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Thymidine phosphorylase Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
Tipiracil hydrochlorideIC5035.0 [1]
Tipiracil hydrochlorideKi17.0 [1], 20.0 [2]
6-Amino-5-bromopyrimidine-2,4(1H,3H)-dioneIC506800.0 [1]
6-Amino-5-bromopyrimidine-2,4(1H,3H)-dioneKi2600.0 [1]
TipiracilIC5020.0 [1], 35.0 [2]
TipiracilKi1.3 [1], 2.1 [2], 5.0 [3], 17.0 [4]
7H-Pyrrolo[2,3-d]pyrimidine-2,4-diolIC5040300.0 [1]
5-Bromo-6-[(2-aminoimidazol-1-yl)methyl]uracil hydrochlorideIC501.9 [1], 19.0 [2], 20.0 [3]
[(E)-(1-Methyl-2,5-dioxo-4-pentylimidazolidin-4-yl)methylideneamino]ureaIC5019600.0 [1], 77000.0 [2]
[(E)-(1-Methyl-2,5-dioxo-4-pentylimidazolidin-4-yl)methylideneamino]ureaKi12500000.0 [1], 25000000.0 [2]
5'-O-TritylinosineIC5030000.0 [1], 67000.0 [2]
[(2R,3Ar,4R,6R,6aR)-6-(hydroxymethyl)-4-(5-methyl-2,4-dioxopyrimidin-1-yl)-3a,4,6,6a-tetrahydrofuro[3,4-d][1,3]dioxol-2-yl]methylphosphonic acidKi236.0 [1]
5-Bromo-6-[(2'-nitroimidazol-1'-yl)methyl]uracilIC5024400.0 [1], 160000.0 [2]
2,4(1H,3H)-Pyrimidinedione, 6-[(2-nitro-1H-imidazol-1-yl)methyl]-IC501600.0 [1], 257700.0 [2]
5-Chloro-6-(2-nitro-imidazol-1-ylmethyl)-1H-pyrimidine-2,4-dioneIC5021700.0 [1], 115000.0 [2]
6-Chloro-5-(cyclopent-1-en-1-yl)-1,2,3,4-tetrahydropyrimidine-2,4-dioneKi200.0 [1], 290.0 [2]
2,4(1H,3H)-Pyrimidinedione, 6-[(2-phenylethyl)amino]-IC50148000.0 [1], 200000.0 [2]
6-[(3-Phenylpropyl)amino]uracilIC5082000.0 [1], 125000.0 [2]
6-(4-Phenylbutylamino)uracilIC5030000.0 [1], 74000.0 [2]
2-(4-Bromo-3-methylphenyl)-5-sulfanylidene-1H-[1,2,4]triazolo[1,5-a][1,3,5]triazin-7-oneIC5013090.0 [1]
1-(8-Phosphonooctyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4(1H,3H)-dioneIC507300.0 [1], 15100.0 [2]
6-Chloro-5-propylpyrimidine-2,4(1H,3H)-dioneKi4020.0 [1], 5810.0 [2]
6-[(2-Amino-1H-imidazol-3-ium-3-yl)methyl]-1H-pyrimidine-2,4-dioneIC50100.0 [1], 560.0 [2]
6-Chloro-5-ethyluracilKi20000.0 [1]
6-Methyl-5-phenyl-2,4(1H,3H)-pyrimidinedioneKi20000.0 [1]
5-Butyl-6-chloropyrimidine-2,4(1H,3H)-dioneKi1030.0 [1], 1650.0 [2]
6-Chloro-5-pentyl-1,2,3,4-tetrahydropyrimidine-2,4-dioneKi3090.0 [1], 3670.0 [2]
6-Chloro-5-hexyl-1,2,3,4-tetrahydropyrimidine-2,4-dioneKi1790.0 [1], 1830.0 [2]
6-Chloro-5-heptyl-1,2,3,4-tetrahydropyrimidine-2,4-dioneKi1060.0 [1], 1600.0 [2]
5-Benzyl-6-chloropyrimidine-2,4(1H,3H)-dioneKi4550.0 [1], 4650.0 [2]
6-Chloro-5-(cyclohex-1-en-1-yl)-1,2,3,4-tetrahydropyrimidine-2,4-dioneKi420.0 [1], 750.0 [2]
6-Chloro-5-(prop-1-en-2-yl)-1,2,3,4-tetrahydropyrimidine-2,4-dioneKi3340.0 [1], 5100.0 [2]
6-Chloro-5-[(2E)-pent-2-en-3-yl]-1,2,3,4-tetrahydropyrimidine-2,4-dioneKi490.0 [1], 910.0 [2]
6-Chloro-5-phenylpyrimidine-2,4(1H,3H)-dioneKi400.0 [1], 430.0 [2]
6-Chloro-5-(3,5-dimethylphenyl)-1,2,3,4-tetrahydropyrimidine-2,4-dioneKi1270.0 [1], 1740.0 [2]
6-Chloro-5-(naphthalen-1-yl)-1,2,3,4-tetrahydropyrimidine-2,4-dioneKi3940.0 [1], 4590.0 [2]
6-Chloro-5-(4-fluorophenyl)-1,2,3,4-tetrahydropyrimidine-2,4-dioneKi710.0 [1], 970.0 [2]
6-Chloro-5-(2-thienyl)pyrimidine-2,4(1H,3H)-dioneKi280.0 [1], 540.0 [2]
6-Chloro-5-[(1E)-prop-1-en-1-yl]-1,2,3,4-tetrahydropyrimidine-2,4-dioneKi1170.0 [1], 1210.0 [2]
5-[(1E)-But-1-en-1-yl]-6-chloro-1,2,3,4-tetrahydropyrimidine-2,4-dioneKi630.0 [1], 920.0 [2]
6-Chloro-5-[(1E)-pent-1-en-1-yl]-1,2,3,4-tetrahydropyrimidine-2,4-dioneKi410.0 [1], 910.0 [2]
6-Fluoro-5-phenyl-1,2,3,4-tetrahydropyrimidine-2,4-dioneKi470.0 [1], 500.0 [2]
6-Bromo-5-phenyl-1,2,3,4-tetrahydropyrimidine-2,4-dioneKi1210.0 [1]
5-Phenyl-6-(pyrrolidin-1-yl)-1,2,3,4-tetrahydropyrimidine-2,4-dioneKi20000.0 [1]
6-[(2-Aminoethyl)amino]-5-phenyl-1,2,3,4-tetrahydropyrimidine-2,4-dioneKi20000.0 [1]
6-Chloro-5-pyridin-3-yl-1H-pyrimidine-2,4-dione;hydrochlorideKi3010.0 [1], 3990.0 [2]
5-Bromo-6-[2-[(5-bromo-2,4-dioxo-1H-pyrimidin-6-yl)amino]ethylamino]-1H-pyrimidine-2,4-dione;dihydrochlorideIC502200.0 [1], 3400.0 [2]
5-Bromo-6-[4-(hydroxymethyl)piperidin-1-yl]-1H-pyrimidine-2,4-dione;hydrochlorideIC506000.0 [1], 7500.0 [2]
5-Bromo-6-[3-(hydroxymethyl)piperidin-1-yl]-1H-pyrimidine-2,4-dione;hydrochlorideIC505000.0 [1], 5200.0 [2]
5-Chloro-6-[4-(2-hydroxyethyl)piperidin-1-yl]-1H-pyrimidine-2,4-dione;hydrochlorideIC507500.0 [1], 9000.0 [2]
5-Bromo-6-[2-(hydroxymethyl)piperidin-1-yl]-1H-pyrimidine-2,4-dione;hydrochlorideIC506000.0 [1], 7000.0 [2]
5-Chloro-6-[3-(hydroxymethyl)piperidin-1-yl]-1H-pyrimidine-2,4-dione;hydrochlorideIC507400.0 [1], 9000.0 [2]
5-Bromo-6-morpholin-4-yl-1H-pyrimidine-2,4-dione;hydrochlorideIC506500.0 [1], 7200.0 [2]
5-Bromo-6-(cyclopropylamino)-1H-pyrimidine-2,4-dione;hydrochlorideIC507200.0 [1], 7400.0 [2]
6-(Azetidin-1-yl)-5-bromo-1H-pyrimidine-2,4-dione;hydrochlorideIC506300.0 [1], 6800.0 [2]
5-Bromo-6-[4-(2-hydroxyethyl)piperidin-1-yl]-1H-pyrimidine-2,4-dione;hydrochlorideIC504600.0 [1], 5000.0 [2]
5-Chloro-6-hydrazinyl-1H-pyrimidine-2,4-dione;hydrochlorideIC504300.0 [1], 10200.0 [2]
5-Bromo-6-hydrazinyl-1H-pyrimidine-2,4-dione;hydrochlorideIC503800.0 [1], 4300.0 [2]
5-Chloro-6-piperidin-1-yl-1H-pyrimidine-2,4-dione;hydrochlorideIC5012100.0 [1], 15700.0 [2]
6-(Azetidin-1-yl)-5-chloro-1H-pyrimidine-2,4-dione;hydrochlorideIC507000.0 [1], 8000.0 [2]
5-Chloro-6-morpholin-4-yl-1H-pyrimidine-2,4-dione;hydrochlorideIC508000.0 [1], 8300.0 [2]
5-Chloro-6-pyrrolidin-1-yl-1H-pyrimidine-2,4-dione;hydrochlorideIC507400.0 [1], 9500.0 [2]
5-Bromo-6-piperidin-1-yl-1H-pyrimidine-2,4-dione;hydrochlorideIC505800.0 [1], 8200.0 [2]
5-Bromo-6-pyrrolidin-1-yl-1H-pyrimidine-2,4-dione;hydrochlorideIC504600.0 [1], 5100.0 [2]
6-Amino-5-chloro-1H-pyrimidine-2,4-dione;hydrochlorideIC508300.0 [1], 11600.0 [2]
5-Bromo-6-[4-(5-bromo-2,4-dioxo-1H-pyrimidin-6-yl)piperazin-1-yl]-1H-pyrimidine-2,4-dione;dihydrochlorideIC503600.0 [1], 4000.0 [2]
5-Chloro-6-(cyclopropylamino)-1H-pyrimidine-2,4-dione;hydrochlorideIC506000.0 [1], 7000.0 [2]
5-Chloro-6-[2-(hydroxymethyl)piperidin-1-yl]-1H-pyrimidine-2,4-dione;hydrochlorideIC508000.0 [1], 8800.0 [2]
5-Chloro-6-[4-(5-chloro-2,4-dioxo-1H-pyrimidin-6-yl)piperazin-1-yl]-1H-pyrimidine-2,4-dione;dihydrochlorideIC503800.0 [1], 7200.0 [2]
8-(2,4-Dioxo-6H-pyrrolo[3,4-d]pyrimidin-1-yl)octylphosphonic acidIC5017000.0 [1], 27000.0 [2]
2-[(3,4-Dichlorophenyl)methyl]-5-sulfanylidene-1H-[1,2,4]triazolo[1,5-a][1,3,5]triazin-7-oneIC502950.0 [1]
2-[(3,4-Dichlorophenyl)methyl]-5-sulfanylidene-1H-[1,2,4]triazolo[1,5-a][1,3,5]triazin-7-oneKi19570.0 [1]
2-(3,4-Dichlorophenyl)-5-sulfanylidene-1H-[1,2,4]triazolo[1,5-a][1,3,5]triazin-7-oneIC5010840.0 [1]
2-(3,4-Dichlorophenyl)-5-sulfanylidene-1H-[1,2,4]triazolo[1,5-a][1,3,5]triazin-7-oneKi20090.0 [1]
7-(3,4-Dichlorophenyl)-2-sulfanylidene-6H-pyrazolo[1,5-a][1,3,5]triazin-4-oneIC509078.21 [1]
7-(3,4-Dichlorophenyl)-2-sulfanylidene-6H-pyrazolo[1,5-a][1,3,5]triazin-4-oneKi1770.0 [1]
[4-Oxo-2-sulfanylidene-8-[[4-(trifluoromethyl)phenyl]methyl]-6H-pyrazolo[1,5-a][1,3,5]triazin-7-yl]thioureaIC503819.44 [1]
[4-Oxo-2-sulfanylidene-8-[[4-(trifluoromethyl)phenyl]methyl]-6H-pyrazolo[1,5-a][1,3,5]triazin-7-yl]thioureaKi1650.0 [1]
2,6-Dihydroxy-3-cyanopyridineIC50100000.0 [1]
6-AminothymineIC5030000.0 [1]
N-Allyl-N'-[(2,4,6-trioxotetrahydro-5(2H)-pyrimidinylidene)methyl]thioureaIC5094800.0 [1]
6-(Benzylamino)pyrimidine-2,4(1H,3H)-dioneIC50200000.0 [1]
(1-Fluoro-3-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)propan-2-yloxy)methylphosphonic acidKi236.0 [1]
4-(5-Mercapto-1,3,4-oxadiazol-2-yl)phenolIC5038240.0 [1]
2,6-Dihydroxy-4-methyl-3-pyridinecarbonitrileIC50100000.0 [1]
6-Amino-5-chloropyrimidine-2,4(1H,3H)-dioneIC5030000.0 [1]
7-Phenyl-2-thioxo-2,3-dihydropyrazolo[1,5-a][1,3,5]triazin-4(1H)-oneIC5048977.88 [1]
Phosphonic acid, ((2-(3,4-dihydro-5-methyl-2,4-dioxo-1(2H)-pyrimidinyl)ethoxy)methyl)-Ki236.0 [1]
1-(3-Hydroxy-2-phosphonomethoxypropyl)-4-hydroxy-5-methylpyrimidin-2(1H)-oneKi236.0 [1]
7-Tert-butyl-2-sulfanylidene-6H-pyrazolo[1,5-a][1,3,5]triazin-4-oneIC5055718.57 [1]
(E)-3-[2-(3,4-Dichlorophenyl)phenyl]-N-thiophen-2-ylsulfonylprop-2-enamideKi770.0 [1]
9-[(2R,3R,4S,5R)-5-[[(4-Chlorophenyl)-diphenylmethoxy]methyl]-3,4-dihydroxyoxolan-2-yl]-1H-purin-6-oneIC504500.0 [1]
[(2S,3Ar,4S,6R,6aR)-4-(hydroxymethyl)-6-(5-methyl-2,4-dioxopyrimidin-1-yl)-2,3,3a,4,6,6a-hexahydrofuro[2,3-c]furan-2-yl]methylphosphonic acidKi1050.0 [1]
5-Fluoro-6-[(2-aminoimidazol-1-yl)methyl]uracilKi17.0 [1]
1-Benzyl-9-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(phenylmethoxymethyl)oxolan-2-yl]purin-6-oneIC50200000.0 [1]
6-[(2-Amino-1H-imidazol-3-ium-3-yl)methyl]-5-chloro-1H-pyrimidine-2,4-dioneIC5049.0 [1]
6-[(2-Amino-4,5-dihydroimidazol-1-yl)methyl]-5-chloro-1H-pyrimidine-2,4-dione;hydrobromideIC5020.0 [1]
7-(3-Benzylguanidino)-1,2,3,4-tetrahydrothieno[3,2-d]pyrimidine-2,4-dioneKi64300.0 [1]
6-[(2-Amino-1H-imidazol-3-ium-3-yl)methyl]-5-chloro-1H-pyrimidine-2,4-dione;chlorideIC5021.0 [1]
1-Benzoyl-6-methyl-1,2,3,4-tetrahydropyrimidine-2,4-dioneIC5092400.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Thymidine phosphorylase Inhibitors (IC50, Ki)." AAT Bioquest, Inc.8 May2024https://www.aatbio.com/data-sets/thymidine-phosphorylase-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024May 8). Quest Database™ Thymidine phosphorylase Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/thymidine-phosphorylase-inhibitors-ic50-ki.
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