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] |
| sirtuin 6/NAD-dependent protein deacetylase sirtuin-6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2163182] [GtoPdb: 2712] [UniProtKB: Q8N6T7] | ||||||||
| ChEMBL | Activation of human SIRT6 deacetylase activity expressed in Escherichia coli BL21(DE3) expressed in Escherichia coli using H3K9Ac peptide substrate | B | 5.51 | pEC50 | 3100 | nM | EC50 | J Med Chem (2021) 64: 9732-9758 [PMID:34213345] |
| ChEMBL | Activation of recombinant His-tagged SIRT6 (unknown origin) deacetylase activity expressed in Escherichia coli using H3K9Ac peptide substrate | B | 5.51 | pEC50 | 3100 | nM | EC50 | J Med Chem (2021) 64: 9732-9758 [PMID:34213345] |
| ChEMBL | Activation of his6-tagged SIRT6 (unknown origin) using H3K9Ac peptide substrate incubated for 30 mins | B | 5.51 | pEC50 | 3100 | nM | EC50 | Eur J Med Chem (2023) 246: 114998-114998 [PMID:36508969] |
| 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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
