DBPR112 [Ligand Id: 12711] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4521381
  • 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 GST-tagged human EGFR kinase domain I858R/T790M mutant (696 to 1022 residues) using EGFR L858R/T790M substrate peptide incubated for 120 mins by kinase-Glo plus luminescent kinase assay B 7.32 pIC50 48 nM IC50 J Med Chem (2019) 62: 10108-10123 [PMID:31560541]
GtoPdb Enzymatic activity inhibition of EGFRL858R/T790M - 7.32 pIC50 48 nM IC50 J Med Chem (2019) 62: 10108-10123 [PMID:31560541]
ChEMBL Inhibition of GST-tagged human EGFR kinase domain (696 to 1022 residues) using poly(Glu, Tyr) 4:1 substrate incubated for 60 mins by kinase-Glo plus luminescent kinase assay B 7.82 pIC50 15 nM IC50 J Med Chem (2019) 62: 10108-10123 [PMID:31560541]
ChEMBL Inhibition of GST-tagged human EGFR D770_N771insNPG mutant using poly(Glu, Tyr) 4:1 substrate incubated for 120 mins by kinase-Glo plus luminescent kinase assay B 9.88 pIC50 0.13 nM IC50 J Med Chem (2019) 62: 10108-10123 [PMID:31560541]
ChEMBL Inhibition of GST-tagged human EGFR A763_Y764insFHEA mutant using poly(Glu, Tyr) 4:1 substrate incubated for 120 mins by kinase-Glo plus luminescent kinase assay B 10.37 pIC50 0.04 nM IC50 J Med Chem (2019) 62: 10108-10123 [PMID:31560541]

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]