EGFR inhibitor [Ligand Id: 5963] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL387187
  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • erb-b2 receptor tyrosine kinase 4/Receptor protein-tyrosine kinase erbB-4 in Human [ChEMBL: CHEMBL3009] [GtoPdb: 1799] [UniProtKB: Q15303]
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  • aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Inhibition of EGFR L858R mutant B 7.2 pIC50 63 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
ChEMBL Inhibition of EGFR B 7.68 pIC50 21 nM IC50 Bioorg Med Chem Lett (2007) 17: 688-691 [PMID:17157005]
ChEMBL Inhibition of wild type EGFR B 7.68 pIC50 21 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
GtoPdb - - 7.68 pIC50 21 nM IC50 Proc Natl Acad Sci USA (2007) 104: 20523-8 [PMID:18077363]
ChEMBL Inhibition of EGFR L861Q mutant B 8.4 pIC50 4 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
erb-b2 receptor tyrosine kinase 4/Receptor protein-tyrosine kinase erbB-4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3009] [GtoPdb: 1799] [UniProtKB: Q15303]
ChEMBL Inhibition of erbB4/Her4 B 5.12 pIC50 7640 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
ChEMBL Inhibition of Aurora-A B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2007) 17: 688-691 [PMID:17157005]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]