JWH-018 [Ligand Id: 9706] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL561013 (JWH-018) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CB1 receptor/Cannabinoid CB1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554] | ||||||||
| GtoPdb | - | - | 8 | pKi | - | - | - | J Pharmacol Exp Ther (1999) 291: 837-44 [PMID:10525107] |
| ChEMBL | Binding affinity to CB1 receptor (unknown origin) | B | 8.02 | pKi | 9.5 | nM | Ki | J Med Chem (2013) 56: 8224-8256 [PMID:23865723] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB1 receptor expressed in CHO cells incubated for 90 mins by liquid scintillation spectrophotometry relative to control | B | 8.05 | pKi | 9 | nM | Ki | J Med Chem (2021) 64: 6381-6396 [PMID:33887913] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB1 receptor | B | 8.37 | pKi | 4.3 | nM | Ki | J Med Chem (2016) 59: 7525-7543 [PMID:27482723] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB1 receptor expressed in CHO cells by liquid scintillation counting | B | 8.7 | pKi | 2 | nM | Ki | Eur J Med Chem (2011) 46: 5086-5098 [PMID:21885167] |
| ChEMBL | Agonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid release | F | 8.3 | pEC50 | 5.01 | nM | EC50 | Eur J Med Chem (2011) 46: 5086-5098 [PMID:21885167] |
| CB1 receptor/Cannabinoid CB1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3037] [GtoPdb: 56] [UniProtKB: P47746] | ||||||||
| ChEMBL | Displacement of [3H]CP-55,940 from CB1 receptor in B6SJL mouse brain membrane after 90 mins by liquid scintillation spectrophotometric analysis | B | 8.89 | pKi | 1.3 | nM | Ki | Drug Metab Dispos (2012) 40: 2174-2184 [PMID:22904561] |
| CB1 receptor/Cannabinoid CB1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272] | ||||||||
| ChEMBL | Displacement of [3H]CP-55940 from CB1 receptor in rat brain by filtration assay | B | 8.04 | pKi | 9.02 | nM | Ki | Eur J Med Chem (2009) 44: 2482-2496 [PMID:19249138] |
| ChEMBL | Activation of CB1 receptor in Wistar rat prelimbic prefrontal cortex assessed as reduction of field excitatory postsynaptic potential amplitude after 20 mins | B | 6.55 | pIC50 | 280 | nM | IC50 | Eur J Med Chem (2011) 46: 5086-5098 [PMID:21885167] |
| CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972] | ||||||||
| ChEMBL | Displacement of [3H]-CP55940 from human CB2 receptor expressed in CHO cells by liquid scintillation counting | B | 8.2 | pKi | 6.31 | nM | Ki | Eur J Med Chem (2011) 46: 5086-5098 [PMID:21885167] |
| GtoPdb | - | - | 8.5 | pKi | - | - | - | J Pharmacol Exp Ther (1999) 291: 837-44 [PMID:10525107] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB2 receptor expressed in CHO cells incubated for 90 mins by liquid scintillation spectrophotometry relative to control | B | 8.53 | pKi | 2.94 | nM | Ki | J Med Chem (2021) 64: 6381-6396 [PMID:33887913] |
| ChEMBL | Binding affinity to CB2 receptor (unknown origin) | B | 8.54 | pKi | 2.9 | nM | Ki | J Med Chem (2013) 56: 8224-8256 [PMID:23865723] |
| ChEMBL | Displacement of [3H]CP-55940 from human cloned CB2 receptor by filtration assay | B | 8.54 | pKi | 2.9 | nM | Ki | Eur J Med Chem (2009) 44: 2482-2496 [PMID:19249138] |
| ChEMBL | Agonist activity at human CB2 receptor expressed in CHO cells assessed as increase of forskolin-stimulated cAMP accumulation after 20 mins | F | 8.3 | pEC50 | 5.01 | nM | EC50 | Eur J Med Chem (2011) 46: 5086-5098 [PMID:21885167] |
| δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533] | ||||||||
| ChEMBL | Displacement of [3H]Ile5,6-deltorphin-2 from DOR in Wistar rat brain membranes after 60 mins by liquid scintillation analysis | B | 5 | pKi | >10000 | nM | Ki | Eur J Med Chem (2019) 178: 571-588 [PMID:31220675] |
| Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144] | ||||||||
| ChEMBL | Displacement of [3H]HS-665 from KOR in guinea pig brain membranes after 60 mins by liquid scintillation analysis | B | 5 | pKi | >10000 | nM | Ki | Eur J Med Chem (2019) 178: 571-588 [PMID:31220675] |
| μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535] | ||||||||
| ChEMBL | Displacement of [3H]DAMGO from MOR in Wistar rat brain membranes after 60 mins by liquid scintillation analysis | B | 5 | pKi | >10000 | nM | Ki | Eur J Med Chem (2019) 178: 571-588 [PMID:31220675] |
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]
