Target Validation Information
TTD ID	T07137
Target Name	Hydroxyphenylpyruvate dioxygenase (HPD)
Type of Target	Successful
Drug Potency against Target	Nitisinone	Drug Info	IC50 = 40 nM	[1]
	(4-Hydroxy-phenoxy)-acetic acid	Drug Info	IC50 = 6000 nM	[2]
	2-(2-Bromo-benzoyl)-cyclohexane-1,3-dione	Drug Info	IC50 = 560 nM	[1]
	2-(2-Chloro-benzoyl)-cyclohexane-1,3-dione	Drug Info	IC50 = 500 nM	[1]
	2-(2-Iodo-benzoyl)-cyclohexane-1,3-dione	Drug Info	IC50 = 760 nM	[1]
	2-(2-Methoxy-benzoyl)-cyclohexane-1,3-dione	Drug Info	IC50 = 11700 nM	[1]
	2-(2-Methyl-benzoyl)-cyclohexane-1,3-dione	Drug Info	IC50 = 3750 nM	[1]
	2-(2-Nitro-benzoyl)-cyclohexane-1,3-dione	Drug Info	IC50 = 160 nM	[1]
	2-acetyl-3-hydroxycyclohex-2-enone	Drug Info	IC50 = 11200 nM	[3]
	2-Acetyl-cyclohexane-1,3-dione	Drug Info	IC50 = 11200 nM	[1]
	2-Cyclopropanecarbonyl-cyclohexane-1,3-dione	Drug Info	IC50 = 6000 nM	[1]
	2-Propionyl-cyclohexane-1,3-dione	Drug Info	IC50 = 17800 nM	[1]
	3-hydroxy-2-propionylcyclohex-2-enone	Drug Info	IC50 = 17800 nM	[3]
	3-Hydroxy-4-phenyl-5H-furan-2-one	Drug Info	IC50 = 500 nM	[2]
References
REF 1	SAR studies of 2-o-substituted-benzoyl- and 2-alkanoyl-cyclohexane-1,3-diones as inhibitors of 4-hydroxyphenylpyruvate dioxygenase. Bioorg Med Chem Lett. 2000 May 1;10(9):843-5.
REF 2	Design, synthesis, and evaluation of postulated transient intermediate and substrate analogues as inhibitors of 4-hydroxyphenylpyruvate dioxygenase. Bioorg Med Chem Lett. 2002 Jul 8;12(13):1709-13.
REF 3	Enzyme inhibition potency enhancement by active site metal chelating and hydrogen bonding induced conformation-restricted cyclopropanecarbonyl deri... Bioorg Med Chem Lett. 2006 Dec 1;16(23):6024-7.

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