arachidonic acid [Ligand Id: 2391] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL15594 (Arachidonic Acid, Cis-5,8,11,14-Eicosatetraenoic Acid)
  • Fatty acid amide hydrolase/Anandamide amidohydrolase in Human [ChEMBL: CHEMBL2243] [GtoPdb: 1400] [UniProtKB: O00519]
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  • cPLA2-4C/Cytosolic phospholipase A2 gamma in Human [ChEMBL: CHEMBL4834] [GtoPdb: 1426] [UniProtKB: Q9UP65]
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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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  • 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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  • TRPV2/Transient receptor potential cation channel subfamily V member 2 in Rat [ChEMBL: CHEMBL2863] [GtoPdb: 508] [UniProtKB: Q9WUD2]
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  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Rat [ChEMBL: CHEMBL3762] [GtoPdb: 529] [UniProtKB: P22002]
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  • Kir2.3 in Human [GtoPdb: 432] [UniProtKB: P48050]
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  • TRPV4 in Mouse [GtoPdb: 510] [UniProtKB: Q9EPK8]
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  • K2P2.1 in Human [GtoPdb: 514] [UniProtKB: O95069]
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  • K2P3.1 in Human [GtoPdb: 515] [UniProtKB: O14649]
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  • Kv4.2 in Rat [GtoPdb: 553] [UniProtKB: Q63881]
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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 4 pIC50 >100000 nM IC50 J. Med. Chem. (2008) 51: 7327-7343 [PMID:18983142]
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 4.55 pIC50 28200 nM IC50 J. Nat. Prod. (2006) 69: 700-703 [PMID:16643058]
cPLA2-4C/Cytosolic phospholipase A2 gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4834] [GtoPdb: 1426] [UniProtKB: Q9UP65]
ChEMBL Concentration required to inhibit human Cytosolic phospholipase A2 B 4 pIC50 >100000 nM IC50 Bioorg. Med. Chem. Lett. (2001) 11: 587-590 [PMID:11229777]
fatty acid binding protein 4/Fatty acid binding protein adipocyte in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2083] [GtoPdb: 2534] [UniProtKB: P15090]
ChEMBL Binding affinity against Adipocyte lipid binding protein B 6.74 pKd 180 nM Kd J. Med. Chem. (2002) 45: 2469-2483 [PMID:12036355]
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 5.92 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 5.51 pIC50 3100 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 5.8 pIC50 1600 nM IC50 Med Chem Res (2013) 22: 3126-3133
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]
Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3762] [GtoPdb: 529] [UniProtKB: P22002]
ChEMBL Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes F 5.07 pIC50 8500 nM IC50 Journal of Applied Toxicology (2012) 32: 858-866 [PMID:22761000]
ChEMBL Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes F 5.24 pIC50 5800 nM IC50 Journal of Applied Toxicology (2012) 32: 858-866 [PMID:22761000]
Kir2.3 in Human [GtoPdb: 432] [UniProtKB: P48050]
GtoPdb - - 6.35 pEC50 - - - Mol. Pharmacol. (2001) 59: 1061-8 [PMID:11306688]
TRPV4 in Mouse [GtoPdb: 510] [UniProtKB: Q9EPK8]
GtoPdb - - 5 pEC50 - - - Nature (2003) 424: 434-8 [PMID:12879072]
K2P2.1 in Human [GtoPdb: 514] [UniProtKB: O95069]
GtoPdb - - 5 pEC50 10000 nM EC50 EMBO J. (1998) 17: 4283-90 [PMID:9687497]
K2P3.1 in Human [GtoPdb: 515] [UniProtKB: O14649]
GtoPdb - - 1 pIC50 - - - EMBO J. (2001) 20: 47-54 [PMID:11226154]
Kv4.2 in Rat [GtoPdb: 553] [UniProtKB: Q63881]
GtoPdb - - 5.7 pIC50 - - - Life Sci. (1999) 65: PL143-9 [PMID:10503950];
J. Neurosci. (1996) 16: 2522-32 [PMID:8786428]

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]