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ChEMBL ligand: CHEMBL499915 (Carbenoxolone) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 | Inhibition of human 11beta-HSD1 by HTRF assay | B | 6.48 | pIC50 | 330 | nM | IC50 | Eur J Med Chem (2020) 191: 112134-112134 [PMID:32088493] |
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] |
ChEMBL | Inhibition of human 11beta-HSD1 | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem Lett (2022) 69: 128782-128782 [PMID:35537608] |
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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]