Reaction Details |
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Target | Epidermal growth factor receptor [669-770,'SVD',771-1210] |
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Ligand | BDBM552599 |
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Substrate/Competitor | n/a |
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Meas. Tech. | Exon20-mutant-EGFR(D770_N771insSVD) kinase assay |
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IC50 | 0.58±n/a nM |
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Citation | Stephan, S; Franziska, S; Volker, S; Markus, B; Keith, G; Ulrich, K; G., MJ; Detlev, S; Ulf, B; Daniel, K; Jens, S; Matthew, M; Heidi, G; Bethany, K N-[2-({4-[3-(ANILINO)-4-OXO-4,5,6,7-TETRAHYDRO-1H-PYRROLO[3,2-C]PYRIDIN-2-YL]PYRIDIN-3-YL)OXY)ETHYL]PROP-2-ENAMIDE DERIVATIVES AND SIMILAR COMPOUNDS AS EGFR INHIBITORS FOR THE TREATMENT OF CANCER WIPOWO2022101184 Publication Date 5/19/2022 |
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More Info.: | Get all data from this article, Assay Method |
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Epidermal growth factor receptor [669-770,'SVD',771-1210] |
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Name: | Epidermal growth factor receptor [669-770,'SVD',771-1210] |
Synonyms: | EGFR | EGFR_HUMAN | ERBB | ERBB1 | Epidermal growth factor receptor [669-769,''ASV'',770-1210] | Epidermal growth factor receptor [669-769,'ASV',770-1210] | HER1 |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 61473.15 |
Organism: | Homo sapiens (Human) |
Description: | P00533[669-770,'SVD',771-1210] |
Residue: | 545 |
Sequence: | RRRHIVRKRTLRRLLQERELVEPLTPSGEAPNQALLRILKETEFKKIKVLGSGAFGTVYK
GLWIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDSVDNPHVCRLLGICLTST
VQLITQLMPFGCLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAARNVLV
KTPQHVKITDFGLAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSYGVTVW
ELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPKFRELI
IEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQQGFFS
SPSTSRTPLLSSLSATSNNSTVACIDRNGLQSCPIKEDSFLQRYSSDPTGALTEDSIDDT
FLPVPEYINQSVPKRPAGSVQNPVYHNQPLNPAPSRDPHYQDPHSTAVGNPEYLNTVQPT
CVNSTFDSPAHWAQKGSHQISLDNPDYQQDFFPKEAKPNGIFKGSTAENAEYLRVAPQSS
EFIGA
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BDBM552599 |
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n/a |
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Name | BDBM552599 |
Synonyms: | N-[2-({4-[3-(3-chloro-2-methoxyanilino)-6,6-dimethyl-4-oxo-4,5,6,7-tetrahydro-1H-pyrrolo[3,2-c]pyridin-2-yl]pyridin-3-yl}oxy)ethyl]-N-methylprop-2-enamide | WO2022101184, Example 12 |
Type | Small organic molecule |
Emp. Form. | C27H30ClN5O4 |
Mol. Mass. | 524.011 |
SMILES | COc1c(Cl)cccc1Nc1c([nH]c2CC(C)(C)NC(=O)c12)-c1ccncc1OCCN(C)C(=O)C=C |
Structure |
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