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) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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 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 33:
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]
