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] |
| 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 | 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 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 | 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 | 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 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 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] |
| 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 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 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 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]
