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BioAssay: AID 402635

Inhibition of human recombinant DNA polymerase beta assessed as fluorescein-12-dCTP incorporation by fluorimetry

Five new acylphloroglucinol derivatives, mahureones A-E (1, 3-6), have been isolated from the leaves of Mahurea palustris, and their structures determined by spectroscopic means. During the isolation process, several byproducts (7-9) were formed by reaction of one of the isoprenyl side chains with TFA, water, and acetonitrile. All the compounds were assayed for their ability to inhibit human DNA polymerase beta. The most active compounds, mahureones A (1) and D (5), exhibited IC50 values in the 10 microM range. ..more
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 Tested Compounds
 Tested Compounds
All(9)
 
 
Active(3)
 
 
Inactive(4)
 
 
Unspecified(2)
 
 
 Tested Substances
 Tested Substances
All(9)
 
 
Active(3)
 
 
Inactive(4)
 
 
Unspecified(2)
 
 
AID: 402635
Data Source: ChEMBL (550664)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-26
Modify Date: 2014-08-23

Data Table ( Complete ):           View Active Data    View All Data
Target
Sequence: RecName: Full=DNA polymerase beta
Description ..   
Protein Family: Nucleotidyltransferase (NT) domain of family X DNA Polymerases
Comment ..   

Gene:POLB     Related Protein 3D Structures     More BioActivity Data..
BioActive Compounds: 3
Description:
Title: Acylphloroglucinol derivatives from Mahurea palustris.

Abstract: Five new acylphloroglucinol derivatives, mahureones A-E (1, 3-6), have been isolated from the leaves of Mahurea palustris, and their structures determined by spectroscopic means. During the isolation process, several byproducts (7-9) were formed by reaction of one of the isoprenyl side chains with TFA, water, and acetonitrile. All the compounds were assayed for their ability to inhibit human DNA polymerase beta. The most active compounds, mahureones A (1) and D (5), exhibited IC50 values in the 10 microM range.
(PMID: 16038535)
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
Result Definitions
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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
6Activity activity commentActivity activity commentString
7Activity standard flagActivity standard flagInteger
8Activity qualifierActivity qualifierString
9Activity published valueActivity published valueFloat
10Activity standard valueActivity standard valueFloat
11Activity data validityActivity data validityString
12Activity binding domainsActivity binding domainsString
13IC50 activity commentIC50 activity commentString
14IC50 standard flagIC50 standard flagInteger
15IC50 qualifierIC50 qualifierString
16IC50 published valueIC50 published valueFloatμM
17IC50 standard valueIC50 standard valueFloatnM
18IC50 data validityIC50 data validityString
19IC50 binding domainsIC50 binding domainsString

* Activity Concentration.

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