cipralisant [Ligand Id: 1244] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL278462 (Cipralisant, Cipralisant, (-)-, (-)-GT-2331, GT-2331) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1] | ||||||||
| ChEMBL | Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in CHO cells | B | 8.4 | pKi | 3.98 | nM | Ki | J Med Chem (2008) 51: 2944-2953 [PMID:18433114] |
| GtoPdb | - | - | 8.6 | pKi | - | - | - | Eur J Pharmacol (2002) 453: 33-41 [PMID:12393057] |
| ChEMBL | Binding affinity for human recombinant H3 receptor | B | 8.67 | pKi | 2.14 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 1325-1328 [PMID:12657274] |
| H3 receptor/Histamine H3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8] | ||||||||
| GtoPdb | - | - | 9.5 | pKi | - | - | - | Eur J Pharmacol (2002) 453: 33-41 [PMID:12393057] |
| ChEMBL | Binding affinity towards rat cortical H3 receptor | B | 9.71 | pKi | 0.2 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 1325-1328 [PMID:12657274] |
| ChEMBL | Binding affinity to rat cortical histamine H3 receptor | B | 9.74 | pKi | 0.18 | nM | Ki | J Med Chem (2011) 54: 26-53 [PMID:21062081] |
| ChEMBL | Binding affinity of compound against Histamine H3 receptor | B | 9.9 | pKi | 0.13 | nM | Ki | J Med Chem (1999) 42: 1193-1202 [PMID:10197963] |
| ChEMBL | Binding affinity at histamine H3 receptor in rat cortical membranes by [3H]Nalpha-methylhistamine displacement. | B | 9.92 | pKi | 0.12 | nM | Ki | J Med Chem (1999) 42: 903-909 [PMID:10072687] |
| ChEMBL | In vitro inhibitory activity against Histamine H3 receptor for K+ evoked depolarization-induced release of [3H]histamine from synaptosomes of rat cerebral cortex | B | 9.92 | pKi | 0.12 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 2379-2382 [PMID:11055360] |
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]
