tetrahydrocannabivarin [Ligand Id: 6418] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2387541 (.delta.9-tetrahydrocannabivarin, Gwp42004, GWP-42004, GWP42004, O-4394, Tetrahydrocannabivarin, Thc-v, THCV) |
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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 | 4.3 | 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 CB1 (unknown origin) receptor assessed as inhibition constant | B | 6 | pKi | 1000 | nM | Ki | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| 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 | Binding affinity to CB1 receptor (unknown origin) assessed as inhibition constant | B | 7.12 | pKi | 75.4 | nM | Ki | J Nat Prod (2024) 87: 167-175 [PMID:38355400] |
| 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] |
| ChEMBL | Displacement of [3H]CP55940 from mouse brain membrane CB1 receptor assessed as inhibition constant | B | 7.12 | pKi | 75 | nM | Ki | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| ChEMBL | Agonist activity at CB1 receptor in albino MF1 mouse vas deferens assessed as inhibition of electrically evoked vas deferens contraction by incubated for 13 mins followed by electrical stimulation for 2 mins | F | 4.9 | pEC50 | 12700 | nM | EC50 | 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 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]CP55940 from human CB2 receptor transfected in CHO cells assessed as inhibition constant | B | 7.2 | pKi | 63 | nM | Ki | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| ChEMBL | Binding affinity to CB2 receptor (unknown origin) assessed as inhibition constant | B | 7.2 | pKi | 62.8 | nM | Ki | J Nat Prod (2024) 87: 167-175 [PMID:38355400] |
| 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] |
| ChEMBL | Agonist activity at CB2 receptor (unknown origin) expressed in CHO cell membranes assessed as increase in [35S]GTPgammaS binding incubated for 60 mins by liquid scintillation spectrometry analysis | F | 7.01 | pEC50 | 98 | nM | EC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| ChEMBL | Agonist activity at human CB2 receptor transfected in CHO cells assessed as inhibition of cyclic AMP production | F | 7.42 | pEC50 | 38 | nM | EC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| GPR55/G-protein coupled receptor 55 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075322] [GtoPdb: 109] [UniProtKB: Q9Y2T6] | ||||||||
| ChEMBL | Antagonist activity at GPR55 (unknown origin) expressed in HEK293 cells assessed as LPI-stimulated ERK1/2 phosphorylation | F | 6.06 | pEC50 | 880 | nM | EC50 | 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] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Displacement of [35S]GTPgammaS from 5HT1A in human CHO cells incubated for 60 mins by radioligand binding assay | B | 7.55 | pEC50 | 28 | nM | EC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
| ChEMBL | Displacement of [35S]GTPgammaS from 5HT1A in Sprague-Dawley rat brainstem incubated for 60 mins by radioligand binding assay | B | 8.27 | pEC50 | 5.4 | nM | EC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| 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] |
| 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 | 5.51 | pIC50 | 3070 | nM | IC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| ChEMBL | Agonist activity at TRPA1 (unknown origin) channel desensitization in presence of icilin | B | 6.06 | pIC50 | 870 | nM | IC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| ChEMBL | Agonist activity at TRPA1 (unknown origin) activation | B | 5.82 | pEC50 | 1500 | nM | EC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| ChEMBL | Agonist activity at TRPA1 (unknown origin) ion channel | B | 7.15 | pEC50 | 70 | nM | EC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| 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 | 7.7 | pIC50 | 20 | nM | IC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| 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 | 6.1 | pIC50 | 800 | nM | IC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| ChEMBL | Agonist activity at ionomycin-stimulated TRPV2 (unknown origin) activation | B | 5.39 | pEC50 | 4100 | nM | EC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| 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 | 5.52 | pIC50 | 3000 | nM | IC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| ChEMBL | Agonist activity at ionomycin-stimulated TRPV3 (unknown origin) activation | B | 5.42 | pEC50 | 3800 | nM | EC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| TRPV3 in Rat [GtoPdb: 509] | ||||||||
| GtoPdb | Calcium imaging | - | 5.42 | pEC50 | 3800 | nM | EC50 | Acta Physiol (Oxf) (2012) 204: 255-66 [PMID:21726418] |
| 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 | 5.49 | pIC50 | 3200 | nM | IC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| ChEMBL | Agonist activity at ionomycin-stimulated TRPV4 (unknown origin) activation | B | 5.19 | pEC50 | 6400 | nM | EC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| TRPV5/Transient receptor potential cation channel subfamily V member 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1628474] [GtoPdb: 511] [UniProtKB: Q9NQA5] | ||||||||
| ChEMBL | Inhibition of TRPV5 channel (unknown origin) by Patch-clamp assay | B | 5.32 | pIC50 | 4800 | nM | IC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| GtoPdb | - | - | 5.4 | pIC50 | 4000 | nM | IC50 | Pharmacol Res (2018) 136: 83-89 [PMID:30170189] |
| TRPV6/Transient receptor potential cation channel subfamily V member 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1628465] [GtoPdb: 512] [UniProtKB: Q9H1D0] | ||||||||
| ChEMBL | Inhibition of TRPV6 channel (unknown origin) by Patch-clamp assay | B | 5.03 | pIC50 | 9400 | nM | IC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| GtoPdb | - | - | 5.05 | pIC50 | 9000 | nM | IC50 | Pharmacol Res (2018) 136: 83-89 [PMID:30170189] |
| TRPV1/Vanilloid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4794] [GtoPdb: 507] [UniProtKB: Q8NER1] | ||||||||
| ChEMBL | Agonist activity at ionomycin-stimulated TRPV1 (unknown origin) channel desensitization in presence of capsaicin | B | 5.89 | pIC50 | 1300 | nM | IC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| ChEMBL | Agonist activity at ionomycin-stimulated TRPV1 (unknown origin) activation | B | 5.82 | pEC50 | 1500 | nM | EC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| ChEMBL | Agonist activity at TRPV1 (unknown origin) ion channel | B | 6.7 | pEC50 | 200 | 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]
