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

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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]
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  • hydroxysteroid 11-beta dehydrogenase 2/11-beta-hydroxysteroid dehydrogenase 2 in Mouse [ChEMBL: CHEMBL3490] [GtoPdb: 3143] [UniProtKB: P51661]
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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 N-terminal MKHQHQHQHQHQHQQPL-tagged 11beta-HSD1 C272S mutant (unknown origin) expressed in Escherichia coli BL21 (DE3) using cortisol as substrate measured for 1 hr in presence of NADPH by fluorescence assay B 7.21 pKi 62 nM Ki J Med Chem (2019) 62: 6925-6940 [PMID:31294974]
ChEMBL Inhibition of human 11beta-HSD1 expressed in CHOK1 cells using XL665-labeled cortisol as substrate measured after 24 hrs by HTRF assay B 5.79 pIC50 1630 nM IC50 Bioorg Med Chem Lett (2020) 30: 126787-126787 [PMID:31759849]
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 Inhibition of N-terminal MKHQHQHQHQHQHQQPL-tagged 11beta-HSD1 C272S mutant (unknown origin) expressed in Escherichia coli BL21 (DE3) using cortisol as substrate measured for 1 hr in presence of NADPH by fluorescence assay B 6.39 pIC50 410 nM IC50 J Med Chem (2019) 62: 6925-6940 [PMID:31294974]
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 Inhibition of mouse 11beta-HSD1 expressed in CHOK1 cells using XL665-labeled cortisol as substrate measured after 24 hrs by HTRF assay B 6.61 pIC50 243 nM IC50 Bioorg Med Chem Lett (2020) 30: 126787-126787 [PMID:31759849]
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]
Px1/Pannexin-1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4879520] [GtoPdb: 735] [UniProtKB: Q9JIP4]
ChEMBL Inhibition of mouse Panx-1 expressed in Xenopus laevis oocytes assessed as inhibition of membrane current cells held at -60 mV and voltage steps to +60 mV in presence of CBX measured by Whole cell voltage clamp assay relative to control B 5 pIC50 10000 nM IC50 Eur J Med Chem (2021) 223: 113650-113650 [PMID:34174741]

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]