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/T790M 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]
ChEMBL Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 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 Del ex19 mutant phosphorylation in human PC9 cells preincubated for 2 hrs by ELISA B 8.7 pIC50 2 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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]