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BioAssay: AID 95526

Ability to inhibit autophosphorylation of KinA/Sp0F assay

A series of diaryltriazole analogs was discovered to inhibit bacterial two-component regulatory systems in our primary assays, KinA/Spo0F and NRII/NRI. They also showed inhibitory activity in whole cell mechanism-based assays, and they possessed potent activities against several strains of Gram-positive pathogenic bacteria in the standard MIC broth assay. ..more
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 Tested Compounds
 Tested Compounds
All(18)
 
 
Active(5)
 
 
Unspecified(13)
 
 
 Tested Substances
 Tested Substances
All(18)
 
 
Active(5)
 
 
Unspecified(13)
 
 
AID: 95526
Data Source: ChEMBL (92720)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-20
Modify Date: 2014-05-12

Data Table ( Complete ):           Active    All
Targets
Sequence: RecName: Full=Sporulation initiation phosphotransferase F; AltName: Full=Stage 0 sporulation protein F
Description ..   
Protein Family: REC
Comment ..   

Gene:SPO0F     Related Protein 3D Structures     More BioActivity Data..


more...  
BioActive Compounds: 5
Description:
Title: SAR studies of diaryltriazoles against bacterial two-component regulatory systems and their antibacterial activities.

Abstract: A series of diaryltriazole analogs was discovered to inhibit bacterial two-component regulatory systems in our primary assays, KinA/Spo0F and NRII/NRI. They also showed inhibitory activity in whole cell mechanism-based assays, and they possessed potent activities against several strains of Gram-positive pathogenic bacteria in the standard MIC broth assay.
(PMID: 9873461)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

BAO: Assay Format: biochemical format

Target Type: Target is a group of closely related proteins

Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1IC50*IC50 PubChem standard valueFloatμM
3BEIBinding Efficiency Index(nM)Float
2SEISurface Efficiency Index(nM)Float
4LELigand EfficiencyFloat
5LLELipophilic Ligand EfficiencyFloat
6IC50 activity commentIC50 activity commentString
7IC50 standard flagIC50 standard flagInteger
8IC50 qualifierIC50 qualifierString
9IC50 published valueIC50 published valueFloatμM
10IC50 standard valueIC50 standard valueFloatnM
11IC50 data validityIC50 data validityString

* Activity Concentration.

Data Table (Concise)
Classification
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