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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]