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 (.delta.9-tetrahydrocannabivarin, Gwp42004, GWP-42004, GWP42004, O-4394, Tetrahydrocannabivarin, Thc-v, THCV) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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] |
ChEMBL | Displacement of [3H]-CP-55,940 from recombinant human CB1R expressed in HEK293 cell membranes after 90 mins | B | 8.82 | pKi | 1.5 | nM | Ki | J Nat Prod (2020) 83: 2060-2065 [PMID:32649196] |
ChEMBL | Displacement of [3H]-CP-55,940 from recombinant human CB1R expressed in HEK293 cell membranes after 90 mins | B | 7.88 | pIC50 | 13.1 | nM | IC50 | J Nat Prod (2020) 83: 2060-2065 [PMID:32649196] |
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] |
ChEMBL | Displacement of [3H]-CP-55,940 from recombinant human CB2R expressed in HEK293 cell membranes after 90 mins | B | 8.55 | pKi | 2.8 | nM | Ki | J Nat Prod (2020) 83: 2060-2065 [PMID:32649196] |
ChEMBL | Displacement of [3H]-CP-55,940 from recombinant human CB2R expressed in HEK293 cell membranes after 90 mins | B | 7.75 | pIC50 | 17.6 | nM | IC50 | J Nat Prod (2020) 83: 2060-2065 [PMID:32649196] |
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] |
TRPV5 in Human [GtoPdb: 511] [UniProtKB: Q9NQA5] | ||||||||
GtoPdb | - | - | 5.4 | pIC50 | 4000 | nM | IC50 | Pharmacol Res (2018) 136: 83-89 [PMID:30170189] |
TRPV6 in Human [GtoPdb: 512] [UniProtKB: Q9H1D0] | ||||||||
GtoPdb | - | - | 5.05 | pIC50 | 9000 | nM | IC50 | Pharmacol Res (2018) 136: 83-89 [PMID:30170189] |
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]