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ChEMBL ligand: CHEMBL307429 (1,5-dideoxy-1,5-imino-, 1,5-dideoxy-1,5-imino-d-glucitol, 1 deoxynojirimycin, 1-deoxynojirimycin, Bay-h-5595, D-1-deoxynojirimycin, Deoxynojirimycin, Duvoglustat, Moranolin, Moranoline, Nojirimycin, 1-deoxy-) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
---|---|---|---|---|---|---|---|---|
alpha glucosidase in Human [GtoPdb: 2611] [UniProtKB: P10253] | ||||||||
GtoPdb | - | - | 6.82 | pKi | 150 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 355-360 |
alpha glucosidase/Acidic alpha-glucosidase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3513] [GtoPdb: 2611] [UniProtKB: Q6P7A9] | ||||||||
ChEMBL | Concentration that causes 50% inhibition of mammalian alpha-glucosidase (lysosomal) was determined in rat liver | B | 4.6 | pIC50 | 25000 | nM | IC50 | J. Med. Chem. (1994) 37: 3701-3706 [PMID:7966130] |
ChEMBL | Inhibition of rat liver lysosome alpha-glucosidase assessed as D-glucose release after 30 mins by Glucose B-test | B | 6.4 | pIC50 | 400 | nM | IC50 | J. Nat. Prod. (2002) 65: 1875-1881 [PMID:12502331] |
ChEMBL | Concentration that causes 50% inhibition of mammalian alpha-glucosidase (lysosomal) was determined in rat liver | B | 6.4 | pIC50 | 400 | nM | IC50 | J. Med. Chem. (1994) 37: 3701-3706 [PMID:7966130] |
ChEMBL | Inhibition of rat intestinal maltase assessed as D-glucose release after 30 mins by Glucose B-test | B | 6.44 | pIC50 | 360 | nM | IC50 | J. Nat. Prod. (2002) 65: 1875-1881 [PMID:12502331] |
ChEMBL | Concentration that causes 50% inhibition of mammalian alpha-glucosidase (maltase) was determined in rat intestine | B | 6.44 | pIC50 | 360 | nM | IC50 | J. Med. Chem. (1994) 37: 3701-3706 [PMID:7966130] |
ChEMBL | Inhibition of rat intestinal maltase using moltose as substrate | B | 6.44 | pIC50 | 360 | nM | IC50 | J. Med. Chem. (2012) 55: 10347-10362 [PMID:23106358] |
ChEMBL | Inhibition of rat intestinal brush border membrane maltase | B | 6.89 | pIC50 | 130 | nM | IC50 | Bioorg. Med. Chem. (2008) 16: 7330-7336 [PMID:18595718] |
Alpha-galactosidase in Coffea arabica (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5217] [UniProtKB: Q42656] | ||||||||
ChEMBL | Inhibition of alpha-galactosidase in green coffee bean after 30 mins by spectrophotometric analysis | B | 4.64 | pIC50 | 23000 | nM | IC50 | MedChemComm (2013) 4: 387-393 |
Alpha-galactosidase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2524] [UniProtKB: P06280] | ||||||||
ChEMBL | Compound tested for inhibition of alpha-galactosidase from Aspergillus niger | B | 4.74 | pKi | 18000 | nM | Ki | Bioorg. Med. Chem. Lett. (2004) 14: 73-75 [PMID:14684301] |
Alpha-glucosidase in Geobacillus stearothermophilus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4412] [UniProtKB: P94451] | ||||||||
ChEMBL | Inhibition of alpha glucosidase from bacillus stearothermophilus | B | 5.78 | pIC50 | 1670 | nM | IC50 | Bioorg. Med. Chem. Lett. (2008) 18: 954-958 [PMID:18166456] |
Alpha-glucosidase in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2974] [UniProtKB: Q9MYM4] | ||||||||
ChEMBL | Inhibition of mammalian alpha-glucosidase (lysosomal) was determined in bovine liver | B | 4.68 | pIC50 | 21000 | nM | IC50 | J. Med. Chem. (1994) 37: 3701-3706 [PMID:7966130] |
ChEMBL | Inhibition of mammalian alpha-glucosidase (lysosomal) was determined in bovine liver | B | 6.4 | pIC50 | 400 | nM | IC50 | J. Med. Chem. (1994) 37: 3701-3706 [PMID:7966130] |
Alpha-glucosidase in Oryza sativa Japonica Group (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5280] [UniProtKB: Q9LGC6] | ||||||||
ChEMBL | Inhibitory activity against alpha-Glucosidase from rice | B | 7.3 | pIC50 | 50 | nM | IC50 | Bioorg. Med. Chem. Lett. (2004) 14: 5991-5995 [PMID:15546715] |
ChEMBL | Inhibitory concentration against rice alpha-glucosidase | B | 7.52 | pIC50 | 30 | nM | IC50 | J. Med. Chem. (2005) 48: 2036-2044 [PMID:15771446] |
Alpha-L-fucosidase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4176] [UniProtKB: P04066] | ||||||||
ChEMBL | Concentration that causes 50% inhibition of mammalian alpha-L-fucosidase was determined in bovine epididymis | B | 4.59 | pIC50 | 26000 | nM | IC50 | J. Med. Chem. (1994) 37: 3701-3706 [PMID:7966130] |
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-galactosidase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2680] [UniProtKB: D3ZUM4] | ||||||||
ChEMBL | Concentration that causes 50% inhibition of mammalian lactase beta-galactosidase was determined in rat intestine | B | 4.52 | pIC50 | 30000 | nM | IC50 | J. Med. Chem. (1994) 37: 3701-3706 [PMID:7966130] |
ChEMBL | Concentration that causes 50% inhibition of mammalian beta-galactosidase (lactase ) was determined in rat intestine | B | 4.57 | pIC50 | 27000 | nM | IC50 | J. Med. Chem. (1994) 37: 3701-3706 [PMID:7966130] |
glucosylceramidase beta/Beta-glucocerebrosidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2179] [GtoPdb: 2978] [UniProtKB: P04062] | ||||||||
ChEMBL | Inhibition of human lysosomal beta-glucocerebrosidase | B | 4.1 | pKi | 79000 | nM | Ki | Bioorg. Med. Chem. Lett. (2014) 24: 2777-2780 [PMID:24803362] |
ChEMBL | Inhibitory activity against beta-glucosidase of sweet almond | B | 4.33 | pKi | 47000 | nM | Ki | Bioorg. Med. Chem. Lett. (1999) 9: 615-618 [PMID:10098675] |
ChEMBL | Competitive Inhibition constant on Asp. Wentii beta Glucosidase at pH 5.0 | B | 5.7 | pKi | 2000 | nM | Ki | Bioorg. Med. Chem. Lett. (1992) 2: 27-32 |
Beta-glucosidase in Agrobacterium tumefaciens (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4663] [UniProtKB: P27034] | ||||||||
ChEMBL | Inhibition of Agrobacterium sp. beta-glucosidase | B | 4.92 | pKi | 12000 | nM | Ki | Bioorg. Med. Chem. Lett. (2006) 16: 2067-2070 [PMID:16481162] |
ChEMBL | Inhibition of Agrobacterium sp. beta glucosidase | B | 4.92 | pKi | 12000 | nM | Ki | Bioorg. Med. Chem. Lett. (2014) 24: 2777-2780 [PMID:24803362] |
Beta-glucosidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3761] [UniProtKB: Q9HCG7] | ||||||||
ChEMBL | Inhibition of non-lysosomal glucosylceramidase | B | 4.52 | pIC50 | 30000 | nM | IC50 | Eur. J. Med. Chem. (2011) 46: 1949-1963 [PMID:21354674] |
ChEMBL | Displacement of 4-methylumbelliferyl from non-lysosomal GBA2 by fluorimetry | B | 4.54 | pIC50 | 28800 | nM | IC50 | Bioorg. Med. Chem. (2010) 18: 267-273 [PMID:19931460] |
ChEMBL | Inhibition of GBA2 by HPLC | B | 4.68 | pIC50 | 21000 | nM | IC50 | J. Med. Chem. (2010) 53: 689-698 [PMID:20000679] |
ChEMBL | Inhibition of human GBA2 | B | 4.7 | pIC50 | 20000 | nM | IC50 | Bioorg. Med. Chem. Lett. (2009) 19: 6600-6603 [PMID:19853441] |
Beta-glucosidase in Prunus avium (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4192] [UniProtKB: Q43014] | ||||||||
ChEMBL | Inhibitory activity against sweet almond Beta-glucosidase | B | 5.02 | pKi | 9500 | nM | Ki | Bioorg. Med. Chem. Lett. (1991) 1: 667-672 |
ChEMBL | Inhibitory activity against beta-Glucosidase from sweet almond | B | 4.09 | pIC50 | 81000 | nM | IC50 | Bioorg. Med. Chem. Lett. (2004) 14: 5991-5995 [PMID:15546715] |
Beta-glucosidase A in Caldicellulosiruptor saccharolyticus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4622] [UniProtKB: P10482] | ||||||||
ChEMBL | Inhibition of Caldocellum saccharolyticum beta-glucosidase assessed as D-glucose release after 30 mins by Glucose B-test | B | 4 | pIC50 | 100000 | nM | IC50 | J. Nat. Prod. (2002) 65: 1875-1881 [PMID:12502331] |
ChEMBL | Inhibitory activity against beta-Glucosidase from Caldocellum saccharolyticum | B | 4.26 | pIC50 | 55000 | nM | IC50 | Bioorg. Med. Chem. Lett. (2004) 14: 5991-5995 [PMID:15546715] |
Beta-glucosidase cytosolic in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3865] [UniProtKB: Q9H227] | ||||||||
ChEMBL | Inhibitory concentration against beta-glucosidase | B | 4.1 | pIC50 | 80000 | nM | IC50 | J. Med. Chem. (2005) 48: 2036-2044 [PMID:15771446] |
UDP-glucose ceramide glucosyltransferase/Ceramide glucosyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2063] [GtoPdb: 2528] [UniProtKB: Q16739] | ||||||||
ChEMBL | Inhibition of GCS by cell-based assay | B | 4 | pIC50 | >100000 | nM | IC50 | J. Med. Chem. (2010) 53: 689-698 [PMID:20000679] |
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] |
Glycogen debranching enzyme in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5273] [UniProtKB: P35574] | ||||||||
ChEMBL | Inhibition of rabbit muscle amylo-1,6-glucosidase | B | 6.72 | pIC50 | 190 | nM | IC50 | Bioorg. Med. Chem. (2008) 16: 7330-7336 [PMID:18595718] |
Lactase-glycosylceramidase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3389] [UniProtKB: Q02401] | ||||||||
ChEMBL | Inhibition of rat intestinal lactase assessed as production of p-nitrophenol by spectrophotometry | B | 4.31 | pIC50 | 49000 | nM | IC50 | Bioorg. Med. Chem. (2011) 19: 3558-3568 [PMID:21546253] |
ChEMBL | Inhibition of Glycosidases (lactase)in rat intestinal brush border membranes by D-glucose oxidase-peroxidase method | B | 4.47 | pIC50 | 34000 | nM | IC50 | J. Med. Chem. (1995) 38: 2349-2356 [PMID:7608901] |
ChEMBL | Concentration that causes 50% inhibition of mammalian lactase beta-galactosidase was determined in rat intestine | B | 4.59 | pIC50 | 26000 | nM | IC50 | J. Med. Chem. (1994) 37: 3701-3706 [PMID:7966130] |
ChEMBL | Inhibition of rat intestinal lactase using lactose as substrate | B | 4.59 | pIC50 | 26000 | nM | IC50 | J. Med. Chem. (2012) 55: 10347-10362 [PMID:23106358] |
Lactase-phlorizin hydrolase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075131] [UniProtKB: P09848] | ||||||||
ChEMBL | Inhibition of lactase by HPLC | B | 4.21 | pIC50 | 62000 | nM | IC50 | J. Med. Chem. (2010) 53: 689-698 [PMID:20000679] |
Liver X receptor-α/LXR-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2808] [GtoPdb: 602] [UniProtKB: Q13133] | ||||||||
ChEMBL | Antagonist activity at human recombinant LXRalpha expressed in HEK293 cells by luciferase reporter gene assay | F | 4 | pIC50 | >100000 | nM | IC50 | Bioorg. Med. Chem. (2008) 16: 4272-4285 [PMID:18343126] |
Liver X receptor-β/LXR-beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4093] [GtoPdb: 601] [UniProtKB: P55055] | ||||||||
ChEMBL | Antagonist activity at human recombinant LXRbeta expressed in HEK293 cells by luciferase reporter gene assay | F | 4 | pIC50 | >100000 | nM | IC50 | Bioorg. Med. Chem. (2008) 16: 4272-4285 [PMID:18343126] |
alpha glucosidase/Lysosomal alpha-glucosidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2608] [GtoPdb: 2611] [UniProtKB: P10253] | ||||||||
ChEMBL | Inhibitory activity against alpha-glucosidase of yeast | B | 4.6 | pKi | 25000 | nM | Ki | Bioorg. Med. Chem. Lett. (1999) 9: 615-618 [PMID:10098675] |
GtoPdb | - | - | 6.82 | pKi | 150 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 355-360 |
ChEMBL | Tested in vitro for the inhibition constant against human lysosomal alpha-glucosidase | B | 6.82 | pKi | 150 | nM | Ki | Bioorg. Med. Chem. Lett. (1997) 7: 355-360 |
ChEMBL | Inhibitory activity was determined against baker's yeast Alpha-Glucosidase | B | 4.04 | pIC50 | 91900 | nM | IC50 | Bioorg. Med. Chem. Lett. (1994) 4: 2643-2648 |
ChEMBL | Inhibition of human lysosomal alpha glucosidase | B | 5.82 | pIC50 | 1500 | nM | IC50 | Bioorg. Med. Chem. Lett. (2009) 19: 6600-6603 [PMID:19853441] |
ChEMBL | Inhibition of lysosomal alpha-glucosidase by HPLC | B | 5.82 | pIC50 | 1500 | nM | IC50 | J. Med. Chem. (2010) 53: 689-698 [PMID:20000679] |
ChEMBL | Inhibition of human lysosomal alpha-glucosidase | B | 6 | pIC50 | 1000 | nM | IC50 | Bioorg. Med. Chem. (2008) 16: 7330-7336 [PMID:18595718] |
ChEMBL | Inhibition of maltase in human Caco-2 cell model system after 2 hrs | B | 7.22 | pIC50 | 60 | nM | IC50 | Bioorg. Med. Chem. (2008) 16: 7330-7336 [PMID:18595718] |
alpha glucosidase/Lysosomal alpha-glucosidase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1667668] [GtoPdb: 2611] [UniProtKB: P70699] | ||||||||
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 | 4.01 | pEC50 | 98800 | 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 | 5.7 | pIC50 | 2000 | nM | IC50 | J. Med. Chem. (2010) 53: 689-698 [PMID:20000679] |
ChEMBL | Inhibition of human alpha-glucosidase | B | 5.85 | pIC50 | 1400 | nM | IC50 | Eur J Med Chem (2021) 224: 113716-113716 [PMID:34340042] |
ChEMBL | Inhibition of Glycosidases (maltase) in rat intestinal brush border membranes by D-glucose oxidase-peroxidase method | B | 6.44 | pIC50 | 360 | nM | IC50 | J. Med. Chem. (1995) 38: 2349-2356 [PMID:7608901] |
ChEMBL | Inhibitory concentration against human alpha-glucosidase | B | 7.4 | pIC50 | 40 | nM | IC50 | J. Med. Chem. (2005) 48: 2036-2044 [PMID:15771446] |
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] |
Neutral alpha-glucosidase AB in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2519] [UniProtKB: Q14697] | ||||||||
ChEMBL | Competitive Inhibition constant on yeast alpha Glucosidase at pH 6.0 | B | 4.64 | pKi | 23000 | nM | Ki | Bioorg. Med. Chem. Lett. (1992) 2: 27-32 |
ChEMBL | Competitive Inhibition constant on yeast alpha Glucosidase at pH 7.0 | B | 4.68 | pKi | 21000 | nM | Ki | Bioorg. Med. Chem. Lett. (1992) 2: 27-32 |
ChEMBL | Competitive Inhibition constant on rice alpha Glucosidase at pH 5.0 | B | 6.8 | pKi | 160 | nM | Ki | Bioorg. Med. Chem. Lett. (1992) 2: 27-32 |
ChEMBL | Competitive Inhibition constant on rice alpha Glucosidase at pH 6.0 | B | 7.85 | pKi | 14 | nM | Ki | Bioorg. Med. Chem. Lett. (1992) 2: 27-32 |
ChEMBL | Concentration that causes 50% inhibition of mammalian alpha-mannosidase (Golgi I) was determined in rat liver | B | 4.6 | pIC50 | 25000 | nM | IC50 | J. Med. Chem. (1994) 37: 3701-3706 [PMID:7966130] |
ChEMBL | Tested for competitive inhibition of endoplasmic reticulum alpha-glucosidase II. | B | 5.89 | pIC50 | 1300 | nM | IC50 | J. Med. Chem. (1994) 37: 3701-3706 [PMID:7966130] |
Neutral alpha-glucosidase C in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3635] [UniProtKB: Q8BVW0] | ||||||||
ChEMBL | Concentration that causes 50% inhibition of mammalian alpha-glucosidase (isomaltase) was determined in rat intestine | B | 4.47 | pIC50 | 34000 | nM | IC50 | J. Med. Chem. (1994) 37: 3701-3706 [PMID:7966130] |
ChEMBL | Concentration that causes 50% inhibition of mammalian alpha-glucosidase (isomaltase) was determined in rat intestine | B | 6.52 | pIC50 | 300 | nM | IC50 | J. Med. Chem. (1994) 37: 3701-3706 [PMID:7966130] |
Sucrase-isomaltase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2748] [UniProtKB: P14410] | ||||||||
ChEMBL | Inhibition of sucrase by HPLC | B | 5.7 | pIC50 | 2000 | nM | IC50 | J. Med. Chem. (2010) 53: 689-698 [PMID:20000679] |
Sucrase-isomaltase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3114] [UniProtKB: P23739] | ||||||||
ChEMBL | Tested in vitro for the inhibition constant against rat small intestinal sucrase | B |