chroman 28 [Ligand Id: 664] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL415848
  • B1 receptor/Bradykinin B1 receptor in Human [ChEMBL: CHEMBL4308] [GtoPdb: 41] [UniProtKB: P46663]
  • Bradykinin B1 receptor in Rabbit [ChEMBL: CHEMBL4087] [UniProtKB: P48748]
  • B1 receptor/Bradykinin B1 receptor in Rat [ChEMBL: CHEMBL4613] [GtoPdb: 41] [UniProtKB: P97583]
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  • B2 receptor/Bradykinin B2 receptor in Human [ChEMBL: CHEMBL3157] [GtoPdb: 42] [UniProtKB: P30411]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
B1 receptor/Bradykinin B1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4308] [GtoPdb: 41] [UniProtKB: P46663]
ChEMBL Antagonist activity at bradykinin B1 receptor assessed as prevention of Lys-desArg9-Bk-induced contraction in human umbilical vein F 7.4 pKd 39.81 nM Kd J Med Chem (2007) 50: 607-610 [PMID:17243660]
ChEMBL Displacement of [3H]DAK from human bradykinin B1 receptor expressed in CHO-D cells B 9.11 pKi 0.77 nM Ki J Med Chem (2007) 50: 607-610 [PMID:17243660]
ChEMBL Displacement of [3H]DAK from human bradykinin B1 receptor expressed in CHOD cells B 9.15 pKi 0.7 nM Ki J Med Chem (2007) 50: 2200-2212 [PMID:17408249]
ChEMBL Antagonistic activity at human bradykinin B1 receptor expressed in CHO cells assessed as effect on DAK-mediated calcium mobilization F 8.47 pIC50 3.4 nM IC50 J Med Chem (2007) 50: 607-610 [PMID:17243660]
ChEMBL Antagonist activity at human bradykinin B1 receptor expressed in CHOD cells assessed as effect on DAK-induced calcium flux F 8.47 pIC50 3.4 nM IC50 J Med Chem (2007) 50: 2200-2212 [PMID:17408249]
GtoPdb - - 8.5 pIC50 - - - J Med Chem (2007) 50: 607-10 [PMID:17243660]
ChEMBL Antagonistic activity at African green monkey bradykinin B1 receptor assessed as effect on DAK-mediated calcium mobilization F 9.4 pIC50 0.4 nM IC50 J Med Chem (2007) 50: 607-610 [PMID:17243660]
Bradykinin B1 receptor in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4087] [UniProtKB: P48748]
ChEMBL Antagonistic activity at rabbit bradykinin B1 receptor expressed in CHO-D cells assessed as effect on DAK-mediated calcium mobilization F 7.77 pIC50 17 nM IC50 J Med Chem (2007) 50: 607-610 [PMID:17243660]
B1 receptor/Bradykinin B1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4613] [GtoPdb: 41] [UniProtKB: P97583]
ChEMBL Antagonistic activity at rat bradykinin B1 receptor assessed as effect on DAK-mediated calcium mobilization F 8.4 pIC50 4 nM IC50 J Med Chem (2007) 50: 607-610 [PMID:17243660]
GtoPdb - - 8.5 pIC50 - - - J Med Chem (2007) 50: 607-10 [PMID:17243660]
B2 receptor/Bradykinin B2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3157] [GtoPdb: 42] [UniProtKB: P30411]
ChEMBL Displacement of [3H]bradykinin from human bradykinin B2 receptor expressed in CHO-K1 cells B 4.3 pKi >50000 nM Ki J Med Chem (2007) 50: 607-610 [PMID:17243660]

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]