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

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