compound 11 [PMID: 12812482] [Ligand Id: 665] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL189123
  • B1 receptor/Bradykinin B1 receptor in Human [ChEMBL: CHEMBL4308] [GtoPdb: 41] [UniProtKB: P46663]
  • Bradykinin B1 receptor in Dog [ChEMBL: CHEMBL4724] [UniProtKB: Q9BDQ5]
  • 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 Binding affinity to human BK1 receptor Q295 mutant B 9.05 pKi 0.89 nM Ki Bioorg Med Chem Lett (2006) 16: 2791-2795 [PMID:16529929]
ChEMBL Binding affinity to human BK1 receptor D291 mutant B 10.31 pKi 0.05 nM Ki Bioorg Med Chem Lett (2006) 16: 2791-2795 [PMID:16529929]
ChEMBL Binding affinity to human BK1 receptor N298 mutant B 10.42 pKi 0.04 nM Ki Bioorg Med Chem Lett (2006) 16: 2791-2795 [PMID:16529929]
ChEMBL Displacement of [3H]Lys0-des-Arg9-BK at human bradykinin B1 receptor expressed in HEK293 cells B 10.47 pKi 0.03 nM Ki J Med Chem (2010) 53: 5383-5399 [PMID:20369879]
ChEMBL Binding affinity to human bradykinin B1 receptor B 10.47 pKi 0.03 nM Ki Bioorg Med Chem Lett (2012) 22: 3095-3099 [PMID:22483585]
ChEMBL Binding affinity to human BK1 receptor B 10.47 pKi 0.03 nM Ki Bioorg Med Chem Lett (2006) 16: 2791-2795 [PMID:16529929]
ChEMBL Displacement of [3H]DAK from human bradykinin B1 receptor expressed in CHO-D-/aequorin cells by rapid filtration technique B 10.47 pKi 0.03 nM Ki Bioorg Med Chem Lett (2008) 18: 4477-4481 [PMID:18674903]
GtoPdb - - 10.5 pKi - - - J Am Chem Soc (2003) 125: 7516-7 [PMID:12812482]
ChEMBL Binding affinity to human Bradykinin receptor B1 over-expressed in transgenic rats was determined by ex vivo receptor occupancy assay B 10.52 pKi 0.03 nM Ki Bioorg Med Chem Lett (2004) 14: 6045-6048 [PMID:15546726]
ChEMBL Antagonist activity at human bradykinin B1 receptor expressed in CHO-D-/aequorin cells F 9.74 pIC50 0.18 nM IC50 Bioorg Med Chem Lett (2008) 18: 4477-4481 [PMID:18674903]
ChEMBL Antagonist activity at human bradykinin B1 receptor in human MR5 cells assessed as [3H]inositol phosphate accumulation F 9.74 pIC50 0.18 nM IC50 J Med Chem (2010) 53: 5383-5399 [PMID:20369879]
Bradykinin B1 receptor in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4724] [UniProtKB: Q9BDQ5]
ChEMBL Antagonist activity at dog bradykinin B1 receptor F 7.79 pIC50 16.3 nM IC50 J Med Chem (2010) 53: 5383-5399 [PMID:20369879]
Bradykinin B1 receptor in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4087] [UniProtKB: P48748]
ChEMBL Inhibition of rabbit bradykinin B1 receptor B 9.59 pIC50 0.26 nM IC50 J Med Chem (2010) 53: 5383-5399 [PMID:20369879]
B1 receptor/Bradykinin B1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4613] [GtoPdb: 41] [UniProtKB: P97583]
GtoPdb - - 7.2 pKi - - - J Am Chem Soc (2003) 125: 7516-7 [PMID:12812482]
ChEMBL Inhibition of rat bradykinin B1 receptor B 6.79 pIC50 163.5 nM IC50 J Med Chem (2010) 53: 5383-5399 [PMID:20369879]
B2 receptor/Bradykinin B2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3157] [GtoPdb: 42] [UniProtKB: P30411]
ChEMBL Binding affinity to human Bradykinin receptor B2 over-expressed in transgenic rats was determined by ex vivo receptor occupancy assay B 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2004) 14: 6045-6048 [PMID:15546726]

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]