JNJ-10191584 [Ligand Id: 1277] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL185951 (JNJ-10191584)
  • H3 receptor/Histamine H3 receptor in Human [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
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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
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]