EGFR/ErbB-2/ErbB-4 inhibitor [Ligand Id: 5965] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL203644
  • 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 2/Receptor protein-tyrosine kinase erbB-2 in Human [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626]
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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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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 EGF stimulated human erbB1 autophosphorylation in NIH3T3 cells F 8.6 pIC50 2.5 nM IC50 J Med Chem (2006) 49: 1475-1485 [PMID:16480284]
GtoPdb - - 9.52 pIC50 0.3 nM IC50 J Med Chem (2006) 49: 1475-85 [PMID:16480284]
ChEMBL Inhibition of erbB1 fusion protein expressed in baculovirus by ELISA B 9.52 pIC50 0.3 nM IC50 J Med Chem (2006) 49: 1475-1485 [PMID:16480284]
erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626]
ChEMBL Inhibition of HER stimulated human erbB autophosphorylation in MDA-MB-453 cells F 7.62 pIC50 24 nM IC50 J Med Chem (2006) 49: 1475-1485 [PMID:16480284]
ChEMBL Inhibition of erbB2 fusion protein expressed in baculovirus by ELISA B 8.96 pIC50 1.1 nM IC50 J Med Chem (2006) 49: 1475-1485 [PMID:16480284]
GtoPdb - - 8.96 pIC50 1.1 nM IC50 J Med Chem (2006) 49: 1475-85 [PMID:16480284]
erb-b2 receptor tyrosine kinase 4/Receptor protein-tyrosine kinase erbB-4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3009] [GtoPdb: 1799] [UniProtKB: Q15303]
GtoPdb - - 9.3 pIC50 0.5 nM IC50 J Med Chem (2006) 49: 1475-85 [PMID:16480284]
ChEMBL Inhibition of erbB4 fusion protein expressed in baculovirus by ELISA B 9.3 pIC50 0.5 nM IC50 J Med Chem (2006) 49: 1475-1485 [PMID:16480284]

ChEMBL data shown on this page come from version 32:

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]