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BioAssay: AID 95387

Inhibition of KinA/Sp0F system two component (TCS) from Bacillus subtilis.

Amidino benzimidazoles have been identified as inhibitors of the bacterial KinA/Spo0F two-component system (TCS). Many of these inhibitors exhibit good in vitro antibacterial activity against a variety of susceptible and resistant Gram-positive organisms. The moiety at the 2-position of the benzimidazole was extensively modified. In addition, the regioisomeric benzoxazoles, heterocyclic replacements for the benzimidazole, have been synthesized and their activity against the TCS evaluated. ..more
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 Tested Compounds
 Tested Compounds
All(21)
 
 
Active(11)
 
 
Unspecified(10)
 
 
 Tested Substances
 Tested Substances
All(21)
 
 
Active(11)
 
 
Unspecified(10)
 
 
AID: 95387
Data Source: ChEMBL (92581)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-20
Modify Date: 2014-08-23

Data Table ( Complete ):           View Active Data    View All Data
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..


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BioActive Compounds: 11
Description:
Title: Amidino benzimidazole inhibitors of bacterial two-component systems.

Abstract: Amidino benzimidazoles have been identified as inhibitors of the bacterial KinA/Spo0F two-component system (TCS). Many of these inhibitors exhibit good in vitro antibacterial activity against a variety of susceptible and resistant Gram-positive organisms. The moiety at the 2-position of the benzimidazole was extensively modified. In addition, the regioisomeric benzoxazoles, heterocyclic replacements for the benzimidazole, have been synthesized and their activity against the TCS evaluated.
(PMID: 11412977)
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 group of closely related proteins
Assay Data Source: Scientific Literature
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)
Data Table ( Complete ):     View Active Data    View All Data
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