cannabigerol [Ligand Id: 11094] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL497318 (Cannabigerol)
  • Fatty acid amide hydrolase/Anandamide amidohydrolase in Rat [ChEMBL: CHEMBL3229] [GtoPdb: 1400] [UniProtKB: P97612]
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  • CB1 receptor/Cannabinoid CB1 receptor in Human [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
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  • CB2 receptor/Cannabinoid CB2 receptor in Human [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
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  • N-Acylethanolamine acid amidase/N-acylsphingosine-amidohydrolase in Human [ChEMBL: CHEMBL4349] [GtoPdb: 1402] [UniProtKB: Q02083]
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  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
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  • Diacylglycerol lipase α/Sn1-specific diacylglycerol lipase alpha in Human [ChEMBL: CHEMBL5545] [GtoPdb: 1396] [UniProtKB: Q9Y4D2]
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  • TRPA1/Transient receptor potential cation channel subfamily A member 1 in Rat [ChEMBL: CHEMBL5160] [GtoPdb: 485] [UniProtKB: Q6RI86]
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  • TRPM8/Transient receptor potential cation channel subfamily M member 8 in Rat [ChEMBL: CHEMBL5011] [GtoPdb: 500] [UniProtKB: Q8R455]
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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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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Fatty acid amide hydrolase/Anandamide amidohydrolase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3229] [GtoPdb: 1400] [UniProtKB: P97612]
ChEMBL Inhibition of FAAH in rat brain membranes using [14C]-AEA as substrate measured after 30 mins by scintillation counting method B 4 pIC50 >100000 nM IC50 J Nat Prod (2019) 82: 636-646 [PMID:30816712]
CB1 receptor/Cannabinoid CB1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
ChEMBL Displacement of [3H]-CP55940 from recombinant human CB1 receptor expressed in Sf9 cell membranes co-expressing Galphai3beta1gamma2 measured after 90 mins by scintillation counting method B 6.05 pKi 897 nM Ki J Nat Prod (2019) 82: 636-646 [PMID:30816712]
ChEMBL Displacement of [3H]-CP-55,940 from human recombinant CB1 receptor expressed in HEK293 cells membrane incubated for 90 mins B 6.12 pKi 760 nM Ki J. Nat. Prod. (2011) 74: 2019-2022 [PMID:21902175]
ChEMBL Displacement of [3H]-CP-55,940 from human recombinant CB1 receptor expressed in HEK293 cells membrane incubated for 90 mins B 5.48 pIC50 3310 nM IC50 J. Nat. Prod. (2011) 74: 2019-2022 [PMID:21902175]
CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
ChEMBL Displacement of [3H]-CP-55,940 from human recombinant CB2 receptor expressed in HEK293 cells membrane incubated for 90 mins B 6.06 pKi 880 nM Ki J. Nat. Prod. (2011) 74: 2019-2022 [PMID:21902175]
ChEMBL Displacement of [3H]-CP55940 from recombinant human CB2 receptor expressed in Sf9 cell membranes co-expressing Galphai3beta1gamma2 measured after 90 mins by scintillation counting method B 6.82 pKi 153 nM Ki J Nat Prod (2019) 82: 636-646 [PMID:30816712]
ChEMBL Displacement of [3H]-CP-55,940 from human recombinant CB2 receptor expressed in HEK293 cells membrane incubated for 90 mins B 5.46 pIC50 3460 nM IC50 J. Nat. Prod. (2011) 74: 2019-2022 [PMID:21902175]
N-Acylethanolamine acid amidase/N-acylsphingosine-amidohydrolase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4349] [GtoPdb: 1402] [UniProtKB: Q02083]
ChEMBL Inhibition of recombinant human NAAA expressed in HEK293 cells using [14C]-N-palmitoylethanolamine as substrate measured after 30 mins by beta-counting method B 4 pIC50 >100000 nM IC50 J Nat Prod (2019) 82: 636-646 [PMID:30816712]
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
ChEMBL Agonist activity at GAL4-tagged PPARgamma (unknown origin) transiently expressed in HEK293T cells co-transfected with GAL4-tagged luc incubated for 6 hrs by dual luciferase reporter gene assay B 4.8 pEC50 15700 nM EC50 J Nat Prod (2020) 83: 1711-1715 [PMID:32315173]
Diacylglycerol lipase α/Sn1-specific diacylglycerol lipase alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5545] [GtoPdb: 1396] [UniProtKB: Q9Y4D2]
ChEMBL Inhibition of recombinant human DAGLalpha expressed in COS7 cells using [14C]-oleoyl-2-arachidonoyl-glycerol as substrate measured after 20 mins by beta-counting method B 4 pIC50 >100000 nM IC50 J Nat Prod (2019) 82: 636-646 [PMID:30816712]
TRPA1/Transient receptor potential cation channel subfamily A member 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5160] [GtoPdb: 485] [UniProtKB: Q6RI86]
ChEMBL Antagonist activity at rat recombinant TRPA1 receptor expressed in HEK293 cells assessed as inhibition of 100 uM allyl isothiocyanate-induced stimulation of intracellular calcium level using Fluo4-AM dye based fluorimetric assay F 4.89 pIC50 13000 nM IC50 J. Nat. Prod. (2011) 74: 2019-2022 [PMID:21902175]
ChEMBL Agonist activity at rat TRPA1 channel expressed in HEK293 cells assessed as increase in intracellular calcium influx F 5.47 pEC50 3400 nM EC50 J. Med. Chem. (2010) 53: 5085-5107 [PMID:20356305]
ChEMBL Agonist activity at rat recombinant TRPA1 receptor expressed in HEK293 cells assessed as stimulation of intracellular calcium level using Fluo4-AM dye based fluorimetric assay F 6.15 pEC50 700 nM EC50 J. Nat. Prod. (2011) 74: 2019-2022 [PMID:21902175]
TRPM8/Transient receptor potential cation channel subfamily M member 8 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5011] [GtoPdb: 500] [UniProtKB: Q8R455]
ChEMBL Antagonist activity at rat recombinant TRPM8 receptor expressed in HEK293 cells assessed as inhibition of 0.25 uM icilin-induced stimulation of intracellular calcium level using Fluo4-AM dye based fluorimetric assay F 6.8 pIC50 160 nM IC50 J. Nat. Prod. (2011) 74: 2019-2022 [PMID:21902175]
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 rat recombinant TRPV2 receptor expressed in HEK293 cells assessed as inhibition of 3 uM lysophosphatidylcholine-induced stimulation of intracellular calcium level using Fluo4-AM dye based fluorimetric assay F 5.82 pIC50 1500 nM IC50 J. Nat. Prod. (2011) 74: 2019-2022 [PMID:21902175]
ChEMBL Agonist activity at rat recombinant TRPV2 receptor expressed in HEK293 cells assessed as stimulation of intracellular calcium level using Fluo4-AM dye based fluorimetric assay F 5.77 pEC50 1700 nM EC50 J. Nat. Prod. (2011) 74: 2019-2022 [PMID:21902175]
TRPV1/Vanilloid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4794] [GtoPdb: 507] [UniProtKB: Q8NER1]
ChEMBL Antagonist activity at human TRPv1 receptor expressed in HEK293 cells assessed as inhibition of 0.1 um capsaicin-induced stimulation of intracellular calcium level using Fluo4-AM dye based fluorimetric assay F 5.59 pIC50 2600 nM IC50 J. Nat. Prod. (2011) 74: 2019-2022 [PMID:21902175]
ChEMBL Agonist activity at human TRPv1 receptor expressed in HEK293 cells assessed as stimulation of intracellular calcium level using Fluo4-AM dye based fluorimetric assay F 5.89 pEC50 1300 nM EC50 J. Nat. Prod. (2011) 74: 2019-2022 [PMID:21902175]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]