[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 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]