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 human HEK293-EBNA cells incubated for 60 mins by radioligand competitive binding assay based liquid scintillation counter | B | 8.59 | pKi | 2.57 | nM | Ki | RSC Med Chem (2022) 13: 156-174 [PMID:35308023] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB1 receptor expressed in human HEK293-EBNA cells incubated for 60 mins by radioligand competitive binding assay based liquid scintillation counter | B | 8.59 | pKi | 2.56 | nM | Ki | RSC Med Chem (2022) 13: 156-174 [PMID:35308023] |
| 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 CB1 receptor (unknown origin) expressed in human HEK293T cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment using furimazine as substrate by Nano-Glo live cell reagent assay | F | 7.45 | pEC50 | 35.5 | nM | EC50 | RSC Med Chem (2022) 13: 156-174 [PMID:35308023] |
| ChEMBL | Agonist activity at CB1 receptor (unknown origin) expressed in human HEK293T cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment using furimazine as substrate by Nano-Glo live cell reagent assay | F | 7.45 | pEC50 | 35.48 | nM | EC50 | RSC Med Chem (2022) 13: 156-174 [PMID:35308023] |
| ChEMBL | Agonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assay | F | 7.74 | pEC50 | 18.2 | nM | EC50 | RSC Med Chem (2022) 13: 156-174 [PMID:35308023] |
| ChEMBL | Agonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assay | F | 7.74 | pEC50 | 18 | nM | EC50 | RSC Med Chem (2022) 13: 156-174 [PMID:35308023] |
| 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 N-terminal 3HA-tagged human CB2 receptor expressed in human HEK293-EBNA cells incubated for 60 mins by radioligand competitive binding assay based liquid scintillation counter | B | 8.02 | pKi | 9.55 | nM | Ki | RSC Med Chem (2022) 13: 156-174 [PMID:35308023] |
| ChEMBL | Displacement of [3H]-CP55940 from N-terminal 3HA-tagged human CB2 receptor expressed in human HEK293-EBNA cells incubated for 60 mins by radioligand competitive binding assay based liquid scintillation counter | B | 8.02 | pKi | 9.55 | nM | Ki | RSC Med Chem (2022) 13: 156-174 [PMID:35308023] |
| 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 mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assay | F | 7.66 | pEC50 | 22 | nM | EC50 | RSC Med Chem (2022) 13: 156-174 [PMID:35308023] |
| ChEMBL | Agonist activity at human CB2 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assay | F | 7.66 | pEC50 | 21.88 | nM | EC50 | RSC Med Chem (2022) 13: 156-174 [PMID:35308023] |
| ChEMBL | Agonist activity at CB2 receptor (unknown origin) expressed in human HEK293T cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment using furimazine as substrate by Nano-Glo live cell reagent assay | F | 8.14 | pEC50 | 7.3 | nM | EC50 | RSC Med Chem (2022) 13: 156-174 [PMID:35308023] |
| ChEMBL | Agonist activity at CB2 receptor (unknown origin) expressed in human HEK293T cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment using furimazine as substrate by Nano-Glo live cell reagent assay | F | 8.14 | pEC50 | 7.24 | nM | EC50 | RSC Med Chem (2022) 13: 156-174 [PMID:35308023] |
| 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 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]
