Target Validation Information
Target ID T59929
Target Name Thymidine phosphorylase
Target Type
Successful
Drug Potency against Target 5-fluoro-6-[(2-aminoimidazol-1-yl)methyl]uracil Drug Info Ki = 17 nM [530697]
6-chloro-5-(2-thienyl)pyrimidine-2,4(1H,3H)-dione Drug Info Ki = 540 nM [529120]
1-benzyl-5'-O-tritylinosine Drug Info IC50 = 11000 nM [528407]
1-(cyclopropyl)methyl-5'-O-tritylinosine Drug Info IC50 = 2300 nM [528407]
5-chloro-6-hydrazinouracil hydrochloride Drug Info IC50 = 4300 nM [527920]
6-fluoro-5-phenylpyrimidine-2,4(1H,3H)-dione Drug Info Ki = 470 nM [529120]
5-butyl-6-chloropyrimidine-2,4(1H,3H)-dione Drug Info Ki = 1650 nM [529120]
5-benzyl-6-chloropyrimidine-2,4(1H,3H)-dione Drug Info Ki = 4550 nM [529120]
6-chloro-5-pentylpyrimidine-2,4(1H,3H)-dione Drug Info Ki = 3090 nM [529120]
6-chloro-5-hexylpyrimidine-2,4(1H,3H)-dione Drug Info Ki = 1790 nM [529120]
6-chloro-5-heptylpyrimidine-2,4(1H,3H)-dione Drug Info Ki = 1600 nM [529120]
6-chloro-5-propylpyrimidine-2,4(1H,3H)-dione Drug Info Ki = 4020 nM [529120]
1-(cyclohexyl)methyl-5'-O-tritylinosine Drug Info IC50 = 4400 nM [528407]
1-propyl-5'-O-tritylinosine Drug Info IC50 = 13000 nM [528407]
6-amino-5-bromouracil Drug Info IC50 = 6800 nM [529048]
5-bromo-6-(cyclopropylamino)uracil hydrochloride Drug Info IC50 = 7400 nM [527920]
5-bromo-6-hydrazinouracil hydrochloride Drug Info IC50 = 4300 nM [527920]
6-bromo-5-phenylpyrimidine-2,4(1H,3H)-dione Drug Info Ki = 1210 nM [529120]
6-chloro-5-phenylpyrimidine-2,4(1H,3H)-dione Drug Info Ki = 430 nM [529120]
6-amino-5-chlorouracil hydrochloride Drug Info IC50 = 8300 nM [527920]
1-allyl-5'-O-tritylinosine Drug Info IC50 = 11000 nM [528407]
References
Ref 530697Bioorg Med Chem Lett. 2010 Mar 1;20(5):1648-51. Epub 2010 Jan 21.The role of phosphate in the action of thymidine phosphorylase inhibitors: Implications for the catalytic mechanism.
Ref 529120J Med Chem. 2007 Nov 29;50(24):6016-23. Epub 2007 Oct 27.Discovery of 5-substituted-6-chlorouracils as efficient inhibitors of human thymidine phosphorylase.
Ref 528407J Med Chem. 2006 Sep 7;49(18):5562-70.5'-O-tritylinosine and analogues as allosteric inhibitors of human thymidine phosphorylase.
Ref 528407J Med Chem. 2006 Sep 7;49(18):5562-70.5'-O-tritylinosine and analogues as allosteric inhibitors of human thymidine phosphorylase.
Ref 527920Bioorg Med Chem Lett. 2006 Mar 1;16(5):1335-7. Epub 2005 Dec 5.Design and synthesis of novel 5,6-disubstituted uracil derivatives as potent inhibitors of thymidine phosphorylase.
Ref 529120J Med Chem. 2007 Nov 29;50(24):6016-23. Epub 2007 Oct 27.Discovery of 5-substituted-6-chlorouracils as efficient inhibitors of human thymidine phosphorylase.
Ref 529120J Med Chem. 2007 Nov 29;50(24):6016-23. Epub 2007 Oct 27.Discovery of 5-substituted-6-chlorouracils as efficient inhibitors of human thymidine phosphorylase.
Ref 529120J Med Chem. 2007 Nov 29;50(24):6016-23. Epub 2007 Oct 27.Discovery of 5-substituted-6-chlorouracils as efficient inhibitors of human thymidine phosphorylase.
Ref 529120J Med Chem. 2007 Nov 29;50(24):6016-23. Epub 2007 Oct 27.Discovery of 5-substituted-6-chlorouracils as efficient inhibitors of human thymidine phosphorylase.
Ref 529120J Med Chem. 2007 Nov 29;50(24):6016-23. Epub 2007 Oct 27.Discovery of 5-substituted-6-chlorouracils as efficient inhibitors of human thymidine phosphorylase.
Ref 529120J Med Chem. 2007 Nov 29;50(24):6016-23. Epub 2007 Oct 27.Discovery of 5-substituted-6-chlorouracils as efficient inhibitors of human thymidine phosphorylase.
Ref 529120J Med Chem. 2007 Nov 29;50(24):6016-23. Epub 2007 Oct 27.Discovery of 5-substituted-6-chlorouracils as efficient inhibitors of human thymidine phosphorylase.
Ref 528407J Med Chem. 2006 Sep 7;49(18):5562-70.5'-O-tritylinosine and analogues as allosteric inhibitors of human thymidine phosphorylase.
Ref 528407J Med Chem. 2006 Sep 7;49(18):5562-70.5'-O-tritylinosine and analogues as allosteric inhibitors of human thymidine phosphorylase.
Ref 529048Eur J Med Chem. 2008 Jun;43(6):1248-60. Epub 2007 Aug 6.Xanthine oxidase-activated prodrugs of thymidine phosphorylase inhibitors.
Ref 527920Bioorg Med Chem Lett. 2006 Mar 1;16(5):1335-7. Epub 2005 Dec 5.Design and synthesis of novel 5,6-disubstituted uracil derivatives as potent inhibitors of thymidine phosphorylase.
Ref 527920Bioorg Med Chem Lett. 2006 Mar 1;16(5):1335-7. Epub 2005 Dec 5.Design and synthesis of novel 5,6-disubstituted uracil derivatives as potent inhibitors of thymidine phosphorylase.
Ref 529120J Med Chem. 2007 Nov 29;50(24):6016-23. Epub 2007 Oct 27.Discovery of 5-substituted-6-chlorouracils as efficient inhibitors of human thymidine phosphorylase.
Ref 529120J Med Chem. 2007 Nov 29;50(24):6016-23. Epub 2007 Oct 27.Discovery of 5-substituted-6-chlorouracils as efficient inhibitors of human thymidine phosphorylase.
Ref 527920Bioorg Med Chem Lett. 2006 Mar 1;16(5):1335-7. Epub 2005 Dec 5.Design and synthesis of novel 5,6-disubstituted uracil derivatives as potent inhibitors of thymidine phosphorylase.
Ref 528407J Med Chem. 2006 Sep 7;49(18):5562-70.5'-O-tritylinosine and analogues as allosteric inhibitors of human thymidine phosphorylase.

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