UCL-2138 [Ligand Id: 1257] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL129257 (UCL-2138)
  • H3 receptor/Histamine H3 receptor in Human [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
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  • H4 receptor/Histamine H4 receptor in Human [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8]
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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 Mean binding affinity for human H3 receptor B 7.6 pKi 25.12 nM Ki J Med Chem (2005) 48: 2229-2238 [PMID:15771465]
GtoPdb - - 7.6 pKi - - - Mol Pharmacol (2001) 59: 420-6 [PMID:11179434]
ChEMBL Binding affinity to the human histamine H3 receptor B 7.6 pKi 25 nM Ki J Med Chem (2003) 46: 3957-3960 [PMID:12954048]
ChEMBL Displacement of [125I]iodoproxyfan from human histamine H3 receptor expressed in HEL293 cells B 7.96 pKi 11 nM Ki Bioorg Med Chem Lett (2009) 19: 2172-2175 [PMID:19286376]
H4 receptor/Histamine H4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8]
ChEMBL Binding affinity to the human histamine H4 receptor B 5 pKi >10000 nM Ki J Med Chem (2003) 46: 3957-3960 [PMID:12954048]

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]