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) |
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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 33:
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]
