JWH-133 [Ligand Id: 747] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL371214 (JWH-133)
  • CB1 receptor/Cannabinoid CB1 receptor in Human [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
  • CB1 receptor/Cannabinoid CB1 receptor in Mouse [ChEMBL: CHEMBL3037] [GtoPdb: 56] [UniProtKB: P47746]
  • CB1 receptor/Cannabinoid CB1 receptor in Rat [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272]
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  • CB2 receptor/Cannabinoid CB2 receptor in Human [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
  • CB2 receptor/Cannabinoid CB2 receptor in Mouse [ChEMBL: CHEMBL5373] [GtoPdb: 57] [UniProtKB: P47936]
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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]
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]