[des-Arg10]kallidin [Ligand Id: 644] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL264100 (des-Arg10-Kallidin)
  • B1 receptor/Bradykinin B1 receptor in Human [ChEMBL: CHEMBL4308] [GtoPdb: 41] [UniProtKB: P46663]
  • B1 receptor in Mouse [GtoPdb: 41] [UniProtKB: Q61125]
  • B1 receptor/Bradykinin B1 receptor in Rat [ChEMBL: CHEMBL4613] [GtoPdb: 41] [UniProtKB: P97583]
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  • B2 receptor in Mouse [GtoPdb: 42] [UniProtKB: P32299]
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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 26:

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]