N-oleoylethanolamide [Ligand Id: 2661] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL280065 (N-(2-Hydroxyethyl)Oleamide, N-Oleoylethanolamine, N-Oleylethanolamine, Oleoylethanolamide, Oleoyl Ethanolamide, Oleoylethanolamine) |
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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 | F | 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 increase in cAMP stimulation measured after 60 mins by TR-FRET assay | F | 5.66 | pEC50 | 2200 | nM | EC50 | Bioorg Med Chem Lett (2017) 27: 2515-2519 [PMID:28408218] |
| ChEMBL | Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay | F | 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 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 GPR119 (unknown origin) assessed as increase in cAMP level by cAMP HTRF assay | F | 6.03 | pEC50 | 930 | nM | EC50 | Bioorg Med Chem Lett (2020) 30: 126855-126855 [PMID:31898998] |
| 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 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]
