The Ligandable Human Proteome

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Epidermal growth factor receptor

Protein kinase domain

IndexLigand NameStructurePDB codeCompound Potency nM
1f62Crystal structure of EGFR 696-1022 T790M in complex with XTF-2625gmp0.8
260dEGFR kinase domain mutant ""TMLR"" with 3-carboxamide azaindole compound 135hcy1.2
34zqEGFR kinase domain mutant ""TMLR"" with compound 41a5cas1.4
44zrEGFR kinase domain mutant ""TMLR"" with compound 41b5cau1.6
5aeeCrystal structure of EGFR kinase domain L858R mutation in complex with AEE7882itt1.7
65n3EGFR kinase (T790M/L858R) with inhibitor compound 15: ~{N}-(7-chloranyl-1~{H}-indazol-3-yl)-7,7-dimethyl-2-(1~{H}-pyrazol-4-yl)-5~{H}-furo[3,4-d]pyrimidin-4-amine5edq2
7633EGFR (L858R, T790M, V948R) in complex with N-{3-[(2-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy]phenyl}prop-2-enamide5hg52
88bpCrystal structure of the EGFR kinase domain (L858R, T790M, V948R) in complex with a covalent inhibitor N-[(3R,4R)-4-fluoro-1-{6-[(1-methyl-1H-pyrazol-4-yl)amino]-9-(propan-2-yl)-9H-purin-2-yl}pyrrolidin-3-yl]propanamide5ug82
9ireCrystal structure of EGFR kinase domain L858R mutation in complex with Iressa2itz2.6
104zjEGFR kinase domain mutant ""TMLR"" with compound 335caq2.7
11fmmEGFR kinase domain complexed with a quinazoline inhibitor- GW5720161xkk3
12634EGFR (L858R, T790M, V948R) in complex with N-[3-({2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)phenyl]prop-2-enamide5hg83
135q3EGFR kinase domain mutant ""TMLR"" with pyridone compound 19: 4-[(2-azanylpyrimidin-4-yl)amino]-~{N}-[4-(4-methylpiperazin-1-yl)phenyl]-2-oxidanylidene-1~{H}-pyridine-3-carboxamide5em64
14630EGFR (L858R, T790M, V948R) in complex with 1-{(3R,4R)-3-[5-Chloro-2-(1-methyl-1H-pyrazol-4-ylamino)-7H-pyrrolo[2,3-d]pyrimidin-4-yloxymethyl]-4-methoxy-pyrrolidin-1-yl}propenone (PF-06459988)5hg74
1560bEGFR kinase domain mutant ""TMLR"" with azabenzimidazole compound 75hcx4.1
1680uCrystal structure of EGFR 696-988 T790M in complex with LXX-6-345gnk5.3
17ireCrystal structure of the mutated EGFR kinase domain (G719S/T790M) in complex with gefitinib3ug25.6
18w2rEGFR kinase domain with compound43w2s6.9
19kj8Crystal structure of EGFR kinase domain in complex with compound 4b4jq88
208amCrystal structure of the EGFR kinase domain (L858R, T790M, V948R) in complex with a covalent inhibitor N-[(3R,4R)-4-fluoro-1-{6-[(3-methoxy-1-methyl-1H-pyrazol-4-yl)amino]-9-(propan-2-yl)-9H-purin-2-yl}pyrrolidin-3-yl]propanamide5ug98
21aeeCrystal structure of EGFR kinase domain G719S mutation in complex with AEE7882itp11.3
228bsCrystal structure of the EGFR kinase domain (L858R, T790M, V948R) in complex with a covalent inhibitor N-[(3R,4R)-4-fluoro-1-{6-[(3-methoxy-1-methyl-1H-pyrazol-4-yl)amino]-9-methyl-9H-purin-2-yl}pyrrolidin-3-yl]propanamide5ugc13
23poxX-ray structure of EGFR in complex with oxime inhibitor3bel14
240unCrystal Structure of EGFR 696-1022 T790M Mutant Covalently Binding to WZ40023ika14
253qwEGFR kinase (T790M/L858R) with inhibitor compound 64rj416
266hjEGFR-T790M in complex with pyrazolopyrimidine inhibitor 1a5j9z16
273qsEGFR kinase (T790M/L858R) with inhibitor compound 84rj817
28w2rEGFR Kinase domain T790M/L858R mutant with compound 43w2r19
295q4EGFR kinase domain mutant ""TMLR"" with pyridone compound 13: 4-[(2-methoxyphenyl)amino]-~{N}-[4-(4-methylpiperazin-1-yl)phenyl]-2-oxidanylidene-1~{H}-pyridine-3-carboxamide5em719
304yvEGFR kinase domain mutant ""TMLR"" with compound 15c8k20
313r1EGFR kinase (T790M/L858R) with inhibitor compound 14rj722
324z8EGFR kinase domain mutant ""TMLR"" with compound 245cal22
3303pEGFR Kinase domain complexed with tak-2853poz23
344yxEGFR kinase domain mutant ""TMLR"" with compound 235c8n28
35kjvCrystal structure of EGFR kinase domain in complex with compound 4c4jrv29
36hyzStructure of EGFR in complex with hydrazone, a potent dual inhibitor2rgp30
375n4EGFR kinase (T790M/L858R) with inhibitor compound 27: ~{N}-(1~{H}-indazol-3-yl)-7,7-dimethyl-2-(2-methylpyrazol-3-yl)-5~{H}-furo[3,4-d]pyrimidin-4-amine5edr34.3
3863aEGFR (L858R, T790M, V948R) in complex with 1-[(3R,4R)-3-[({2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-(trifluoromethyl)pyrrolidin-1-yl]prop-2-en-1-one5hg935
39w19EGFR kinase domain complexed with compound 19b3w3336
404zgEGFR kinase domain mutant ""TMLR"" with compound 295cao38
414zhEGFR kinase domain mutant ""TMLR"" with compound 305cap52
426hlEGFR-T790M in complex with pyrazolopyrimidine inhibitor 1b5j9y58
43itiEGFR kinase domain complexed with an imidazo[2,1-b]thiazole inhibitor3lzb63
444ywEGFR kinase domain mutant ""TMLR"" with compound 175c8m64
45hkiEGFR kinase domain T790M/L858R mutant with HKI-2723w2q66
46w32EGFR kinase domain complexed with compound 20a3w3275
473r0EGFR kinase (T790M/L858R) with inhibitor compound 44rj676
484zbEGFR kinase domain mutant ""TMLR"" with compound 275can124
498bmCrystal structure of the EGFR kinase domain (L858R, T790M, V948R) in complex with 4-(4-{[2-{[(3S)-1-acetylpyrrolidin-3-yl]amino}-9-(propan-2-yl)-9H-purin-6-yl]amino}phenyl)-1-methylpiperazin-1-ium5uga161
508bmCrystal structure of the EGFR kinase domain in complex with 4-(4-{[2-{[(3S)-1-acetylpyrrolidin-3-yl]amino}-9-(propan-2-yl)-9H-purin-6-yl]amino}phenyl)-1-methylpiperazin-1-ium5ugb161
511e8Crystal structure of EGFR 696-1022 T790M in complex with Ibrutinib5yu9180
524zqEGFR kinase domain with compound 41a5cav216
53kjrCrystal structure of EGFR kinase domain in complex with compound 3g4jr3218
545q2EGFR kinase domain mutant ""TMLR"" with pyridone compound 2: 4-[2-(4-chlorophenyl)ethylamino]-~{N}-[4-(4-methylpiperazin-1-yl)phenyl]-2-oxidanylidene-1~{H}-pyridine-3-carboxamide5em5262
55kjqCrystal structure of EGFR kinase domain in complex with compound 2a4jq7393
565q4EGFR kinase domain with pyridone compound 13: 4-[(2-methoxyphenyl)amino]-~{N}-[4-(4-methylpiperazin-1-yl)phenyl]-2-oxidanylidene-1~{H}-pyridine-3-carboxamide5em81090
57w2pEGFR Kinase domain T790M/L858R mutant with compound 23w2p8100
5803pEGFR Kinase domain T790M/L858R Mutant with TAK-2853w2o8400