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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL267476 (Linoleic acid, NSC-281243, FEMA NO. 3380, LINOLEIC ACID-, Octadeca-9,12-Dienoic Acid)
  • A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
  • This target only has 0 pki data point
1 CHEMBL267476_lig_chart_1 Adenosine A1 receptor Rat
There should be some charts here, you may need to enable JavaScript!
  • coagulation factor VII/Coagulation factor VII/tissue factor in Human [ChEMBL: CHEMBL2095194] [GtoPdb: 2363] [UniProtKB: P08709P13726]
  • This target only has 0 pki data point
2 CHEMBL267476_lig_chart_2 Coagulation factor VII/tissue factor Human
There should be some charts here, you may need to enable JavaScript!
  • COX-1 /Cyclooxygenase-1 in Human [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219]
  • This target only has 0 pki data point
3 CHEMBL267476_lig_chart_3 Cyclooxygenase-1 Human
There should be some charts here, you may need to enable JavaScript!
  • Cyclooxygenase-2 in Sheep [ChEMBL: CHEMBL4102] [UniProtKB: P79208]
  • This target only has 0 pki data point
4 CHEMBL267476_lig_chart_4 Cyclooxygenase-2 Sheep
There should be some charts here, you may need to enable JavaScript!
  • CYP19A1/Cytochrome P450 19A1 in Human [ChEMBL: CHEMBL1978] [GtoPdb: 1362] [UniProtKB: P11511]
  • This target only has 0 pki data point
5 CHEMBL267476_lig_chart_5 Cytochrome P450 19A1 Human
There should be some charts here, you may need to enable JavaScript!
  • Dual specificity protein phosphatase 3 in Human [ChEMBL: CHEMBL2635] [UniProtKB: P51452]
  • This target only has 0 pki data point
6 CHEMBL267476_lig_chart_6 Dual specificity protein phosphatase 3 Human
There should be some charts here, you may need to enable JavaScript!
  • fatty acid binding protein 4/Fatty acid binding protein adipocyte in Human [ChEMBL: CHEMBL2083] [GtoPdb: 2534] [UniProtKB: P15090]
  • This target only has 1 pki data point
7 CHEMBL267476_lig_chart_7 Fatty acid binding protein adipocyte Human
There should be some charts here, you may need to enable JavaScript!
  • fatty acid binding protein 3/Fatty acid binding protein muscle in Human [ChEMBL: CHEMBL3344] [GtoPdb: 2533] [UniProtKB: P05413]
  • This target only has 1 pki data point
8 CHEMBL267476_lig_chart_8 Fatty acid binding protein muscle Human
There should be some charts here, you may need to enable JavaScript!
  • FFA1 receptor/Free fatty acid receptor 1 in Human [ChEMBL: CHEMBL4422] [GtoPdb: 225] [UniProtKB: O14842]
  • This target only has 0 pki data point
9 CHEMBL267476_lig_chart_9 Free fatty acid receptor 1 Human
There should be some charts here, you may need to enable JavaScript!
  • FFA4 receptor/G-protein coupled receptor 120 in Human [ChEMBL: CHEMBL5339] [GtoPdb: 127] [UniProtKB: Q5NUL3]
  • This target only has 0 pki data point
10 CHEMBL267476_lig_chart_10 G-protein coupled receptor 120 Human
There should be some charts here, you may need to enable JavaScript!
  • Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
  • This target only has 0 pki data point
11 CHEMBL267476_lig_chart_11 Peroxisome proliferator-activated receptor alpha Human
There should be some charts here, you may need to enable JavaScript!
  • Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
  • This target only has 0 pki data point
12 CHEMBL267476_lig_chart_12 Peroxisome proliferator-activated receptor delta Human
There should be some charts here, you may need to enable JavaScript!
  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
  • This target only has 0 pki data point
13 CHEMBL267476_lig_chart_13 Peroxisome proliferator-activated receptor gamma Human
There should be some charts here, you may need to enable JavaScript!
  • Protein-tyrosine phosphatase LC-PTP in Human [ChEMBL: CHEMBL2219] [UniProtKB: P35236]
  • This target only has 0 pki data point
14 CHEMBL267476_lig_chart_14 Protein-tyrosine phosphatase LC-PTP Human
There should be some charts here, you may need to enable JavaScript!
  • Seed lipoxygenase-1 in Glycine max [ChEMBL: CHEMBL4586] [UniProtKB: P08170]
  • This target only has 0 pki data point
15 CHEMBL267476_lig_chart_15 Seed lipoxygenase-1 Glycine max
There should be some charts here, you may need to enable JavaScript!
  • Kv2.1 in Human [GtoPdb: 546] [UniProtKB: Q14721]
  • This target only has 0 pki data point
16 CHEMBL267476_lig_chart_16 Kv2.1 Human
There should be some charts here, you may need to enable JavaScript!
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]
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 4.39 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]
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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]