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 [35S]GTPgammaS from human CB1 receptor expressed in CHO cells | B | 5.59 | pKi | 2600 | nM | Ki | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| 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] |
| CB1 receptor/Cannabinoid CB1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272] | ||||||||
| ChEMBL | Displacement of [35S]GTPgammaS from CB1 receptor in rat brain | B | 6.36 | pKi | 440 | nM | Ki | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972] | ||||||||
| ChEMBL | Displacement of [3H]-CP55940 from CB2 receptor (unknown origin) expressed in CHO cells | B | 5.57 | pKi | 2700 | nM | Ki | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| ChEMBL | Displacement of [3H]-WIN55212-2 from human CB2 receptor transfected in CHO cell membrane incubated for 90 mins by Liquid scintillation counter analysis | B | 5.91 | pKi | 1220 | nM | Ki | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| 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] |
| Inhibin alpha chain in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5169109] [UniProtKB: P05111] | ||||||||
| ChEMBL | Inhibition of Inh (unknown origin) | B | 5.28 | pIC50 | 5200 | nM | IC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| 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 Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6007] [GtoPdb: 485] [UniProtKB: O75762] | ||||||||
| ChEMBL | Agonist activity at TRPA1 (unknown origin) channel desensitization in presence of isothiocyanate | B | 4.89 | pIC50 | 13000 | nM | IC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| ChEMBL | Agonist activity at TRPA1 (unknown origin) activation | B | 6.15 | pEC50 | 700 | nM | EC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| 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 | Antagonist activity at rat TRPA1 transfected in HEK293 cells assessed as desensitization by measuring inhibition of AITC induced increase in intracellular Ca2+ concentration preincubated for 5 mins followed by AITC stimulation by Fluo4-AM dye based assay | B | 4.89 | pIC50 | 13000 | nM | IC50 | J Nat Prod (2024) 87: 722-732 [PMID:38408345] |
| 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] |
| GtoPdb | - | - | 6.15 | pEC50 | 700 | nM | EC50 | J Nat Prod (2024) 87: 722-732 [PMID:38408345] |
| 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] |
| ChEMBL | Agonist activity at rat TRPA1 transfected in HEK293 cells assessed as increase in intracellular Ca2+ concentration by Fluo4-AM dye based assay | B | 6.15 | pEC50 | 700 | nM | EC50 | J Nat Prod (2024) 87: 722-732 [PMID:38408345] |
| TRPM8/Transient receptor potential cation channel subfamily M member 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075319] [GtoPdb: 500] [UniProtKB: Q7Z2W7] | ||||||||
| ChEMBL | Antagonist activity at TRPM8 (unknown origin) ion channel | B | 6.8 | pIC50 | 160 | nM | IC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| ChEMBL | Antagonist activity at TRPM8 (unknown origin) | B | 6.8 | pIC50 | 160 | nM | IC50 | J Med Chem (2016) 59: 10006-10029 [PMID:27437828] |
| 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] |
| ChEMBL | Antagonist activity at rat TRPM8 transfected in HEK293 cells assessed as inhibition of icilin induced increase in intracellular Ca2+ concentration preincubated for 5 mins followed by icilin stimulation by Fluo4-AM dye based assay | B | 6.8 | pIC50 | 160 | nM | IC50 | J Nat Prod (2024) 87: 722-732 [PMID:38408345] |
| GtoPdb | - | - | 6.8 | pIC50 | 160 | nM | IC50 | J Nat Prod (2024) 87: 722-732 [PMID:38408345] |
| TRPV2/Transient receptor potential cation channel subfamily V member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5051] [GtoPdb: 508] [UniProtKB: Q9Y5S1] | ||||||||
| ChEMBL | Agonist activity at ionomycin-stimulated TRPV2 (unknown origin) channel desensitization in presence of lysophosphatidylcholine | B | 5.82 | pIC50 | 1500 | nM | IC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| ChEMBL | Agonist activity at ionomycin-stimulated TRPV2 (unknown origin) activation | B | 5.77 | pEC50 | 1700 | nM | EC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| 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] |
| TRPV3/Transient receptor potential cation channel subfamily V member 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5522] [GtoPdb: 509] [UniProtKB: Q8NET8] | ||||||||
| ChEMBL | Agonist activity at ionomycin-stimulated TRPV3 (unknown origin) channel desensitization in presence of carvacrol | B | 4.18 | pIC50 | 66000 | nM | IC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| ChEMBL | Agonist activity at ionomycin-stimulated TRPV3 (unknown origin) activation | B | 6 | pEC50 | 1000 | nM | EC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| TRPV4/Transient receptor potential cation channel subfamily V member 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3119] [GtoPdb: 510] [UniProtKB: Q9HBA0] | ||||||||
| ChEMBL | Agonist activity at ionomycin-stimulated TRPV4 (unknown origin) channel desensitization in presence of 4alphaPDD | B | 5.89 | pIC50 | 1300 | nM | IC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| ChEMBL | Agonist activity at ionomycin-stimulated TRPV4 (unknown origin) activation | B | 5.29 | pEC50 | 5100 | nM | EC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| 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 ionomycin-stimulated TRPV1 (unknown origin) channel desensitization in presence of capsaicin | B | 5.59 | pIC50 | 2600 | nM | IC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| 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 | Agonist activity at ionomycin-stimulated TRPV1 (unknown origin) activation | B | 5.89 | pEC50 | 1300 | nM | EC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
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]
