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]
  • 7.2
1 CHEMBL189123_lig_chart_1 Bradykinin B1 receptor HumanDogRabbitRat
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  • B2 receptor/Bradykinin B2 receptor in Human [ChEMBL: CHEMBL3157] [GtoPdb: 42] [UniProtKB: P30411]
  • This target only has 1 pki data point
  • 5
2 CHEMBL189123_lig_chart_2 Bradykinin B2 receptor Human
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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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]