Target Validation Information
TTD ID	T59929
Target Name	Thymidine phosphorylase (TYMP)
Type of Target	Successful
Drug Potency against Target	1-(cyclohexyl)methyl-5'-O-tritylinosine	Drug Info	IC50 = 4400 nM	[2]
	1-(cyclopropyl)methyl-5'-O-tritylinosine	Drug Info	IC50 = 2300 nM	[2]
	1-allyl-5'-O-tritylinosine	Drug Info	IC50 = 11000 nM	[2]
	1-benzyl-5'-O-tritylinosine	Drug Info	IC50 = 11000 nM	[2]
	1-propyl-5'-O-tritylinosine	Drug Info	IC50 = 13000 nM	[2]
	5-benzyl-6-chloropyrimidine-2,4(1H,3H)-dione	Drug Info	Ki = 4550 nM	[4]
	5-bromo-6-(cyclopropylamino)uracil hydrochloride	Drug Info	IC50 = 7400 nM	[1]
	5-bromo-6-hydrazinouracil hydrochloride	Drug Info	IC50 = 4300 nM	[1]
	5-butyl-6-chloropyrimidine-2,4(1H,3H)-dione	Drug Info	Ki = 1650 nM	[4]
	5-chloro-6-hydrazinouracil hydrochloride	Drug Info	IC50 = 4300 nM	[1]
	5-fluoro-6-[(2-aminoimidazol-1-yl)methyl]uracil	Drug Info	Ki = 17 nM	[5]
	6-amino-5-bromouracil	Drug Info	IC50 = 6800 nM	[3]
	6-amino-5-chlorouracil hydrochloride	Drug Info	IC50 = 8300 nM	[1]
	6-bromo-5-phenylpyrimidine-2,4(1H,3H)-dione	Drug Info	Ki = 1210 nM	[4]
	6-chloro-5-(2-thienyl)pyrimidine-2,4(1H,3H)-dione	Drug Info	Ki = 540 nM	[4]
	6-chloro-5-heptylpyrimidine-2,4(1H,3H)-dione	Drug Info	Ki = 1600 nM	[4]
	6-chloro-5-hexylpyrimidine-2,4(1H,3H)-dione	Drug Info	Ki = 1790 nM	[4]
	6-chloro-5-pentylpyrimidine-2,4(1H,3H)-dione	Drug Info	Ki = 3090 nM	[4]
	6-chloro-5-phenylpyrimidine-2,4(1H,3H)-dione	Drug Info	Ki = 430 nM	[4]
	6-chloro-5-propylpyrimidine-2,4(1H,3H)-dione	Drug Info	Ki = 4020 nM	[4]
	6-fluoro-5-phenylpyrimidine-2,4(1H,3H)-dione	Drug Info	Ki = 470 nM	[4]
References
REF 1	Design and synthesis of novel 5,6-disubstituted uracil derivatives as potent inhibitors of thymidine phosphorylase. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1335-7.
REF 2	5'-O-tritylinosine and analogues as allosteric inhibitors of human thymidine phosphorylase. J Med Chem. 2006 Sep 7;49(18):5562-70.
REF 3	Xanthine oxidase-activated prodrugs of thymidine phosphorylase inhibitors. Eur J Med Chem. 2008 Jun;43(6):1248-60.
REF 4	Discovery of 5-substituted-6-chlorouracils as efficient inhibitors of human thymidine phosphorylase. J Med Chem. 2007 Nov 29;50(24):6016-23.
REF 5	The role of phosphate in the action of thymidine phosphorylase inhibitors: Implications for the catalytic mechanism. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1648-51.

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