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BioAssay: AID 421040

Inhibition of PDGF-BB-stimulated RhoA activity in human aortic smooth muscle cells assessed as reduction in ratio of RhoAGTP/RhoA levels at 25 uM after 4 hrs by pull-down assay

Rac1 protein is implicated in several events of atherosclerotic plaque development and represents a new potential pharmacological target for cardiovascular diseases. In this paper we describe a pharmacophore virtual screening followed by molecular docking calculations leading to the identification of five new Rac1 inhibitors. These compounds were shown to be more effective than the reference compound NSC23766 in reducing the intracellular levels of Rac1-GTP, thus supporting this approach for the development of new Rac1 inhibitors. ..more
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 Tested Compounds
 Tested Compounds
All(5)
 
 
Inactive(5)
 
 
 Tested Substances
 Tested Substances
All(5)
 
 
Inactive(5)
 
 
 Related BioAssays
 Related BioAssays
AID: 421040
Data Source: ChEMBL (572384)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-26
Modify Date: 2013-11-16

Data Table ( Complete ):           All
Target
Sequence: RecName: Full=Transforming protein RhoA; AltName: Full=Rho cDNA clone 12; Short=h12; Flags: Precursor
Description ..   
Protein Family: Ras homology family A (RhoA)-like includes RhoA, RhoB and RhoC
Comment ..   

Gene:RHOA     Related Protein 3D Structures     More BioActivity Data..
Tested Compounds:
Description:
Title: Virtual screening approach for the identification of new Rac1 inhibitors.

Abstract: Rac1 protein is implicated in several events of atherosclerotic plaque development and represents a new potential pharmacological target for cardiovascular diseases. In this paper we describe a pharmacophore virtual screening followed by molecular docking calculations leading to the identification of five new Rac1 inhibitors. These compounds were shown to be more effective than the reference compound NSC23766 in reducing the intracellular levels of Rac1-GTP, thus supporting this approach for the development of new Rac1 inhibitors.
(PMID: 19527032)
Categorized Comment
ChEMBL Assay Type: Binding

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 102393

ChEMBL Target Type: Target is a single protein chain

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Activity activity commentActivity activity commentString
2Activity standard flagActivity standard flagInteger
3Activity qualifierActivity qualifierString
4Activity published valueActivity published valueFloat
5Activity standard valueActivity standard valueFloat

Data Table (Concise)
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