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ChEMBL ligand: CHEMBL185951 (JNJ-10191584) |
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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 | 4.7 | pKi | 20000 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1156-1159 [PMID:22189138] |
ChEMBL | Binding affinity to histamine H3 receptor | B | 4.85 | pKi | 14053 | nM | Ki | J Med Chem (2005) 48: 8289-8298 [PMID:16366610] |
ChEMBL | Binding affinity towards human histamine H3 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes | B | 5.4 | pKi | 3981.07 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 5251-5256 [PMID:15454206] |
ChEMBL | Effective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cells | B | 5.5 | pEC50 | 3162.28 | nM | EC50 | Bioorg Med Chem Lett (2004) 14: 5251-5256 [PMID:15454206] |
H4 receptor/Histamine H4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8] | ||||||||
ChEMBL | Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity | F | 7.7 | pKd | 19.95 | nM | Kd | J Med Chem (2005) 48: 8289-8298 [PMID:16366610] |
GtoPdb | - | - | 7.1 | pKi | - | - | - | Bioorg Med Chem Lett (2004) 14: 5251-6 [PMID:15454206] |
ChEMBL | Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes | B | 7.1 | pKi | 79.43 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 5251-5256 [PMID:15454206] |
ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique | B | 7.32 | pKi | 47.7 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 6591-6595 [PMID:21955944] |
ChEMBL | Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay | B | 7.32 | pKi | 47.7 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1156-1159 [PMID:22189138] |
ChEMBL | Antagonist activity at human histamine H4 receptor by functional assay | F | 7.4 | pKi | 39.6 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 6591-6595 [PMID:21955944] |
ChEMBL | Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay | F | 7.4 | pKi | 39.6 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1156-1159 [PMID:22189138] |
ChEMBL | Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes | B | 7.59 | pKi | 26 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 461-467 [PMID:22153663] |
ChEMBL | Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells | B | 7.59 | pKi | 26 | nM | Ki | J Med Chem (2005) 48: 8289-8298 [PMID:16366610] |
ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor | B | 7.59 | pKi | 26 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 3113-3116 [PMID:21458260] |
ChEMBL | Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis | B | 7.7 | pKi | 20 | nM | Ki | J Med Chem (2014) 57: 2429-2439 [PMID:24495018] |
ChEMBL | Inhibition of human eosinophil chemotaxis mediated by histamine H4 receptor | F | 6.28 | pIC50 | 530 | nM | IC50 | J Med Chem (2005) 48: 8289-8298 [PMID:16366610] |
ChEMBL | Inhibition of mouse bone-marrow mast cell chemotaxis mediated by histamine H4 receptor | F | 6.86 | pIC50 | 138 | nM | IC50 | J Med Chem (2005) 48: 8289-8298 [PMID:16366610] |
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]