HU-308 [Ligand Id: 746] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL497392 (HU-308)
  • CB1 receptor/Cannabinoid CB1 receptor in Human [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
  • 5
1 CHEMBL497392_lig_chart_1 Cannabinoid CB1 receptor Human
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  • CB2 receptor/Cannabinoid CB2 receptor in Human [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
  • CB2 receptor/Cannabinoid CB2 receptor in Rat [ChEMBL: CHEMBL2470] [GtoPdb: 57] [UniProtKB: Q9QZN9]
  • 7.64
2 CHEMBL497392_lig_chart_2 Cannabinoid CB2 receptor HumanRat
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  • glycine receptor α2 subunit in Human [GtoPdb: 424] [UniProtKB: P23416]
  • This target only has 0 pki data point
  • 0
3 CHEMBL497392_lig_chart_3 glycine receptor α2 subunit Human
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  • glycine receptor α3 subunit in Human [GtoPdb: 425] [UniProtKB: O75311]
  • This target only has 0 pki data point
  • 0
4 CHEMBL497392_lig_chart_4 glycine receptor α3 subunit Human
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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 to CB1 receptor B 5 pKi 10000 nM Ki J. Med. Chem. (2009) 52: 369-378 [PMID:19143566]
ChEMBL Binding affinity to cannabinoid CB1 receptor B 5 pKi >=10000 nM Ki J. Med. Chem. (2010) 53: 4332-4353 [PMID:20218623]
ChEMBL Displacement of [3H]CP 55940 from human CB1 receptor in cell free system B 5 pKi 10000 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]
GtoPdb - - 7.6 pKi 25.1 nM Ki Proc Natl Acad Sci USA (1999) 96: 14228-33 [PMID:10588688]
ChEMBL Binding affinity to CB2 receptor B 7.64 pKi 22.7 nM Ki J. Med. Chem. (2009) 52: 369-378 [PMID:19143566]
ChEMBL Binding affinity to cannabinoid CB2 receptor B 7.64 pKi 22.7 nM Ki J. Med. Chem. (2010) 53: 4332-4353 [PMID:20218623]
ChEMBL Displacement of [3H]CP 55940 from human CB2 receptor in cell free system B 7.64 pKi 22.7 nM Ki Eur. J. Med. Chem. (2011) 46: 547-555 [PMID:21183257]
ChEMBL Agonist activity at human CB2 receptor expressed in HEK293 cell membranes assessed as induction of [35S]-GTPgammaS binding after 60 mins by liquid scintillation spectrometric method B 7.19 pEC50 64.5 nM EC50 J Med Chem (2016) 59: 6753-6771 [PMID:27309150]
ChEMBL Agonist activity at human CB2 receptor expressed in HEK293 cell membranes assessed as induction of [35S]-GTPgammaS binding after 60 mins by liquid scintillation spectrometric method B 7.19 pEC50 64.5 nM EC50 J Med Chem (2016) 59: 6753-6771 [PMID:27309150]
CB2 receptor/Cannabinoid CB2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2470] [GtoPdb: 57] [UniProtKB: Q9QZN9]
ChEMBL Displacement of [3H]HU-243 from rat CB2 receptor expressed in African green monkey COS7 cell membranes after 90 mins B 7.64 pKi 22.7 nM Ki J Med Chem (2016) 59: 6753-6771 [PMID:27309150]
ChEMBL Displacement of [3H]HU-243 from rat CB2 receptor expressed in African green monkey COS7 cell membranes after 90 mins B 7.64 pKi 22.7 nM Ki J Med Chem (2016) 59: 6753-6771 [PMID:27309150]
glycine receptor α2 subunit in Human [GtoPdb: 424] [UniProtKB: P23416]
GtoPdb - - 6 pIC50 1100 nM IC50
glycine receptor α3 subunit in Human [GtoPdb: 425] [UniProtKB: O75311]
GtoPdb - - 7 pIC50 97 nM IC50

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]