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Target
Epidermal growth factor receptor [669-770,'SVD',771-1210]
Ligand
BDBM552601
Substrate
n/a
Meas. Tech.
Exon20-mutant-EGFR(D770_N771insSVD) kinase assay
IC50
0.57±n/a nM
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 WIPO 0:0 (2022) [PubMed] 
Target
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:
RRRHIVRKRTLRRLLQERELVEPLTPSGEAPNQALLRILKETEFKKIKVLGSGAFGTVYKGLWIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDSVDNPHVCRLLGICLTSTVQLITQLMPFGCLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAARNVLVKTPQHVKITDFGLAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSYGVTVWELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPKFRELIIEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQQGFFSSPSTSRTPLLSSLSATSNNSTVACIDRNGLQSCPIKEDSFLQRYSSDPTGALTEDSIDDTFLPVPEYINQSVPKRPAGSVQNPVYHNQPLNPAPSRDPHYQDPHSTAVGNPEYLNTVQPTCVNSTFDSPAHWAQKGSHQISLDNPDYQQDFFPKEAKPNGIFKGSTAENAEYLRVAPQSSEFIGA
  
Inhibitor
Name:
BDBM552601
Synonyms:
N-(2-{[4-(3-{[2-(difluoromethoxy)phenyl]amino}-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 14
Type:
Small organic molecule
Emp. Form.:
C25H25F2N5O4
Mol. Mass.:
497.4939
SMILES:
CN(CCOc1cnccc1-c1[nH]c2CCNC(=O)c2c1Nc1ccccc1OC(F)F)C(=O)C=C
Structure:
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