FR173657 [Ligand Id: 674] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL130517 (FK-3657) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| B2 receptor/Bradykinin B2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3157] [GtoPdb: 42] [UniProtKB: P30411] | ||||||||
| GtoPdb | - | - | 8.1 | pIC50 | 7.95 | nM | IC50 | Mol Pharmacol (1997) 51: 171-6 [PMID:9203620] |
| ChEMBL | Inhibition specific binding of [3H]BK (1.0 nM) to human Bradykinin receptor B2 which was expressed in CHO (Chinese hamster ovary) cells by 50%. | B | 8.85 | pIC50 | 1.4 | nM | IC50 | J Med Chem (1998) 41: 4062-4079 [PMID:9767643] |
| ChEMBL | Inhibition of the specific binding of [3H]BK to human recombinant Bradykinin receptor B2 expressed in CHO cells. | B | 8.85 | pIC50 | 1.4 | nM | IC50 | J Med Chem (1998) 41: 4587-4598 [PMID:9804698] |
| ChEMBL | Displacement of [3H]bradykinin from human recombinant B2 receptor expressed in HEK293 cells | B | 8.85 | pIC50 | 1.4 | nM | IC50 | J Med Chem (2009) 52: 4370-4379 [PMID:19552431] |
| GtoPdb | - | - | 8.2 | pA2 | - | - | - | Hypertension (1997) 29: 951-6 [PMID:9095082] |
| Bradykinin B2 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4111] [UniProtKB: O70526] | ||||||||
| ChEMBL | Concentration required to inhibit specific binding of [ 3H]BK (0.06 nM) to Bradykinin receptor B2 in guinea pig ileum membrane preparations by 50%. | B | 9.34 | pIC50 | 0.46 | nM | IC50 | J Med Chem (1998) 41: 4062-4079 [PMID:9767643] |
| ChEMBL | Inhibition of the specific binding of [3H]BK to Bradykinin receptor B2 in guinea pig ileum membrane preparations | B | 9.34 | pIC50 | 0.46 | nM | IC50 | J Med Chem (1998) 41: 4587-4598 [PMID:9804698] |
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]
