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BioAssay: AID 107430

Inhibition of metallo-beta-lactamase (MBL) from Pseudomonas aeruginosa mediated by the plasmid-borne IMP-1 enzyme.

Resistance to carbapenem antibiotics in gram-negative bacteria is due, in part, to expression of a wide spectrum metallo-beta-lactamase, which renders the drug inactive. Biphenyl tetrazoles containing 3-n-butyl-1-phenylpyrazole-5-carboxylates or the corresponding 5-ethyl esters were found to inhibit metallo-beta-lactamases as well as renal dehydropeptidase I to a lesser extent. ..more
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 Tested Compounds
 Tested Compounds
All(25)
 
 
Unspecified(25)
 
 
 Tested Substances
 Tested Substances
All(25)
 
 
Unspecified(25)
 
 
 Related BioAssays
 Related BioAssays
AID: 107430
Data Source: ChEMBL (104648)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-20
Modify Date: 2013-11-11

Data Table ( Complete ):           All
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: Structure-activity relationships of biphenyl tetrazoles as metallo-beta-lactamase inhibitors.

Abstract: Resistance to carbapenem antibiotics in gram-negative bacteria is due, in part, to expression of a wide spectrum metallo-beta-lactamase, which renders the drug inactive. Biphenyl tetrazoles containing 3-n-butyl-1-phenylpyrazole-5-carboxylates or the corresponding 5-ethyl esters were found to inhibit metallo-beta-lactamases as well as renal dehydropeptidase I to a lesser extent.
(PMID: 10509927)
Categorized Comment
ChEMBL Assay Type: Binding

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 103677

ChEMBL Target Type: Target is a single protein chain

Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1IC50*IC50 PubChem standard valueFloatμM
2BEIBinding Efficiency Index(nM)Float
3SEISurface 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
12IC50 binding domainsIC50 binding domainsString

* Activity Concentration.

Data Table (Concise)
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