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BioAssay: AID 761509

Inhibition of wild type human USP5 expressed in Escherichia coli BL21(DE3) using Ub-AMC as substrate after 60 mins by fluorometric analysis

Vialinin A, a small compound isolated from the Chinese mushroom Thelephora vialis, exhibits more effective anti-inflammatory activity than the widely used immunosuppressive drug tacrolimus (FK506). Here, we show that ubiquitin-specific peptidase 5/isopeptidase T (USP5/IsoT) is a target molecule of vialinin A, identified by using a beads-probe method. Vialinin A inhibited the peptidase activity of more ..
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Active(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Active(1)
 
 
AID: 761509
Data Source: ChEMBL (974345)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2014-05-03
Modify Date: 2014-08-24

Data Table ( Complete ):           View Active Data    View All Data
Target
Sequence: RecName: Full=Ubiquitin carboxyl-terminal hydrolase 5; AltName: Full=Deubiquitinating enzyme 5; AltName: Full=Isopeptidase T; AltName: Full=Ubiquitin thioesterase 5; AltName: Full=Ubiquitin-specific-processing protease 5
Description ..   
Protein Family: Peptidase_C19B
Comment ..   

Gene:USP5     Related Protein 3D Structures     More BioActivity Data..
BioActive Compound: 1
Description:
Title: Vialinin A is a ubiquitin-specific peptidase inhibitor.

Abstract: Vialinin A, a small compound isolated from the Chinese mushroom Thelephora vialis, exhibits more effective anti-inflammatory activity than the widely used immunosuppressive drug tacrolimus (FK506). Here, we show that ubiquitin-specific peptidase 5/isopeptidase T (USP5/IsoT) is a target molecule of vialinin A, identified by using a beads-probe method. Vialinin A inhibited the peptidase activity of USP5/IsoT and also inhibited the enzymatic activities of USP4 among deubiquitinating enzymes tested. Although USPs are a member of thiol protease family, vialinin A exhibited no inhibitions for other thiol proteases, such as calpain and cathepsin.
(PMID: 23791076)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.
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
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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 valueFloatμM
6IC50 standard valueIC50 standard valueFloatnM
7IC50 Binding Efficiency Index(nM)IC50 Binding Efficiency Index(nM)Float
8IC50 Surface Efficiency Index(nM)IC50 Surface Efficiency Index(nM)Float
9IC50 Ligand EfficiencyIC50 Ligand EfficiencyFloat
10IC50 Lipophilic Ligand EfficiencyIC50 Lipophilic Ligand EfficiencyFloat
11Ki activity commentKi activity commentString
12Ki standard flagKi standard flagInteger
13Ki qualifierKi qualifierString
14Ki published valueKi published valueFloatμM
15Ki standard valueKi standard valueFloatnM
16Ki Binding Efficiency Index(nM)Ki Binding Efficiency Index(nM)Float
17Ki Surface Efficiency Index(nM)Ki Surface Efficiency Index(nM)Float
18Ki Ligand EfficiencyKi Ligand EfficiencyFloat
19Ki Lipophilic Ligand EfficiencyKi Lipophilic Ligand EfficiencyFloat

* Activity Concentration.

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