Target Validation Information
TTD ID	T83391
Target Name	Fructose-1,6-bisphosphatase (FBP)
Type of Target	Clinical trial
Drug Potency against Target	MB07803	Drug Info	IC50 = 21 nM
	1-(2-mercaptoethyl)-3-(m-tolylsulfonyl)urea	Drug Info	IC50 = 10589 nM	[3]
	1-(4-aminophenylsulfonyl)-3-(2-mercaptoethyl)urea	Drug Info	IC50 = 1600 nM	[3]
	2-(4-(4-Hydroxyphenyl)thiazol-2-ylamino)phenol	Drug Info	IC50 = 15000 nM	[4]
	3-(4-(4-Hydroxyphenyl)thiazol-2-ylamino)phenol	Drug Info	IC50 = 13000 nM	[4]
	4-(2-amino-1,3-thiazol-4-yl)phenol	Drug Info	IC50 = 1100 nM	[4]
	N-(5-chlorobenzo[d]oxazol-2-yl)benzenesulfonamide	Drug Info	IC50 = 7700 nM	[2]
Action against Disease Model	MB07803	Drug Info	MB06322 inhibited glucose production from a variety of GNG substrates in rat hepatocytes and from bicarbonate in male Zucker diabetic fatty rats.	[1]
References
REF 1	MB06322 (CS-917): A potent and selective inhibitor of fructose 1,6-bisphosphatase for controlling gluconeogenesis in type 2 diabetes. Proc Natl Acad Sci U S A. 2005 May 31;102(22):7970-5.
REF 2	Benzoxazole benzenesulfonamides as allosteric inhibitors of fructose-1,6-bisphosphatase. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1807-10.
REF 3	Allosteric FBPase inhibitors gain 10(5) times in potency when simultaneously binding two neighboring AMP sites. Bioorg Med Chem Lett. 2008 Aug 15;18(16):4708-12.
REF 4	A library of novel allosteric inhibitors against fructose 1,6-bisphosphatase. Bioorg Med Chem. 2009 Jun 1;17(11):3916-22.

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