GSK-189254 [Ligand Id: 10736] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL517140 (Gsk189254, GSK189254)
  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
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  • H2 receptor/Histamine H2 receptor in Human [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
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  • 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]
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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
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
ChEMBL Binding affinity to human histamine H1 receptor B 5.6 pKi >2511.89 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 6890-6896 [PMID:24269482]
H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
ChEMBL Binding affinity to human histamine H2 receptor B 5.5 pKi >3162.28 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 6890-6896 [PMID:24269482]
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
ChEMBL Displacement of [3H]N-R-methylhistamine from human H3 receptor isolated from C6 cells B 9.59 pKi 0.26 nM Ki J. Med. Chem. (2010) 53: 7869-7873 [PMID:20945906]
ChEMBL Displacement of [3H]-R-alpha-ethylhistamine from histamine H3 receptor in human cerebral cortical tissue membranes after 45 mins by liquid scintillation spectrometry B 9.59 pKi 0.26 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 6890-6896 [PMID:24269482]
GtoPdb - - 9.7 pKi 0.2 nM Ki J Pharmacol Exp Ther (2007) 321: 1032-45 [PMID:17327487]
ChEMBL Antagonist activity at human histamine H3 receptor expressed in CHOK1 cells assessed as inhibition of GTPgammaS binding F 9.7 pKi 0.2 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 6890-6896 [PMID:24269482]
ChEMBL Binding affinity to human histamine H3 receptor B 9.9 pKi 0.13 nM Ki J. Med. Chem. (2011) 54: 26-53 [PMID:21062081]
ChEMBL Displacement of [3H]-R-alpha-ethylhistamine from human histamine H3 receptor expressed in HEK293 cells after 45 mins by liquid scintillation spectrometry B 9.9 pKi 0.13 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 6890-6896 [PMID:24269482]
ChEMBL Binding affinity to histamine H3 receptor B 9.92 pKi 0.12 nM Ki J. Med. Chem. (2009) 52: 3855-3868 [PMID:19456097]
ChEMBL Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding F 9.26 pIC50 0.55 nM IC50 J. Med. Chem. (2008) 51: 6889-6901 [PMID:18841880]
H3 receptor/Histamine H3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8]
ChEMBL Displacement of [3H]-R-alpha-ethylhistamine from histamine H3 receptor in rat cerebral cortical tissue membranes after 45 mins by liquid scintillation spectrometry B 8.58 pKi 2.63 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 6890-6896 [PMID:24269482]
ChEMBL Displacement of [3H]-R-alpha-ethylhistamine from rat histamine H3 receptor expressed in HEK293 cells after 45 mins by liquid scintillation spectrometry B 9.17 pKi 0.68 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 6890-6896 [PMID:24269482]
ChEMBL Binding affinity to rat cortical histamine H3 receptor B 9.2 pKi 0.63 nM Ki J. Med. Chem. (2011) 54: 26-53 [PMID:21062081]
H4 receptor/Histamine H4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8]
ChEMBL Binding affinity to human histamine H4 receptor B 5.5 pKi >3162.28 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 6890-6896 [PMID:24269482]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]