L-759,656 [Ligand Id: 749] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL294013 (L-759656)
  • 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 4.7 pKi >20000 nM Ki Bioorg Med Chem Lett (1996) 6: 189-194
ChEMBL Binding affinity to human CB1 receptor B 4.7 pKi >20000 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 5.31 pKi 4888 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 7.71 pKi 19.4 nM Ki Bioorg Med Chem Lett (1996) 6: 189-194
ChEMBL Binding affinity to human CB2 receptor B 7.71 pKi 19.4 nM Ki J Med Chem (2013) 56: 8224-8256 [PMID:23865723]
GtoPdb - - 7.9 pKi 12.6 nM Ki Br J Pharmacol (1999) 126: 665-672 [PMID:10188977];
Bioorg Med Chem Lett (1996) 6: 189-194
ChEMBL Displacement of [3H]CP 55940 from human CB2 receptor in cell free system B 7.93 pKi 11.8 nM Ki Eur J Med Chem (2011) 46: 547-555 [PMID:21183257]

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]