Bookmark and Share
BioAssay: AID 382280

Inhibition of Trypanosoma brucei phosphofructokinase

The glycolytic pathway has been considered a potential drug target against the parasitic protozoan species of Trypanosoma and Leishmania. We report the design and the synthesis of inhibitors targeted against Trypanosoma brucei phosphofructokinase (PFK) and Leishmania mexicana pyruvate kinase (PyK). Stepwise library synthesis and inhibitor design from a rational starting point identified furanose more ..
_
   
 Tested Compounds
 Tested Compounds
All(5)
 
 
Active(2)
 
 
Unspecified(3)
 
 
 Tested Substances
 Tested Substances
All(5)
 
 
Active(2)
 
 
Unspecified(3)
 
 
 Related BioAssays
 Related BioAssays
AID: 382280
Data Source: ChEMBL (530309)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-26
Modify Date: 2013-11-21

Data Table ( Complete ):           Active    All
Target
Sequence: 6-phospho-1-fructokinase (ATP-dependent phosphofructokinase)
Description ..   
Comment ..   

     More BioActivity Data..
BioActive Compounds: 2
Description:
Title: Design, synthesis and trypanocidal activity of lead compounds based on inhibitors of parasite glycolysis.

Abstract: The glycolytic pathway has been considered a potential drug target against the parasitic protozoan species of Trypanosoma and Leishmania. We report the design and the synthesis of inhibitors targeted against Trypanosoma brucei phosphofructokinase (PFK) and Leishmania mexicana pyruvate kinase (PyK). Stepwise library synthesis and inhibitor design from a rational starting point identified furanose sugar amino amides as a novel class of inhibitors for both enzymes with IC(50) values of 23microM and 26microM against PFK and PyK, respectively. Trypanocidal activity also showed potency in the low micromolar range and confirms these inhibitors as promising candidates for the development towards the design of anti-trypanosomal drugs.
(PMID: 18387804)
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: 101284

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 valueFloatmM
10IC50 standard valueIC50 standard valueFloatnM
11IC50 data validityIC50 data validityString
12IC50 binding domainsIC50 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)
PageFrom: