acarbose [Ligand Id: 6791] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1566 (Acarbose, BAY G 5421, BAY-G-5421, Glucobay, NSC-758915, Precose) |
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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 | 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] |
| 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 | 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] |
| alpha glucosidase/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: P0DUB6] | ||||||||
| 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 34:
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]
