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 (2018) |
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]
