cipralisant [Ligand Id: 1244] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL278462 (Cipralisant, Cipralisant, (-)-, (-)-GT-2331, GT-2331)
  • H3 receptor/Histamine H3 receptor in Human [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
  • H3 receptor/Histamine H3 receptor in Rat [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8]
There should be some charts here, you may need to enable JavaScript!
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 32:

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]