carbenoxolone [Ligand Id: 4151] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL499915 (Carbenoxolone)
  • hydroxysteroid 11-beta dehydrogenase 1/11-beta-hydroxysteroid dehydrogenase 1 in Human [ChEMBL: CHEMBL4235] [GtoPdb: 2763] [UniProtKB: P28845]
  • hydroxysteroid 11-beta dehydrogenase 1/11-beta-hydroxysteroid dehydrogenase 1 in Mouse [ChEMBL: CHEMBL3910] [GtoPdb: 2763] [UniProtKB: P50172]
There should be some charts here, you may need to enable JavaScript!
  • hydroxysteroid 11-beta dehydrogenase 2/11-beta-hydroxysteroid dehydrogenase 2 in Mouse [ChEMBL: CHEMBL3490] [GtoPdb: 3143] [UniProtKB: P51661]
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
hydroxysteroid 11-beta dehydrogenase 1/11-beta-hydroxysteroid dehydrogenase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4235] [GtoPdb: 2763] [UniProtKB: P28845]
ChEMBL Inhibition of 11beta-HSD1 in human microsomes by HTRF cortisol assay B 6.3 pIC50 500 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 1065-1069 [PMID:20045318]
ChEMBL Inhibition of human 11beta-HSD1 expressed in CHO cells after 3 hrs by HTRF cortisol assay B 6.3 pIC50 500 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 435-439 [PMID:21093259]
ChEMBL Inhibition of human 11beta-HSD1 expressed in CHO-K1 cells using cortisone as substrate after 3 hrs by HTRF assay B 6.3 pIC50 500 nM IC50 ACS Med. Chem. Lett. (2012) 3: 88-93 [PMID:24900439]
ChEMBL In vitro inhibitory activity against human 11 beta hydroxysteroid dehydrogenase type 1 using scintillation proximity assay (SPA) B 6.48 pIC50 330 nM IC50 J. Med. Chem. (2002) 45: 3813-3815 [PMID:12190302]
ChEMBL Ability to convert [3H]cortisol to the tritium labeled cortisone in the presence of human 11 beta hydroxysteroid dehydrogenase type 2 B 7.08 pIC50 83 nM IC50 J. Med. Chem. (2002) 45: 3813-3815 [PMID:12190302]
hydroxysteroid 11-beta dehydrogenase 1/11-beta-hydroxysteroid dehydrogenase 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3910] [GtoPdb: 2763] [UniProtKB: P50172]
ChEMBL Inhibition of mouse 11beta-HSD1 expressed in CHO cells after 3 hrs by HTRF cortisol assay B 6.6 pIC50 250 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 435-439 [PMID:21093259]
ChEMBL In vitro inhibitory activity against mouse 11 beta hydroxysteroid dehydrogenase type 1 using scintillation proximity assay (SPA). B 6.97 pIC50 108 nM IC50 J. Med. Chem. (2002) 45: 3813-3815 [PMID:12190302]
hydroxysteroid 11-beta dehydrogenase 2/11-beta-hydroxysteroid dehydrogenase 2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3490] [GtoPdb: 3143] [UniProtKB: P51661]
ChEMBL Inhibition of mouse 11beta-HSD2 expressed in HEK293 cells assessed as conversion of [3H]cortisone into [3H]cortisol by scintillation proximity assay B 6.69 pIC50 206 nM IC50 J. Nat. Prod. (2012) 75: 599-604 [PMID:22360639]
ChEMBL Inhibition of mouse microsomal 11beta-HSD2 expressed in HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay B 7.09 pIC50 82 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 4455-4458 [PMID:19564108]
ChEMBL Inhibition of mouse 11beta-HSD2 expressed in HEK293 cells assessed as [3H]cortisol production after 60 mins by SPA B 7.09 pEC50 82 nM EC50 Bioorg. Med. Chem. Lett. (2012) 22: 2748-2752 [PMID:22440625]

ChEMBL data shown on this page come from version 27:

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]