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

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ChEMBL ligand: CHEMBL3236549 (Jnj 39758979, Jnj-39758979, JNJ39758979)
  • H3 receptor/Histamine H3 receptor in Human [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
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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 F 7.9 pKd 12.59 nM Kd J Med Chem (2014) 57: 2429-2439 [PMID:24495018]
ChEMBL Cell based cAMP Assays (pA2) B 7.9 pKd 12.59 nM Kd Data for DCP probe JNJ-39758979
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 Binding assay B 7.9 pKi 12.5 nM Ki Data for DCP probe JNJ-39758979
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 F 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]
ChEMBL mBMMC chemotaxis B 8.1 pIC50 8 nM IC50 Data for DCP probe JNJ-39758979
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 F 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]
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL M1 (h) CEREP panel B 8 pKi >10 nM Ki Data for DCP probe JNJ-39758979
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL M2 (h) CEREP panel B 8 pKi >10 nM Ki Data for DCP probe JNJ-39758979
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
ChEMBL M3 (h) CEREP panel B 8 pKi >10 nM Ki Data for DCP probe JNJ-39758979
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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]