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BioAssay: AID 421037

Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of ratio of Rac1GTP/Rac1 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)
 
 
Active(4)
 
 
Unspecified(1)
 
 
 Tested Substances
 Tested Substances
All(5)
 
 
Active(4)
 
 
Unspecified(1)
 
 
AID: 421037
Data Source: ChEMBL (572381)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-26
Modify Date: 2014-08-24

Data Table ( Complete ):           View Active Data    View All Data
Target
Sequence: RecName: Full=Ras-related C3 botulinum toxin substrate 1; AltName: Full=Cell migration-inducing gene 5 protein; AltName: Full=Ras-like protein TC25; AltName: Full=p21-Rac1; Flags: Precursor
Description ..   
Protein Family: Ras-related C3 botulinum toxin substrate 1 (rho family, small GTP binding protein Rac1)-like consists of Rac1, Rac2 and Rac3
Comment ..   

Gene:RAC1     Related Protein 3D Structures     More BioActivity Data..
BioActive Compounds: 4
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 - additional comments and annotations
From BioAssay Depositor:
Assay Type: Binding
Target Type: Target is a single protein chain
Assay Data Source: Scientific Literature
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)
Data Table ( Complete ):     View Active Data    View All Data
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