oleamide [Ligand Id: 284] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL15927 (Octadec-9-Enoic Acid Amide, Oleamide)
  • Acyl coenzyme A:cholesterol acyltransferase 1 in Human [ChEMBL: CHEMBL2782] [UniProtKB: P35610]
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  • Fatty acid amide hydrolase/Anandamide amidohydrolase in Human [ChEMBL: CHEMBL2243] [GtoPdb: 1400] [UniProtKB: O00519]
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  • CB1 receptor/Cannabinoid CB1 receptor in Rat [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272]
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
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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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  • 5-HT7 receptor in Human [GtoPdb: 12] [UniProtKB: P34969]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Acyl coenzyme A:cholesterol acyltransferase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2782] [UniProtKB: P35610]
ChEMBL Inhibitory activity against human Acyl coenzyme A:cholesterol acyltransferase 1 B 4.07 pIC50 85000 nM IC50 Bioorg Med Chem Lett (2004) 14: 4277-4280 [PMID:15261286]
ChEMBL Inhibitory activity against human Acyl coenzyme A:cholesterol acyltransferase 2 B 4.2 pIC50 63000 nM IC50 Bioorg Med Chem Lett (2004) 14: 4277-4280 [PMID:15261286]
Fatty acid amide hydrolase/Anandamide amidohydrolase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2243] [GtoPdb: 1400] [UniProtKB: O00519]
ChEMBL Inhibition of fatty acid amide hydrolase; range = 22-68 uM B 4.17 pIC50 68000 nM IC50 J Med Chem (2005) 48: 5059-5087 [PMID:16078824]
CB1 receptor/Cannabinoid CB1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272]
ChEMBL Inhibition of [3H]CP-55940 binding to rat cannabinoid receptor 1 B 5.94 pKi 1140 nM Ki J Med Chem (2005) 48: 5059-5087 [PMID:16078824]
GABAA receptor π subunit/GABAA receptor β1 subunit/GABAA receptor δ subunit/GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor γ1 subunit/GABAA receptor α2 subunit/GABAA receptor α4 subunit/GABAA receptor γ3 subunit/GABAA receptor α6 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit/GABAA receptor β2 subunit/GABAA receptor ε subunit/GABA-A receptor; anion channel in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907607] [GtoPdb: 419, 410, 416, 414, 408, 406, 413, 405, 407, 415, 409, 404, 412, 411, 417] [UniProtKB: O09028, P15431, P18506, P18508, P19969, P20236, P23574, P23576, P28471, P28473, P30191, P62813, P63079, P63138, Q91ZM7, Q9ES14]
ChEMBL Inhibitory activity against Gamma-aminobutyric acid A (GABA-A) receptor from rat cultured cortical neuron RNA expressed in Xenopus oocytes F 4.82 pEC50 15000 nM EC50 J Med Chem (2000) 43: 1427-1447 [PMID:10780899]
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL GPCR PRESTO-Tango dose-response in agonist mode with target: CHRM2 F 5 pEC50 >10000 nM EC50 EUbOPEN Chemogenomics Library - GPCR Dose-Respose
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 5.68 pIC50 2100 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 5.68 pIC50 2100 nM IC50 J Med Chem (2018) 61: 8255-8281 [PMID:30176215]
5-HT7 receptor in Human [GtoPdb: 12] [UniProtKB: P34969]
GtoPdb - - 8.6 pKd - - - Biochem Pharmacol (1999) 58: 1807-13 [PMID:10571256]

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]