enoxolone [Ligand Id: 11264] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL230006 (Enoxolona, Enoxolone, NSC-35347, NSC-35350) |
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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 human 11beta-HSD1 expressed in HEK293 cells measured after 10 mins | B | 6.11 | pIC50 | 779 | nM | IC50 | Eur J Med Chem (2020) 191: 112134-112134 [PMID:32088493] |
| ChEMBL | Inhibition of human recombinant 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [1,2-[3H]cortisone to cortisol after 10 mins by scintillation counting | B | 6.11 | pIC50 | 778 | nM | IC50 | Bioorg Med Chem (2011) 19: 1866-1880 [PMID:21376605] |
| ChEMBL | Inhibition of human recombinant 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [1,2-3H]-cortisone to cortisol by scintillation counting | B | 6.11 | pIC50 | 778 | nM | IC50 | Bioorg Med Chem (2010) 18: 7522-7541 [PMID:20851614] |
| ChEMBL | Inhibition of human 11beta-HSD1 expressed in HEK293 cell microsomes assessed as inhibition of [3H]cortisone conversion to [3H]cortisol by scintillation proximity assay | B | 7.54 | pIC50 | 29.1 | nM | IC50 | Eur J Med Chem (2013) 65: 403-414 [PMID:23747808] |
| ChEMBL | Inhibition of human 11beta-HSD1 overexpressed in microsomal fraction of HEK293 cells assessed as formation of [3H]-cortisol from [3H]-cortisone by scintillation proximity assay in presence of NADPH | B | 7.54 | pIC50 | 29.1 | nM | IC50 | J Nat Prod (2015) 78: 330-334 [PMID:25590374] |
| GtoPdb | - | - | 7.54 | pIC50 | 29 | nM | IC50 | J Nat Prod (2015) 78: 330-4 [PMID:25590374] |
| ChEMBL | Inhibition of human 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay in presence of NADPH | B | 7.89 | pIC50 | 13 | nM | IC50 | Eur J Med Chem (2009) 44: 1167-1171 [PMID:18653260] |
| GtoPdb | - | - | 7.89 | pIC50 | 13 | nM | IC50 | Eur J Med Chem (2009) 44: 1167-71 [PMID:18653260] |
| ChEMBL | Inhibition of human 11beta-HSD1 | B | 7.93 | pIC50 | 11.78 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 1340-1345 [PMID:18242087] |
| ChEMBL | Inhibition of full-length human 11beta-HSD1 expressed in HEK293 microsomal fraction using [3H]cortisone as substrate after 2 hr by scintillation proximity assay | B | 7.95 | pIC50 | 11.3 | nM | IC50 | Eur J Med Chem (2017) 135: 324-338 [PMID:28458137] |
| ChEMBL | Inhibition of human microsomal 11beta-HSD1 overexpressed in HEK293 cells using [3H]-cortisone as substrate assessed as formation of [3H]-cortisol using [3H]cortisone by scintillation proximity assay in presence of NADPH | B | 8.06 | pIC50 | 8.8 | nM | IC50 | J Nat Prod (2016) 79: 899-906 [PMID:26936592] |
| ChEMBL | Inhibition of human 11beta HSD1 expressed in HEK293 cells assessed as assessed as inhibition of [1,2-(n)3H]cortisone to [3H]-cortisol after 60 mins by scintillation proximity assay | B | 8.07 | pIC50 | 8.6 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 5739-5744 [PMID:21873057] |
| 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 overexpressed in microsomal fraction of HEK293 cells assessed as formation of [3H]-cortisol from [3H]-cortisone by scintillation proximity assay in presence of NADPH | B | 7.4 | pIC50 | 40.2 | nM | IC50 | J Nat Prod (2015) 78: 330-334 [PMID:25590374] |
| ChEMBL | Inhibition of mouse 11beta-HSD1 | B | 7.98 | pIC50 | 10.58 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 1340-1345 [PMID:18242087] |
| ChEMBL | Inhibition of mouse microsomal 11beta-HSD1 overexpressed in HEK293 cells using [3H]-cortisone as substrate assessed as formation of [3H]-cortisol using [3H]cortisone by scintillation proximity assay in presence of NADPH | B | 8.03 | pIC50 | 9.4 | nM | IC50 | J Nat Prod (2016) 79: 899-906 [PMID:26936592] |
| ChEMBL | Inhibition of full-length mouse 11beta-HSD1 expressed in HEK293 microsomal fraction using [3H]cortisone as substrate after 1 hr by scintillation proximity assay | B | 8.13 | pIC50 | 7.4 | nM | IC50 | Eur J Med Chem (2017) 135: 324-338 [PMID:28458137] |
| ChEMBL | Inhibition of mouse 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay in presence of NADPH | B | 8.3 | pIC50 | 5 | nM | IC50 | Eur J Med Chem (2009) 44: 1167-1171 [PMID:18653260] |
| ChEMBL | Inhibition of mouse 11beta-HSD1 expressed in HEK293 cell microsomes assessed as inhibition of [3H]cortisone conversion to [3H]cortisol by scintillation proximity assay | B | 8.7 | pIC50 | 2 | nM | IC50 | Eur J Med Chem (2013) 65: 403-414 [PMID:23747808] |
| hydroxysteroid 11-beta dehydrogenase 1/11-beta-hydroxysteroid dehydrogenase 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2391] [GtoPdb: 2763] [UniProtKB: P16232] | ||||||||
| ChEMBL | Inhibition of 11beta-HSD1 in rat liver assessed as cortisone level | B | 7.05 | pIC50 | 90 | nM | IC50 | Bioorg Med Chem (2010) 18: 433-454 [PMID:19914836] |
| ChEMBL | Inhibition of rat hepatic 11beta-HSD1 | B | 7.05 | pIC50 | 90 | nM | IC50 | Bioorg Med Chem (2011) 19: 1866-1880 [PMID:21376605] |
| GtoPdb | - | - | 7.05 | pIC50 | 90 | nM | IC50 | Bioorg Med Chem (2010) 18: 433-54 [PMID:19914836] |
| hydroxysteroid 11-beta dehydrogenase 2/11-beta-hydroxysteroid dehydrogenase type 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3746] [GtoPdb: 3143] [UniProtKB: P80365] | ||||||||
| ChEMBL | Inhibition of human recombinant 11beta-HSD2 expressed in HEK293 cells assessed as conversion of [1,2,6,7-3H]-cortisol to cortisone by scintillation counting | B | 6.59 | pIC50 | 257 | nM | IC50 | Bioorg Med Chem (2010) 18: 7522-7541 [PMID:20851614] |
| ChEMBL | Inhibition of human 11beta-HSD2 expressed in HEK293 cells assessed as conversion of [1,2,6,7-[3H]cortisol to cortisone after 10 mins by scintillation counting | B | 6.59 | pIC50 | 257 | nM | IC50 | Bioorg Med Chem (2011) 19: 1866-1880 [PMID:21376605] |
| ChEMBL | Inhibition of full-length human 11beta-HSD2 expressed in HEK293 microsomal fraction using [3H]cortisone as substrate after 2 hr by scintillation proximity assay | B | 8.89 | pIC50 | 1.3 | nM | IC50 | Eur J Med Chem (2017) 135: 324-338 [PMID:28458137] |
| ChEMBL | Inhibition of human 11beta-HSD2 | B | 8.91 | pIC50 | 1.22 | nM | IC50 | Eur J Med Chem (2013) 65: 403-414 [PMID:23747808] |
| GtoPdb | - | - | 8.92 | pIC50 | 1.2 | nM | IC50 | J Nat Prod (2015) 78: 330-4 [PMID:25590374] |
| ChEMBL | Inhibition of human 11beta-HSD2 overexpressed in microsomal fraction of HEK293 cells using [3H]-cortisol as substrate by scintillation proximity assay in presence of NAD+ | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Nat Prod (2015) 78: 330-334 [PMID:25590374] |
| 11-beta-hydroxysteroid dehydrogenase type 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2908] [UniProtKB: P50233] | ||||||||
| ChEMBL | Inhibition of rat renal 11beta-HSD2 in rat liver assessed as inhibition of cortisone production | B | 6.44 | pIC50 | 360 | nM | IC50 | Bioorg Med Chem (2010) 18: 433-454 [PMID:19914836] |
| ChEMBL | Inhibition of rat renal 11beta-HSD2 | B | 6.44 | pIC50 | 360 | nM | IC50 | Bioorg Med Chem (2011) 19: 1866-1880 [PMID:21376605] |
| Acetylcholinesterase in Electrophorus electricus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4078] [UniProtKB: O42275] | ||||||||
| ChEMBL | Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate after 20 mins measured for 1 min interval for 30 mins by Ellman's method | B | 4 | pKi | >100000 | nM | Ki | Bioorg Med Chem (2014) 22: 3370-3378 [PMID:24853320] |
| Aldo-keto reductase family 1 member B10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5983] [UniProtKB: O60218] | ||||||||
| ChEMBL | Inhibition of reductase activity of N-terminal 6His-tagged human AKR1B10 expressed in Escherichia coli BL21(DE3) assessed as pyridine-3-aldehyde reduction | B | 5.31 | pIC50 | 4900 | nM | IC50 | J Nat Prod (2011) 74: 1201-1206 [PMID:21561086] |
| Beta-glucuronidase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4814] [UniProtKB: P06760] | ||||||||
| ChEMBL | Inhibition of rat liver beta-glucuronidase | B | 4.01 | pIC50 | 97210 | nM | IC50 | Eur J Med Chem (2020) 187: 111921-111921 [PMID:31835168] |
| Beta-glucuronidase in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3217380] [UniProtKB: P05804] | ||||||||
| ChEMBL | Inhibition of Escherichia coli beta-glucuronidase | B | 4.92 | pIC50 | 12150 | nM | IC50 | Eur J Med Chem (2020) 187: 111921-111921 [PMID:31835168] |
| Cholinesterase in Equus caballus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5763] [UniProtKB: P81908] | ||||||||
| ChEMBL | Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate after 20 mins measured for 1 min interval for 30 mins by Ellman's method | B | 4 | pKi | >100000 | nM | Ki | Bioorg Med Chem (2014) 22: 3370-3378 [PMID:24853320] |
| carboxylesterase 2/Cocaine esterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3180] [GtoPdb: 3298] [UniProtKB: O00748] | ||||||||
| ChEMBL | Inhibition of CE2 in human liver microsomes using fluorescein diacetate as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by LC-UV analysis | B | 4.16 | pIC50 | 69260 | nM | IC50 | Eur J Med Chem (2016) 112: 280-288 [PMID:26900660] |
| Glycogen phosphorylase, muscle form in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4696] [UniProtKB: P00489] | ||||||||
| ChEMBL | Inhibition of rabbit muscle glycogen phosphorylase A assessed as phosphate release from glucose-1-phosphate | B | 4.18 | pIC50 | 66000 | nM | IC50 | J Med Chem (2008) 51: 3540-3554 [PMID:18517260] |
| Lactoylglutathione lyase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2175] [UniProtKB: Q9CPU0] | ||||||||
| ChEMBL | Inhibition of recombinant mouse Glyoxalase-1 expressed in Escherichia coli BL21 (DE3) pLysS cells using GSH and MGO as substrate by Dixon plot | B | 6.54 | pKi | 290 | nM | Ki | Bioorg Med Chem (2020) 28: 115243-115243 [PMID:31879183] |
| carboxylesterase 1/Liver carboxylesterase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2265] [GtoPdb: 2592] [UniProtKB: P23141] | ||||||||
| ChEMBL | Inhibition of CE1 in human liver microsomes using 2-(2-Benzoyl-3-methoxyphenyl) benzothiazole as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by LC-UV analysis | B | 4.68 | pIC50 | 20970 | nM | IC50 | Eur J Med Chem (2016) 112: 280-288 [PMID:26900660] |
| peptidylprolyl cis/trans isomerase, NIMA-interacting 1/Peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2288] [GtoPdb: 3171] [UniProtKB: Q13526] | ||||||||
| ChEMBL | Inhibition of Pin1 (unknown origin) assessed as reduction in peptidyl-prolyl isomerase activity incubated for 30 mins using Suc-Ala-Glu-cis-Pro-Phe-4-nitroanilide substrate by protease coupled assay | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem (2017) 25: 5441-5451 [PMID:28838831] |
| 5-LOX/Polyunsaturated fatty acid 5-lipoxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL215] [GtoPdb: 1385] [UniProtKB: P09917] | ||||||||
| ChEMBL | Inhibition of human recombinant 5-LOX expressed in insect cells assessed as decrease in production of 5-HPETE and 5-HETE using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 20 mins in dark by ferric ion oxidation-xylenol orange method | B | 4.61 | pIC50 | 24800 | nM | IC50 | J Nat Prod (2019) 82: 3311-3320 [PMID:31774676] |
| 15-LOX-2/Polyunsaturated fatty acid lipoxygenase ALOX15B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2457] [GtoPdb: 1389] [UniProtKB: O15296] | ||||||||
| ChEMBL | Inhibition of human recombinant N-terminal His-tagged 15-LOX2 expressed in Escherichia coli using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 20 mins in dark by ferric ion oxidation-xylenol orange assay | B | 4.4 | pIC50 | >40000 | nM | IC50 | J Nat Prod (2019) 82: 3311-3320 [PMID:31774676] |
| COX-2 /Prostaglandin G/H synthase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354] | ||||||||
| ChEMBL | Inhibition of human recombinant COX2 expressed in baculovirus infected sf21 cells assessed as decrease in PGE2 formation using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition measured after 45 mins by LC-MS analysis | B | 4.4 | pIC50 | >40000 | nM | IC50 | J Nat Prod (2019) 82: 3311-3320 [PMID:31774676] |
| protein kinase C eta/Protein kinase C eta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3616] [GtoPdb: 1487] [UniProtKB: P24723] | ||||||||
| ChEMBL | Binding affinity to recombinant human PKCeta in after 2 hrs by microequilibrium dialysis assay | B | 6.6 | pKd | 250 | nM | Kd | J Nat Prod (2010) 73: 1659-1666 [PMID:20836515] |
| 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 | pKi | 10000 | nM | Ki | US-11660306-B2. Treatment of Rett syndrome (2023) |
| ChEMBL | Inhibition of recombinant PTP1B | B | 4.34 | pIC50 | 45800 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 730-733 [PMID:21193311] |
| ChEMBL | Inhibition of PTP1B by pNPP assay | B | 4.7 | pIC50 | >20000 | nM | IC50 | Bioorg Med Chem (2008) 16: 8697-8705 [PMID:18707891] |
| protein tyrosine phosphatase non-receptor type 11/Tyrosine-protein phosphatase non-receptor type 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3864] [GtoPdb: 3203] [UniProtKB: Q06124] | ||||||||
| ChEMBL | Inhibition of recombinant SHP2 | B | 5.02 | pIC50 | 9600 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 730-733 [PMID:21193311] |
| ChEMBL | Inhibition of SHP2 (unknown origin) | B | 5.02 | pIC50 | 9600 | nM | IC50 | J Med Chem (2022) 65: 3066-3079 [PMID:35157464] |
| protein tyrosine phosphatase non-receptor type 2/Tyrosine-protein phosphatase non-receptor type 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3807] [GtoPdb: 3255] [UniProtKB: P17706] | ||||||||
| ChEMBL | Inhibition of TCPTP by pNPP assay | B | 4.7 | pIC50 | >20000 | nM | IC50 | Bioorg Med Chem (2008) 16: 8697-8705 [PMID:18707891] |
| Tyrosine-protein phosphatase non-receptor type 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3166] [UniProtKB: P29350] | ||||||||
| ChEMBL | Inhibition of recombinant SHP1 | B | 4.18 | pIC50 | 65400 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 730-733 [PMID:21193311] |
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]
