[des-Arg10]kallidin [Ligand Id: 644] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL264100 (des-Arg10-Kallidin) |
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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 | Displacement of [3H](Des-Arg10)-Kallidin from bradykinin B1 receptor in human IMR90 cells after 60 mins | B | 9.66 | pKi | 0.22 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082] |
| ChEMBL | Binding affinity (radioligand) to human Bradykinin receptor B1 over-expressed in transgenic rats was determined by ex vivo receptor occupancy assay; value ranges from 0.1-0.2 nM | B | 9.7 | pKi | <0.2 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 6045-6048 [PMID:15546726] |
| GtoPdb | - | - | 10 | pKi | - | - | - |
J Biol Chem (1997) 272: 11420-5 [PMID:9111052]; Eur J Pharmacol (1999) 374: 423-433 [PMID:10422787]; Br J Pharmacol (1997) 122: 393-9 [PMID:9313952]; Br J Pharmacol (1996) 118: 289-94 [PMID:8735629] |
| ChEMBL | Displacement of [3H](Des-Arg10)-Kallidin from bradykinin B1 receptor in human IMR90 cells after 60 mins | B | 9.06 | pIC50 | 0.87 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082] |
| B1 receptor in Mouse [GtoPdb: 41] [UniProtKB: Q61125] | ||||||||
| GtoPdb | - | - | 8.8 | pKi | - | - | - | Immunopharmacology (1996) 33: 1-8 [PMID:8856107] |
| B1 receptor/Bradykinin B1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4613] [GtoPdb: 41] [UniProtKB: P97583] | ||||||||
| GtoPdb | - | - | 8.9 | pKi | - | - | - | Eur J Pharmacol (1999) 374: 423-433 [PMID:10422787] |
| ChEMBL | Compound was evaluated for agonist activity against B1 receptor in rat ileum longitudinal smooth muscle | F | 7.07 | pEC50 | 85 | nM | EC50 | Bioorg Med Chem Lett (1997) 7: 2661-2664 |
| B2 receptor in Mouse [GtoPdb: 42] [UniProtKB: P32299] | ||||||||
| GtoPdb | - | - | 4.6 | pIC50 | - | - | - | Mol Pharmacol (1994) 45: 1-8 [PMID:8302267] |
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]
