EPA [Ligand Id: 3362] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL460026 (All-cis-fatty acid 20:5 omega-3, C20:5 (n-3), Eicosapentaenoate, Eicosapentaenoic acid, Eicosapentaenoic acid (c20:5 n3), EPA 45G, Icosapent, Incromega e 7010sr, Omega-3 marine triglycerides, Ropufa 70, Timnodonic acid)
  • coagulation factor VII/coagulation factor III, tissue factor/Coagulation factor VII/tissue factor in Human [ChEMBL: CHEMBL2095194] [GtoPdb: 2363, 3192] [UniProtKB: P08709, P13726]
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  • Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
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  • Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
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  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
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  • Retinoid X receptor-α/Retinoid X receptor alpha in Human [ChEMBL: CHEMBL2061] [GtoPdb: 610] [UniProtKB: P19793]
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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 4.11 pIC50 78000 nM IC50 J Nat Prod (1998) 61: 1352-1355 [PMID:9834151]
Cyclooxygenase-1 in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2860] [UniProtKB: O62664]
ChEMBL Inhibition of bovine COX1-mediated prostaglandin biosynthesis using [1-14C]arachidonic acid B 4.89 pIC50 13000 nM IC50 J Nat Prod (2001) 64: 745-749 [PMID:11421736]
Cyclooxygenase-2 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4102] [UniProtKB: P79208]
ChEMBL Inhibition of sheep COX2-mediated prostaglandin biosynthesis using [1-14C]arachidonic acid B 5.15 pIC50 7100 nM IC50 J Nat Prod (2001) 64: 745-749 [PMID:11421736]
CYP19A1/Cytochrome P450 19A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1978] [GtoPdb: 1362] [UniProtKB: P11511]
ChEMBL Inhibition of aromatase in human placental microsomes by radiometric method B 4.27 pIC50 53200 nM IC50 J Nat Prod (2006) 69: 700-703 [PMID:16643058]
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 5.96 pIC50 1100 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 5.96 pIC50 1100 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 5.4 pIC50 4000 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 Binding affinity to PPARgamma B 5.7 pKd 2000 nM Kd J Med Chem (2012) 55: 4027-4061 [PMID:22260081]
ChEMBL Displacement of [3H]BRL49653 from Homo sapiens (human) PPARgamma receptor by scintillation proximity assay B 5.8 pIC50 1600 nM IC50 Med Chem Res (2013) 22: 3126-3133
Retinoid X receptor-α/Retinoid X receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2061] [GtoPdb: 610] [UniProtKB: P19793]
ChEMBL Displacement of CU-6PMN from human RXRalpha LBD incubated for 2 hrs by fluorescence based assay B 5.12 pKi 7632 nM Ki J Med Chem (2019) 62: 8809-8818 [PMID:31483660]

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]