nabilone [Ligand Id: 9071] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2218896 (Cesamet, CPD 109514, CPD-109514, Nabilona, Nabilone)
  • CB1 receptor/Cannabinoid receptor 1 in Human [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
  • CB1 receptor/Cannabinoid receptor 1 in Rat [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272]
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  • CB2 receptor/Cannabinoid receptor 2 in Human [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
  • CB2 receptor/Cannabinoid receptor 2 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 receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells B 8.29 pKi 5.1 nM Ki Bioorg Med Chem Lett (2010) 20: 4992-4998 [PMID:20688519]
GtoPdb - - 8.4 pKi 3.98 nM Ki Eur J Med Chem (2011) 46: 5086-98 [PMID:21885167]
ChEMBL Displacement of [3H]-CP55940 from human CB1 receptor expressed in CHO cells by liquid scintillation counting B 8.4 pKi 3.98 nM Ki Eur J Med Chem (2011) 46: 5086-5098 [PMID:21885167]
ChEMBL Binding affinity against human cannabinoid receptor by using radioligand ([3H]CP-55940) assay. B 8.66 pKi 2.19 nM Ki Bioorg Med Chem Lett (1996) 6: 189-194
ChEMBL Binding affinity to human CB1 receptor B 8.66 pKi 2.19 nM Ki J Med Chem (2013) 56: 8224-8256 [PMID:23865723]
ChEMBL Agonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assay F 8.4 pEC50 3.98 nM EC50 Bioorg Med Chem Lett (2010) 20: 4992-4998 [PMID:20688519]
ChEMBL Agonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid release F 8.4 pEC50 3.98 nM EC50 Eur J Med Chem (2011) 46: 5086-5098 [PMID:21885167]
CB1 receptor/Cannabinoid receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272]
ChEMBL Displacement of [3H]CP55940 from rat brain CB1 receptor B 8.66 pKi 2.2 nM Ki J Med Chem (2010) 53: 6996-7010 [PMID:20925434]
CB2 receptor/Cannabinoid receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in CHO cells B 7.75 pKi 17.6 nM Ki Bioorg Med Chem Lett (2010) 20: 4992-4998 [PMID:20688519]
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 - - 8.2 pKi 6.31 nM Ki Eur J Med Chem (2011) 46: 5086-98 [PMID:21885167]
ChEMBL Binding affinity against human Cannabinoid receptor 2 by using radioligand ([3H]CP-55940) assay. B 8.74 pKi 1.84 nM Ki Bioorg Med Chem Lett (1996) 6: 189-194
ChEMBL Binding affinity to human CB2 receptor B 8.74 pKi 1.84 nM Ki J Med Chem (2013) 56: 8224-8256 [PMID:23865723]
ChEMBL Agonist activity at human CB2 receptor expressed in CHO cells assessed as increase of forskolin-stimulated cAMP accumulation after 20 mins F 7.8 pEC50 15.85 nM EC50 Eur J Med Chem (2011) 46: 5086-5098 [PMID:21885167]
CB2 receptor/Cannabinoid receptor 2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5373] [GtoPdb: 57] [UniProtKB: P47936]
ChEMBL Displacement of [3H]CP55940 from mouse spleen CB2 receptor B 8.74 pKi 1.8 nM Ki J Med Chem (2010) 53: 6996-7010 [PMID:20925434]

ChEMBL data shown on this page come from version 36:

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]