Target Information
Target General Information | Top | |||||
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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
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[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 | |||||
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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 |
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Drug Property Profile of Target | Top | |
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(1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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(5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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"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 | |||||
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Co-Targets |
Target Poor or Non Binders | Top | |||||
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Target Poor or Non Binders |
Target Regulators | Top | |||||
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Target-regulating microRNAs | ||||||
Target-regulating Transcription Factors | ||||||
Target-interacting Proteins |
Target Profiles in Patients | Top | |||||
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Target Expression Profile (TEP) | ||||||
Drug Resistance Mutation (DRM) |
Target-Related Models and Studies | Top | |||||
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Target Validation | ||||||
Target QSAR Model |
References | Top | |||||
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