zorifertinib [Ligand Id: 10456] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3623290 (Azd 3759, Azd-3759, Azd3759, AZD3759, Zorifertinib)
  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
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  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
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  • Kv11.1 in Human [GtoPdb: 572] [UniProtKB: Q12809]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Inhibition of recombinant D2 receptor (unknown origin) B 6.1 pIC50 797 nM IC50 J Med Chem (2015) 58: 8200-8215 [PMID:26313252]
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 (unknown origin) by HTRF assay in presence of 2 mM of ATP B 6.99 pIC50 102 nM IC50 J Med Chem (2015) 58: 8200-8215 [PMID:26313252]
ChEMBL Inhibition of EGFR phosphorylation in human H838 cells B 7.19 pIC50 64.5 nM IC50 J Med Chem (2015) 58: 8200-8215 [PMID:26313252]
ChEMBL Inhibition of EGFR L858R mutant (unknown origin) by HTRF assay in presence of 2 mM of ATP B 8.12 pIC50 7.6 nM IC50 J Med Chem (2015) 58: 8200-8215 [PMID:26313252]
GtoPdb Inhibition of EGFRL858R in vitro. - 8.14 pIC50 7.2 nM IC50 J Med Chem (2015) 58: 8200-15 [PMID:26313252]
ChEMBL Inhibition of EGFR L858R mutant phosphorylation in human H3255 cells B 8.14 pIC50 7.2 nM IC50 J Med Chem (2015) 58: 8200-8215 [PMID:26313252]
ChEMBL Inhibition of human EGFR using poly[Glu:Tyr] (4:1) as substrate measured after 20 mins in presence of [gamma33P]ATP by filter-binding assay B 9.3 pIC50 <0.5 nM IC50 ACS Med Chem Lett (2019) 10: 22-26 [PMID:30655941]
GtoPdb Inhibition of wild type EGFR in vitro, at Km of ATP. - 9.52 pIC50 0.3 nM IC50 J Med Chem (2015) 58: 8200-15 [PMID:26313252]
ChEMBL Inhibition of EGFR (unknown origin) by HTRF assay in presence of Km of ATP B 9.52 pIC50 0.3 nM IC50 J Med Chem (2015) 58: 8200-8215 [PMID:26313252]
ChEMBL Inhibition of EGFR L858R mutant (unknown origin) by HTRF assay in presence of Km of ATP B 9.7 pIC50 0.2 nM IC50 J Med Chem (2015) 58: 8200-8215 [PMID:26313252]
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
ChEMBL Inhibition of recombinant Src (unknown origin) after 40 mins by scintillation counting analysis in presence of [gamma33P]-ATP B 6.21 pIC50 622 nM IC50 J Med Chem (2015) 58: 8200-8215 [PMID:26313252]
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
ChEMBL Inhibition of recombinant KDR (unknown origin) after 40 mins by scintillation counting analysis in presence of [gamma33P]-ATP B 6.81 pIC50 156 nM IC50 J Med Chem (2015) 58: 8200-8215 [PMID:26313252]
Kv11.1 in Human [GtoPdb: 572] [UniProtKB: Q12809]
GtoPdb Channel inhibition measured in a conventional manual whole-cell patch clamp study. - 4.88 pIC50 13300 nM IC50 J Med Chem (2015) 58: 8200-15 [PMID:26313252]

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]