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 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]
