cannabinol [Ligand Id: 740] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL74415 (Cannabinol, NSC-134455) |
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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 towards cloned human Cannabinoid receptor 1 | B | 2.49 | pKi | 2.49 | nM | Log Ki | J Med Chem (2000) 43: 2300-2309 [PMID:10882356] |
| ChEMBL | Binding affinity to CB1 (unknown origin) assessed as inhibition constant | B | 5.96 | pKi | 1100 | nM | Ki | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| GtoPdb | - | - | 6.5 | pKi | - | - | - |
Mol Pharmacol (1995) 48: 443-50 [PMID:7565624]; J Pharmacol Exp Ther (1996) 278: 989-99 [PMID:8819477] |
| ChEMBL | Binding affinity was determined for Cannabinoid receptor 1 | B | 6.51 | pKi | 308 | nM | Ki | J Med Chem (2000) 43: 3778-3785 [PMID:11020293] |
| ChEMBL | Binding affinity to to CB1 (unknown origin) expressed in CHO -k1 cells assessed as inhibition constant | B | 7.15 | pKi | 70 | 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 | 7.89 | pKi | 13 | nM | Ki | J Nat Prod (2019) 82: 636-646 [PMID:30816712] |
| ChEMBL | Displacement of 3H-CP-55940 from recombinant full length human CB1 receptor expressed in HEK293 cell membranes after 90 mins by topcount scintillation counting analysis | B | 7.12 | pEC50 | 75 | nM | EC50 | J Nat Prod (2018) 81: 630-633 [PMID:29240420] |
| CB1 receptor/Cannabinoid CB1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272] | ||||||||
| ChEMBL | Binding affinity of compound towards Cannabinoid receptor 1 in rat brain synaptosomal membrane preparations | B | 6.41 | pKi | 392.2 | nM | Ki | J Med Chem (1997) 40: 3228-3233 [PMID:9379442] |
| ChEMBL | Binding affinity of compound towards Cannabinoid receptor 1 in african green monkey COS-7 cells transfected with cDNA of rat CB1 receptor | B | 6.68 | pKi | 211.2 | nM | Ki | J Med Chem (1997) 40: 3228-3233 [PMID:9379442] |
| ChEMBL | Displacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptor | F | 6.5 | pEC50 | 316.23 | nM | EC50 | J Med Chem (2006) 49: 554-566 [PMID:16420041] |
| ChEMBL | Effective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptor | F | 6.92 | pEC50 | 120 | nM | EC50 | J Med Chem (1997) 40: 3228-3233 [PMID:9379442] |
| CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972] | ||||||||
| ChEMBL | Binding affinity towards cloned human cannabinoid receptor 2 | B | 1.98 | pKi | 1.98 | nM | Log Ki | J Med Chem (2000) 43: 2300-2309 [PMID:10882356] |
| ChEMBL | Binding affinity to to CB2 receptor (unknown origin) expressed in AtT20 cells assessed as inhibition constant | B | 6.52 | pKi | 300 | nM | Ki | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| ChEMBL | Binding affinity of compound towards Cannabinoid receptor 2 in african green monkey COS-7 cells transfected with cDNA of human CB2 receptor | B | 6.9 | pKi | 126.4 | nM | Ki | J Med Chem (1997) 40: 3228-3233 [PMID:9379442] |
| ChEMBL | Binding affinity was determined for Cannabinoid receptor 2 | B | 7.02 | pKi | 96 | nM | Ki | J Med Chem (2000) 43: 3778-3785 [PMID:11020293] |
| ChEMBL | Binding affinity to to CB2 receptor (unknown origin) expressed in CHO -k1 cells assessed as inhibition constant | B | 7.15 | pKi | 70 | nM | Ki | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| 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 | 7.8 | pKi | 16 | nM | Ki | J Nat Prod (2019) 82: 636-646 [PMID:30816712] |
| ChEMBL | Displacement of 35S]GTPgammaS from human CB2 receptor transfected in CHO cells assessed as inhibition forskolin-stimulated cyclic AMP production | B | 0.06 | pEC50 | 0.06 | % | pEC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| ChEMBL | Effective concentration for inhibition of human Cannabinoid receptor 2-mediated adenylyl cyclase using African green monkey (COS-7) cells transfected with the cDNA of human CB2 receptor | F | 6.58 | pEC50 | 261.2 | nM | EC50 | J Med Chem (1997) 40: 3228-3233 [PMID:9379442] |
| ChEMBL | Displacement of 3H-CP-55940 from recombinant full length human CB2 receptor expressed in HEK293 cell membranes after 90 mins by topcount scintillation counting analysis | B | 7.14 | pEC50 | 73 | nM | EC50 | J Nat Prod (2018) 81: 630-633 [PMID:29240420] |
| CYP1B1/Cytochrome P450 1B1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4878] [GtoPdb: 1320] [UniProtKB: Q16678] | ||||||||
| ChEMBL | Competitive inhibition of human liver microsomes CYP1B1 expressed in supersomes coexpressing NADPH-CYP reductase using 7-Ethoxyresorufin as substrate measured every 5 mins for 30 mins in presence of NADPH by fluorescence assay | B | 6.83 | pKi | 148 | nM | Ki | Eur J Med Chem (2017) 135: 296-306 [PMID:28458135] |
| 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 | 4.3 | pIC50 | >50000 | 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 | 4.6 | pEC50 | >25000 | 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 | 4.3 | 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 | 6.4 | pIC50 | 400 | 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 | 6.68 | pIC50 | 210 | nM | IC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| ChEMBL | Agonist activity at TRPA1 (unknown origin) activation | B | 6.74 | pEC50 | 180 | 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 | Agonist activity at recombinant rat TRPA1 expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo4-AM probe based fluorescence assay | B | 6.74 | pEC50 | 180 | nM | EC50 | J Nat Prod (2018) 81: 630-633 [PMID:29240420] |
| 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 recombinant rat TRPM8 expressed in HEK293 cells assessed as inhibition of icilin-induced intracellular calcium level incubated for 5 mins followed by agonist stimulation by Fluo4-AM probe based fluorescence assay | B | 6.68 | pIC50 | 210 | nM | IC50 | J Nat Prod (2018) 81: 630-633 [PMID:29240420] |
| 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 | 4.8 | pIC50 | 15700 | nM | IC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| ChEMBL | Agonist activity at ionomycin-stimulated TRPV2 (unknown origin) activation | B | 4.72 | pEC50 | 19000 | 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] | ||||||||
| GtoPdb | - | - | 4.11 | pEC50 | 77000 | nM | EC50 | J Neurosci (2008) 28: 6231-8 [PMID:18550765] |
| ChEMBL | Agonist activity at recombinant rat TRPV2 expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo4-AM probe based fluorescence assay | B | 4.72 | pEC50 | 19000 | nM | EC50 | J Nat Prod (2018) 81: 630-633 [PMID:29240420] |
| 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 | 5.03 | pIC50 | 9400 | nM | IC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| ChEMBL | Agonist activity at ionomycin-stimulated TRPV3 (unknown origin) activation | B | 5.28 | pEC50 | 5300 | nM | EC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| Transient receptor potential cation channel, subfamily V, member 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295541] [UniProtKB: E9PU00] | ||||||||
| ChEMBL | Agonist activity at recombinant rat TRPV3 expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo4-AM probe based fluorescence assay | B | 5.28 | pEC50 | 5300 | nM | EC50 | J Nat Prod (2018) 81: 630-633 [PMID:29240420] |
| 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 | 5.27 | pIC50 | 5400 | nM | IC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| ChEMBL | Agonist activity at ionomycin-stimulated TRPV4 (unknown origin) activation | B | 4.79 | pEC50 | 16100 | nM | EC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| TRPV4/Transient receptor potential cation channel subfamily V member 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2775] [GtoPdb: 510] [UniProtKB: Q9ERZ8] | ||||||||
| ChEMBL | Agonist activity at recombinant rat TRPV4 expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo4-AM probe based fluorescence assay | B | 4.79 | pEC50 | 16100 | nM | EC50 | J Nat Prod (2018) 81: 630-633 [PMID:29240420] |
| 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 | 4.09 | pIC50 | 82000 | nM | IC50 | J Nat Prod (2021) 84: 142-160 [PMID:33356248] |
| ChEMBL | Agonist activity at human TRPV1 expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo4-AM probe based fluorescence assay | B | 5.21 | pEC50 | 6200 | nM | EC50 | J Nat Prod (2018) 81: 630-633 [PMID:29240420] |
| ChEMBL | Agonist activity at ionomycin-stimulated TRPV1 (unknown origin) activation | B | 5.21 | pEC50 | 6200 | 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]
