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BioAssay: AID 724304

Inhibition of pure alpha-glucosidase (unknown origin) assessed as para-nitrophenol release at 420 nm OD

A novel series of substituted (E)-3-(Benzo [d]thiazol-2-ylamino)phenylprop-2-en-1-onewere synthesized starting from 2-aminobenzothiazole and 1-aryl-3,3-bis- (methylsulfanyl)-2-propen-1-onesin the presence of a catalytic amount of sodium hydride in THF. The synthesised compounds' structures were confirmed by IR, Mass spectrometry, (1)H NMR, (13)C NMR and HRMS spectral data. These compounds were evaluated for their antidiabetic activity, and most of the derivatives of (E)-3-(Benzo [d]thiazol-2-ylamino)phenylprop-2-en-1-one displayed significant antidiabetic activity. ..more
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 Tested Compounds
 Tested Compounds
All(12)
 
 
Active(1)
 
 
Inactive(10)
 
 
Unspecified(1)
 
 
 Tested Substances
 Tested Substances
All(12)
 
 
Active(1)
 
 
Inactive(10)
 
 
Unspecified(1)
 
 
AID: 724304
Data Source: ChEMBL (936870)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2013-11-07
Modify Date: 2014-08-27

Data Table ( Complete ):           View Active Data    View All Data
Target
Sequence: RecName: Full=Lysosomal alpha-glucosidase; AltName: Full=Acid maltase; AltName: Full=Aglucosidase alfa; Contains: RecName: Full=76 kDa lysosomal alpha-glucosidase; Contains: RecName: Full=70 kDa lysosomal alpha-glucosidase; Flags: Precursor
Description ..   
Protein Family: GH31_MGAM_SI_GAA
Comment ..   

Gene:GAA     Related Protein 3D Structures     More BioActivity Data..
BioActive Compound: 1
Description:
Title: Synthesis, crystal structure and antidiabetic activity of substituted (E)-3-(Benzo [d]thiazol-2-ylamino) phenylprop-2-en-1-one.

Abstract: A novel series of substituted (E)-3-(Benzo [d]thiazol-2-ylamino)phenylprop-2-en-1-onewere synthesized starting from 2-aminobenzothiazole and 1-aryl-3,3-bis- (methylsulfanyl)-2-propen-1-onesin the presence of a catalytic amount of sodium hydride in THF. The synthesised compounds' structures were confirmed by IR, Mass spectrometry, (1)H NMR, (13)C NMR and HRMS spectral data. These compounds were evaluated for their antidiabetic activity, and most of the derivatives of (E)-3-(Benzo [d]thiazol-2-ylamino)phenylprop-2-en-1-one displayed significant antidiabetic activity.
(PMID: 23262035)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: Binding
Target Type: Target is a single protein chain
Assay Data Source: Scientific Literature
Protein Target Class: enzyme hydrolase
Result Definitions
Show more
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1IC50*IC50 PubChem standard valueFloatμM
3BEIBinding Efficiency Index(nM)Float
2SEISurface Efficiency Index(nM)Float
4LELigand EfficiencyFloat
5LLELipophilic Ligand EfficiencyFloat
6IC50 activity commentIC50 activity commentString
7IC50 standard flagIC50 standard flagInteger
8IC50 qualifierIC50 qualifierString
9IC50 published valueIC50 published valueFloatμM
10IC50 standard valueIC50 standard valueFloatnM
11IC50 data validityIC50 data validityString

* Activity Concentration.

Data Table (Concise)
Data Table ( Complete ):     View Active Data    View All Data
Classification
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