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ChEMBL ligand: CHEMBL371214 (JWH-133) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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CB1 receptor/Cannabinoid CB1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554] | ||||||||
ChEMBL | Displacement of human recombinant CB1 receptor expressed in HEK293 cell membranes incubated for 90 mins by Cheng-Prusoff equation based analysis | B | 5 | pKi | >10000 | nM | Ki | Medchemcomm (2014) 5: 1571-1576 |
ChEMBL | Displacement of [3H]-CP-55940 from human CB1 receptor expressed in CHO cell membranes after 1 hr by beta-counting analysis | B | 6 | pKi | >1000 | nM | Ki | Eur J Med Chem (2019) 165: 347-362 [PMID:30583970] |
ChEMBL | Binding affinity to cannabinoid CB1 receptor | B | 6.17 | pKi | 677 | nM | Ki | J Med Chem (2010) 53: 4332-4353 [PMID:20218623] |
ChEMBL | Displacement of [3H]CP 55940 from human CB1 receptor in cell free system | B | 6.17 | pKi | 677 | nM | Ki | Eur J Med Chem (2011) 46: 547-555 [PMID:21183257] |
ChEMBL | Binding affinity to CB1 receptor | B | 6.17 | pKi | 677 | nM | Ki | Bioorg Med Chem (2011) 19: 5698-5707 [PMID:21872477] |
ChEMBL | Displacement of [3H]CP55,940 from human recombinant CB1 receptor expressed in HEK293 cell membranes after 90 mins | B | 6.17 | pKi | 677 | nM | Ki | Eur J Med Chem (2014) 74: 524-532 [PMID:24518874] |
ChEMBL | Displacement of [3H]CP-55,940 from human recombinant CB1R expressed in HEK-293 cells after 90 mins by liquid scintillation counting | B | 6.17 | pKi | 677 | nM | Ki | J Med Chem (2014) 57: 8777-8791 [PMID:25272206] |
ChEMBL | Displacement of [3H]CP55,940 from human recombinant CB1 receptor expressed in HEK293 cell membranes after 90 mins | B | 6.17 | pKi | 677 | nM | Ki | Eur J Med Chem (2015) 90: 526-536 [PMID:25486424] |
ChEMBL | Displacement of [3H]-CP-55940 from recombinant human CB1 receptor overexpressed in HEK293 cell membranes after 90 mins | B | 6.17 | pKi | 677 | nM | Ki | Eur J Med Chem (2015) 97: 10-18 [PMID:25935384] |
ChEMBL | Binding affinity to CB1 receptor | B | 6.17 | pKi | 677 | nM | Ki | J Med Chem (2009) 52: 369-378 [PMID:19143566] |
ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells | B | 6.17 | pKi | 677 | nM | Ki | J Med Chem (2009) 52: 3644-3651 [PMID:19435366] |
ChEMBL | Displacement of [3H]CP55940 from recombinant human CB1 receptor expressed in human HEK293 cell membrane after 90 mins | B | 6.93 | pKi | 116.8 | nM | Ki | Eur J Med Chem (2012) 52: 284-294 [PMID:22483967] |
ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor | B | 9.1 | pKi | 0.8 | nM | Ki | J Med Chem (2009) 52: 369-378 [PMID:19143566] |
ChEMBL | Displacement of human recombinant CB1 receptor expressed in HEK293 cell membranes incubated for 90 mins by radioligand binding assay | B | 5 | pIC50 | >10000 | nM | IC50 | Medchemcomm (2014) 5: 1571-1576 |
CB1 receptor/Cannabinoid CB1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3037] [GtoPdb: 56] [UniProtKB: P47746] | ||||||||
ChEMBL | Displacement of [3H]CP-55940 from CB1 receptor in DBA/J2 mouse brain | B | 6.34 | pKi | 458 | nM | Ki | J Med Chem (2006) 49: 5947-5957 [PMID:17004710] |
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 Sprague-Dawley rat brain membranes after 1 hr by liquid scintillation spectrophotometry | B | 6.17 | pKi | 677 | nM | Ki | Bioorg Med Chem (2010) 18: 7809-7815 [PMID:20943404] |
ChEMBL | Binding affinity to rat CB1 receptor | B | 6.17 | pKi | 677 | nM | Ki | J Med Chem (2013) 56: 8224-8256 [PMID:23865723] |
ChEMBL | Displacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptor | F | 5.7 | pEC50 | 1995.26 | nM | EC50 | J Med Chem (2006) 49: 554-566 [PMID:16420041] |
CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972] | ||||||||
ChEMBL | Displacement of human recombinant CB2 receptor expressed in HEK293 cell membranes incubated for 90 mins by Cheng-Prusoff equation based analysis | B | 6.85 | pKi | 140 | nM | Ki | Medchemcomm (2014) 5: 1571-1576 |
ChEMBL | Displacement of [3H]CP-55940 from human CB2 receptor | B | 7.69 | pKi | 20.3 | nM | Ki | J Med Chem (2006) 49: 70-79 [PMID:16392793] |
ChEMBL | Displacement of [3H]-CP-55940 from human CB2 receptor expressed in CHO cell membranes after 1 hr by beta-counting analysis | B | 8.1 | pKi | 8 | nM | Ki | Eur J Med Chem (2019) 165: 347-362 [PMID:30583970] |
ChEMBL | Binding affinity to CB2 receptor | B | 8.47 | pKi | 3.4 | nM | Ki | J Med Chem (2009) 52: 369-378 [PMID:19143566] |
ChEMBL | Binding affinity to cannabinoid CB2 receptor | B | 8.47 | pKi | 3.4 | nM | Ki | J Med Chem (2010) 53: 4332-4353 [PMID:20218623] |
ChEMBL | Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO cells after 1 hr by liquid scintillation spectrophotometry | B | 8.47 | pKi | 3.4 | nM | Ki | Bioorg Med Chem (2010) 18: 7809-7815 [PMID:20943404] |
ChEMBL | Displacement of [3H]CP 55940 from human CB2 receptor in cell free system | B | 8.47 | pKi | 3.4 | nM | Ki | Eur J Med Chem (2011) 46: 547-555 [PMID:21183257] |
ChEMBL | Binding affinity to CB2 receptor | B | 8.47 | pKi | 3.4 | nM | Ki | Bioorg Med Chem (2011) 19: 5698-5707 [PMID:21872477] |
ChEMBL | Binding affinity to human CB2 receptor | B | 8.47 | pKi | 3.4 | nM | Ki | J Med Chem (2013) 56: 8224-8256 [PMID:23865723] |
ChEMBL | Displacement of [3H]-CP55940 from human CB2 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation spectrometric method | B | 8.47 | pKi | 3.4 | nM | Ki | J Med Chem (2016) 59: 6753-6771 [PMID:27309150] |
GtoPdb | - | - | 8.5 | pKi | 3.16 | nM | Ki |
Bioorg Med Chem (1999) 7: 2905-14 [PMID:10658595]; Expert Opin Investig Drugs (2000) 9: 1553-71 [PMID:11060760] |
ChEMBL | Displacement of [3H]-CP-55940 from recombinant human CB2 receptor overexpressed in HEK293 cell membranes after 90 mins | B | 8.52 | pKi | 3 | nM | Ki | Eur J Med Chem (2015) 97: 10-18 [PMID:25935384] |
ChEMBL | Displacement of [3H]CP-55,940 from human recombinant CB2R expressed in HEK-293 cells after 90 mins by liquid scintillation counting | B | 8.52 | pKi | 3 | nM | Ki | J Med Chem (2014) 57: 8777-8791 [PMID:25272206] |
ChEMBL | Displacement of [3H]CP55,940 from human recombinant CB2 receptor expressed in HEK293 cell membranes after 90 mins | B | 8.52 | pKi | 3 | nM | Ki | Eur J Med Chem (2015) 90: 526-536 [PMID:25486424] |
ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells | B | 8.52 | pKi | 3 | nM | Ki | J Med Chem (2009) 52: 3644-3651 [PMID:19435366] |
ChEMBL | Displacement of [3H]CP55,940 from human recombinant CB2 receptor expressed in HEK293 cell membranes after 90 mins | B | 8.52 | pKi | 3 | nM | Ki | Eur J Med Chem (2014) 74: 524-532 [PMID:24518874] |
ChEMBL | Displacement of [3H]CP55940 from recombinant human CB2 receptor expressed in human HEK293 cell membrane after 90 mins | B | 8.74 | pKi | 1.82 | nM | Ki | Eur J Med Chem (2012) 52: 284-294 [PMID:22483967] |
ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB2 receptor | B | 10.64 | pKi | 0.02 | nM | Ki | J Med Chem (2009) 52: 369-378 [PMID:19143566] |
ChEMBL | Displacement of human recombinant CB2 receptor expressed in HEK293 cell membranes incubated for 90 mins by radioligand binding assay | B | 6.26 | pIC50 | 550 | nM | IC50 | Medchemcomm (2014) 5: 1571-1576 |
ChEMBL | Agonist activity at human CB2 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 mins by HTRF assay | F | 7.09 | pIC50 | 81.8 | nM | IC50 | J Med Chem (2016) 59: 6753-6771 [PMID:27309150] |
ChEMBL | Agonist activity at human CB2 receptor expressed in CHO-K1 cells assessed as inhibition of NKH-477 induced cAMP production incubated for 30 mins by luminescence based analysis | F | 3.77 | pEC50 | 168600 | nM | EC50 | Eur J Med Chem (2023) 248: 115109-115109 [PMID:36657299] |
ChEMBL | Agonist activity at recombinant human CB2R expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels after 30 mins by chemiluminescent detection based cAMP Hunter assay | F | 6.41 | pEC50 | 391.1 | nM | EC50 | J Med Chem (2020) 63: 7369-7391 [PMID:32515588] |
ChEMBL | Agonist activity at human CB2 receptor overexpressed in CHO-K1 cells assessed as cAMP level incubated for 30 mins by luminescence based assay | F | 6.77 | pEC50 | 168.6 | nM | EC50 | J Med Chem (2023) 66: 235-250 [PMID:36542836] |
ChEMBL | Effect on [35S]GTP-gamma-S binding to human CB2 receptor | F | 6.84 | pEC50 | 145.6 | nM | EC50 | J Med Chem (2006) 49: 70-79 [PMID:16392793] |
ChEMBL | Agonist activity at human CB2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 1.5 hrs by liquid scintillation spectrophotometry | F | 8.4 | pEC50 | 4 | nM | EC50 | Bioorg Med Chem (2010) 18: 7809-7815 [PMID:20943404] |
CB2 receptor/Cannabinoid CB2 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5373] [GtoPdb: 57] [UniProtKB: P47936] | ||||||||
ChEMBL | Displacement of [3H]CP-55940 from CB2 receptor in DBA/J2 mouse spleen | B | 7.19 | pKi | 65 | nM | Ki | J Med Chem (2006) 49: 5947-5957 [PMID:17004710] |
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]