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
Click to Show/Hide
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| Gene Name |
EGFR
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 10 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 | Non-small-cell lung cancer [ICD-11: 2C25] | |||||
| 8 | Renal cell carcinoma [ICD-11: 2C90] | |||||
| 9 | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||||
| 10 | 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).
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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) | [+] 19 Approved Drugs | + | ||||
| 1 | Amivantamab | Drug Info | Approved | Non-small-cell lung cancer | [2] | |
| 2 | BIBW 2992 | Drug Info | Approved | Non-small-cell lung cancer | [3], [4] | |
| 3 | Cetuximab | Drug Info | Approved | Colorectal cancer | [5], [6] | |
| 4 | Dacomitinib | Drug Info | Approved | Non-small-cell lung cancer | [7] | |
| 5 | Epidermal growth factor | Drug Info | Approved | Vulnerary | [8] | |
| 6 | Erlotinib | Drug Info | Approved | Non-small-cell lung cancer | [6], [9] | |
| 7 | Gefitinib | Drug Info | Approved | Solid tumour/cancer | [10], [11] | |
| 8 | HEGF | Drug Info | Approved | Diabetic foot ulcer | [12] | |
| 9 | Lapatinib | Drug Info | Approved | Breast cancer | [13], [14] | |
| 10 | Merimepodib | Drug Info | Approved | Breast cancer | [15] | |
| 11 | Necitumumab | Drug Info | Approved | Colorectal cancer | [16], [17] | |
| 12 | NERATINIB MALEATE | Drug Info | Approved | HER2/NEU overexpressing breast cancer | [18] | |
| 13 | Nitroglycerin | Drug Info | Approved | Diabetic foot ulcer | [12] | |
| 14 | Osimertinib | Drug Info | Approved | Non-small-cell lung cancer | [19] | |
| 15 | Panitumumab | Drug Info | Approved | Colorectal cancer | [20], [21] | |
| 16 | SKI-758 | Drug Info | Approved | Ischemia | [8], [22] | |
| 17 | Sorafenib | Drug Info | Approved | Renal cell carcinoma | [23], [24] | |
| 18 | Vandetanib | Drug Info | Approved | Solid tumour/cancer | [25], [26] | |
| 19 | Icotinib hydrochloride | Drug Info | Registered | Non-small-cell lung cancer | [27], [28], [29] | |
| Clinical Trial Drug(s) | [+] 62 Clinical Trial Drugs | + | ||||
| 1 | Almonertinib | Drug Info | Phase 3 | Non-small-cell lung cancer | [30] | |
| 2 | ASP1929 | Drug Info | Phase 3 | Head and neck cancer | [31] | |
| 3 | Bevacizumab + Erlotinib | Drug Info | Phase 3 | Metastatic colorectal cancer | [32], [33] | |
| 4 | CO-1686 | Drug Info | Phase 3 | Lung cancer | [34] | |
| 5 | DE-766 | Drug Info | Phase 3 | Non-small-cell lung cancer | [35], [36] | |
| 6 | EGF816 | Drug Info | Phase 3 | Non-small-cell lung cancer | [37] | |
| 7 | HKI-272 | Drug Info | Phase 3 | Breast cancer | [38], [37] | |
| 8 | Rindopepimut | Drug Info | Phase 3 | Glioblastoma multiforme | [39] | |
| 9 | SYM-004 | Drug Info | Phase 3 | Metastatic colorectal cancer | [37] | |
| 10 | Zalutumumab | Drug Info | Phase 3 | Head and neck cancer | [40] | |
| 11 | Indium-111 | Drug Info | Phase 2/3 | Solid tumour/cancer | [41] | |
| 12 | Varlitinib | Drug Info | Phase 2/3 | Metastatic biliary tract neoplasms | [37] | |
| 13 | ABT-414 | Drug Info | Phase 2 | Glioblastoma multiforme | [42], [43] | |
| 14 | ASP8273 | Drug Info | Phase 2 | Non-small-cell lung cancer | [44] | |
| 15 | BMS-599626 | Drug Info | Phase 2 | Solid tumour/cancer | [45], [46] | |
| 16 | BMS-690514 | Drug Info | Phase 2 | Chronic pain | [47] | |
| 17 | CetuGEX | Drug Info | Phase 2 | Solid tumour/cancer | [48] | |
| 18 | CI-1033 | Drug Info | Phase 2 | Lymphoma | [49], [50] | |
| 19 | Depatuxizumab | Drug Info | Phase 2 | Glioblastoma of brain | [51] | |
| 20 | HER1-VSSP vaccine | Drug Info | Phase 2 | Solid tumour/cancer | [52], [53] | |
| 21 | HM-78136B | Drug Info | Phase 2 | Solid tumour/cancer | [54], [55] | |
| 22 | Matuzumab | Drug Info | Phase 2 | Gastric adenocarcinoma | [56] | |
| 23 | MEHD-7945A | Drug Info | Phase 2 | Colorectal cancer | [57], [58] | |
| 24 | Pazopanib + Tyverb/Tykerb | Drug Info | Phase 2 | Inflammatory breast cancer | [59] | |
| 25 | Pelitinib | Drug Info | Phase 2 | Lymphoma | [60], [61] | |
| 26 | RM-1929 | Drug Info | Phase 2 | Head and neck cancer | [37], [62] | |
| 27 | Tarloxotinib | Drug Info | Phase 2 | Non-small-cell lung cancer | [63] | |
| 28 | TT-100 | Drug Info | Phase 2 | Non-small-cell lung cancer | [64] | |
| 29 | VATALANIB | Drug Info | Phase 2 | Solid tumour/cancer | [65], [66] | |
| 30 | AFM24 | Drug Info | Phase 1/2 | Solid tumour/cancer | [67] | |
| 31 | BDTX-189 | Drug Info | Phase 1/2 | Solid tumour/cancer | [68] | |
| 32 | CART-EGFR | Drug Info | Phase 1/2 | Solid tumour/cancer | [69] | |
| 33 | EGFR CART | Drug Info | Phase 1/2 | Colorectal cancer | [70] | |
| 34 | EMB-01 | Drug Info | Phase 1/2 | Neoplasm | [71] | |
| 35 | EMD 55900 | Drug Info | Phase 1/2 | Glioma | [72] | |
| 36 | SN-32793 | Drug Info | Phase 1/2 | Non-small-cell lung cancer | [73] | |
| 37 | Sym013 | Drug Info | Phase 1/2 | Epithelial ovarian cancer | [37] | |
| 38 | Sym015 | Drug Info | Phase 1/2 | Solid tumour/cancer | [62], [37] | |
| 39 | ZN-e4 | Drug Info | Phase 1/2 | Non-small-cell lung cancer | [74] | |
| 40 | S-222611 | Drug Info | Phase 1b | Malignant solid tumour | [75] | |
| 41 | AMG 595 | Drug Info | Phase 1 | Glioblastoma multiforme | [76] | |
| 42 | Anti-EGFR CAR T | Drug Info | Phase 1 | Glioma | [77] | |
| 43 | Anti-HER3/EGFR DAF | Drug Info | Phase 1 | Metastatic epithelial tumour | [78] | |
| 44 | AP32788 | Drug Info | Phase 1 | Non-small-cell lung cancer | [37] | |
| 45 | AST-1306 | Drug Info | Phase 1 | Solid tumour/cancer | [79] | |
| 46 | BCA101 | Drug Info | Phase 1 | Solid tumour/cancer | [80] | |
| 47 | BIBX-1382 | Drug Info | Phase 1 | Chronic lymphocytic leukaemia | [81], [82] | |
| 48 | Cipatinib | Drug Info | Phase 1 | Solid tumour/cancer | [83] | |
| 49 | CLN-081 | Drug Info | Phase 1 | Non-small-cell lung cancer | [84] | |
| 50 | CUDC-101 | Drug Info | Phase 1 | Solid tumour/cancer | [85] | |
| 51 | D2C7 | Drug Info | Phase 1 | Glioblastoma of brain | [86] | |
| 52 | EGFR806-specific CAR T cell | Drug Info | Phase 1 | Atypical teratoid/rhabdoid tumour | [87] | |
| 53 | HER-2/HER-1 vaccine | Drug Info | Phase 1 | Solid tumour/cancer | [88] | |
| 54 | IMGN289 | Drug Info | Phase 1 | Solid tumour/cancer | [89] | |
| 55 | JNJ-26483327 | Drug Info | Phase 1 | Solid tumour/cancer | [90] | |
| 56 | LY3164530 | Drug Info | Phase 1 | Advanced cancer | [91] | |
| 57 | MCLA-158 | Drug Info | Phase 1 | Solid tumour/cancer | [92] | |
| 58 | MM-151 | Drug Info | Phase 1 | Solid tumour/cancer | [93] | |
| 59 | MR1-1 | Drug Info | Phase 1 | Brain cancer | [94] | |
| 60 | PF-05230907 | Drug Info | Phase 1 | Nontraumatic intracerebral hemorrhage | [95] | |
| 61 | SI-B001 | Drug Info | Phase 1 | Metastatic epithelial tumour | [96] | |
| 62 | 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 | Amivantamab | Drug Info | [111] | |||
| 2 | BIBW 2992 | Drug Info | [112] | |||
| 3 | Erlotinib | Drug Info | [116] | |||
| 4 | Gefitinib | Drug Info | [117], [118] | |||
| 5 | Lapatinib | Drug Info | [119], [120] | |||
| 6 | Merimepodib | Drug Info | [121] | |||
| 7 | Osimertinib | Drug Info | [123] | |||
| 8 | SKI-758 | Drug Info | [125] | |||
| 9 | Sorafenib | Drug Info | [126] | |||
| 10 | Vandetanib | Drug Info | [127], [128] | |||
| 11 | Almonertinib | 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], [127] | |||
| 18 | BMS-690514 | Drug Info | [143] | |||
| 19 | CI-1033 | Drug Info | [127] | |||
| 20 | HM-78136B | Drug Info | [37], [144] | |||
| 21 | Pazopanib + Tyverb/Tykerb | Drug Info | [121] | |||
| 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 | [115] | |||
| 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 | [128] | |||
| 40 | TAK165 | Drug Info | [127] | |||
| 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 | [115] | |||
| 92 | HDS-029 | Drug Info | [196] | |||
| 93 | HKI-9924129 | Drug Info | [197] | |||
| 94 | HM-61713B | Drug Info | [115] | |||
| 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 | [115] | |||
| 100 | MT-062 | Drug Info | [115] | |||
| 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 | [115] | |||
| 111 | ON-128 | Drug Info | [115] | |||
| 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 | [115] | |||
| 123 | Ro-4396686 | Drug Info | [212] | |||
| 124 | Theliatinib | Drug Info | [115] | |||
| 125 | Tyrphostin ag-1478 | Drug Info | [184] | |||
| 126 | WHI-P154 | Drug Info | [213] | |||
| 127 | WZ-3146 | Drug Info | [115] | |||
| Antagonist | [+] 13 Antagonist drugs | + | ||||
| 1 | Dacomitinib | Drug Info | [115] | |||
| 2 | NERATINIB MALEATE | Drug Info | [18] | |||
| 3 | Icotinib hydrochloride | Drug Info | [129] | |||
| 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 | [115] | |||
| 12 | IPS-01003 | Drug Info | [115] | |||
| 13 | RX-1792 | Drug Info | [115] | |||
| Modulator | [+] 27 Modulator drugs | + | ||||
| 1 | Epidermal growth factor | Drug Info | [115] | |||
| 2 | Necitumumab | Drug Info | [122] | |||
| 3 | CO-1686 | Drug Info | [133] | |||
| 4 | DE-766 | Drug Info | [115] | |||
| 5 | Rindopepimut | Drug Info | [122] | |||
| 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 | [115] | |||
| 22 | AL-6802 | Drug Info | [115] | |||
| 23 | LA22-radioimmunoconjugates | Drug Info | [115] | |||
| 24 | MG-111 | Drug Info | [199] | |||
| 25 | PF 5208766 | Drug Info | [208] | |||
| 26 | SYM-011 | Drug Info | [115] | |||
| 27 | TGF alpha | Drug Info | [115] | |||
| Activator | [+] 2 Activator drugs | + | ||||
| 1 | HEGF | Drug Info | [12] | |||
| 2 | Nitroglycerin | Drug Info | [12] | |||
| Suppressor | [+] 1 Suppressor drugs | + | ||||
| 1 | Panitumumab | Drug Info | [124] | |||
| 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] | |||
| Cell-based Target Expression Variations | Top | |||||
|---|---|---|---|---|---|---|
| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: Lapatinib | Ligand Info | |||||
| Structure Description | EGFR kinase domain complexed with a quinazoline inhibitor- GW572016 | PDB:1XKK | ||||
| Method | X-ray diffraction | Resolution | 2.40 Å | Mutation | No | [214] |
| PDB Sequence |
ALLRILKETE
711 FKKIKVLGSG721 AFGTVYKGLW731 IPVKIPVAIK745 ELREKANKEI759 LDEAYVMASV 769 DNPHVCRLLG779 ICLTSTVQLI789 TQLMPFGCLL799 DYVREHKDNI809 GSQYLLNWCV 819 QIAKGMNYLE829 DRRLVHRDLA839 ARNVLVKTPQ849 HVKITDFGLA859 KLLGAEEKVP 877 IKWMALESIL887 HRIYTHQSDV897 WSYGVTVWEL907 MTFGSKPYDG917 IPASEISSIL 927 EKGERLPQPP937 ICTIDVYMIM947 VKCWMIDADS957 RPKFRELIIE967 FSKMARDPQR 977 YLVIQGDERM987 SNFYRALMDE1004 VVDADEYLI
|
|||||
|
|
LEU718
3.870
GLY719
4.124
VAL726
3.854
ALA743
3.334
ILE744
4.349
LYS745
3.414
MET766
3.317
CYS775
3.424
ARG776
3.123
LEU777
3.371
LEU788
3.100
ILE789
4.160
THR790
3.138
GLN791
3.195
|
|||||
| Ligand Name: Brigatinib | Ligand Info | |||||
| Structure Description | Studies Towards a Reversible EGFR C797S Triple Mutant Inhibitor Series | PDB:7AEM | ||||
| Method | X-ray diffraction | Resolution | 2.65 Å | Mutation | No | [215] |
| PDB Sequence |
SGEAPNQALL
704 RILKETEFKK714 IKVLGSGAFG724 TVYKGLWIPE734 GEKVKIPVAI744 KELATSPKAN 756 KEILDEAYVM766 ASVDNPHVCR776 LLGICLTSTV786 QLITQLMPFG796 CLLDYVREHK 806 DNIGSQYLLN816 WCVQIAKGMN826 YLEDRRLVHR836 DLAARNVLVK846 TPQHVKITDF 856 GLAKLLGAEE866 KEYHAEGGKV876 PIKWMALESI886 LHRIYTHQSD896 VWSYGVTVWE 906 LMTFGSKPYD916 GIPASEISSI926 LEKGERLPQP936 PICTIDVYMI946 MVKCWMIDAD 956 SRPKFRELII966 EFSKMARDPQ976 RYLVIQGDER986 MHLPLMDEED1006 MDDVVDADEY 1016 LI
|
|||||
|
|
LEU718
3.663
GLY719
3.649
PHE723
3.562
VAL726
3.766
ALA743
3.266
LYS745
4.226
THR790
3.893
GLN791
3.498
LEU792
3.620
MET793
2.921
PRO794
3.438
|
|||||
| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
|---|---|
|
Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Tissue Distribution
of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.
The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects
(Nat Rev Drug Discov, 20: 64-81, 2021).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Tissue Distribution
Human Pathway Affiliation
Biological Network Descriptors
|
|
|
Note:
If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.
|
| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
|---|---|---|---|
| MAPK signaling pathway | hsa04010 | Affiliated Target |
|
| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| ErbB signaling pathway | hsa04012 | Affiliated Target |
|
| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| Ras signaling pathway | hsa04014 | Affiliated Target |
|
| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| Rap1 signaling pathway | hsa04015 | Affiliated Target |
|
| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| Calcium signaling pathway | hsa04020 | Affiliated Target |
|
| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| HIF-1 signaling pathway | hsa04066 | Affiliated Target |
|
| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| FoxO signaling pathway | hsa04068 | Affiliated Target |
|
| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| Phospholipase D signaling pathway | hsa04072 | Affiliated Target |
|
| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| Endocytosis | hsa04144 | Affiliated Target |
|
| Class: Cellular Processes => Transport and catabolism | Pathway Hierarchy | ||
| PI3K-Akt signaling pathway | hsa04151 | Affiliated Target |
|
| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| Focal adhesion | hsa04510 | Affiliated Target |
|
| Class: Cellular Processes => Cellular community - eukaryotes | Pathway Hierarchy | ||
| Adherens junction | hsa04520 | Affiliated Target |
|
| Class: Cellular Processes => Cellular community - eukaryotes | Pathway Hierarchy | ||
| Gap junction | hsa04540 | Affiliated Target |
|
| Class: Cellular Processes => Cellular community - eukaryotes | Pathway Hierarchy | ||
| JAK-STAT signaling pathway | hsa04630 | Affiliated Target |
|
| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| Regulation of actin cytoskeleton | hsa04810 | Affiliated Target |
|
| Class: Cellular Processes => Cell motility | Pathway Hierarchy | ||
| GnRH signaling pathway | hsa04912 | Affiliated Target |
|
| Class: Organismal Systems => Endocrine system | Pathway Hierarchy | ||
| Estrogen signaling pathway | hsa04915 | Affiliated Target |
|
| Class: Organismal Systems => Endocrine system | Pathway Hierarchy | ||
| Oxytocin signaling pathway | hsa04921 | Affiliated Target |
|
| Class: Organismal Systems => Endocrine system | Pathway Hierarchy | ||
| Relaxin signaling pathway | hsa04926 | Affiliated Target |
|
| Class: Organismal Systems => Endocrine system | Pathway Hierarchy | ||
| Parathyroid hormone synthesis, secretion and action | hsa04928 | Affiliated Target |
|
| Class: Organismal Systems => Endocrine system | Pathway Hierarchy | ||
| Click to Show/Hide the Information of Affiliated Human Pathways | |||
| Degree | 137 | Degree centrality | 1.47E-02 | Betweenness centrality | 2.54E-02 |
|---|---|---|---|---|---|
| Closeness centrality | 2.82E-01 | Radiality | 1.48E+01 | Clustering coefficient | 6.91E-02 |
| Neighborhood connectivity | 3.41E+01 | Topological coefficient | 2.04E-02 | Eccentricity | 11 |
| Download | Click to Download the Full PPI Network of This Target | ||||
| 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 | FDA Approved Drug Products from FDA Official Website. 2022. Application Number: 761210. | |||||
| REF 3 | 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 4 | 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 5 | 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 6 | 2004 approvals: the demise of the blockbuster. Nat Rev Drug Discov. 2005 Feb;4(2):93-4. | |||||
| REF 7 | 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89. | |||||
| REF 8 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| 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: 4920). | |||||
| REF 10 | 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 11 | Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91. | |||||
| REF 12 | Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24. | |||||
| REF 13 | 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 14 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 022059. | |||||
| REF 15 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 022059. | |||||
| REF 16 | 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 17 | 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 18 | 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85. | |||||
| REF 19 | The ChEMBL database in 2017. Nucleic Acids Res. 2017 Jan 4;45(D1):D945-D954. | |||||
| REF 20 | 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 21 | 2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101. | |||||
| REF 22 | Nat Rev Drug Discov. 2013 Feb;12(2):87-90. | |||||
| REF 23 | 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 24 | 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 25 | 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 26 | 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4. | |||||
| REF 27 | 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 28 | Clinical pipeline report, company report or official report of Beta Pharma. | |||||
| REF 29 | 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 30 | 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 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. | |||||
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