GR 175737 [Ligand Id: 1243] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL276798 (GR-175737)
  • H3 receptor in Human [GtoPdb: 264] [UniProtKB: Q9Y5N1]
  • H3 receptor/Histamine H3 receptor in Rat [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
H3 receptor in Human [GtoPdb: 264] [UniProtKB: Q9Y5N1]
GtoPdb - - 8.6 pKi - - - Eur J Pharmacol (2002) 453: 33-41 [PMID:12393057]
H3 receptor/Histamine H3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8]
ChEMBL Inhibition of [3H]- N-alpha-methylhistamine from histamine H3 receptor B 8.15 pKi 7 nM Ki Bioorg Med Chem Lett (1998) 8: 1133-1138 [PMID:9871722]
ChEMBL Binding affinity against H3 receptor in rat cerebral cortex membranes was evaluated using [3H]N-methyl-histamine as radioligand B 8.2 pKi 6.31 nM Ki Bioorg Med Chem Lett (1996) 6: 833-838
GtoPdb - - 8.3 pKi - - - Eur J Pharmacol (2002) 453: 33-41 [PMID:12393057]
ChEMBL Displacement of [3H](R)-alpha-methylhistamine from histamine H3 receptor in rat brain membranes B 8.6 pKi 2.5 nM Ki Bioorg Med Chem (2018) 26: 4034-4046 [PMID:29960729]

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]