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

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ChEMBL ligand: CHEMBL406291 (Bradykinin, BRS-640, Callidin i, Kallidin-9, Kallidin i)
  • 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]
Olfactory receptor 51E2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523454] [UniProtKB: Q9H255]
ChEMBL Agonist activity at PSGR/OR51E2 (unknown origin) expressed in human Hana3A cells co-transfected with CRE-Luc by luciferase reporter gene assay F 8.89 pEC50 1.3 nM EC50 US-20180116992-A1. Modulators of Prostate-Specific G-Protein Receptor (PSGR/OR51E2) and Methods of Using Same (null)

ChEMBL data shown on this page come from version 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]