bradykinin [Ligand Id: 649] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL406291 (Bradykinin, BRS-640)
  • B1 receptor/Bradykinin B1 receptor in Human [ChEMBL: CHEMBL4308] [GtoPdb: 41] [UniProtKB: P46663]
  • B1 receptor in Mouse [GtoPdb: 41] [UniProtKB: Q61125]
  • B1 receptor in Rat [GtoPdb: 41] [UniProtKB: P97583]
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  • B2 receptor/Bradykinin B2 receptor in Human [ChEMBL: CHEMBL3157] [GtoPdb: 42] [UniProtKB: P30411]
  • B2 receptor in Mouse [GtoPdb: 42] [UniProtKB: P32299]
  • B2 receptor/Bradykinin B2 receptor in Rat [ChEMBL: CHEMBL2501] [GtoPdb: 42] [UniProtKB: P25023]
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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]
GtoPdb - - 4 pKi - - - J. Biol. Chem. (1997) 272: 11420-5 [PMID:9111052]
ChEMBL Ability to bind to human cloned B1 receptor in competition binding experiments with [3H][des-Arg10,Leu9]-Kallidin. B 8 pKi >10 nM Ki J. Med. Chem. (2000) 43: 2382-2386 [PMID:10882364]
B1 receptor in Mouse [GtoPdb: 41] [UniProtKB: Q61125]
GtoPdb - - 6.7 pKi - - - Immunopharmacology (1996) 33: 1-8 [PMID:8856107]
B1 receptor in Rat [GtoPdb: 41] [UniProtKB: P97583]
GtoPdb - - 5.3 pKi - - - Eur J Pharmacol (1999) 374: 423-433 [PMID:10422787]
B2 receptor/Bradykinin B2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3157] [GtoPdb: 42] [UniProtKB: P30411]
ChEMBL Displacement of [3H]Bradykinin from human recombinant bradykinin B2 receptor expressed in CHEM1 cells after 60 mins B 8.96 pKi 1.1 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL Binding affinity towards Bradykinin receptor B2 in human S34 clone cells B 9.17 pKi 0.68 nM Ki J. Med. Chem. (1996) 39: 1472-1484 [PMID:8691478]
ChEMBL Binding affinity against human cloned Bradykinin receptor B2 expressed in CHO cells using [3H]-bradykinin as radioligand B 9.19 pKi 0.65 nM Ki J. Med. Chem. (1999) 42: 4185-4192 [PMID:10514288]
ChEMBL Ability to bind to human cloned B2 receptor in competition binding experiments with [3H]- bradykinin B 9.96 pKi 0.11 nM Ki J. Med. Chem. (2000) 43: 2382-2386 [PMID:10882364]
ChEMBL Binding affinity towards human cloned Bradykinin receptor B2 expressed in CHO cells by [3H]bradykinin displacement. B 10.19 pKi 0.07 nM Ki J. Med. Chem. (1999) 42: 4193-4201 [PMID:10514289]
ChEMBL Displacement of [3H]Bradykinin from human recombinant bradykinin B2 receptor expressed in CHEM1 cells after 60 mins B 8.74 pIC50 1.8 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 1834-1838 [PMID:23403082]
GtoPdb - - 9.3 pIC50 - - - Mol Pharmacol (1994) 45: 1-8 [PMID:8302267];
Mol. Pharmacol. (1997) 51: 171-6 [PMID:9203620]
ChEMBL Antagonist activity at human recombinant bradykinin 2 receptor expressed in CHO cells assessed as inhibition of bradykinin-induced intracellular calcium mobilization F 10.31 pEC50 0.05 nM EC50 J. Med. Chem. (2009) 52: 4068-4071 [PMID:19473027]
B2 receptor in Mouse [GtoPdb: 42] [UniProtKB: P32299]
GtoPdb - - 9.3 pIC50 - - - Mol Pharmacol (1994) 45: 1-8 [PMID:8302267]
B2 receptor/Bradykinin B2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2501] [GtoPdb: 42] [UniProtKB: P25023]
ChEMBL Binding affinity against rat Bradykinin receptor B2 expressed in CHO cells using [3H]-bradykinin as radioligand B 9.34 pKi 0.46 nM Ki J. Med. Chem. (1999) 42: 4185-4192 [PMID:10514288]

ChEMBL data shown on this page come from version 27:

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]