GSK-189254 [Ligand Id: 10736] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL517140 (Gsk189254, GSK189254) |
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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 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]
