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 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]
