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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  • 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]
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 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]