α-linolenic acid [Ligand Id: 1049] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL8739
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  • FFA1 receptor/Free fatty acid receptor 1 in Human [ChEMBL: CHEMBL4422] [GtoPdb: 225] [UniProtKB: O14842]
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  • FFA4 receptor/G-protein coupled receptor 120 in Human [ChEMBL: CHEMBL5339] [GtoPdb: 127] [UniProtKB: Q5NUL3]
  • FFA4 receptor in Rat [GtoPdb: 127] [UniProtKB: Q2AC31]
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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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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
coagulation factor VII/Coagulation factor VII/tissue factor in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095194] [GtoPdb: 2363] [UniProtKB: P08709P13726]
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]
COX-1 /Cyclooxygenase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219]
ChEMBL Inhibition of COX-1 (unknown origin) using arachidonic acid as substrate assessed as formation of prostanoid products preincubated for 10 mins prior to substrate addition measured after 2 mins by Ellman's method B 5.4 pKi 4000 nM Ki J. Med. Chem. (2013) 56: 8377-8388 [PMID:24088053]
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 4.03 pIC50 93000 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 4.92 pIC50 12000 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 4.35 pIC50 44200 nM IC50 J. Nat. Prod. (2006) 69: 700-703 [PMID:16643058]
FFA1 receptor/Free fatty acid receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4422] [GtoPdb: 225] [UniProtKB: O14842]
ChEMBL Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay F 4.96 pEC50 11090 nM EC50 Eur J Med Chem (2018) 158: 123-133 [PMID:30212763]
ChEMBL Agonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay F 5.28 pEC50 5200 nM EC50 J. Med. Chem. (2008) 51: 7640-7644 [PMID:19007110]
ChEMBL Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay B 5.5 pEC50 3162.28 nM EC50 J. Med. Chem. (2016) 59: 2841-2846 [PMID:26928019]
ChEMBL Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay B 5.52 pEC50 3000 nM EC50 J. Med. Chem. (2016) 59: 2841-2846 [PMID:26928019]
ChEMBL Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay F 5.54 pEC50 2884.03 nM EC50 J. Med. Chem. (2012) 55: 4511-4515 [PMID:22519963]
GtoPdb - - 5.7 pEC50 - - - J Biol Chem (2003) 278: 11303-11 [PMID:12496284];
Biochem Biophys Res Commun (2003) 301: 406-10 [PMID:12565875];
Nature (2003) 422: 173-6 [PMID:12629551]
FFA4 receptor/G-protein coupled receptor 120 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5339] [GtoPdb: 127] [UniProtKB: Q5NUL3]
ChEMBL Agonist activity at GPR120 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 5 mins by BRET assay F 5.49 pEC50 3235.94 nM EC50 J. Med. Chem. (2012) 55: 4511-4515 [PMID:22519963]
GtoPdb - - 5.5 pEC50 - - - J Med Chem (2012) 55: 4511-5 [PMID:22519963]
ChEMBL Agonist activity at human GPR120-G-alpha-16 fusion protein expressed in Flp-in HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay F 5.59 pEC50 2600 nM EC50 J. Med. Chem. (2008) 51: 7640-7644 [PMID:19007110]
FFA4 receptor in Rat [GtoPdb: 127] [UniProtKB: Q2AC31]
GtoPdb - - 5.06 pEC50 - - - Naunyn Schmiedebergs Arch Pharmacol (2008) 377: 515-22 [PMID:18320172]
Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
ChEMBL Binding affinity to PPAR-alpha (unknown origin) by fluorescence-based assay B 8.1 pKd 7.9 nM Kd Med Chem Res (2009) 18: 8-19
ChEMBL Inhibition of PPAR-alpha (unknown origin) by SPA assay B 5.92 pIC50 1200 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 5.92 pIC50 1200 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 4.8 pIC50 16000 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 5.22 pIC50 6000 nM IC50 Med Chem Res (2013) 22: 3126-3133

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]