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ChEMBL ligand: CHEMBL3623290 (Azd 3759, Azd-3759, Azd3759, AZD3759, Zorifertinib) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]