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BioAssay: AID 721628

Inhibition of glycation of bovine serum albumin assessed as advanced glycated end product measured after 7 days by spectrofluorimeter in presence of glucose anhydrous

Synthesis of a new series of urea/thiourea derivatives of Gly/Pro conjugated benzisoxazole has been reported. Structure of the compounds was characterized by physical and spectroscopical data and has been screened for their in vitro antiglycation activity. Several compounds showed promising activity with IC(50) < 5 muM compared to standard rutin (IC(50) = 41.9 muM). Further, it was found that compounds containing methoxy and bromine substituents have exerted highly potent activity. Thus, the title compounds represent novel class of potent antiglycating agents. ..more
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 Tested Compounds
 Tested Compounds
All(45)
 
 
Active(23)
 
 
Inactive(4)
 
 
Unspecified(18)
 
 
 Tested Substances
 Tested Substances
All(45)
 
 
Active(23)
 
 
Inactive(4)
 
 
Unspecified(18)
 
 
 Related BioAssays
 Related BioAssays
AID: 721628
Data Source: ChEMBL (934194)
Depositor Category: Literature, Extracted
Deposit Date: 2013-11-07

Data Table ( Complete ):           Active    All
Target
Sequence: RecName: Full=Serum albumin; AltName: Full=BSA; AltName: Allergen=Bos d 6; Flags: Precursor
Description ..   
Protein Family: ALBUMIN
Comment ..   

Gene:ALB     Related Protein 3D Structures     More BioActivity Data..
BioActive Compounds: 23
Description:
Title: Inhibition of protein glycation by urea and thiourea derivatives of glycine/proline conjugated benzisoxazole analogue - synthesis and structure-activity studies.

Abstract: Synthesis of a new series of urea/thiourea derivatives of Gly/Pro conjugated benzisoxazole has been reported. Structure of the compounds was characterized by physical and spectroscopical data and has been screened for their in vitro antiglycation activity. Several compounds showed promising activity with IC(50) < 5 muM compared to standard rutin (IC(50) = 41.9 muM). Further, it was found that compounds containing methoxy and bromine substituents have exerted highly potent activity. Thus, the title compounds represent novel class of potent antiglycating agents.
(PMID: 23314045)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Categorized Comment
ChEMBL Assay Type: Binding

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 12879

ChEMBL Target Type: Target is a single protein chain

Result Definitions
Show more
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1IC50*IC50 PubChem standard valueFloatμM
2BEIBinding Efficiency Index(nM)Float
3SEISurface 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)
Classification
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