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BioAssay: AID 638649

Inhibition of Pseudomonas aeruginosa beta-lactamase IMP-1 expressed in Escherichia coli BL21(DE3) at 10 uM using CENTA as chromogenic substrate

The production of beta-lactamases is an effective strategy by which pathogenic bacteria can develop resistance against beta-lactam antibiotics. While inhibitors of serine-beta-lactamases are widely used in combination therapy with beta-lactam antibiotics, there are no clinically available inhibitors of metallo-beta-lactamases (MBLs), and so there is a need for the development of such inhibitors. more ..
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 Tested Compounds
 Tested Compounds
All(25)
 
 
Inconclusive(8)
 
 
Unspecified(17)
 
 
 Tested Substances
 Tested Substances
All(25)
 
 
Inconclusive(8)
 
 
Unspecified(17)
 
 
 Related BioAssays
 Related BioAssays
AID: 638649
Data Source: ChEMBL (796097)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2014-08-23

Data Table ( Complete ):           View All Data
Target
Sequence: Metallo-beta-lactamase IMP-1 (Beta-lactamase IMP-1) (Metallo-beta-lactamase) (IMP-1 metallo-beta-lactmase) (Beta-lactamase) (Extended-spectrum B-lactamase) (Bla-imp protein)
Description ..   
Comment ..   

     More BioActivity Data..
Tested Compounds:
Description:
Title: 3-mercapto-1,2,4-triazoles and N-acylated thiosemicarbazides as metallo-beta-lactamase inhibitors.

Abstract: The production of beta-lactamases is an effective strategy by which pathogenic bacteria can develop resistance against beta-lactam antibiotics. While inhibitors of serine-beta-lactamases are widely used in combination therapy with beta-lactam antibiotics, there are no clinically available inhibitors of metallo-beta-lactamases (MBLs), and so there is a need for the development of such inhibitors. This work describes the optimisation of a lead inhibitor previously identified by fragment screening of a compound library. We also report that thiosemicarbazide intermediates in the syntheses of these compounds are also moderately potent inhibitors of the IMP-1 MBL from Pseudomonas aeruginosa. The interactions of these inhibitors with the active site of IMP-1 were examined using in silico methods.
(PMID: 22115595)
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
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)
Data Table ( Complete ):     View All Data
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