FR190997 [Ligand Id: 668] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL99869
  • B2 receptor/Bradykinin B2 receptor in Human [ChEMBL: CHEMBL3157] [GtoPdb: 42] [UniProtKB: P30411]
  • Bradykinin B2 receptor in Guinea pig [ChEMBL: CHEMBL4111] [UniProtKB: O70526]
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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 - - 7.3 pKi - - - Mol Pharmacol (1997) 52: 16-20 [PMID:9224807]
ChEMBL Inhibition of [3H]BK (1.0 nM) binding to the human bradykinin receptor B2, expressed in CHO cells B 9.39 pIC50 0.41 nM IC50 J Med Chem (2004) 47: 2853-2863 [PMID:15139763]
ChEMBL Displacement of [3H]BK from cloned human B2 bradykinin receptor expressed in CHO cells after 2 hrs by liquid scintillation counter B 9.39 pIC50 0.41 nM IC50 J Med Chem (2016) 59: 810-840 [PMID:26390077]
ChEMBL Agonist activity at bradykinin B2 receptor (unknown origin) B 9.39 pIC50 0.41 nM IC50 Eur J Med Chem (2021) 210: 112948-112948 [PMID:33139111]
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 the bradykinin receptor B2 B 8.64 pIC50 2.3 nM IC50 J Med Chem (2004) 47: 2853-2863 [PMID:15139763]

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]