diroleuton [Ligand Id: 9775] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL465183 (20:3(N-6), 20:3 (.omega.-6) fatty acid, 8z,11z,14z-eicosatrienoic acid, Bishomo-.gamma.-linolenic acid, Cis-8,11,14-Eicosatrienoicacid, Daleuton, Dihomo-.gamma.-linolenic acid, Dihomo-gamma-linolenic acid, Diroleuton, Ds-107, Ds107, DS-107G, DS107G, .gamma.-homolinolenic acid, RO 12-1989) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| coagulation factor VII/coagulation factor III, tissue factor/Coagulation factor VII/tissue factor in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095194] [GtoPdb: 2363, 3192] [UniProtKB: P08709, P13726] | ||||||||
| ChEMBL | Inhibition of amidolytic activity of human tissue factor/human factor 7a | B | 4.12 | pIC50 | 75000 | nM | IC50 | J Nat Prod (1998) 61: 1352-1355 [PMID:9834151] |
| ChEMBL | Inhibition of amidolytic activity of human tissue factor/human factor 7a | B | 4.52 | pIC50 | 30000 | nM | IC50 | J Nat Prod (1998) 61: 1352-1355 [PMID:9834151] |
| OXE receptor/Oxoeicosanoid receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1628461] [GtoPdb: 271] [UniProtKB: Q8TDS5] | ||||||||
| ChEMBL | Antagonist activity at human OXE receptor fused with G-alphai assessed as inhibition of 5-oxo-ETE-induced GTPgammaS binding after 60 mins by liquid scintillation counting analysis | F | 5.7 | pIC50 | 2000 | nM | IC50 | J Med Chem (2014) 57: 364-377 [PMID:24351031] |
| Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869] | ||||||||
| ChEMBL | Inhibition of PPAR-alpha (unknown origin) by SPA assay | B | 5.85 | pIC50 | 1400 | nM | IC50 | Med Chem Res (2009) 18: 8-19 |
| ChEMBL | Displacement of [3H]GW2331 from Homo sapiens (human) PPARalpha receptor by scintillation proximity assay | B | 5.85 | pIC50 | 1400 | nM | IC50 | Med Chem Res (2013) 22: 3126-3133 |
| Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181] | ||||||||
| ChEMBL | Displacement of [3H]GW2433 from Homo sapiens (human) PPARdelta receptor by scintillation proximity assay | B | 5.37 | pIC50 | 4300 | nM | IC50 | Med Chem Res (2013) 22: 3126-3133 |
| Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231] | ||||||||
| ChEMBL | Displacement of [3H]BRL49653 from Homo sapiens (human) PPARgamma receptor by scintillation proximity assay | B | 5.62 | pIC50 | 2400 | nM | IC50 | Med Chem Res (2013) 22: 3126-3133 |
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]
