Bookmark and Share
BioAssay: AID 349748

Destabilizing effect on human recombinant PHD2 (181-426) expressed in Escherichia coli BL21 (DE3) assessed as half life by limited trypsinolysis/MALDI-MS analysis in presence of ferrous ion

Limited proteolysis coupled to matrix-assisted laser desorption/ionization (MALDI) mass spectrometric analyses can be used to screen for compounds that alter protein structure by monitoring stabilizing/destabilizing effects with respect to the rate and nature of proteolysis. When applied to prolyl hydroxylase 2, a key enzyme involved in human oxygen sensing, the method efficiently revealed differential effects on proteolytic stability for structurally similar compounds and for different substrates. ..more
_
   
 Tested Compounds
 Tested Compounds
All(7)
 
 
Active(5)
 
 
Unspecified(2)
 
 
 Tested Substances
 Tested Substances
All(7)
 
 
Active(5)
 
 
Unspecified(2)
 
 
 Related BioAssays
 Related BioAssays
AID: 349748
Data Source: ChEMBL (497777)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-26
Modify Date: 2014-05-16

Data Table ( Complete ):           Active    All
BioActive Compounds: 5
Description:
Title: Application of a proteolysis/mass spectrometry method for investigating the effects of inhibitors on hydroxylase structure.

Abstract: Limited proteolysis coupled to matrix-assisted laser desorption/ionization (MALDI) mass spectrometric analyses can be used to screen for compounds that alter protein structure by monitoring stabilizing/destabilizing effects with respect to the rate and nature of proteolysis. When applied to prolyl hydroxylase 2, a key enzyme involved in human oxygen sensing, the method efficiently revealed differential effects on proteolytic stability for structurally similar compounds and for different substrates.
(PMID: 19364117)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Putative Target:

ChEMBL Target ID: 22226
Target Type: UNCHECKED
Pref Name: Unchecked
Confidence: Default value - Target unknown or has yet to be assigned
Relationship Type: Default value - Target has yet to be curated
Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1IC50*IC50 PubChem standard valueFloatμM
2IC50 activity commentIC50 activity commentString
3IC50 standard flagIC50 standard flagInteger
4IC50 qualifierIC50 qualifierString
5IC50 published valueIC50 published valueFloatμM
6IC50 standard valueIC50 standard valueFloatnM
7IC50 data validityIC50 data validityString

* Activity Concentration.

Data Table (Concise)
PageFrom: