999 May 20;42(10):1803-15. | |||||
| REF 204 | Novel nitrogen mustard-armed combi-molecules for the selective targeting of epidermal growth factor receptor overexperessing solid tumors: discover... J Med Chem. 2007 May 31;50(11):2605-8. | |||||
| REF 205 | The combi-targeting concept: synthesis of stable nitrosoureas designed to inhibit the epidermal growth factor receptor (EGFR). J Med Chem. 2006 Jun 15;49(12):3544-52. | |||||
| REF 206 | Selected novel anticancer treatments targeting cell signaling proteins. Oncologist. 2001;6(6):517-37. | |||||
| REF 207 | Growth factors and their receptors: new targets for prostate cancer therapy. Urology. 2001 Aug;58(2 Suppl 1):114-22. | |||||
| REF 208 | Optimization of 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor... J Med Chem. 2005 Feb 24;48(4):1107-31. | |||||
| REF 209 | Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity. J Med Chem. 2014 Jun 26;57(12):5112-28. | |||||
| REF 210 | Tyrosine kinase inhibitors. 8. An unusually steep structure-activity relationship for analogues of 4-(3-bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a potent inhibitor of the epidermal growth factor receptor. J Med Chem. 1996 Jan 5;39(1):267-76. | |||||
| REF 211 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol. 2008 Nov;4(11):691-9. | |||||
| REF 212 | Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1950-3. | |||||
| REF 213 | The specificity of JAK3 kinase inhibitors. Blood. 2008 Feb 15;111(4):2155-7. | |||||
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