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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 |
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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]