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ChEMBL ligand: CHEMBL2151157 (GSK334429) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1] | ||||||||
ChEMBL | Binding affinity to human histamine H3 receptor | B | 9.5 | pKi | 0.32 | nM | Ki | J Med Chem (2011) 54: 26-53 [PMID:21062081] |
GtoPdb | - | - | 9.89 | pKi | 0.13 | nM | Ki |
J Med Chem (2011) 54: 26-53 [PMID:21062081]; Eur J Med Chem (2014) 86: 578-88 [PMID:25218907] |
ChEMBL | Displacement of [3H]N-alpha-Methylhistamine from human recombinant H3 receptor expressed in HEK293 cells by competitive binding assay | B | 9.9 | pKi | 0.13 | nM | Ki | Eur J Med Chem (2014) 86: 578-588 [PMID:25218907] |
ChEMBL | Inverse agonist activity at human histamine H3 receptor by GTPgammaS binding assay | F | 8.6 | pIC50 | 2.51 | nM | IC50 | J Med Chem (2011) 54: 26-53 [PMID:21062081] |
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]