Acarbose (CID 444254) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(42)
 
 
Inactive(4)
 
 
Inconclusive(1)
 
 
Unspecified(1593)
 
 
Top Targets:
GH31 MGAM SI..(23)
 
 
 
7TM GPCR Srx(12)
 
 
7TM GPCR Srsx(9)
 
 
p450(8)
 
 
AmyAc SI Olig..(4)
 
 
BioAssay Types:
Literature(128)
 
 
 
 
Screening(2)
 
 
Confirmatory(2)
 
 
BioActivity Types:
IC50(158)
 
 
 
 
Ki(9)
 
 
 
Potency(2)
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 1639    Data Row: 1640   Total Pages: 33   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103585278]
Ki 0.009Inhibition of mouse his-tagged ctMGAM-N2 expressed in Sf9 cells assessed as amount of glucose produced using maltose as a substrate after 45 mins by glucose oxidase assay [AID620760, Type: Literature]
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2
[SID103585278]
Ki 0.028Inhibition of mouse his-tagged ctMGAM-N20 expressed in Sf9 cells assessed as amount of glucose produced using maltose as a substrate after 45 mins by glucose oxidase assay [AID620761, Type: Literature]
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3
[SID103585278]
IC50 0.033Inhibition of Bacillus stearothermophilus alpha-glucosidase type IV [AID427710, Type: Literature]
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4
[SID103585278]
IC50 0.049Inhibition of Bacillus stearothermophilus alpha glucosidase-4 [AID497106, Type: Literature]
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5
[SID103585278]
IC50 0.1Inhibition of Bacillus stearothermophilus alpha-glucosidase [AID391607, Type: Literature]
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6
[SID103585278]
IC50 0.1Inhibition of Saccharomyces cerevisiae alpha-glucosidase [AID391608, Type: Literature]
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7
[SID103585278]
IC50 0.16Inhibition of Wistar rat small intestine maltase after 30 mins [AID550393, Type: Literature]Lysosomal alpha-glucosidase [gi:81885339]
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8
[SID103585278]
Ki 0.246Inhibition of mouse his-tagged ctSI expressed in Sf9 cells assessed as amount of glucose produced using maltose as a substrate after 45 mins by glucose oxidase assay [AID620763, Type: Literature]
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9
[SID103585278]
Ki 0.34Competitive inhibition of Bacillus stearothermophilus alpha-glucosidase assessed as production of chromogenic p-Nitrphenol measured after 3 mins by HPLC and Michaelis-Menton equation [AID590733, Type: Literature]Exo-alpha-1,4-glucosidase [gi:75499522]
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10
[SID103585278]
IC50 0.35Inhibition of rat intestinal brush border membrane maltase [AID342793, Type: Literature]Lysosomal alpha-glucosidase [gi:81885339]
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11
[SID103585278]
IC50 0.56Inhibition of rat intestinal brush border membrane sucrase [AID342797, Type: Literature]Sucrase-isomaltase, intestinal [gi:1351132]
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12
[SID103585278]
IC50 0.996Inhibition of human salivary alpha-amylase [AID404692, Type: Literature]Alpha-amylase 1 [gi:1351933]
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13
[SID103585278]
IC50 1.5Inhibition of rat small intestinal sucrase after 30 mins by glucose-oxidase method [AID594100, Type: Literature]Sucrase-isomaltase, intestinal [gi:1351132]
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14
[SID103585278]
IC50 1.5Inhibition of rat intestinal alpha-glucosidase maltase using maltose as substrate preincubated for 10 mins prior substrate addition measured after 40 mins by spectrophotometry [AID647236, Type: Literature]Lysosomal alpha-glucosidase [gi:81885339]
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15
[SID103585278]
IC50 1.7Inhibition of alpha-glucosidase activity of sucrase in rat small intestinal brush border membrane fraction using maltose as substrate after 30 mins [AID641148, Type: Literature]Sucrase-isomaltase, intestinal [gi:1351132]
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16
[SID103585278]
IC50 1.7Inhibition of rat small intestinal maltase after 30 mins by glucose-oxidase method [AID594099, Type: Literature]Lysosomal alpha-glucosidase [gi:81885339]
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17
[SID103585278]
IC50 1.7Inhibition of rat small intestinal maltase after 30 mins [AID593351, Type: Literature]Lysosomal alpha-glucosidase [gi:81885339]
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18
[SID103585278]
IC50 1.7Inhibition of rat intestinal sucrase [AID578320, Type: Literature]Sucrase-isomaltase, intestinal [gi:1351132]
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19
[SID103585278]
IC50 2Inhibition of rat small intestinal sucrase after 30 mins [AID593349, Type: Literature]Sucrase-isomaltase, intestinal [gi:1351132]
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20
[SID103585278]
IC50 2Inhibition of rat intestinal maltase [AID578319, Type: Literature]Lysosomal alpha-glucosidase [gi:81885339]
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21
[SID103585278]
IC50 2Inhibition of alpha-glucosidase activity of maltase in rat small intestinal brush border membrane fraction using maltose as substrate after 30 mins [AID641146, Type: Literature]Lysosomal alpha-glucosidase [gi:81885339]
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22
[SID103585278]
IC50 2.38Inhibition of rat intestinal alpha-glucosidase sucrase using sucrose as substrate preincubated for 10 mins prior substrate addition measured after 40 mins by spectrophotometry [AID647238, Type: Literature]Sucrase-isomaltase, intestinal [gi:1351132]
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23
[SID103585278]
IC50 2.9Inhibition of Wistar rat small intestine sucrase after 30 mins [AID550397, Type: Literature]Sucrase-isomaltase, intestinal [gi:1351132]
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24
[SID103585278]
Ki 3.5Competitive inhibition of rat alpha-glucosidase assessed as production of chromogenic p-Nitrphenol measured after 3 mins by HPLC and Michaelis-Menton equation [AID590735, Type: Literature]Lysosomal alpha-glucosidase [gi:81885339]
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25
[SID103585278]
Ki 4.2Competitive inhibition of rice alpha-glucosidase assessed as production of chromogenic p-Nitrphenol measured after 3 mins by HPLC and Michaelis-Menton equation [AID590734, Type: Literature]
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26
[SID103585278]
IC50 5Inhibition of maltase in human Caco-2 cell model system after 2 hrs [AID342811, Type: Literature]Lysosomal alpha-glucosidase [gi:317373572]
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27
[SID103585278]
IC50 5Inhibition of maltase in human Caco-2 cell model system after 2 hrs [AID342811, Type: Literature]Lysosomal alpha-glucosidase [gi:317373572]
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28
[SID103585278]
IC50 5Inhibition of maltase in human Caco-2 cell model system after 2 hrs [AID342811, Type: Literature]Lysosomal alpha-glucosidase [gi:317373572]
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29
[SID103585278]
IC50 6.38Inhibition of rat intestinal alpha-glucosidase [AID317574, Type: Literature]
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30
[SID103585278]
Ki 14Inhibition of human ntSI expressed in Drosophila S2 cells assessed as amount of glucose produced using maltose as a substrate after 45 mins by glucose oxidase assay [AID620764, Type: Literature]
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31
[SID103585278]
IC50 23.8Inhibition of rat intestinal alpha-glucosidase activity [AID352467, Type: Literature]
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32
[SID103585278]
IC50 30Inhibition of Saccharomyces cerevisiae alpha glucosidase [AID422282, Type: Literature]
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33
[SID103585278]
IC50 42Inhibition of human lysosomal alpha-glucosidase [AID342799, Type: Literature]Lysosomal alpha-glucosidase [gi:317373572]
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34
[SID103585278]
IC50 42Inhibition of human lysosomal alpha-glucosidase [AID342799, Type: Literature]Lysosomal alpha-glucosidase [gi:317373572]
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35
[SID103585278]
IC50 42Inhibition of human lysosomal alpha-glucosidase [AID342799, Type: Literature]Lysosomal alpha-glucosidase [gi:317373572]
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36
[SID46393315]
 Experimentally measured binding affinity data derived from PDB [AID1811, Type: Literature]Chain A, Crystal Structure Of Y100l Mutant Cyclodextrin Glucanotransferase Compexed With An Acarbose [gi:46015837]
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37
[SID46391424]
 Experimentally measured binding affinity data derived from PDB [AID1811, Type: Literature]Chain A, Refined Structure For The Complex Of Acarbose With Glucoamylase From Aspergillus Awamori Va [gi:157829865]
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38
[SID103585278]
 Antidiabetic activity in streptozotocin-induced diabetic ICR mouse assessed as lowering of blood glucose level by oral sucrose tolerance test [AID592245, Type: Literature]
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39
[SID103585278]
 FDA HLAED, liver enzyme composite activity [AID588214, Type: Literature]
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40
[SID103585278]
 FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase [AID588216, Type: Literature]
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41
[SID103585278]
 FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase [AID588217, Type: Literature]
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42
[SID103585278]
 FDA HLAED, gamma-glutamyl transferase (GGT) increase [AID588219, Type: Literature]
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43
[SID103585278]
 Antihyperglycemic activity in overnight fasted starch-induced hyperglycemic Wistar rat assessed as decrease in plasma glucose level at 10 mg/kg, po administered 15 mins before starch challenge measured after 30 to 120 mins by glucose oxidase method [AID456206, Type: Literature]
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44
[SID103585278]
 Antihyperglycemic activity in Wistar rat assessed as reduction in postprandial blood glucose rise at 100 mg/kg, po by carbohydrate tolerance test [AID344180, Type: Literature]
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45
[SID103585278]
 Hypoglycemic activity in maltose-fed Wistar rat assessed as reduction in postprandial blood glucose level at 50 mg/kg, po administered 15 mins before maltose challenge measured after 30 mins of maltose infusion [AID462734, Type: Literature]
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46
[SID103585278]
 Hypoglycemic activity in maltose-fed Wistar rat assessed as reduction in postprandial blood glucose level at 50 mg/kg, po administered 15 mins before maltose challenge measured after 60 mins of maltose infusion [AID462735, Type: Literature]
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47
[SID103585278]
IC50 60.8Inhibitory activity against baker's yeast alpha glucosidase [AID257318, Type: Literature]Alpha-glucosidase MAL62 [gi:126716]
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48
[SID103585278]
Ki 62Inhibition of human ntMGAM expressed in Drosophila S2 cells assessed as amount of glucose produced using maltose as a substrate after 45 mins by glucose oxidase assay [AID620762, Type: Literature]
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49
[SID103585278]
IC50 108.8Inhibition of yeast alpha-glucosidase MAL12 assessed as inhibition of p-nitrophenol release by spectrophotometry [AID462732, Type: Literature]Alpha-glucosidase MAL12 [gi:1708906]
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50
[SID103585278]
IC50 155Inhibition of rat intestinal isomaltase [AID578321, Type: Literature]Sucrase-isomaltase, intestinal [gi:1351132]
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