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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL3623290 (Azd 3759, Azd-3759, Azd3759, AZD3759, Zorifertinib)
  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
There should be some charts here, you may need to enable JavaScript!
  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
There should be some charts here, you may need to enable JavaScript!
  • SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
There should be some charts here, you may need to enable JavaScript!
  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
There should be some charts here, you may need to enable JavaScript!
  • Kv11.1 in Human [GtoPdb: 572] [UniProtKB: Q12809]
There should be some charts here, you may need to enable JavaScript!
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]
ChEMBL Inhibition of EGFR exon19 deletion mutant phosphorylation in human PC9 cells B 8.13 pIC50 7.4 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 EGFR exon19 deletion mutant (unknown origin) by HTRF assay in presence of 2mM of ATP B 8.62 pIC50 2.4 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]
ChEMBL Inhibition of EGFR exon19 deletion 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 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]