miglustat [Ligand Id: 4841] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1029 (Butyldeoxynojirimycin, Miglustat, N-butyldeoxynojirimycin, OGT 918, OGT-918, Zavesca) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| alpha glucosidase/Acidic alpha-glucosidase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3513] [GtoPdb: 2611] [UniProtKB: Q6P7A9] | ||||||||
| ChEMBL | Inhibition of rat liver lysosomal alpha-glucosidase using p-nitrophenyl alpha-D-glucopyranoside as substrate by colorimetric method | B | 5.28 | pIC50 | 5300 | nM | IC50 | J Med Chem (2017) 60: 9462-9469 [PMID:29112434] |
| ChEMBL | Inhibition of rat intestinal maltase using moltose as substrate | B | 5.68 | pIC50 | 2100 | nM | IC50 | J Med Chem (2012) 55: 10347-10362 [PMID:23106358] |
| Alpha-glucosidase in Oryza sativa Japonica Group (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5280] [UniProtKB: Q9LGC6] | ||||||||
| ChEMBL | Inhibitory activity against alpha-Glucosidase from rice | B | 6.38 | pIC50 | 420 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 5991-5995 [PMID:15546715] |
| Alpha-mannosidase 2C1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2852] [UniProtKB: P21139] | ||||||||
| ChEMBL | Inhibition of soluble Alpha-mannosidase II in rat liver | B | 4.3 | pIC50 | <50000 | nM | IC50 | J Med Chem (1995) 38: 2349-2356 [PMID:7608901] |
| Beta-glucosidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3761] [UniProtKB: Q9HCG7] | ||||||||
| ChEMBL | Inhibition of non-lysosomal glucosylceramidase | B | 6.52 | pIC50 | 300 | nM | IC50 | Eur J Med Chem (2011) 46: 1949-1963 [PMID:21354674] |
| ChEMBL | Inhibition of GBA2 by HPLC | B | 6.64 | pIC50 | 230 | nM | IC50 | J Med Chem (2010) 53: 689-698 [PMID:20000679] |
| ChEMBL | Inhibition of recombinant GBA2 preincubated with compound for 30 mins using 4-methylumbelliferyl-B-glucoside substrate by fluorimetric assay | B | 6.64 | pIC50 | 230 | nM | IC50 | ACS Med Chem Lett (2011) 2: 119-123 [PMID:24900289] |
| ChEMBL | Inhibition of human GBA2 | B | 6.64 | pIC50 | 230 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 6600-6603 [PMID:19853441] |
| ChEMBL | Inhibition of GBA2 (unknown origin) | B | 6.64 | pIC50 | 230 | nM | IC50 | J Med Chem (2014) 57: 9096-9104 [PMID:25250725] |
| ChEMBL | Inhibition of glucosylceramidase 2 from spleen of patient with gaucher's disease by fluorimetric analysis | B | 6.64 | pIC50 | 230 | nM | IC50 | ACS Med Chem Lett (2011) 2: 519-522 [PMID:24900342] |
| ChEMBL | Inhibition of NLGase in human SH-SY5Y cells using MUG-Gluc as fluorogenic substrate preincubated for 30 mins followed by substrate addition and measured after 2 hrs in presence of AMP-DNM by fluorescence based assay | B | 7.85 | pIC50 | 14 | nM | IC50 | Eur J Med Chem (2019) 175: 63-71 [PMID:31075609] |
| UDP-glucose ceramide glucosyltransferase/Ceramide glucosyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2063] [GtoPdb: 2528] [UniProtKB: Q16739] | ||||||||
| GtoPdb | - | - | 5.13 | pKi | 7400 | nM | Ki | Tetrahedron: Assymetry (2000) 11: 113-124 |
| ChEMBL | Inhibition of GCS by cell-based assay | B | 4.3 | pIC50 | 50000 | nM | IC50 | J Med Chem (2010) 53: 689-698 [PMID:20000679] |
| ChEMBL | Inhibition of glucosylceramide synthase (unknown origin) assessed as catabolism of NBD-glucosylceramide | B | 4.6 | pIC50 | 25000 | nM | IC50 | J Med Chem (2014) 57: 9096-9104 [PMID:25250725] |
| ChEMBL | Inhibition of GCS assessed as amount of UDP-glucose consumed during enzyme-catalyzed reaction | B | 4.66 | pIC50 | 22000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6773-6777 [PMID:21974949] |
| ChEMBL | Inhibition of GCS assessed as amount of UDP glucose after 3 hrs by Fluorometry analysis | B | 4.66 | pIC50 | 22000 | nM | IC50 | J Med Chem (2012) 55: 4322-4335 [PMID:22497444] |
| ChEMBL | Inhibition of glucosylceramide synthase (unknown origin) | B | 4.7 | pIC50 | 20000 | nM | IC50 | Medchemcomm (2014) 5: 1106-1125 |
| UDP-glucose ceramide glucosyltransferase/Ceramide glucosyltransferase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6013] [GtoPdb: 2528] [UniProtKB: O88693] | ||||||||
| ChEMBL | Inhibition of glucosylceramide synthase in mouse RAW cells preincubated with compound for 15 mins by in-situ enzyme inhibition assay | B | 4.3 | pIC50 | 50000 | nM | IC50 | ACS Med Chem Lett (2011) 2: 119-123 [PMID:24900289] |
| ChEMBL | Inhibition of glucosylceramide synthase in mouse RAW cells preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence scanner | B | 4.3 | pIC50 | 50000 | nM | IC50 | ACS Med Chem Lett (2011) 2: 519-522 [PMID:24900342] |
| ChEMBL | Inhibition mouse glucosylceramide synthase | B | 4.64 | pIC50 | 22900 | nM | IC50 | J Biol Chem (2007) 282: 32655-32664 [PMID:17848577] |
| Glycogen debranching enzyme in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5272] [UniProtKB: P35573] | ||||||||
| ChEMBL | Inhibition of glycogen glycogen de-branching enzyme by HPLC | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2010) 53: 689-698 [PMID:20000679] |
| Lactase-phlorizin hydrolase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075131] [UniProtKB: P09848] | ||||||||
| ChEMBL | Inhibition of lactase by HPLC | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2010) 53: 689-698 [PMID:20000679] |
| alpha glucosidase/Lysosomal alpha-glucosidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2608] [GtoPdb: 2611] [UniProtKB: P10253] | ||||||||
| ChEMBL | Inhibition of human GAA using 4-methylumbelliferyl-alpha-D-glucopyranoside as substrate preincubated for 45 min followed by substrate addition and measured after 30 min by fluorescence spectrophotometer analysis | B | 6.7 | pKi | 200 | nM | Ki | J Med Chem (2022) 65: 2329-2341 [PMID:35072486] |
| ChEMBL | Inhibition of human lysosomal alpha glucosidase | B | 7 | pIC50 | 100 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 6600-6603 [PMID:19853441] |
| ChEMBL | Inhibition of lysosomal alpha-glucosidase by HPLC | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2010) 53: 689-698 [PMID:20000679] |
| alpha glucosidase/Lysosomal alpha-glucosidase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1667668] [GtoPdb: 2611] [UniProtKB: P70699] | ||||||||
| ChEMBL | Inhibition of maltase in mouse intestinal input by glucose release assay | B | 5.05 | pIC50 | 9000 | nM | IC50 | ACS Med Chem Lett (2011) 2: 119-123 [PMID:24900289] |
| ChEMBL | Enzyme Activity Assay: Cells were washed two times with 200 μL dPBS followed by the addition of 70 μL of substrate (2.11 mM 3 mM 4-MU-α-D-glu) in citrate-phosphate buffer (30 mM sodium citrate, 40 mM sodium phosphate dibasic, pH 4.0), and 2.5% DMSO to rows 1-12. Following incubation at 37° C. with 5% CO2 for about 3 h, 70 μL of stop buffer (0.4 M glycine pH 10.8) was added to rows 1-12. The plate was read in a Victor2 multilabel counter-Wallac fluorescent plate reader and the fluorescence at F460 nm was determined b at an excitation of 355 nm and emission of 460 nm using 1 second read time per well. Enzyme activity per μg of protein in the supernatant was calculated from the amount of fluorescence emitted, which is directly proportional to the amount of substrate hydrolyzed, and hence, the amount of Gaa activity in the lysate. | B | 4.93 | pEC50 | 11800 | nM | EC50 | US-9181184-B2. Method for the treatment of pompe disease using 1-deoxynojirimycin and derivatives (2015) |
| maltase-glucoamylase/Maltase-glucoamylase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2074] [GtoPdb: 2627] [UniProtKB: O43451] | ||||||||
| ChEMBL | Inhibition of maltase by HPLC | B | 5.05 | pIC50 | 9000 | nM | IC50 | J Med Chem (2010) 53: 689-698 [PMID:20000679] |
| ChEMBL | Inhibition of Glycosidases (maltase) in rat intestinal brush border membranes by D-glucose oxidase-peroxidase method maltase | B | 5.68 | pIC50 | 2100 | nM | IC50 | J Med Chem (1995) 38: 2349-2356 [PMID:7608901] |
| Mannosidase 2 alpha 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2257] [UniProtKB: P28494] | ||||||||
| ChEMBL | Competitive Inhibitory activity against Golgi Alpha-mannosidase II | B | 4.3 | pKi | <50000 | nM | Ki | J Med Chem (1995) 38: 2349-2356 [PMID:7608901] |
| ChEMBL | Inhibition of golgi Alpha-mannosidase II in rat liver | B | 4.3 | pIC50 | <50000 | nM | IC50 | J Med Chem (1995) 38: 2349-2356 [PMID:7608901] |
| Mannosidase 2, alpha B1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3448] [UniProtKB: Q6P762] | ||||||||
| ChEMBL | Inhibition of lysosomal Alpha-mannosidase II in rat liver | B | 4.3 | pIC50 | <50000 | nM | IC50 | J Med Chem (1995) 38: 2349-2356 [PMID:7608901] |
| Non-lysosomal glucosylceramidase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5614] [UniProtKB: Q69ZF3] | ||||||||
| ChEMBL | Inhibition of conduritol beta-epoxide-sensitive mouse glucosylceramidase | B | 6.85 | pIC50 | 140 | nM | IC50 | J Biol Chem (2007) 282: 32655-32664 [PMID:17848577] |
| Sucrase-isomaltase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2748] [UniProtKB: P14410] | ||||||||
| ChEMBL | Inhibition of sucrase by HPLC | B | 6.3 | pIC50 | 500 | nM | IC50 | J Med Chem (2010) 53: 689-698 [PMID:20000679] |
| Sucrase-isomaltase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1667666] [UniProtKB: B5THE3] | ||||||||
| ChEMBL | Inhibition of wild type C57BL/6 mouse small intestinal sucrase/isomaltase using sucrose as substrate after 30 mins | B | 5.82 | pIC50 | 1500 | nM | IC50 | J Med Chem (2017) 60: 9462-9469 [PMID:29112434] |
| ChEMBL | Inhibition of sucrase in mouse intestinal input by glucose release assay | B | 6.22 | pIC50 | 600 | nM | IC50 | ACS Med Chem Lett (2011) 2: 119-123 [PMID:24900289] |
| Sucrase-isomaltase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3114] [UniProtKB: P23739] | ||||||||
| ChEMBL | Inhibition of rat intestinal sucrase using disaccharide | B | 4.24 | pIC50 | 58000 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 5991-5995 [PMID:15546715] |
| ChEMBL | Inhibition of rat intestinal sucrase using sucrose as substrate | B | 4.24 | pIC50 | 58000 | nM | IC50 | J Med Chem (2012) 55: 10347-10362 [PMID:23106358] |
| ChEMBL | Inhibition of rat intestinal isomaltase using disaccharide | B | 5.57 | pIC50 | 2700 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 5991-5995 [PMID:15546715] |
| ChEMBL | Inhibition of rat intestinal isomaltase using isomaltase as substrate | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (2012) 55: 10347-10362 [PMID:23106358] |
| ChEMBL | Inhibition of Glycosidases (isomaltase)in rat intestinal brush border membranes by D-glucose oxidase-peroxidase method | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (1995) 38: 2349-2356 [PMID:7608901] |
| ChEMBL | Inhibition of rat intestinal maltase using disaccharide | B | 5.68 | pIC50 | 2100 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 5991-5995 [PMID:15546715] |
| ChEMBL | Inhibition of Sucrase in rat intestinal brush border membranes by D-glucose oxidase-peroxidase method | B | 6.24 | pIC50 | 580 | nM | IC50 | J Med Chem (1995) 38: 2349-2356 [PMID:7608901] |
| Trehalase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3248] [UniProtKB: O70282] | ||||||||
| ChEMBL | Inhibition of rat intestinal trehalase | B | 4.42 | pIC50 | 38000 | nM | IC50 | J Med Chem (2012) 55: 10347-10362 [PMID:23106358] |
| ChEMBL | Inhibition of Glycosidases (trehalase)in rat intestinal brush border membranes by D-glucose oxidase-peroxidase method | B | 4.89 | pIC50 | 13000 | nM | IC50 | J Med Chem (1995) 38: 2349-2356 [PMID:7608901] |
| Uncharacterized protein in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2176863] [UniProtKB: I3LIR5] | ||||||||
| ChEMBL | Inhibition of porcine kidney trehalase | B | 4.44 | pIC50 | 36000 | nM | IC50 | J Med Chem (2012) 55: 10347-10362 [PMID:23106358] |
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]
