acarbose [Ligand Id: 6791] 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: CHEMBL1566 (BAY-G-5421, Acarbose, Glucobay, Precose)
  • glucosidase alpha, acid/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 Geobacillus stearothermophilus [ChEMBL: CHEMBL4412] [UniProtKB: P94451]
There should be some charts here, you may need to enable JavaScript!
  • glucosidase alpha, acid/Lysosomal alpha-glucosidase in Human [ChEMBL: CHEMBL2608] [GtoPdb: 2611] [UniProtKB: P10253]
  • glucosidase alpha, acid/Lysosomal alpha-glucosidase in Mouse [ChEMBL: CHEMBL1667668] [GtoPdb: 2611] [UniProtKB: P70699]
There should be some charts here, you may need to enable JavaScript!
  • Oligo-1,6-glucosidase in Saccharomyces cerevisiae S288c [ChEMBL: CHEMBL5848] [UniProtKB: P53051]
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!
  • amylase alpha 2A in Pig [GtoPdb: 2596]
There should be some charts here, you may need to enable JavaScript!
  • maltase-glucoamylase in Mouse [GtoPdb: 2627]
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
glucosidase alpha, acid/Acidic alpha-glucosidase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3513] [GtoPdb: 2611] [UniProtKB: Q6P7A9]
ChEMBL Competitive inhibition of rat alpha-glucosidase assessed as production of chromogenic p-Nitrphenol measured after 3 mins by HPLC and Michaelis-Menten equation B 5.46 pKi 3500 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 2441-2444 [PMID:21397496]
ChEMBL Inhibition of rat intestinal maltase using maltose as substrate by colorimetric analysis B 4.59 pIC50 25520 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 2022-2026 [PMID:23466232]
ChEMBL Inhibition of rat intestinal alpha-glucosidase using para-nitrophenyl-alpha-D-glucopyranoside as substrate incubated for 5 min prior to substrate addition measured after 5 min by spectrophotometric analysis B 4.73 pIC50 18600 nM IC50 Med Chem Res (2012) 21: 760-774
ChEMBL Inhibition of maltase in rat intestinal mucosa pre-incubated for 40 mins using maltose substrate B 4.79 pIC50 16100 nM IC50 J. Nat. Prod. (2015) 78: 1977-1989 [PMID:26287401]
ChEMBL Inhibition of rat intestinal alpha-glucosidase using p-nitrophenyl- alpha-D-glucopyranoside as substrate preincubated for 5 min before addition of substrate measured after 10 min B 5.2 pIC50 6380 nM IC50 Med Chem Res (2011) 20: 1431-1437
ChEMBL Inhibition of rat intestinal maltase using maltose as substrate assessed as D-glucose release from substrate preincubated for 15 mins measured after 60 mins B 5.48 pIC50 3300 nM IC50 Bioorg. Med. Chem. (2013) 21: 5442-5450 [PMID:23810673]
ChEMBL Inhibition of rat intestinal Maltase using maltose as substrate assessed as glucose release after 10 mins by glucose oxidase method B 5.68 pIC50 2100 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 4529-4533 [PMID:26343830]
ChEMBL Inhibition of rat intestinal maltase B 5.7 pIC50 2000 nM IC50 Bioorg. Med. Chem. (2011) 19: 2015-2022 [PMID:21345683]
ChEMBL Inhibition of alpha-glucosidase activity of maltase in rat small intestinal brush border membrane fraction using maltose as substrate after 30 mins B 5.7 pIC50 2000 nM IC50 Bioorg. Med. Chem. (2012) 20: 832-840 [PMID:22209731]
ChEMBL Inhibition of rat small intestinal maltase after 30 mins B 5.77 pIC50 1700 nM IC50 Bioorg. Med. Chem. (2011) 19: 2252-2262 [PMID:21420866]
ChEMBL Inhibition of rat small intestinal maltase after 30 mins by glucose-oxidase method B 5.77 pIC50 1700 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 3159-3162 [PMID:21454075]
ChEMBL Inhibition of rat intestinal alpha-glucosidase maltase using maltose as substrate preincubated for 10 mins prior substrate addition measured after 40 mins by spectrophotometry B 5.82 pIC50 1500 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 1538-1540 [PMID:22290077]
ChEMBL Inhibition of rat intestine maltase using maltose as substrate incubated for 10 mins prior to substrate addition measured after 40 mins by glucose oxidase colorimetric method B 5.82 pIC50 1500 nM IC50 Eur. J. Med. Chem. (2013) 66: 296-304 [PMID:23811091]
ChEMBL Inhibition of rat intestinal brush border membrane maltase B 6.46 pIC50 350 nM IC50 Bioorg. Med. Chem. (2008) 16: 7330-7336 [PMID:18595718]
ChEMBL Inhibition of Wistar rat intestinal maltase assessed as inhibition of D-glucose release after 30 mins by spectrophotometry B 6.74 pIC50 180 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 3298-3301 [PMID:24973028]
ChEMBL Inhibition of rat intestinal maltase using moltose as substrate B 6.74 pIC50 180 nM IC50 J. Med. Chem. (2012) 55: 10347-10362 [PMID:23106358]
ChEMBL Inhibition of Wistar rat small intestine maltase after 30 mins B 6.8 pIC50 160 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 738-741 [PMID:21185187]
Alpha-glucosidase in Geobacillus stearothermophilus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4412] [UniProtKB: P94451]
ChEMBL Competitive inhibition of Bacillus stearothermophilus alpha-glucosidase assessed as production of chromogenic p-Nitrphenol measured after 3 mins by HPLC and Michaelis-Menten equation B 6.47 pKi 340 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 2441-2444 [PMID:21397496]
glucosidase alpha, acid/Lysosomal alpha-glucosidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2608] [GtoPdb: 2611] [UniProtKB: P10253]
ChEMBL Inhibition of human lysosomal alpha-glucosidase B 4.38 pIC50 42000 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 5.3 pIC50 5000 nM IC50 Bioorg. Med. Chem. (2008) 16: 7330-7336 [PMID:18595718]
glucosidase alpha, acid/Lysosomal alpha-glucosidase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1667668] [GtoPdb: 2611] [UniProtKB: P70699]
ChEMBL Inhibition of liver glucosidase in Swiss mouse liver extracts B 4 pIC50 >100000 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 7011-7014 [PMID:23102653]
Oligo-1,6-glucosidase in Saccharomyces cerevisiae S288c (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5848] [UniProtKB: P53051]
ChEMBL Inhibition of Saccharomyces cerevisiae alpha-glucosidase using p-nitrophenyl-alpha-D-glucopyranoside as substrate preincubated for 10 mins measured after 30 mins B 4.42 pIC50 38250 nM IC50 Bioorg. Med. Chem. (2014) 22: 1195-1200 [PMID:24398385]
Pancreatic alpha-amylase in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5730] [UniProtKB: P00690]
ChEMBL Inhibition of porcine pancreatic alpha amylase using starch as substrate by Bernfeld method B 4.45 pIC50 35500 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 7011-7014 [PMID:23102653]
ChEMBL Inhibition of pig pancreatic alpha-amylase by Bernfeld method B 4.45 pIC50 35500 nM IC50 Eur. J. Med. Chem. (2013) 59: 304-309 [PMID:23262035]
Salivary alpha-amylase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2478] [UniProtKB: P04745]
ChEMBL Inhibition of human salivary alpha-amylase B 6 pIC50 996 nM IC50 J. Med. Chem. (2008) 51: 3555-3561 [PMID:18507367]
ChEMBL Inhibition of human salivary alpha-amylase using GalG2CNP as substrate by UV-Vis spectrophotometric analysis B 6.3 pIC50 500 nM IC50 Bioorg. Med. Chem. (2015) 23: 6725-6732 [PMID:26395057]
Sucrase-isomaltase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3114] [UniProtKB: P23739]
ChEMBL Inhibition of rat intestinal sucrase using p-nitrophenyl-alpha-d-glucopyranoside as substrate incubated for 10 mins prior to substrate addition measured after 5 mins by spectrophotometry B 4.3 pIC50 <50000 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 1192-1196 [PMID:24461297]
ChEMBL Inhibition of rat intestinal Sucrase using sucrose as substrate assessed as glucose release after 40 mins by glucose oxidase method B 4.59 pIC50 26000 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 4529-4533 [PMID:26343830]
ChEMBL Inhibition of sucrase in rat intestinal mucosa pre-incubated for 40 mins using sucrose substrate B 4.69 pIC50 20200 nM IC50 J. Nat. Prod. (2015) 78: 1977-1989 [PMID:26287401]
ChEMBL Inhibition of Wistar rat intestinal sucrase assessed as inhibition of D-glucose release after 30 mins by spectrophotometry B 5.54 pIC50 2900 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 3298-3301 [PMID:24973028]
ChEMBL Inhibition of Wistar rat small intestine sucrase after 30 mins B 5.54 pIC50 2900 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 738-741 [PMID:21185187]
ChEMBL Inhibition of rat intestinal sucrase using sucrose as substrate B 5.54 pIC50 2900 nM IC50 J. Med. Chem. (2012) 55: 10347-10362 [PMID:23106358]
ChEMBL Inhibition of rat intestinal sucrase using sucrose substrate incubated for 10 mins B 5.62 pIC50 2400 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 5530-5533 [PMID:25451999]
ChEMBL Inhibition of rat intestinal alpha-glucosidase sucrase using sucrose as substrate preincubated for 10 mins prior substrate addition measured after 40 mins by spectrophotometry B 5.62 pIC50 2380 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 1538-1540 [PMID:22290077]
ChEMBL Inhibition of sucrase in rat small intestine using sucrose as substrate after 40 mins by microplate reader analysis B 5.64 pIC50 2300 nM IC50 MedChemComm (2012) 3: 1466-1470
ChEMBL Inhibition of rat intestine sucrase using sucrose as substrate incubated for 10 mins prior to substrate addition measured after 40 mins by glucose oxidase colorimetric method B 5.64 pIC50 2300 nM IC50 Eur. J. Med. Chem. (2013) 66: 296-304 [PMID:23811091]
ChEMBL Inhibition of rat small intestinal sucrase after 30 mins B 5.7 pIC50 2000 nM IC50 Bioorg. Med. Chem. (2011) 19: 2252-2262 [PMID:21420866]
ChEMBL Inhibition of rat intestinal sucrase B 5.77 pIC50 1700 nM IC50 Bioorg. Med. Chem. (2011) 19: 2015-2022 [PMID:21345683]
ChEMBL Inhibition of alpha-glucosidase activity of sucrase in rat small intestinal brush border membrane fraction using maltose as substrate after 30 mins B 5.77 pIC50 1700 nM IC50 Bioorg. Med. Chem. (2012) 20: 832-840 [PMID:22209731]
ChEMBL Inhibition of rat small intestinal sucrase after 30 mins by glucose-oxidase method B 5.82 pIC50 1500 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 3159-3162 [PMID:21454075]
ChEMBL Inhibition of rat intestinal brush border membrane sucrase B 6.25 pIC50 560 nM IC50 Bioorg. Med. Chem. (2008) 16: 7330-7336 [PMID:18595718]
ChEMBL Inhibition of rat intestinal sucrase using sucrose as substrate assessed as D-glucose release from substrate preincubated for 15 mins measured after 60 mins B 6.4 pIC50 400 nM IC50 Bioorg. Med. Chem. (2013) 21: 5442-5450 [PMID:23810673]
amylase alpha 2A in Pig [GtoPdb: 2596]
GtoPdb - - 4.45 pIC50 35500 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 7011-4 [PMID:23102653]
maltase-glucoamylase in Mouse [GtoPdb: 2627]
GtoPdb Affinity measured across splice variants of mouse MGAM catalytic subunit ctMGAM - 8.05 pKi 9 nM Ki Bioorg. Med. Chem. (2011) 19: 3929-34 [PMID:21669536]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]