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BioAssay: AID 393171

Cytotoxicity against human HepG2 cells

Plasmodium falciparum, the Apicomplexan parasite that is responsible for the most lethal forms of human malaria, is exposed to radically different environments and stress factors during its complex lifecycle. In any organism, Hsp70 chaperones are typically associated with tolerance to stress. We therefore reasoned that inhibition of P. falciparum Hsp70 chaperones would adversely affect parasite more ..
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 Tested Compounds
 Tested Compounds
All(10)
 
 
Active(1)
 
 
Unspecified(9)
 
 
 Tested Substances
 Tested Substances
All(10)
 
 
Active(1)
 
 
Unspecified(9)
 
 
 Related BioAssays
 Related BioAssays
AID: 393171
Data Source: ChEMBL (541200)
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 ):           View Active Data    View All Data
BioActive Compound: 1
Description:
Title: Select pyrimidinones inhibit the propagation of the malarial parasite, Plasmodium falciparum.

Abstract: Plasmodium falciparum, the Apicomplexan parasite that is responsible for the most lethal forms of human malaria, is exposed to radically different environments and stress factors during its complex lifecycle. In any organism, Hsp70 chaperones are typically associated with tolerance to stress. We therefore reasoned that inhibition of P. falciparum Hsp70 chaperones would adversely affect parasite homeostasis. To test this hypothesis, we measured whether pyrimidinone-amides, a new class of Hsp70 modulators, could inhibit the replication of the pathogenic P. falciparum stages in human red blood cells. Nine compounds with IC(50) values from 30 nM to 1.6 micrOM were identified. Each compound also altered the ATPase activity of purified P. falciparum Hsp70 in single-turnover assays, although higher concentrations of agents were required than was necessary to inhibit P. falciparum replication. Varying effects of these compounds on Hsp70s from other organisms were also observed. Together, our data indicate that pyrimidinone-amides constitute a novel class of anti-malarial agents.
(PMID: 19195901)
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: 81020
Target Type: CELL-LINE
Cell Line: HepG2
Tissue: Hepatoblastoma cells
Pref Name: HepG2
Organism: Homo sapiens
Tax ID: 9606
Confidence: Target assigned is non-molecular
Relationship Type: Non-molecular target assigned
Categorized Comment
Assay Type: ADME

Assay Data Source: Scientific Literature

BAO: Assay Format: cell-based format

Assay Cell Type: HepG2

Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1GI50*GI50 PubChem standard valueFloatμM
2GI50 activity commentGI50 activity commentString
3GI50 standard flagGI50 standard flagInteger
4GI50 qualifierGI50 qualifierString
5GI50 published valueGI50 published valueFloatnM
6GI50 standard valueGI50 standard valueFloatnM
7GI50 activity commentGI50 activity commentString
8GI50 standard flagGI50 standard flagInteger
9GI50 qualifierGI50 qualifierString
10GI50 published valueGI50 published valueFloatμM
11GI50 standard valueGI50 standard valueFloatnM

* Activity Concentration.

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