The Ligandable Human Proteome

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Epidermal growth factor receptor

Protein kinase domain

IndexLigand NameStructurePDB codeligand desolvation
157nEGFR kinase domain in complex with mutant selective allosteric inhibitor5d4197.87
2jbjEGFR with an allosteric inhibitor6duk95.1
380uCrystal structure of EGFR 696-988 T790M in complex with LXX-6-345gnk95.1
49llCrystal structure of EGFR 675-1022 T790M/C797S/V948R in complex with EAI0455zwj93
5w2rEGFR kinase domain with compound43w2s91.47
663nEGFR kinase domain mutant ""TMLR"" with a imidazopyridinyl-aminopyrimidine inhibitor5hic91.11
7w2rEGFR Kinase domain T790M/L858R mutant with compound 43w2r90.49
8w19EGFR kinase domain complexed with compound 19b3w3389.29
960bEGFR kinase domain mutant ""TMLR"" with azabenzimidazole compound 75hcx88.53
1063mEGFR kinase domain mutant ""TMLR"" with a pyrazolopyrimidine inhibitor5hib88.48
1103pEGFR Kinase domain complexed with tak-2853poz88.11
12hyzStructure of EGFR in complex with hydrazone, a potent dual inhibitor2rgp88.09
134zhEGFR kinase domain mutant ""TMLR"" with compound 305cap87.95
141e8Crystal structure of EGFR 696-1022 T790M in complex with Ibrutinib5yu986.98
154z8EGFR kinase domain mutant ""TMLR"" with compound 245cal86.88
16fmmEGFR kinase domain complexed with a quinazoline inhibitor- GW5720161xkk86.64
174zgEGFR kinase domain mutant ""TMLR"" with compound 295cao86.45
18djkCrystal structure of EGFR kinase domain in complex with an irreversible inhibitor 34-jab2j5f86.38
194zbEGFR kinase domain mutant ""TMLR"" with compound 275can86
20w32EGFR kinase domain complexed with compound 20a3w3285.44
216hlEGFR-T790M in complex with pyrazolopyrimidine inhibitor 1b5j9y85.34
226hjEGFR-T790M in complex with pyrazolopyrimidine inhibitor 1a5j9z85.23
231c9Structure of T790M EGFR kinase domain co-crystallized with dacomitinib4i2484.7
24poxX-ray structure of EGFR in complex with oxime inhibitor3bel84.59
25itiEGFR kinase domain complexed with an imidazo[2,1-b]thiazole inhibitor3lzb84.21
265n3EGFR 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-amine5edq83.9
27djkEGFR L858R in complex with PD1683934lqm83.12
284ywEGFR kinase domain mutant ""TMLR"" with compound 175c8m82.92
291c9Crystal structure of the wild-type EGFR kinase domain in complex with dacomitinib (soaked)4i2382.57
304zjEGFR kinase domain mutant ""TMLR"" with compound 335caq82.54
318bpCrystal 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]propanamide5ug882.53
325n4EGFR 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-amine5edr82.23
334yvEGFR kinase domain mutant ""TMLR"" with compound 15c8k82.18
343qsEGFR kinase (T790M/L858R) with inhibitor compound 84rj882.01
35kjrCrystal structure of EGFR kinase domain in complex with compound 3g4jr381.92
36kjqCrystal structure of EGFR kinase domain in complex with compound 2a4jq781.86
378amCrystal 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]propanamide5ug981.49
384zqEGFR kinase domain mutant ""TMLR"" with compound 41a5cas81.29
394zrEGFR kinase domain mutant ""TMLR"" with compound 41b5cau81.04
40kj8Crystal structure of EGFR kinase domain in complex with compound 4b4jq880.92
414zqEGFR kinase domain with compound 41a5cav80.31
4263aEGFR (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-one5hg979.84
43kjvCrystal structure of EGFR kinase domain in complex with compound 4c4jrv79.83
448bsCrystal 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]propanamide5ugc79.43
4560dEGFR kinase domain mutant ""TMLR"" with 3-carboxamide azaindole compound 135hcy79.39
46aq4Crystal structure of the inactive EGFR tyrosine kinase domain with erlotinib4hjo79.25
474yxEGFR kinase domain mutant ""TMLR"" with compound 235c8n78.92
48630EGFR (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)5hg778.61
493r1EGFR kinase (T790M/L858R) with inhibitor compound 14rj778.6
507xoCrystal structure of EGFR 696-1022 T790M/V948R in complex with SKLB(3)5x2a77.75
51634EGFR (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-enamide5hg877.54
523qwEGFR kinase (T790M/L858R) with inhibitor compound 64rj477.37
5360eEGFR kinase domain mutant ""TMLR"" with 3-azetidinyl azaindazole compound 215hcz77.3
543r0EGFR kinase (T790M/L858R) with inhibitor compound 44rj675.78
555x4EGFR kinase domain T790M mutant in complex with a covalent aminobenzimidazole inhibitor.5fee75.66
56o44Crystal structure of EGFR kinase domain in complex with a sulfonyl fluoride probe XO445u8l75.51
5703pEGFR Kinase domain T790M/L858R Mutant with TAK-2853w2o75.48
58fzpDiscovery of a Highly Potent and Broadly Effective EGFR and HER2 Exon 20 Insertion Mutant Inhibitor6d8e75.09
59hkiEGFR kinase domain T790M/L858R mutant with HKI-2723w2q74.93
60ire1.85 angstrom structure of EGFR kinase domain with gefitinib4wkq74.71
61ireCrystal structure of EGFR kinase domain L858R mutation in complex with Iressa2itz74.57
62aeeCrystal structure of EGFR kinase domain G719S mutation in complex with AEE7882itp74.56
630wnCrystal structure of EGFR kinase in complex with BIBW29924g5j73.94
64aq4Epidermal Growth Factor Receptor tyrosine kinase domain with 4-anilinoquinazoline inhibitor erlotinib1m1773.62
65aeeCrystal structure of EGFR kinase domain L858R mutation in complex with AEE7882itt73.52
667xoCrystal structure of EGFR 696-1022 L858R in complex with SKLB(3)5x2673.42
675x4EGFR kinase domain in complex with a covalent aminobenzimidazole inhibitor.5fed73.27
687xrCrystal structure of EGFR 696-1022 L858R in complex with SKLB(5)5x2773.2
697xrCrystal structure of EGFR 696-1022 T790M/V948R in complex with SKLB(5)5x2c72.92
70ireStructure of the monomeric (V948R)gefitinib/erlotinib resistant double mutant (L858R+T790M) EGFR kinase domain co-crystallized with gefitinib4i2272.92
715q3EGFR 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-carboxamide5em672.26
72w2pEGFR Kinase domain T790M/L858R mutant with compound 23w2p72.05
735q4EGFR 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-carboxamide5em771.61
747xuCrystal structure of EGFR 696-1022 T790M/V948R in complex with SKLB(6)5x2f71.05
755q2EGFR 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-carboxamide5em570.99
7681cCrystal structure of EGFR 696-1022 T790M in complex with JTS-1-395gtz70.26
777xuCrystal structure of EGFR 696-1022 L858R in complex with SKLB(6)5x2869.36
788bmCrystal 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-ium5uga69.3
790unCrystal Structure of EGFR 696-1022 T790M Mutant Covalently Binding to WZ40023ika67.75
80633EGFR (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-enamide5hg567.08
81l0nCrystal Structure of EGFR-T790M/C797S in Complex with Covalent Pyrrolopyrimidine 19h6s8a66.47
82f62Crystal structure of EGFR 696-1022 T790M in complex with XTF-2625gmp66.13
835q4EGFR kinase domain with pyridone compound 13: 4-[(2-methoxyphenyl)amino]-~{N}-[4-(4-methylpiperazin-1-yl)phenyl]-2-oxidanylidene-1~{H}-pyridine-3-carboxamide5em865.82
848bmCrystal 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-ium5ugb65.44
85ireCrystal structure of the mutated EGFR kinase domain (G719S/T790M) in complex with gefitinib3ug263.45
86yy3AZD9291 complex with wild type EGFR4zau59.15
87l0qCrystal Structure of EGFR-T790M/C797S in Complex with Covalent Pyrrolopyrimidine 19g6s8954.25
880wmCrystal structure of EGFR kinase in complex with BIBW29924g5j36.5