Target Validation Information
Target ID T07137
Target Name 4-hydroxyphenylpyruvate dioxygenase
Target Type
Successful
Drug Potency against Target 2-(2-Methyl-benzoyl)-cyclohexane-1,3-dione Drug Info IC50 = 3750 nM [525791]
Nitisinone Drug Info IC50 = 40 nM [525791]
2-(2-Chloro-benzoyl)-cyclohexane-1,3-dione Drug Info IC50 = 500 nM [525791]
2-(2-Nitro-benzoyl)-cyclohexane-1,3-dione Drug Info IC50 = 160 nM [525791]
2-Cyclopropanecarbonyl-cyclohexane-1,3-dione Drug Info IC50 = 6000 nM [525791]
2-(2-Iodo-benzoyl)-cyclohexane-1,3-dione Drug Info IC50 = 760 nM [525791]
2-(2-Bromo-benzoyl)-cyclohexane-1,3-dione Drug Info IC50 = 560 nM [525791]
2-Propionyl-cyclohexane-1,3-dione Drug Info IC50 = 17800 nM [525791]
2-acetyl-3-hydroxycyclohex-2-enone Drug Info IC50 = 11200 nM [528436]
3-hydroxy-2-propionylcyclohex-2-enone Drug Info IC50 = 17800 nM [528436]
2-(2-Methoxy-benzoyl)-cyclohexane-1,3-dione Drug Info IC50 = 11700 nM [525791]
2-Acetyl-cyclohexane-1,3-dione Drug Info IC50 = 11200 nM [525791]
(4-Hydroxy-phenoxy)-acetic acid Drug Info IC50 = 6000 nM [526361]
3-Hydroxy-4-phenyl-5H-furan-2-one Drug Info IC50 = 500 nM [526361]
References
Ref 525791Bioorg Med Chem Lett. 2000 May 1;10(9):843-5.SAR studies of 2-o-substituted-benzoyl- and 2-alkanoyl-cyclohexane-1,3-diones as inhibitors of 4-hydroxyphenylpyruvate dioxygenase.
Ref 525791Bioorg Med Chem Lett. 2000 May 1;10(9):843-5.SAR studies of 2-o-substituted-benzoyl- and 2-alkanoyl-cyclohexane-1,3-diones as inhibitors of 4-hydroxyphenylpyruvate dioxygenase.
Ref 525791Bioorg Med Chem Lett. 2000 May 1;10(9):843-5.SAR studies of 2-o-substituted-benzoyl- and 2-alkanoyl-cyclohexane-1,3-diones as inhibitors of 4-hydroxyphenylpyruvate dioxygenase.
Ref 525791Bioorg Med Chem Lett. 2000 May 1;10(9):843-5.SAR studies of 2-o-substituted-benzoyl- and 2-alkanoyl-cyclohexane-1,3-diones as inhibitors of 4-hydroxyphenylpyruvate dioxygenase.
Ref 525791Bioorg Med Chem Lett. 2000 May 1;10(9):843-5.SAR studies of 2-o-substituted-benzoyl- and 2-alkanoyl-cyclohexane-1,3-diones as inhibitors of 4-hydroxyphenylpyruvate dioxygenase.
Ref 525791Bioorg Med Chem Lett. 2000 May 1;10(9):843-5.SAR studies of 2-o-substituted-benzoyl- and 2-alkanoyl-cyclohexane-1,3-diones as inhibitors of 4-hydroxyphenylpyruvate dioxygenase.
Ref 525791Bioorg Med Chem Lett. 2000 May 1;10(9):843-5.SAR studies of 2-o-substituted-benzoyl- and 2-alkanoyl-cyclohexane-1,3-diones as inhibitors of 4-hydroxyphenylpyruvate dioxygenase.
Ref 525791Bioorg Med Chem Lett. 2000 May 1;10(9):843-5.SAR studies of 2-o-substituted-benzoyl- and 2-alkanoyl-cyclohexane-1,3-diones as inhibitors of 4-hydroxyphenylpyruvate dioxygenase.
Ref 528436Bioorg Med Chem Lett. 2006 Dec 1;16(23):6024-7. Epub 2006 Sep 18.Enzyme inhibition potency enhancement by active site metal chelating and hydrogen bonding induced conformation-restricted cyclopropanecarbonyl derivatives.
Ref 528436Bioorg Med Chem Lett. 2006 Dec 1;16(23):6024-7. Epub 2006 Sep 18.Enzyme inhibition potency enhancement by active site metal chelating and hydrogen bonding induced conformation-restricted cyclopropanecarbonyl derivatives.
Ref 525791Bioorg Med Chem Lett. 2000 May 1;10(9):843-5.SAR studies of 2-o-substituted-benzoyl- and 2-alkanoyl-cyclohexane-1,3-diones as inhibitors of 4-hydroxyphenylpyruvate dioxygenase.
Ref 525791Bioorg Med Chem Lett. 2000 May 1;10(9):843-5.SAR studies of 2-o-substituted-benzoyl- and 2-alkanoyl-cyclohexane-1,3-diones as inhibitors of 4-hydroxyphenylpyruvate dioxygenase.
Ref 526361Bioorg Med Chem Lett. 2002 Jul 8;12(13):1709-13.Design, synthesis, and evaluation of postulated transient intermediate and substrate analogues as inhibitors of 4-hydroxyphenylpyruvate dioxygenase.
Ref 526361Bioorg Med Chem Lett. 2002 Jul 8;12(13):1709-13.Design, synthesis, and evaluation of postulated transient intermediate and substrate analogues as inhibitors of 4-hydroxyphenylpyruvate dioxygenase.

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