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 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]
