N-oleoylethanolamide [Ligand Id: 2661] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL280065 (Oleoylethanolamine, N-Oleoylethanolamine, N-Oleylethanolamine, Oleoylethanolamide, Oleoyl Ethanolamide, N-(2-Hydroxyethyl)Oleamide)
  • CB1 receptor/Cannabinoid CB1 receptor in Human [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
  • CB1 receptor/Cannabinoid CB1 receptor in Rat [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272]
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  • CB2 receptor/Cannabinoid CB2 receptor in Human [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
  • CB2 receptor/Cannabinoid CB2 receptor in Mouse [ChEMBL: CHEMBL5373] [GtoPdb: 57] [UniProtKB: P47936]
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  • GPR119/Glucose-dependent insulinotropic receptor in Human [ChEMBL: CHEMBL5652] [GtoPdb: 126] [UniProtKB: Q8TDV5]
  • GPR119/Glucose-dependent insulinotropic receptor in Mouse [ChEMBL: CHEMBL5263] [GtoPdb: 126] [UniProtKB: Q7TQP3]
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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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  • TRPV2/Transient receptor potential cation channel subfamily V member 2 in Rat [ChEMBL: CHEMBL2863] [GtoPdb: 508] [UniProtKB: Q9WUD2]
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  • GPR55 in Human [GtoPdb: 109] [UniProtKB: Q9Y2T6]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CB1 receptor/Cannabinoid CB1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
ChEMBL Binding affinity to human recombinant CB1 receptor expressed in COS cells B 5.96 pKi 1100 nM Ki J. Med. Chem. (2006) 49: 2333-2338 [PMID:16570929]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cell membrane B 5.96 pKi 1100 nM Ki J. Med. Chem. (2009) 52: 3001-3009 [PMID:19361197]
CB1 receptor/Cannabinoid CB1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272]
ChEMBL Binding affinity towards cannabinoid receptor 1 from rat forebrain membranes in the absence of phenylmethanesulfonylfluoride (PMSF) using 0.8 nM [3H]CP-55940 as radioligand B 4.36 pKi 44000 nM Ki J. Med. Chem. (1998) 41: 5353-5361 [PMID:9876105]
ChEMBL Binding affinity towards cannabinoid receptor 1 from rat forebrain membranes in the presence of phenylmethanesulfonylfluoride (PMSF) using 0.8 nM [3H]CP-55940 as radioligand B 4.7 pKi 20000 nM Ki J. Med. Chem. (1998) 41: 5353-5361 [PMID:9876105]
ChEMBL Tested for binding affinity to Cannabinoid receptor 1 B 5 pKi >10000 nM Ki J. Med. Chem. (1999) 42: 896-902 [PMID:10072686]
CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
ChEMBL Binding affinity to human recombinant CB2 receptor expressed in COS cells B 5 pKi >10000 nM Ki J. Med. Chem. (2006) 49: 2333-2338 [PMID:16570929]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK293 cell membrane B 5 pKi >10000 nM Ki J. Med. Chem. (2009) 52: 3001-3009 [PMID:19361197]
CB2 receptor/Cannabinoid CB2 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5373] [GtoPdb: 57] [UniProtKB: P47936]
ChEMBL Binding affinity towards Cannabinoid receptor 2 from mouse spleen membranes using 0.8 nM [3H]CP-55940 as radioligand B 4.51 pKi 31000 nM Ki J. Med. Chem. (1998) 41: 5353-5361 [PMID:9876105]
GPR119/Glucose-dependent insulinotropic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5652] [GtoPdb: 126] [UniProtKB: Q8TDV5]
ChEMBL Agonist activity at recombinant GPR119 receptor (unknown origin) B 5.49 pEC50 3200 nM EC50 J. Med. Chem. (2013) 56: 1811-1829 [PMID:23384387]
ChEMBL Agonist activity at GPR119 (unknown origin) F 5.49 pEC50 3200 nM EC50 Bioorg Med Chem (2018) 26: 4080-4087 [PMID:30100020]
ChEMBL Agonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamine B 5.66 pEC50 2200 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 1519-1521 [PMID:23374864]
ChEMBL Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 60 mins F 5.66 pEC50 2200 nM EC50 Bioorg. Med. Chem. (2013) 21: 1349-1356 [PMID:23357035]
ChEMBL Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay B 5.66 pEC50 2200 nM EC50 Bioorg Med Chem (2017) 25: 254-260 [PMID:27825553]
ChEMBL Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay B 5.66 pEC50 2200 nM EC50 Bioorg Med Chem Lett (2017) 27: 2515-2519 [PMID:28408218]
GtoPdb - - 6.3 pEC50 - - - Cell Metab (2006) 3: 167-75 [PMID:16517404];
Mol Endocrinol (2010) 24: 161-70 [PMID:19901198];
J Biomol Screen (2013) 18: 599-609 [PMID:23396314]
GPR119/Glucose-dependent insulinotropic receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5263] [GtoPdb: 126] [UniProtKB: Q7TQP3]
ChEMBL Agonist activity at mouse GPR119 receptor cotransformed in Saccharomyces cerevisiae cells after 4 hrs by fluorescent Fus1p-LacZ reporter gene assay B 5.54 pEC50 2900 nM EC50 J. Med. Chem. (2016) 59: 3579-3592 [PMID:26512410]
Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
GtoPdb - - 6.92 pIC50 - - - Nature (2003) 425: 90-3 [PMID:12955147];
Neuropharmacology (2005) 48: 1147-53 [PMID:15910890]
ChEMBL Agonist activity at human PPARalpha expressed in MCF7 cells co-transfected CPTI DR1-type RE after 6 hrs by luciferase reporter gene assay F 6.73 pEC50 185 nM EC50 ACS Med. Chem. Lett. (2011) 2: 793-797 [PMID:24936232]
ChEMBL Agonist activity at human PPARalpha expressed in MCF7 cells co-transfected CPTI DR1-type RE after 16 hrs by luciferase reporter gene assay F 6.82 pEC50 152 nM EC50 ACS Med. Chem. Lett. (2011) 2: 793-797 [PMID:24936232]
ChEMBL Agonist activity at human PPARalpha transfected in human MCF7 cells after 16 hrs by luciferase reporter gene assay B 6.82 pEC50 152 nM EC50 J. Med. Chem. (2015) 58: 6639-6652 [PMID:26226490]
ChEMBL Transactivation of human Gal4 fused PPARalpha LBD transfected in human HeLa cells after 7 hrs by dual-luciferase reporter gene assay B 6.92 pEC50 120 nM EC50 Bioorg Med Chem (2016) 24: 5455-5461 [PMID:27622746]
ChEMBL Activation of human PPARalpha by GST pull down assay B 6.96 pEC50 110 nM EC50 J. Med. Chem. (2007) 50: 389-393 [PMID:17228882]
Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
ChEMBL Transactivation of human Gal4 fused PPARdelta LBD transfected in human HeLa cells after 7 hrs by dual-luciferase reporter gene assay B 5.96 pEC50 1100 nM EC50 Bioorg Med Chem (2016) 24: 5455-5461 [PMID:27622746]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay F 5.1 pIC50 7943.28 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F 5.2 pIC50 6309.57 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay F 5.2 pIC50 6309.57 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 5.3 pIC50 5011.87 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay F 5.4 pIC50 3981.07 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 5.5 pIC50 3162.28 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 5.7 pIC50 1995.26 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
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 CBD-induced Ca2+ levels preincubated for 5 mins followed by agonist addition by Fuo-4-AM based spectrofluorimetry B 5.27 pIC50 5400 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 LPC-induced Ca2+ levels preincubated for 5 mins followed by agonist addition by Fuo-4-AM based spectrofluorimetry B 5.74 pIC50 1800 nM IC50 J Med Chem (2018) 61: 8255-8281 [PMID:30176215]
TRPV1/Vanilloid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4794] [GtoPdb: 507] [UniProtKB: Q8NER1]
ChEMBL Agonist activity at human recombinant TRPV1 expressed in HEK293 cells assessed as increase in intracellular calcium level F 5.44 pEC50 3650 nM EC50 J. Med. Chem. (2009) 52: 3001-3009 [PMID:19361197]
ChEMBL Agonist activity on human recombinant TRPV1-mediated enhancement of intracellular calcium concentration in HEK293 cells F 6.05 pEC50 890 nM EC50 J. Med. Chem. (2006) 49: 2333-2338 [PMID:16570929]
ChEMBL Agonist activity at TRPV1 receptor (unknown origin) B 7.4 pEC50 40 nM EC50 J. Med. Chem. (2013) 56: 1811-1829 [PMID:23384387]
GPR55 in Human [GtoPdb: 109] [UniProtKB: Q9Y2T6]
GtoPdb - - 6.5 pEC50 315 nM EC50 Br J Pharmacol (2007) 152: 1092-101 [PMID:17876302]

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]