tetrahydrocannabivarin [Ligand Id: 6418] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL2387541 (Gwp42004, Tetrahydrocannabivarin, GWP-42004, O-4394, THCV, GWP42004)
  • Fatty acid amide hydrolase/Anandamide amidohydrolase in Rat [ChEMBL: CHEMBL3229] [GtoPdb: 1400] [UniProtKB: P97612]
There should be some charts here, you may need to enable JavaScript!
  • CB1 receptor/Cannabinoid CB1 receptor in Human [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
  • CB1 receptor/Cannabinoid CB1 receptor in Mouse [ChEMBL: CHEMBL3037] [GtoPdb: 56] [UniProtKB: P47746]
There should be some charts here, you may need to enable JavaScript!
  • CB2 receptor/Cannabinoid CB2 receptor in Human [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
There should be some charts here, you may need to enable JavaScript!
  • N-Acylethanolamine acid amidase/N-acylsphingosine-amidohydrolase in Human [ChEMBL: CHEMBL4349] [GtoPdb: 1402] [UniProtKB: Q02083]
There should be some charts here, you may need to enable JavaScript!
  • Diacylglycerol lipase α/Sn1-specific diacylglycerol lipase alpha in Human [ChEMBL: CHEMBL5545] [GtoPdb: 1396] [UniProtKB: Q9Y4D2]
There should be some charts here, you may need to enable JavaScript!
  • TRPV3 in Rat [GtoPdb: 509]
There should be some charts here, you may need to enable JavaScript!
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 4.3 pIC50 >50000 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 Binding affinity to human CB1 receptor B 7.12 pKi 75.4 nM Ki J Nat Prod (2020) 83: 88-98 [PMID:31891265]
CB1 receptor/Cannabinoid CB1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3037] [GtoPdb: 56] [UniProtKB: P47746]
ChEMBL Displacement of [3H]-CP55940 from CB1 receptor in mouse whole brain membrane measured after 60 mins by liquid scintillation counting method B 7.12 pKi 75.4 nM Ki J Nat Prod (2019) 82: 636-646 [PMID:30816712]
CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
ChEMBL Displacement of [3H]-CP55940 from recombinant human CB2 receptor expressed in CHO cell membranes measured after 60 mins by liquid scintillation counting method B 7.2 pKi 63 nM Ki J Nat Prod (2019) 82: 636-646 [PMID:30816712]
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]
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 4.3 pIC50 >50000 nM IC50 J Nat Prod (2019) 82: 636-646 [PMID:30816712]
TRPV3 in Rat [GtoPdb: 509]
GtoPdb Calcium imaging - 5.42 pEC50 3800 nM EC50 Acta Physiol (Oxf) (2012) 204: 255-66 [PMID:21726418]

ChEMBL data shown on this page come from version 28:

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]