NESS0327 [Ligand Id: 14325] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL376700
  • CB1 receptor/Cannabinoid receptor 1 in Human [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
  • CB1 receptor/Cannabinoid receptor 1 in Mouse [ChEMBL: CHEMBL3037] [GtoPdb: 56] [UniProtKB: P47746]
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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]-CP55,940 from human CB1 receptor transfected in CHO cell membranes B 6.9 pKi 126 nM Ki Eur J Med Chem (2016) 121: 194-208 [PMID:27240274]
ChEMBL Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells B 7.74 pKi 18.4 nM Ki J Med Chem (2008) 51: 3526-3539 [PMID:18512901]
ChEMBL Displacement of [3H]SR141716 from human CB1 receptor expressed in CHO-K1 cells B 8.26 pKi 5.55 nM Ki J Med Chem (2008) 51: 3526-3539 [PMID:18512901]
GtoPdb Determined as displacement of [3H]SR141716 from human CB1 expressed in CHO-K1 cells - 8.26 pKi 5.55 nM Ki J Med Chem (2008) 51: 3526-39 [PMID:18512901]
CB1 receptor/Cannabinoid receptor 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3037] [GtoPdb: 56] [UniProtKB: P47746]
ChEMBL Displacement of [3H]-CP55,940 from CB1 receptor in mouse whole brain membranes after 60 mins by liquid scintillation spectrometry B 8.09 pKi 8.18 nM Ki Eur J Med Chem (2016) 121: 194-208 [PMID:27240274]
ChEMBL Displacement of [3H]-CP55,940 from CB1 receptor in mouse whole brain membranes after 60 mins by liquid scintillation spectrometry B 8.38 pKi 4.2 nM Ki Eur J Med Chem (2016) 121: 194-208 [PMID:27240274]
ChEMBL Displacement of [3H]CP-55940 from CB1 receptor in CD1 mouse brain B 12.46 pKi 0 nM Ki J Med Chem (2005) 48: 7351-7362 [PMID:16279795]
CB2 receptor/Cannabinoid receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
ChEMBL Displacement of [3H]-CP55,940 from human CB2 receptor transfected in CHO cell membranes after 60 mins by liquid scintillation spectrometry B 7.07 pKi 85.2 nM Ki Eur J Med Chem (2016) 121: 194-208 [PMID:27240274]
ChEMBL Displacement of [3H]-CP55,940 from human CB2 receptor transfected in CHO cell membranes after 60 mins by liquid scintillation spectrometry B 7.25 pKi 55.7 nM Ki Eur J Med Chem (2016) 121: 194-208 [PMID:27240274]
ChEMBL Binding affinity to CB2 receptor B 7.68 pKi 21 nM Ki J Med Chem (2008) 51: 2439-2446 [PMID:18363352]
ChEMBL Binding affinity to CB2 receptor B 7.7 pKi 20 nM Ki J Med Chem (2008) 51: 3526-3539 [PMID:18512901]
CB2 receptor/Cannabinoid receptor 2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5373] [GtoPdb: 57] [UniProtKB: P47936]
ChEMBL Displacement of [3H]CP-55940 from CB2 receptor in CD1 mouse spleen B 7.68 pKi 21 nM Ki J Med Chem (2005) 48: 7351-7362 [PMID:16279795]
ChEMBL Displacement of [3H]-CP55,940 from CB2 receptor in CD1 mouse spleen homogenates after 60 mins by liquid scintillation counting method B 7.68 pKi 21 nM Ki Eur J Med Chem (2016) 121: 194-208 [PMID:27240274]

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]