VUF 5207 [Ligand Id: 1245] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL206548
  • 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 Displacement of [3H]N-alpha-methylhistamine from human H3 receptor expressed in SK-N-MC cells B 7.8 pKi 15.85 nM Ki J Med Chem (2006) 49: 2549-2557 [PMID:16610798]
GtoPdb - - 7.8 pKi - - - J Pharmacol Exp Ther (2001) 299: 908-14 [PMID:11714875]
ChEMBL Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells F 7.5 pEC50 31.62 nM EC50 J Med Chem (2006) 49: 2549-2557 [PMID:16610798]
H4 receptor/Histamine H4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8]
ChEMBL Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells B 6.3 pKi 501.19 nM Ki J Med Chem (2006) 49: 2549-2557 [PMID:16610798]

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]