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BioAssay: AID 524790

Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay

Studies of gene function and molecular mechanisms in Plasmodium falciparum are hampered by difficulties in characterizing and measuring phenotypic differences between individual parasites. We screened seven parasite lines for differences in responses to 1,279 bioactive chemicals. Hundreds of compounds were active in inhibiting parasite growth; 607 differential chemical phenotypes, defined as more ..
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 Tested Compounds
 Tested Compounds
All(534)
 
 
Active(534)
 
 
 Tested Substances
 Tested Substances
All(541)
 
 
Active(541)
 
 
 Related BioAssays
 Related BioAssays
AID: 524790
Data Source: ChEMBL (672658)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2011-09-18
Modify Date: 2013-11-17

Data Table ( Complete ):           Active    All
BioActive Compounds: 534
Description:
Title: Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.

Abstract: Studies of gene function and molecular mechanisms in Plasmodium falciparum are hampered by difficulties in characterizing and measuring phenotypic differences between individual parasites. We screened seven parasite lines for differences in responses to 1,279 bioactive chemicals. Hundreds of compounds were active in inhibiting parasite growth; 607 differential chemical phenotypes, defined as pairwise IC(50) differences of fivefold or more between parasite lines, were cataloged. We mapped major determinants for three differential chemical phenotypes between the parents of a genetic cross, and we identified target genes by fine mapping and testing the responses of parasites in which candidate genes were genetically replaced with mutant alleles. Differential sensitivity to dihydroergotamine methanesulfonate (1), a serotonin receptor antagonist, was mapped to a gene encoding the homolog of human P-glycoprotein (PfPgh-1). This study identifies new leads for antimalarial drugs and demonstrates the utility of a high-throughput chemical genomic strategy for studying malaria traits.
(PMID: 19734910)
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
ChEMBL Assay Type: Functional

ChEMBL Assay Data Source: Scientific Literature

Result Definitions
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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 valueFloat
6IC50 standard valueIC50 standard valueFloatnM
7IC50 activity commentIC50 activity commentString
8IC50 standard flagIC50 standard flagInteger
9IC50 qualifierIC50 qualifierString
10IC50 published valueIC50 published valueFloatnM
11IC50 standard valueIC50 standard valueFloatnM

* Activity Concentration.

Data Table (Concise)
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