JNJ-39758979 [Ligand Id: 8984] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3236549 (Jnj 39758979, Jnj-39758979, JNJ39758979) |
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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 35:
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]
