ChEMBL ligand: CHEMBL499915 (Carbenoxolona, 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 type 2 in Mouse [ChEMBL: CHEMBL3490] [GtoPdb: 3143] [UniProtKB: P51661] There should be some charts here, you may need to enable JavaScript!
Px1/Pannexin-1 in Mouse [ChEMBL: CHEMBL4879520] [GtoPdb: 735] [UniProtKB: Q9JIP4] There should be some charts here, you may need to enable JavaScript!
protein tyrosine phosphatase non-receptor type 1/Tyrosine-protein phosphatase non-receptor type 1 in Human [ChEMBL: CHEMBL335] [GtoPdb: 2976] [UniProtKB: P18031] 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	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 type 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]
protein tyrosine phosphatase non-receptor type 1/Tyrosine-protein phosphatase non-receptor type 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL335] [GtoPdb: 2976] [UniProtKB: P18031]
ChEMBL	Metabolic Measurements: Glucose in tail blood was measured using a glucometer (One-Touch Basic; Lifescan, CA). For glucose tolerance tests (GTTs), mice were fasted for 10 hours and then injected with 20% D-glucose (2 mg/g body weight) and the blood glucose was monitored immediately before and at 15, 30, 60 and 120 mins following the injection. For insulin tolerance tests (ITTs), 4-h fasted animals were given insulin (0.75 mU/g) and blood glucose was measured immediately before and at 30, 60 and 120 minutes postinjection. Serum insulin, cholesterol, triglycerides (Stanbio Labs, TX), BDNF (Abnova), IGF1 and IGFBPs (R&D Systems) were determined by enzyme-linked immunosorbent assay.	B	5.15	pKi	7000	nM	Ki	US-11660306-B2. Treatment of Rett syndrome (2023)

ChEMBL data shown on this page come from version 36:

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]