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BioAssay: AID 2281

qHTS Assay for Inhibitors of Ubiquitin-specific Protease USP2a: Summary

Homeostasis of cellular proteins is maintained through a combination of synthesis and degradation. The pathway that accounts for the majority of protein degradation is the ubiquitin-proteasomal pathway. Ubiquitin (Ub) is highly conserved in all cells and the generation of a multi-Ub chain typically targets proteins for degradation by the proteasome. However, ubiquitination is highly reversible more ..
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 Tested Compounds
 Tested Compounds
All(29)
 
 
Active(6)
 
 
Inactive(23)
 
 
 Tested Substances
 Tested Substances
All(29)
 
 
Active(6)
 
 
Inactive(23)
 
 
AID: 2281
Data Source: NCGC (UBPA872)
BioAssay Type: Summary, Candidate Probes/Leads with Supporting Evidence
Depositor Category: NIH Molecular Libraries Probe Production Network
BioAssay Version:
Deposit Date: 2010-01-21
Modify Date: 2010-09-24

Data Table ( Complete ):           Active    All
Target
Sequence: ubiquitin specific peptidase 2 isoform a [Homo sapiens]
Description ..   
Protein Family: Peptidase_C19R

Gene:USP2          More BioActivity Data..
BioActive Compounds: 6
Depositor Specified Assays
Show more
AIDNameTypeComment
927qHTS Assay for Inhibitors of Ubiquitin-specific Protease USP2aconfirmatoryPrimary screen for inhibitors of USP2a
1455Confirmation Concentration-response Assay for Inhibitors of Ubiquitin-specific Protease USP2aconfirmatoryConfirmation assay for inhibitors of USP2a
463254qHTS Assay for Inhibitors of Ubiquitin-specific Protease USP2a Using CHOP2 as the ReporterconfirmatoryPrimary rescreen for inhibitors of USP2a using CHOP2 coupling enzyme
463106qHTS Validation Assay for Inhibitors of Ubiquitin-specific Protease USP2a Using CHOP2 as the Reporterconfirmatory
493168Confirmation Assay for Inhibitors of Ubiquitin-specific Protease USP2a Using CHOP2 as the Reporterconfirmatory
493169CHOP2 Reporter Counterscreen Assay for Inhibitors of Ubiquitin-specific Protease USP2aconfirmatory
493170Ub-rhodamine 110 based assay for inhibitors Ubiquitin-specific Protease USP2aconfirmatory
652168qHTS for Inhibitors of Ubiquitin-specific Protease USP2a Using CHOP2 as the Reporter: K633 Counterscreenconfirmatory
652170qHTS for Inhibitors of Ubiquitin-specific Protease USP2a Using CHOP2 as the Reporter: Cytotox Assayconfirmatory
652172Confirmation Assay for Inhibitors of Ubiquitin-specific Protease USP2a Using CHOP2 as the Reporter: K633confirmatory
652173qHTS for Inhibitors of Ubiquitin-specific Protease USP2a Using CHOP2 as the Reporter: K484 Substrateconfirmatory
652174Confirmation Assay for Inhibitors of Ubiquitin-specific Protease USP2a Using CHOP2 as the Reporter: SARconfirmatory
652251qHTS for Inhibitors of Ubiquitin-specific Protease USP2a Using CHOP2 as the Reporter: Cyclin D1 Western Blotother
652254qHTS for Inhibitors of Ubiquitin-specific Protease USP2a Using CHOP2 as the Reporter: Clonogenic Assayother
652264qHTS for Inhibitors of Ubiquitin-specific Protease USP2a Using CHOP2 as the Reporter: Cell Cycleother
652277qHTS for Inhibitors of Ubiquitin-specific Protease USP2a Using CHOP2 as the Reporter: Caspase 6 Assayconfirmatory
Description:
NIH Molecular Libraries Screening Centers Network [MLSCN]
NIH Chemical Genomics Center [NCGC]

MLSCN Grant: XO1-MH079852-01
PI Name: Nicholson, Ben. Progenra Inc, Malvern, PA

NCGC Assay Overview:

Homeostasis of cellular proteins is maintained through a combination of synthesis and degradation. The pathway that accounts for the majority of protein degradation is the ubiquitin-proteasomal pathway. Ubiquitin (Ub) is highly conserved in all cells and the generation of a multi-Ub chain typically targets proteins for degradation by the proteasome. However, ubiquitination is highly reversible and dynamic. Deubiquitination, the reverse process, is catalyzed through the action of enzymes referred to as isopeptidases or deubiquitinating enzymes (DUBs) [1, 2]. This group of enzymes is collectively responsible for maintaining adequate pools of free ubiquitin and regulating the ubiquitination status of cellular proteins. The class of DUBs referred to as the ubiquitin-specific proteases (USP) family functions endoproteolytically to cleave Ub chains from a wide range of protein substrates. USP2a deubiquitinates fatty acid synthase (FASN) which has recently been identified as an emerging oncology target [3-6]. To identify inhibitors of USP2a a cell-free assay was employed.

The primary qHTS data of human the USP2a-PLA2 coupled assay and confirmatory data are available in PubChem (AIDs: 927, 1455). The rescreen data using CHOP2 coupled enzyme assay is available in PubChem (AID: 463254).
Protocol
Please refer to other AIDs (927, 1455 and 463254) for detailed assay protocols.
Comment
This summary assay will be updated as additional screens are run and small molecule probes have been developed.
Molecules pending validation are given a score of 50. Inactive compounds are given a score of 0.
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
ScoreThe BioAssay activity ranking scoreInteger
1PhenotypeIndicates type of activity observed based on the compound activity in GALK confirmation and counter assays.String
2Potency in Confirmation AssayThe concentration of sample yielding half-maximal inhibition in USP2a confirmation assay.FloatμM
3Potency in PLA2 CounterscreenThe concentration of sample yielding half-maximal inhibition in PLA2 counterscreen.FloatμM
Additional Information
Grant Number: XO1-MH079852-01

Data Table (Concise)
Classification
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