JNJ-39758979 [Ligand Id: 8984] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3236549
  • H3 receptor/Histamine H3 receptor in Human [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
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  • H1 receptor in Human [GtoPdb: 262] [UniProtKB: P35367]
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  • H2 receptor in Human [GtoPdb: 263] [UniProtKB: P25021]
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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 Displacement of [3H]N-alpha-methylhistamine from human recombinant histamine H3 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis B 5.98 pKi 1043 nM Ki J. Med. Chem. (2014) 57: 2429-2439 [PMID:24495018]
GtoPdb - - 6 pKi 1000 nM Ki Pharmacol Rev (2015) 67: 601-55 [PMID:26084539]
H4 receptor/Histamine H4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8]
ChEMBL Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis B 7.9 pKd 12.59 nM Kd J. Med. Chem. (2014) 57: 2429-2439 [PMID:24495018]
ChEMBL Agonist activity at human H4 receptor B 5 pKi >10000 nM Ki J. Med. Chem. (2014) 57: 2429-2439 [PMID:24495018]
GtoPdb - - 7.9 pKi 12.5 nM Ki Pharmacol Rev (2015) 67: 601-55 [PMID:26084539];
J Med Chem (2014) 57: 2429-39 [PMID:24495018]
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 7.9 pKi 12.5 nM Ki J. Med. Chem. (2014) 57: 2429-2439 [PMID:24495018]
ChEMBL Displacement of [3H]histamine from human recombinant histamine H4 receptor B 7.92 pKi 12 nM Ki Bioorg. Med. Chem. Lett. (2015) 25: 956-959 [PMID:25595684]
ChEMBL Displacement of [3H]histamine from human recombinant histamine H4 receptor B 7.92 pKi 12 nM Ki J. Med. Chem. (2015) 58: 7119-7127 [PMID:25993395]
H4 receptor/Histamine H4 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5657] [GtoPdb: 265] [UniProtKB: Q91ZY2]
ChEMBL Antagonist activity at mouse histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis B 8.3 pKd 5.01 nM Kd J. Med. Chem. (2014) 57: 2429-2439 [PMID:24495018]
ChEMBL Displacement of [3H]histamine from mouse histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis B 8.28 pKi 5.3 nM Ki J. Med. Chem. (2014) 57: 2429-2439 [PMID:24495018]
ChEMBL Displacement of [3H]histamine from mouse recombinant histamine H4 receptor B 8.28 pKi 5.3 nM Ki J. Med. Chem. (2015) 58: 7119-7127 [PMID:25993395]
H4 receptor/Histamine H4 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4468] [GtoPdb: 265] [UniProtKB: Q91ZY1]
ChEMBL Antagonist activity at rat histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis B 7.2 pKd 63.1 nM Kd J. Med. Chem. (2014) 57: 2429-2439 [PMID:24495018]
ChEMBL Displacement of [3H]histamine from rat histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis B 6.73 pKi 188 nM Ki J. Med. Chem. (2014) 57: 2429-2439 [PMID:24495018]
ChEMBL Displacement of [3H]histamine from rat recombinant histamine H4 receptor B 6.73 pKi 188 nM Ki J. Med. Chem. (2015) 58: 7119-7127 [PMID:25993395]
Histamine H4 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1255160] [UniProtKB: Q91ZY3]
ChEMBL Binding affinity to guinea pig histamine H4 receptor B 6.51 pKi 306 nM Ki J. Med. Chem. (2014) 57: 2429-2439 [PMID:24495018]
ChEMBL Displacement of [3H]histamine from guinea pig recombinant histamine H4 receptor B 6.51 pKi 306 nM Ki J. Med. Chem. (2015) 58: 7119-7127 [PMID:25993395]
H1 receptor in Human [GtoPdb: 262] [UniProtKB: P35367]
GtoPdb - - 6 pKi >1000 nM Ki Pharmacol Rev (2015) 67: 601-55 [PMID:26084539]
H2 receptor in Human [GtoPdb: 263] [UniProtKB: P25021]
GtoPdb - - 6 pKi >1000 nM Ki Pharmacol Rev (2015) 67: 601-55 [PMID:26084539]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]