miglustat [Ligand Id: 4841] 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: CHEMBL1029 (OGT 918, Zavesca, Miglustat, OGT-918)
  • alpha glucosidase/Acidic alpha-glucosidase in Rat [ChEMBL: CHEMBL3513] [GtoPdb: 2611] [UniProtKB: Q6P7A9]
There should be some charts here, you may need to enable JavaScript!
  • Alpha-glucosidase in Oryza sativa Japonica Group [ChEMBL: CHEMBL5280] [UniProtKB: Q9LGC6]
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!
  • UDP-glucose ceramide glucosyltransferase/Ceramide glucosyltransferase in Human [ChEMBL: CHEMBL2063] [GtoPdb: 2528] [UniProtKB: Q16739]
  • UDP-glucose ceramide glucosyltransferase/Ceramide glucosyltransferase in Mouse [ChEMBL: CHEMBL6013] [GtoPdb: 2528] [UniProtKB: O88693]
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!
  • alpha glucosidase/Lysosomal alpha-glucosidase in Human [ChEMBL: CHEMBL2608] [GtoPdb: 2611] [UniProtKB: P10253]
  • alpha glucosidase/Lysosomal alpha-glucosidase in Mouse [ChEMBL: CHEMBL1667668] [GtoPdb: 2611] [UniProtKB: P70699]
There should be some charts here, you may need to enable JavaScript!
  • maltase-glucoamylase/Maltase-glucoamylase in Human [ChEMBL: CHEMBL2074] [GtoPdb: 2627] [UniProtKB: O43451]
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!
  • Non-lysosomal glucosylceramidase in Mouse [ChEMBL: CHEMBL5614] [UniProtKB: Q69ZF3]
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!
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
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 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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]