L-759,633 [Ligand Id: 748] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL57367 (L-759633)
  • CB1 receptor/Cannabinoid CB1 receptor in Human [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
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  • CB2 receptor/Cannabinoid CB2 receptor in Human [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
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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 Binding affinity against human cannabinoid receptor by using radioligand ([3H]CP-55940) assay. B 4.8 pKi 15850 nM Ki Bioorg. Med. Chem. Lett. (1996) 6: 189-194
ChEMBL Binding affinity to human CB1 receptor B 4.8 pKi 15850 nM Ki J. Med. Chem. (2013) 56: 8224-8256 [PMID:23865723]
ChEMBL Displacement of [3H]CP 55940 from human CB1 receptor in cell free system B 5.98 pKi 1043 nM Ki Eur. J. Med. Chem. (2011) 46: 547-555 [PMID:21183257]
CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
ChEMBL Binding affinity against human Cannabinoid receptor 2 by using radioligand ([3H]CP-55940) assay. B 7.7 pKi 20 nM Ki Bioorg. Med. Chem. Lett. (1996) 6: 189-194
ChEMBL Binding affinity to human CB2 receptor B 7.7 pKi 20 nM Ki J. Med. Chem. (2013) 56: 8224-8256 [PMID:23865723]
ChEMBL Displacement of [3H]CP 55940 from human CB2 receptor in cell free system B 8.19 pKi 6.4 nM Ki Eur. J. Med. Chem. (2011) 46: 547-555 [PMID:21183257]
GtoPdb - - 8.2 pKi 6.31 nM Ki Br J Pharmacol (1999) 126: 665-672 [PMID:10188977];
Bioorg Med Chem Lett (1996) 6: 189-194

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]