oleic acid [Ligand Id: 1054] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL8659 (18:1(N-9), 9-octadecenoic acid, (z)-, 9z-octadecenoic acid, FEMA NO. 2815, NSC-9856, Oleate, Oleic acid, Priolene 6936, Vopcolene 27, Wecoline oo)
  • Fatty acid amide hydrolase/Anandamide amidohydrolase in Human [ChEMBL: CHEMBL2243] [GtoPdb: 1400] [UniProtKB: O00519]
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  • coagulation factor VII/coagulation factor III, tissue factor/Coagulation factor VII/tissue factor in Human [ChEMBL: CHEMBL2095194] [GtoPdb: 23633192] [UniProtKB: P08709P13726]
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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 5/Fatty acid binding protein epidermal in Human [ChEMBL: CHEMBL3674] [GtoPdb: 2535] [UniProtKB: Q01469]
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  • fatty acid binding protein 1/Fatty acid-binding protein, liver in Human [ChEMBL: CHEMBL5421] [GtoPdb: 2531] [UniProtKB: P07148]
  • fatty acid binding protein 1/Fatty acid-binding protein, liver in Rat [ChEMBL: CHEMBL5738] [GtoPdb: 2531] [UniProtKB: P02692]
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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 non-receptor type 1/Protein-tyrosine phosphatase 1B in Human [ChEMBL: CHEMBL335] [GtoPdb: 2976] [UniProtKB: P18031]
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  • Telomerase reverse transcriptase in Human [ChEMBL: CHEMBL2916] [UniProtKB: O14746]
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  • TRPV2/Transient receptor potential cation channel subfamily V member 2 in Rat [ChEMBL: CHEMBL2863] [GtoPdb: 508] [UniProtKB: Q9WUD2]
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  • FFA4 receptor in Human [GtoPdb: 127] [UniProtKB: Q5NUL3]
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  • FFA1 receptor in Human [GtoPdb: 225] [UniProtKB: O14842]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Fatty acid amide hydrolase/Anandamide amidohydrolase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2243] [GtoPdb: 1400] [UniProtKB: O00519]
ChEMBL Inhibition of FAAH B 5.22 pKi 6000 nM Ki J. Med. Chem. (2008) 51: 7327-7343 [PMID:18983142]
coagulation factor VII/coagulation factor III, tissue factor/Coagulation factor VII/tissue factor in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095194] [GtoPdb: 23633192] [UniProtKB: P08709P13726]
ChEMBL Inhibition of amidolytic activity of human tissue factor/human factor 7a B 4.1 pIC50 80000 nM IC50 J. Nat. Prod. (1998) 61: 1352-1355 [PMID:9834151]
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 4.49 pIC50 32700 nM IC50 J. Nat. Prod. (2006) 69: 700-703 [PMID:16643058]
DNA topoisomerase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1781] [GtoPdb: 2636] [UniProtKB: P11387]
ChEMBL Inhibition of DNA topoisomerase 1 B 4.51 pIC50 31000 nM IC50 J. Nat. Prod. (2002) 65: 1715-1718 [PMID:12444712]
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 5.82 pKi 1500 nM Ki Bioorg. Med. Chem. (2016) 24: 4310-4317 [PMID:27460668]
ChEMBL Displacement of 1,8-ANS from aFABP by fluorescence based-assay B 6.73 pKi 185 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 3511-3515 [PMID:17502136]
ChEMBL Displacement of 8-anilino-1-naphthalene-sulfonic acid from human His-FABP4 expressed in Escherichia coli BL21 (DE3) cells after 3 mins B 4.58 pIC50 26100 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 3675-3679 [PMID:20471252]
fatty acid binding protein 5/Fatty acid binding protein epidermal in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3674] [GtoPdb: 2535] [UniProtKB: Q01469]
ChEMBL Displacement of 1,8-ANS from eFABP by fluorescence based-assay B 6.61 pKi 248 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 3511-3515 [PMID:17502136]
fatty acid binding protein 1/Fatty acid-binding protein, liver in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5421] [GtoPdb: 2531] [UniProtKB: P07148]
ChEMBL Binding affinity to L-FABP low binding affinity site by titration calorimetry method B 6.05 pKd 900 nM Kd J. Med. Chem. (2008) 51: 3755-3764 [PMID:18533710]
ChEMBL Binding affinity to L-FABP high binding affinity site by titration calorimetry method B 6.7 pKd 200 nM Kd J. Med. Chem. (2008) 51: 3755-3764 [PMID:18533710]
fatty acid binding protein 1/Fatty acid-binding protein, liver in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5738] [GtoPdb: 2531] [UniProtKB: P02692]
ChEMBL Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FABP low binding affinity site expressed in Escherichia coli BL21 by competitive fluorescence displacement assay B 5.54 pKi 2900 nM Ki J. Med. Chem. (2008) 51: 3755-3764 [PMID:18533710]
ChEMBL Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FABP high binding affinity site expressed in Escherichia coli BL21 by competitive fluorescence displacement assay B 6.74 pKi 180 nM Ki J. Med. Chem. (2008) 51: 3755-3764 [PMID:18533710]
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 6.22 pIC50 600 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 6.22 pIC50 600 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 5.28 pIC50 5300 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 Displacement of [3H]BRL49653 from Homo sapiens (human) PPARgamma receptor by scintillation proximity assay B 5.39 pIC50 4100 nM IC50 Med Chem Res (2013) 22: 3126-3133
protein tyrosine phosphatase non-receptor type 1/Protein-tyrosine phosphatase 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL335] [GtoPdb: 2976] [UniProtKB: P18031]
ChEMBL Inhibition of PTP1B (unknown origin) using pNPP as substrate incubated for 30 mins by photometric method B 5.21 pIC50 6200 nM IC50 J Nat Prod (2020) 83: 1598-1610 [PMID:32255628]
Seed lipoxygenase-1 in Glycine max (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4586] [UniProtKB: P08170]
ChEMBL Binding affinity to soybean LO1 B 4.66 pKi 22000 nM Ki Bioorg. Med. Chem. (2009) 17: 6534-6539 [PMID:19716306]
Telomerase reverse transcriptase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2916] [UniProtKB: O14746]
ChEMBL Inhibition of telomerase extracted from human K562 cells preincubated for 10 mins followed by dNTPs and telomerase substrate primer TS-A addition measured after 30 mins by TRAP assay B 5.07 pIC50 8600 nM IC50 MedChemComm (2011) 2: 229-245
TRPV2/Transient receptor potential cation channel subfamily V member 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2863] [GtoPdb: 508] [UniProtKB: Q9WUD2]
ChEMBL Antagonist activity at recombinant rat TRPV2 expressed in HEK293 cells assessed as inhibition of LPC-induced Ca2+ levels preincubated for 5 mins followed by agonist addition by Fuo-4-AM based spectrofluorimetry B 5 pIC50 >10000 nM IC50 J Med Chem (2018) 61: 8255-8281 [PMID:30176215]
ChEMBL Antagonist activity at recombinant rat TRPV2 expressed in HEK293 cells assessed as inhibition of CBD-induced Ca2+ levels preincubated for 5 mins followed by agonist addition by Fuo-4-AM based spectrofluorimetry B 5 pIC50 >10000 nM IC50 J Med Chem (2018) 61: 8255-8281 [PMID:30176215]
FFA4 receptor in Human [GtoPdb: 127] [UniProtKB: Q5NUL3]
GtoPdb - - 4.7 pEC50 - - - Mol Pharmacol (2012) 81: 631-42 [PMID:22282525]
FFA1 receptor in Human [GtoPdb: 225] [UniProtKB: O14842]
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]

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, 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]