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Target
Epidermal growth factor receptor [669-770,'SVD',771-1210]
Ligand
BDBM555137
Substrate
n/a
Meas. Tech.
Kinase Assay
IC50
0.099±n/a nM
Citation
 Siegel, S; Siegel, F; Schulze, V; Berger, M; Graham, K; Klar, U; Eis, K; Sülzle, D; Bömer, U; Korr, D; Petersen, K; Mönning, U; Eberspächer, U; Moosmayer, D; Meyerson, M; Greulich, H; Kaplan, B; Harb, HY; Dinh, PM 4H-pyrrolo[3,2-c]pyridin-4-one derivatives US Patent  US11339157 Publication Date 5/24/2022 
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:
BDBM555137
Synonyms:
3-[(3,5-difluoro-2-methoxyphenyl)amino]-2-[3-(2-methoxy-2-methylpropoxy)pyridin-4-yl]-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridin-4-one | US11339157, Example 31
Type:
Small organic molecule
Emp. Form.:
C24H26F2N4O4
Mol. Mass.:
472.4844
SMILES:
COc1c(F)cc(F)cc1Nc1c([nH]c2CCNC(=O)c12)-c1ccncc1OCC(C)(C)OC
Structure:
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