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BioAssay: AID 626092

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

There are currently no clinically useful inhibitors against metallo-beta-lactamases (MBLs), enzymes that confer resistance against a broad spectrum of commonly used antibiotics and that are produced by an increasing number of bacterial pathogens. New pyrrole derivatives were synthesized and assayed for their inhibitory effect on the catalytic activity of the IMP-1 MBL from Pseudomonas aeruginosa more ..
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 Tested Compounds
 Tested Compounds
All(11)
 
 
Unspecified(11)
 
 
 Tested Substances
 Tested Substances
All(11)
 
 
Unspecified(11)
 
 
 Related BioAssays
 Related BioAssays
AID: 626092
Data Source: ChEMBL (775598)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2014-08-25

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: Synthesis and kinetic testing of new inhibitors for a metallo-beta-lactamase from Klebsiella pneumonia and Pseudomonas aeruginosa.

Abstract: There are currently no clinically useful inhibitors against metallo-beta-lactamases (MBLs), enzymes that confer resistance against a broad spectrum of commonly used antibiotics and that are produced by an increasing number of bacterial pathogens. New pyrrole derivatives were synthesized and assayed for their inhibitory effect on the catalytic activity of the IMP-1 MBL from Pseudomonas aeruginosa and Klebsiella pneumoniae. Six compounds tested (3a-3c, 5, 7 and 8) show micromolar inhibition constants (K(i) values range from #10 to 30 muM). In silico docking was employed to investigate the binding mode of the strongest inhibitor, 3b, in the active site of IMP-1. Implications for further improvements of binding efficiency and specificity are discussed.
(PMID: 22051063)
Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

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)
Data Table ( Complete ):     View All Data
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