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 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]