lenabasum [Ligand Id: 9772] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL456341 (Ajulemic acid, Ajulemic Acid, CPL7075, CPL-7075, CT-3, HU-239, IP-751, JBT-101, Lenabasum, Resunab)
  • 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]
GtoPdb - - 7.49 pKi 32.3 nM Ki J Med Chem (2013) 56: 8224-56 [PMID:23865723];
J Med Chem (1997) 40: 3228-33 [PMID:9379442]
ChEMBL Binding affinity to human CB1 receptor B 7.49 pKi 32.3 nM Ki J. Med. Chem. (2013) 56: 8224-8256 [PMID:23865723]
ChEMBL Binding affinity to CB1 receptor (unknown origin) B 8.24 pKi 5.7 nM Ki Bioorg. Med. Chem. (2014) 22: 2830-2843 [PMID:24731541]
ChEMBL Agonist activity at CB1 receptor (unknown origin) assessed as cAMP production F 6.03 pEC50 927 nM EC50 J. Med. Chem. (2013) 56: 8224-8256 [PMID:23865723]
CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
ChEMBL Binding affinity to human CB2 receptor B 6.77 pKi 170.5 nM Ki J. Med. Chem. (2013) 56: 8224-8256 [PMID:23865723]
GtoPdb - - 6.77 pKi 170 nM Ki J Med Chem (2013) 56: 8224-56 [PMID:23865723];
J Med Chem (1997) 40: 3228-33 [PMID:9379442]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]