linoleic acid [Ligand Id: 1052] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL267476 (9,12-linoleic acid, C18:2 (n-6), Emersol 315, FEMA NO. 3380, LINOLEIC ACID-, Linoleate, Linoleic acid, Linolic acid, NSC-281243, Octadeca-9,12-Dienoic Acid, Polylin 515, Ronacare asc 3, Unifac 6550)
  • A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
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  • AKR1C3/Aldo-keto-reductase family 1 member C3 in Human [ChEMBL: CHEMBL4681] [GtoPdb: 1382] [UniProtKB: P42330]
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  • 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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  • Dual specificity protein phosphatase 3 in Human [ChEMBL: CHEMBL2635] [UniProtKB: P51452]
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  • fatty acid binding protein 4/Fatty acid binding protein adipocyte in Human [ChEMBL: CHEMBL2083] [GtoPdb: 2534] [UniProtKB: P15090]
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  • fatty acid binding protein 3/Fatty acid binding protein muscle in Human [ChEMBL: CHEMBL3344] [GtoPdb: 2533] [UniProtKB: P05413]
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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]
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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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  • Protein-tyrosine phosphatase LC-PTP in Human [ChEMBL: CHEMBL2219] [UniProtKB: P35236]
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  • Kv2.1 in Human [GtoPdb: 546] [UniProtKB: Q14721]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL Displacement of [3H]DPCPX from rat adenosine A1 receptor by liquid scintillation counting B 4.19 pIC50 65000 nM IC50 J Nat Prod (1999) 62: 912-914 [PMID:10395519]
AKR1C3/Aldo-keto-reductase family 1 member C3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4681] [GtoPdb: 1382] [UniProtKB: P42330]
ChEMBL Inhibition of human AKR1C3 expressed in Escherichia coli BL21(DE3) pLysS cells using 9,10-phenanthrenequinone as substrate B 6.16 pIC50 690 nM IC50 J Med Chem (2020) 63: 11305-11329 [PMID:32463235]
ChEMBL Inhibition of human AKR1C3 expressed in Escherichia coli BL21(DE3) pLysS cells using S-tetralol as substrate B 6.16 pIC50 690 nM IC50 J Med Chem (2020) 63: 11305-11329 [PMID:32463235]
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 4.39 pIC50 41000 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 COX1 B 4.89 pIC50 13000 nM IC50 J Nat Prod (2005) 68: 985-991 [PMID:16038536]
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 4.03 pIC50 94000 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 4.32 pIC50 48000 nM IC50 J Nat Prod (2006) 69: 700-703 [PMID:16643058]
Dual specificity protein phosphatase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2635] [UniProtKB: P51452]
ChEMBL Inhibition of GST-tagged human VHR using pNpp as substrate after 30 mins B 4 pIC50 >100000 nM IC50 Bioorg Med Chem Lett (2011) 21: 6833-6837 [PMID:21962577]
fatty acid binding protein 4/Fatty acid binding protein adipocyte in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2083] [GtoPdb: 2534] [UniProtKB: P15090]
ChEMBL Displacement of 1,8-ANS from His6-tagged FABP4 (unknown origin) expressed in Escherichia coli BL21(DE3) cells by fluorescence assay B 5.17 pKi 6800 nM Ki Bioorg Med Chem (2016) 24: 4310-4317 [PMID:27460668]
ChEMBL Inhibition of FABP4 (unknown origin) B 4.75 pIC50 17700 nM IC50 Eur J Med Chem (2015) 90: 241-250 [PMID:25461324]
ChEMBL Displacement of 8-anilino-1-naphthalene-sulfonic acid from human His-FABP4 expressed in Escherichia coli BL21 (DE3) cells after 3 mins B 4.87 pIC50 13600 nM IC50 Bioorg Med Chem Lett (2010) 20: 3675-3679 [PMID:20471252]
ChEMBL Displacement of 8-anilino-1-naphthalene-sulfonic acid from human His-FABP4 expressed in Escherichia coli BL21 (DE3) cells after 3 mins relative to linoleic acid B 6 pIC50 1000 nM IC50 Bioorg Med Chem Lett (2010) 20: 3675-3679 [PMID:20471252]
fatty acid binding protein 3/Fatty acid binding protein muscle in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3344] [GtoPdb: 2533] [UniProtKB: P05413]
ChEMBL Displacement of 1,8-ANS from His6-tagged FABP3 (unknown origin) expressed in Escherichia coli BL21(DE3) cells by fluorescence assay B 5.03 pKi 9300 nM Ki Bioorg Med Chem (2016) 24: 4310-4317 [PMID:27460668]
ChEMBL Displacement of 8-anilino-1-naphthalene-sulfonic acid from human His-FABP3 expressed in Escherichia coli BL21 (DE3) cells after 3 mins relative to linoleic acid B 6 pIC50 1000 nM IC50 Bioorg Med Chem Lett (2010) 20: 3675-3679 [PMID:20471252]
ChEMBL Inhibition of FABP4 (unknown origin) relative to linoleic acid B 6 pIC50 1000 nM IC50 Eur J Med Chem (2015) 90: 241-250 [PMID:25461324]
ChEMBL Inhibition of FABP3 (unknown origin) relative to linoleic acid B 6 pIC50 1000 nM IC50 Eur J Med Chem (2015) 90: 241-250 [PMID:25461324]
FFA1 receptor/Free fatty acid receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4422] [GtoPdb: 225] [UniProtKB: O14842]
ChEMBL Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay F 5.32 pEC50 4800 nM EC50 Bioorg Med Chem (2018) 26: 5780-5791 [PMID:30392954]
ChEMBL Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay F 5.32 pEC50 4800 nM EC50 Bioorg Med Chem Lett (2019) 29: 848-852 [PMID:30685095]
GtoPdb - - 5.7 pEC50 1990 nM EC50 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]
ChEMBL Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay F 5.74 pEC50 1800 nM EC50 Bioorg Med Chem Lett (2008) 18: 6357-6361 [PMID:18993064]
ChEMBL Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay F 6.26 pEC50 549.54 nM EC50 Bioorg Med Chem Lett (2008) 18: 6357-6361 [PMID:18993064]
ChEMBL Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay F 6.27 pEC50 540 nM EC50 Bioorg Med Chem Lett (2008) 18: 6357-6361 [PMID:18993064]
ChEMBL Agonist activity at GPR40 F 6.27 pEC50 540 nM EC50 Bioorg Med Chem Lett (2008) 18: 6357-6361 [PMID:18993064]
FFA4 receptor/G-protein coupled receptor 120 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5339] [GtoPdb: 127] [UniProtKB: Q5NUL3]
GtoPdb - - 5.89 pEC50 - - EC50 Br J Pharmacol (2006) 148: 619-28 [PMID:16702987]
ChEMBL Agonist activity at human FFA4 receptor expressed in U2OS cells assessed as calcium mobilization after 24 hrs by FLIPR F 6.5 pEC50 316.23 nM EC50 Bioorg Med Chem Lett (2014) 24: 3100-3103 [PMID:24881566]
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 8.32 pKd 4.8 nM Kd Med Chem Res (2009) 18: 8-19
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 pIC50 10000 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]
GtoPdb - - 5.3 pKd - - - Eur J Pharmacol (2001) 417: 77-89 [PMID:11301062];
Eur J Biochem (2004) 271: 386-97 [PMID:14717706]
ChEMBL Displacement of [3H]BRL49653 from Homo sapiens (human) PPARgamma receptor by scintillation proximity assay B 5.21 pIC50 6200 nM IC50 Med Chem Res (2013) 22: 3126-3133
Protein-tyrosine phosphatase LC-PTP in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2219] [UniProtKB: P35236]
ChEMBL Inhibition of GST-tagged human HePTP using pNpp as substrate after 30 mins B 4 pIC50 >100000 nM IC50 Bioorg Med Chem Lett (2011) 21: 6833-6837 [PMID:21962577]
Seed lipoxygenase-1 in Glycine max (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4586] [UniProtKB: P08170]
ChEMBL Mixed-type inhibition of soybean LO1 B 4.89 pIC50 13000 nM IC50 Bioorg Med Chem (2009) 17: 6534-6539 [PMID:19716306]
ChEMBL Competitive inhibition of soybean LO1 B 4.96 pIC50 11000 nM IC50 Bioorg Med Chem (2009) 17: 6534-6539 [PMID:19716306]
ChEMBL Allosteric inhibition of soybean LO1 B 6 pIC50 1000 nM IC50 Bioorg Med Chem (2009) 17: 6534-6539 [PMID:19716306]
Kv2.1 in Human [GtoPdb: 546] [UniProtKB: Q14721]
GtoPdb - - 5.1 pIC50 - - - Am J Physiol, Cell Physiol (2001) 281: C1277-84 [PMID:11546665]
GtoPdb - - 5.6 pEC50 - - - Am J Physiol, Cell Physiol (2001) 281: C1277-84 [PMID:11546665]

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]