AZ5104 [Ligand Id: 11580] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3353411
  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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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 wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay B 4.48 pIC50 33000 nM IC50 J Med Chem (2014) 57: 8249-8267 [PMID:25271963]
ChEMBL Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay B 5.7 pIC50 2000 nM IC50 J Med Chem (2014) 57: 8249-8267 [PMID:25271963]
GtoPdb Inhibition of wild type EGFR phosphorylation in human LoVo cells - 7.48 pIC50 33 nM IC50 Bioorg Med Chem Lett (2016) 26: 1861-8 [PMID:26968253]
ChEMBL Inhibition of wild type EGFR phosphorylation in human LoVo cells preincubated for 2 hrs followed by EGF stimulation measured after 30 mins by ELISA B 7.48 pIC50 33 nM IC50 Bioorg Med Chem Lett (2016) 26: 1861-1868 [PMID:26968253]
ChEMBL Inhibition of EGFR T790M/L858R double mutant phosphorylation in human H1975 cells preincubated for 2 hrs by ELISA B 8.7 pIC50 2 nM IC50 Bioorg Med Chem Lett (2016) 26: 1861-1868 [PMID:26968253]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG B 4.76 pIC50 17500 nM IC50 J Med Chem (2014) 57: 8249-8267 [PMID:25271963]

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]