cannabigerol [Ligand Id: 11094] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL497318 (Cannabigerol) |
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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 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]
