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BioAssay: AID 725597

inhibition of human PAD4 preincubated at 1 uM for 15 mins before substrate addition measured after 20 mins by spectrophotometry

Protein arginin deaminase 4 (PAD4) is a calcium dependent enzyme which catalyses the conversion of peptidyl-arginine into peptidyl-citrulline and is implicated in several diseases such as rheumatoid arthritis (RA) and cancer. Herein we report the discovery of novel small-molecule, non peptidic PAD4 inhibitors incorporating primary/secondary guanidine moieties. ..more
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 Tested Compounds
 Tested Compounds
All(13)
 
 
Unspecified(13)
 
 
 Tested Substances
 Tested Substances
All(13)
 
 
Unspecified(13)
 
 
 Related BioAssays
 Related BioAssays
AID: 725597
Data Source: ChEMBL (938163)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2013-11-07
Modify Date: 2014-05-27

Data Table ( Complete ):           All
Target
Sequence: RecName: Full=Protein-arginine deiminase type-4; AltName: Full=HL-60 PAD; AltName: Full=Peptidylarginine deiminase IV; AltName: Full=Protein-arginine deiminase type IV
Description ..   
Protein Family: Protein-arginine deiminase (PAD)
Comment ..   

Gene:PADI4     Related Protein 3D Structures     More BioActivity Data..
Tested Compounds:
Description:
Title: Novel small molecule protein arginine deiminase 4 (PAD4) inhibitors.

Abstract: Protein arginin deaminase 4 (PAD4) is a calcium dependent enzyme which catalyses the conversion of peptidyl-arginine into peptidyl-citrulline and is implicated in several diseases such as rheumatoid arthritis (RA) and cancer. Herein we report the discovery of novel small-molecule, non peptidic PAD4 inhibitors incorporating primary/secondary guanidine moieties.
(PMID: 23265898)
Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

BAO: Assay Format: biochemical format

Target Type: Target is a single protein chain

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Inhibition activity commentInhibition activity commentString
2Inhibition standard flagInhibition standard flagInteger
3Inhibition qualifierInhibition qualifierString
4Inhibition published valueInhibition published valueFloat%
5Inhibition standard valueInhibition standard valueFloat%

Data Table (Concise)
Classification
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