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 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]