Target Validation Information
Target ID T38179
Target Name Beta-lactamase
Target Type
Successful
Drug Potency against Target Clavulanate Drug Info IC50 = 20 nM [552352]
Tazobactam Drug Info IC50 = 151 nM [552899]
Diisopropyl 1-mercaptopropylphosphonate Drug Info Ki = 2000 nM [530954]
2-(Sulfanylmethyl)phenylphosphonic acid Drug Info Ki = 2000 nM [530954]
Alpha-Sulfanyl(4-bromobenzyl)phosphonic acid Drug Info Ki = 8400 nM [530954]
2-mercaptophenylphosphonic acid Drug Info Ki = 9000 nM [530954]
Benzo[b]thiophen-2-ylboronic acid Drug Info Ki = 27 nM [529114]
Diisopropyl mercapto(phenyl)methylphosphonate Drug Info Ki = 16000 nM [530954]
Alpha-Sulfanyl(4-fluorobenzyl)phosphonic acid Drug Info Ki = 18000 nM [530954]
Diisopropyl 2-(sulfanylmethyl)phenylphosphonate Drug Info Ki = 3000 nM [530954]
5-Fluoro-2-sulfanyl-phenylphosphonic acid Drug Info Ki = 4000 nM [530954]
Alpha-Sulfanylpropylphosphonic acid Drug Info Ki = 15000 nM [530954]
Alpha-Sulfanyl(2-methoxybenzyl)phosphonic acid Drug Info Ki = 9000 nM [530954]
Alpha-Sulfanylbenzylphosphonic acid Drug Info Ki = 11000 nM [530954]
Alpha-Sulfanyl(4-chlorobenzyl)phosphonic acid Drug Info Ki = 3800 nM [530954]
Alpha-Sulfanyl(2,4-dichlorobenzyl)phosphonic acid Drug Info Ki = 400 nM [530954]
5-hydroxymethylbenzo[b]thiophen-2-ylboronic acid Drug Info Ki = 43 nM [529114]
Thiophene-2-ylboronic acid Drug Info Ki = 2500 nM [529114]
4-Methyl-3-(2-oxo-azetidin-1-yl)-benzoic acid Drug Info Ki = 10000 nM [533436]
5-methyl-benzo[b]thiophen-2-ylboronic acid Drug Info Ki = 30 nM [529114]
References
Ref 552352Effect of D240G substitution in a novel ESBL CTX-M-27. J Antimicrob Chemother. 2003 Jul;52(1):29-35. Epub 2003 May 29.
Ref 552899In vitro activity of LK-157, a novel tricyclic carbapenem as broad-spectrum {beta}-lactamase inhibitor. Antimicrob Agents Chemother. 2009 Feb;53(2):505-11. doi: 10.1128/AAC.00085-08. Epub 2008 Dec 15.
Ref 530954J Med Chem. 2010 Jul 8;53(13):4862-76.Mercaptophosphonate compounds as broad-spectrum inhibitors of the metallo-beta-lactamases.
Ref 530954J Med Chem. 2010 Jul 8;53(13):4862-76.Mercaptophosphonate compounds as broad-spectrum inhibitors of the metallo-beta-lactamases.
Ref 530954J Med Chem. 2010 Jul 8;53(13):4862-76.Mercaptophosphonate compounds as broad-spectrum inhibitors of the metallo-beta-lactamases.
Ref 530954J Med Chem. 2010 Jul 8;53(13):4862-76.Mercaptophosphonate compounds as broad-spectrum inhibitors of the metallo-beta-lactamases.
Ref 529114J Med Chem. 2007 Nov 15;50(23):5644-54. Epub 2007 Oct 23.Optimizing cell permeation of an antibiotic resistance inhibitor for improved efficacy.
Ref 530954J Med Chem. 2010 Jul 8;53(13):4862-76.Mercaptophosphonate compounds as broad-spectrum inhibitors of the metallo-beta-lactamases.
Ref 530954J Med Chem. 2010 Jul 8;53(13):4862-76.Mercaptophosphonate compounds as broad-spectrum inhibitors of the metallo-beta-lactamases.
Ref 530954J Med Chem. 2010 Jul 8;53(13):4862-76.Mercaptophosphonate compounds as broad-spectrum inhibitors of the metallo-beta-lactamases.
Ref 530954J Med Chem. 2010 Jul 8;53(13):4862-76.Mercaptophosphonate compounds as broad-spectrum inhibitors of the metallo-beta-lactamases.
Ref 530954J Med Chem. 2010 Jul 8;53(13):4862-76.Mercaptophosphonate compounds as broad-spectrum inhibitors of the metallo-beta-lactamases.
Ref 530954J Med Chem. 2010 Jul 8;53(13):4862-76.Mercaptophosphonate compounds as broad-spectrum inhibitors of the metallo-beta-lactamases.
Ref 530954J Med Chem. 2010 Jul 8;53(13):4862-76.Mercaptophosphonate compounds as broad-spectrum inhibitors of the metallo-beta-lactamases.
Ref 530954J Med Chem. 2010 Jul 8;53(13):4862-76.Mercaptophosphonate compounds as broad-spectrum inhibitors of the metallo-beta-lactamases.
Ref 530954J Med Chem. 2010 Jul 8;53(13):4862-76.Mercaptophosphonate compounds as broad-spectrum inhibitors of the metallo-beta-lactamases.
Ref 529114J Med Chem. 2007 Nov 15;50(23):5644-54. Epub 2007 Oct 23.Optimizing cell permeation of an antibiotic resistance inhibitor for improved efficacy.
Ref 529114J Med Chem. 2007 Nov 15;50(23):5644-54. Epub 2007 Oct 23.Optimizing cell permeation of an antibiotic resistance inhibitor for improved efficacy.
Ref 533436J Med Chem. 1988 Feb;31(2):370-4.N-aryl 3-halogenated azetidin-2-ones and benzocarbacephems, inhibitors of beta-lactamases.
Ref 529114J Med Chem. 2007 Nov 15;50(23):5644-54. Epub 2007 Oct 23.Optimizing cell permeation of an antibiotic resistance inhibitor for improved efficacy.

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