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(E)-3-(2,2-difluoroethoxy)-N-(7-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2-methylhept-5-en-2-yl)benzenesulfonamide
-
(E)-3-(cyclopentyloxy)-N-(7-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2-methylhept-5-en-2-yl)benzenesulfonamide
-
(E)-3-(cyclopropylmethoxy)-N-(7-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2-methylhept-5-en-2-yl)benzenesulfonamide
-
(E)-N-(7-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2-methylhept-5-en-2-yl)-3-methoxybenzenesulfonamide
-
(E)-N-(7-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2-methylhept-5-en-2-yl)benzenesulfonamide
-
(R)-1-(3-(2-(hydroxydiphenylmethyl)-pyrrolidin-1-ylsulfonyl)propyl)pyrimidine-2,4(1H,3H)-dione
-
(R)-1-(4-(2-(hydroxydiphenylmethyl)-pyrrolidin-1-yl)-4-oxobutyl)pyrimidine-2,4(1H,3H)-dione
-
(R)-N-(1-(3-(2,2-difluoroethoxy)phenyl)ethyl)-4-((2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)benzenesulfonamide
-
(R)-N-(1-(3-(cyclopentyloxy)phenyl)ethyl)-4-((2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)benzenesulfonamide
-
(R)-N-(1-(3-(cyclopropylmethoxy)phenyl)ethyl)-4-((2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-benzenesulfonamide
-
(R,E)-N-(1-(3-(2,2-difluoroethoxy)phenyl)ethyl)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)pent-3-ene-1-sulfonamide
-
(R,E)-N-(1-(3-(cyclopentyloxy)phenyl)ethyl)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)pent-3-ene-1-sulfonamide
-
(R,E)-N-(1-(3-(cyclopropylmethoxy)phenyl)ethyl)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)pent-3-ene-1-sulfonamide
-
(S)-1-(4-(2-(hydroxydiphenylmethyl)-pyrrolidin-1-yl)-4-oxobutyl)pyrimidine-2,4(1H,3H)-dione
-
1-(2-amido-4-trityloxybutyl)uracil
-
1-(2-dimethylamido-4-trityloxybutyl)uracil
-
1-(2-morpholinamido-4-trityloxybutyl)uracil
-
1-(3-tert-butyldimethylsilyloxypropyl)uracil
1-(3-triphenylsilyloxypropyl)uracil
1-(3-tritylaminopropyl)uracil
1-(3-trityloxypropyl)uracil
1-(3-[[(2S)-2-[hydroxy[bis(2-methoxyphenyl)]methyl]pyrrolidin-1-yl]sulfonyl]propyl)pyrimidine-2,4(1H,3H)-dione
-
1-(3-[[(2S)-2-[hydroxy[bis(3-methoxyphenyl)]methyl]pyrrolidin-1-yl]sulfonyl]propyl)pyrimidine-2,4(1H,3H)-dione
-
1-(4-[(2S)-2-[bis(3-chlorophenyl)(hydroxy)methyl]pyrrolidin-1-yl]-4-oxobutyl)pyrimidine-2,4(1H,3H)-dione
-
1-(4-[(2S)-2-[bis(3-fluorophenyl)(hydroxy)methyl]pyrrolidin-1-yl]-4-oxobutyl)pyrimidine-2,4(1H,3H)-dione
-
1-(4-[(2S)-2-[bis(4-chlorophenyl)(hydroxy)methyl]pyrrolidin-1-yl]-4-oxobutyl)pyrimidine-2,4(1H,3H)-dione
-
1-(4-[(2S)-2-[bis(4-fluorophenyl)(hydroxy)methyl]pyrrolidin-1-yl]-4-oxobutyl)pyrimidine-2,4(1H,3H)-dione
-
1-(5-triphenylsilyloxypentyl)uracil
1-(5-tritylaminopentyl)uracil
1-(5-trityloxypentyl)uracil
1-[(1E,8E)-5-([[(E)-(3,4-dihydroxy-5-methoxybenzylidene)amino]oxy]methyl)-1-(3,4-dihydroxy-5-methoxyphenyl)-3,7-dioxa-2,8-diazadeca-1,8-dien-10-yl]pyrimidine-2,4(1H,3H)-dione
-
1-[(1Z,8E)-5-([[(E)-(3,4-dihydroxy-5-methoxybenzylidene)amino]oxy]methyl)-1-(3,4-dihydroxy-5-methoxyphenyl)-3,7-dioxa-2,8-diazadeca-1,8-dien-10-yl]pyrimidine-2,4(1H,3H)-dione
-
1-[(2E)-4-(trityloxy)but-2-en-1-yl]pyrimidine-2,4(1H,3H)-dione
-
1-[(2R,5S)-5-([[tert-butyl(diphenyl)silyl]oxy]methyl)-2,5-dihydrofuran-2-yl]pyrimidine-2,4(1H,3H)-dione
-
1-[(2R,5S)-5-[(trityloxy)methyl]-2,5-dihydrofuran-2-yl]pyrimidine-2,4(1H,3H)-dione
-
1-[(E)-4-trityloxy-2-butenyl]uracil
1-[(Z)-4-trityloxy-2-butenyl]uracil
1-[2-(acetamido)-4-(tert-butyldiphenylsilyloxy)butyl]uracil
-
1-[2-(acetamido)-4-(triphenylmethyl)aminobutyl]uracil
-
1-[2-(azidomethyl)-4-(trityloxy)butyl]uracil
1-[2-(carbobenzoxymethyl)-4-(triphenylmethyl)aminobutyl]uracil
-
1-[2-(carboethoxyethylamido)-4-trityloxybutyl]uracil
-
1-[2-(carboxy)-4-(tert-butyldiphenylsilyloxy)butyl]uracil
-
1-[2-(carboxy)-4-(triphenylmethyl)aminobutyl]uracil
-
1-[2-(carboxyethylamido)-4-trityloxybutyl]uracil
-
1-[2-(diethylamido)-4-(tert-butyldiphenylsilyloxy)butyl]uracil
-
1-[2-(ethylamido)-4-(tert-butyldiphenylsilyloxy) butyl]uracil
-
1-[2-(hydroxyethylamido)-4-trityloxybutyl]uracil
-
1-[2-(hydroxymethyl)-4-(trityloxy)butyl]uracil
1-[2-(methoxyethylamido)-4-trityloxybutyl]uracil
-
1-[2-(methylamido)-4-(tert-butyldiphenylsilyloxy)butyl]uracil
-
1-[2-(N,N-dimethylaminoethylamido)-4-trityloxybutyl]uracil
-
1-[2-(N-benzyloxycarbonylpiperazinamido)-4-(tert-butyldiphenylsilyloxy)butyl]uracil
-
1-[2-(N-methylpiperazine)amido-4-trityloxybutyl]uracil
-
1-[2-(tert-butyldiphenylsilyloxyethylamido)-4-trityloxybutyl]uracil
-
1-[2-(trityloxy)ethoxymethyl]uracil
1-[3-(4-benzylpiperidin-1-yl)-3-oxopropyl]pyrimidine-2,4(1H,3H)-dione
-
1-[3-(benzhydrylaminocarbonyl)propyl]uracil
-
1429fold selectivity over human enzyme
1-[3-(tritylamino)propyl]pyrimidine-2,4(1H,3H)-dione
-
1-[3-(tritylaminocarbonyl)propyl]uracil
-
4545fold selectivity over human enzyme
1-[3-([(2R)-2-[hydroxy(diphenyl)methyl]pyrrolidin-1-yl]sulfonyl)propyl]pyrimidine-2,4(1H,3H)-dione
-
1-[3-([(2S)-2-[bis(3-fluorophenyl)(hydroxy)methyl]pyrrolidin-1-yl]sulfonyl)propyl]pyrimidine-2,4(1H,3H)-dione
-
1-[3-([(2S)-2-[bis(4-fluorophenyl)(hydroxy)methyl]pyrrolidin-1-yl]sulfonyl)propyl]pyrimidine-2,4(1H,3H)-dione
-
1-[3-[(2S)-2-(diphenylmethyl)pyrrolidin-1-yl]-3-oxopropyl]pyrimidine-2,4(1H,3H)-dione
-
1-[4-(tert-butoxycarbonylamino)-3-(trityloxymethyl)butyl]uracil
1-[4-acetoxy-3-(tritylaminomethyl)butyl]uracil
1-[4-hydroxy-2-(trityloxymethyl)butyl]uracil
1-[4-hydroxy-3-(tritylaminomethyl)butyl]uracil
1-[4-hydroxy-3-[(tritylamino)methyl]butyl]pyrimidine-2,4(1H,3H)-dione
-
1-[4-[(2S)-2-(diphenylmethyl)pyrrolidin-1-yl]-4-oxobutyl]pyrimidine-2,4(1H,3H)-dione
-
1-[4-[(2S)-2-[bis[2-(benzyloxy)phenyl](hydroxy)methyl]pyrrolidin-1-yl]-4-oxobutyl]pyrimidine-2,4(1H,3H)-dione
-
1-[4-[(2S)-2-[bis[3-(benzyloxy)phenyl](hydroxy)methyl]pyrrolidin-1-yl]-4-oxobutyl]pyrimidine-2,4(1H,3H)-dione
-
1-[4-[(2S)-2-[bis[4-(benzyloxy)phenyl](hydroxy)methyl]pyrrolidin-1-yl]-4-oxobutyl]pyrimidine-2,4(1H,3H)-dione
-
1-[4-[(2S)-2-[hydroxy[di(thiophen-3-yl)]methyl]pyrrolidin-1-yl]-4-oxobutyl]pyrimidine-2,4(1H,3H)-dione
-
1-[6-(tritylamino)hexyl]pyrimidine-2,4(1H,3H)-dione
-
1-[N-(2-triphenylmethylaminoethyl)-acetamide]uracil
-
-
1-[N-(3-triphenylmethylaminopropyl)-acetamide]uracil
-
-
1-[N-(4-triphenylmethylaminobutyl)-acetamide]uracil
-
-
1-[N-(triphenylmethyl) diaminodi(n-propyl) acetamide]uracil
-
-
1-[N-(triphenylmethylaminoethyl)-N-(aminoethyl) acetamide]uracil
-
-
1-[N-hydroxyethyl-N-(triphenylmethylamino) ethyl-acetamide]uracil
-
-
1-[[2-(trityloxy)ethoxy]methyl]pyrimidine-2,4(1H,3H)-dione
2',3',5'-trideoxy-3'-fluoro-5'-(tritylamino)uridine
-
activity against the parasites with IC50: 0.0053 mM
2',3'-didehydro-2',3'-dideoxyuridine 5'-diphenyl phosphate
2',3'-dideoxy-3'-fluoro-5'-O-trityluridine
2',5'-dideoxy-5'-(tritylamino)uridine
2',5'-dideoxyuridine 5'-N-diphenylphosphoramidate
2'-deoxy-5'-O-(triphenylsilyl)uridine
-
activity against the parasites with IC50: 0.0011 mM
2'-deoxy-5'-O-trityluridine
2'-deoxy-5'-O-[tris(1-methylethoxy)silyl]uridine
-
activity against the parasites with IC50: 0.013 mM
2'-deoxy-5'-phenylmethylaminouracil
-
-
2'-deoxy-5'-triphenylmethanyluracil
-
-
2'-deoxyuracil 5'-diphenyl phosphate
-
-
2'-deoxyuridine
-
competitive inhibition
2'-deoxyuridine 5'-(alpha,beta-imido)triphosphate
3'-azido-2',3'-dideoxy-UTP
-
competitive inhibitor
3'-deoxy-5'-O-(hydroxy{[hydroxy(phosphonooxy)phosphoryl]amino}phosphoryl)uridine
3'-deoxy-5'-O-[hydroxy(phosphonoamino)phosphoryl]uridine
competitive inhibition
3'-O-tert-butyldimethylsilyl-2',5'-dideoxyuridine 5'-N-diphenylphosphoramidate
3'-O-tert-butyldimethylsilyl-5'-O-sulfamoyl-2'-deoxyuridine
3-(2,2-difluoroethoxy)-N-(2-(4-((2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)phenyl)propan-2-yl)-benzenesulfonamide
-
3-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(2,4,4-trimethylpentan-2-yl)propanamide
-
3-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(2-methylbutan-2-yl)propanamide
-
3-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(2-phenylethyl)propanamide
-
3-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(3-ethylhexan-3-yl)propanamide
-
3-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(3-phenylpropyl)propanamide
-
3-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(diphenylmethyl)propanamide
-
3-(cyclopentyloxy)-N-(2-(4-((2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)phenyl)propan-2-yl)-benzenesulfonamide
-
3-(cyclopropylmethoxy)-N-(2-(4-((2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)phenyl)propan-2-yl)-benzenesulfonamide
-
3-(cyclopropylmethoxy)-N-[5-[(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methoxy]-2-methylpentan-2-yl]benzenesulfonamide
-
3-[5-(trityloxy)tetrahydrofuran-2-yl]pyridine-2,6(1H,3H)-dione
-
-
4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(1-hydroxy-2-methyl-1,1-diphenylpropan-2-yl)butanamide
-
4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(1-hydroxy-2-methylpropan-2-yl)butanamide
-
4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(2,2-diphenylethyl)-N-methylbutanamide
-
4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(2,2-diphenylethyl)butanamide
-
4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(2,4,4-trimethylpentan-2-yl)butanamide
-
4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(2-hydroxy-2,2-diphenylethyl)-N-methylbutanamide
-
4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(2-methyl-1-phenylpropan-2-yl)butanamide
-
4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(2-methyl-4-phenylbutan-2-yl)butanamide
-
4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(2-phenylpropan-2-yl)butanamide
-
4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(3-ethylpentan-3-yl)butanamide
-
4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(diphenylmethyl)butanamide
-
4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-phenylbutanamide
-
4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-[2-methyl-1-(naphthalen-2-yl)propan-2-yl]butanamide
-
4-hydroxymercuribenzoate
-
5 mM, complete inhibition
5'-(2,2-dimethyl-1,1-diphenylpropan-1-yl)-2',3'-dideoxyuracil
-
-
5'-(2,2-dimethyl-1,1-diphenylpropan-1-yl)-2'-deoxyuracil
-
-
5'-(2,2-dimethyl-1,1-diphenylpropan-1-yl)-3'-methyl-2',3'-dideoxyuracil
-
-
5'-(2,3,3-trimethylbutan-2-yl)-3'-methyl-2',3'-dideoxyuracil
-
-
5'-(2,4-dimethyl-3-(1-methylethyl)pentan-3-yl)-2'-deoxyuracil
-
-
5'-(P3-benzyl-alpha,beta-methylene)-2'deoxyuridine
-
5'-adamantoyl-3'-methyl-2',3'-dideoxyuracil
-
-
5'-hexadecanoyl-3'-methyl-2',3'-dideoxyuracil
-
-
5'-O-(1-adamantoyl)-2',3'-didehydro-2',3'-dideoxyuridine
5'-O-(4,4'-dimethoxytrityl)-2'-deoxyuridine
-
-
5'-O-sulfamoylcarbamoyl-2',3'-didehydro-2',3'-dideoxyuridine
5'-O-triphenylsilyl-2',3'-didehydro-2',3'-dideoxyuridine
5'-O-triphenylsilyl-2',3'-dideoxy-3'-fluorouridine
5'-O-triphenylsilyl-2'-deoxyuridine
5'-pentanoylamino-2',5'-dideoxyuridine
5'-tert-butyldiphenylsilyloxy-2',3'-dideoxy-3'-fluorouridine
5'-tritylamino-2',5'-dideoxyuridine
5'-tritylamino-3'-fluoro-2',3',5'-trideoxyuridine
5-Aminouracil
-
5 mM, 50% loss of activity
6-aminouracil
-
5 mM, 60% loss of activity
8-azido-ATP
-
competitive
alpha-beta-imido-dUTP
-
competitive, strong inhibition
Ba2+
Spbetavirus SPbeta
-
-
bacteriophage PBS2-induced inhibitor
-
seems to form a high MW complex with the Bacillus subtilis dUTPase, the lower MW enzyme form of dUTPase is not inactivated by the protease inhibitor
-
beta-hydroxyisovalerylshikonin
an ATP-noncompetitive inhibitor of protein tyrosine kinases, induces apoptosis in human lung cancer DMS114 cells through reduction of dUTP nucleotidohydrolase activity, acts synergistically with 5-fluorouracil, overview
bovine serum albumin
38% inhibition at 0.01%
-
Cd2+
Spbetavirus SPbeta
-
-
guanidine hydrochloride
kinetics of GuHCl-induced denaturation of the two dUTPase isozymes at pH 7.5, 4 °C and 1.5-4 M
KCl
-
0.4 mM, 29% loss of activity
Mg2+
-
complete inhibition by extensive dialysis against 0.0125 M MgCl2
N,N-dibenzyl-3-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)propanamide
-
N-(2-(4-((2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-phenyl)propan-2-yl)-3-methoxybenzenesulfonamide
-
N-(2-(4-((2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-phenyl)propan-2-yl)benzenesulfonamide
-
N-benzyl-4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)butanamide
-
N-tert-butyl-4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)butanamide
-
N-[(1R)-1-[3-(cyclopropylmethoxy)-4-fluorophenyl]ethyl]-3-[(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methoxy]propane-1-sulfonamide
-
N-[(1R)-1-[3-(cyclopropylmethoxy)phenyl]ethyl]-3-[(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methoxy]propane-1-sulfonamide
-
N-[(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)acetyl]-D-alanyl-L-tyrosine
-
-
N-[(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)acetyl]-L-alanyl-L-aspartic acid
-
-
N-[(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)acetyl]-L-alanyl-L-glutamic acid
-
-
N-[(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)acetyl]-L-alanyl-L-glutamine
-
-
N-[(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)acetyl]-L-alanyl-L-lysine
-
-
N-[(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)acetyl]-L-alanyl-L-threonine
-
-
N-[(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)acetyl]-L-alanylglycine
-
-
N-[(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)acetyl]glycyl-L-lysine
-
-
N-[(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)acetyl]glycyl-L-threonine
-
-
N-[(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)acetyl]glycyl-L-tyrosine
-
-
N-[(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)acetyl]glycylglycine
-
-
N-[2-[3-(cyclopropylmethoxy)phenyl]propan-2-yl]-3-[(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methoxy]propane-1-sulfonamide
-
N-[3-(tert-butyl diphenyl silanyloxy)-propyl]-2-uracil acetamide
-
-
N-[4-(tert-butyl diphenyl silanyloxy)-butyl]-2-uracil acetamide
-
-
N-[5-[(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methoxy]-2-methylpentan-2-yl]benzenesulfonamide
-
NEM
-
12 mM, 14% loss of activity
siRNAdUT3
a 21 base-pair double-stranded RNA molecule targeted against the motif 3 of the enzyme, time- and dose-dependent decrease in the dUTPase activity in transfected cells
-
staphylococcal repressor protein StlSaPIBov1
-
highly potent inhibitor
-
Stl repressor protein from Staphylococcus aureus
-
-
-
thymidine 5'-(alpha,beta-imido)triphosphate
-
thymidine triphosphate
binding of thymidine triphosphate leads to disordered C-terminal arranged as a lid covering the active site, and the enzyme adapts an inactive conformation as a result of structural changes in the active site, mechanism, overview
1,10-phenanthroline
-
-
1,10-phenanthroline
-
50 mM, 30% inhibition
1-(3-tert-butyldimethylsilyloxypropyl)uracil
-
-
1-(3-tert-butyldimethylsilyloxypropyl)uracil
-
-
1-(3-triphenylsilyloxypropyl)uracil
-
-
1-(3-triphenylsilyloxypropyl)uracil
-
-
1-(3-tritylaminopropyl)uracil
-
-
1-(3-tritylaminopropyl)uracil
-
-
1-(3-trityloxypropyl)uracil
-
-
1-(3-trityloxypropyl)uracil
-
-
1-(5-triphenylsilyloxypentyl)uracil
-
-
1-(5-triphenylsilyloxypentyl)uracil
-
-
1-(5-tritylaminopentyl)uracil
-
-
1-(5-tritylaminopentyl)uracil
-
-
1-(5-trityloxypentyl)uracil
-
-
1-(5-trityloxypentyl)uracil
-
-
1-[(E)-4-trityloxy-2-butenyl]uracil
-
-
1-[(E)-4-trityloxy-2-butenyl]uracil
-
-
1-[(Z)-4-trityloxy-2-butenyl]uracil
-
-
1-[(Z)-4-trityloxy-2-butenyl]uracil
-
-
1-[2-(azidomethyl)-4-(trityloxy)butyl]uracil
-
-
1-[2-(azidomethyl)-4-(trityloxy)butyl]uracil
-
-
1-[2-(hydroxymethyl)-4-(trityloxy)butyl]uracil
-
-
1-[2-(hydroxymethyl)-4-(trityloxy)butyl]uracil
-
-
1-[2-(trityloxy)ethoxymethyl]uracil
-
-
1-[2-(trityloxy)ethoxymethyl]uracil
-
-
1-[4-(tert-butoxycarbonylamino)-3-(trityloxymethyl)butyl]uracil
-
-
1-[4-(tert-butoxycarbonylamino)-3-(trityloxymethyl)butyl]uracil
-
-
1-[4-acetoxy-3-(tritylaminomethyl)butyl]uracil
-
-
1-[4-acetoxy-3-(tritylaminomethyl)butyl]uracil
-
-
1-[4-hydroxy-2-(trityloxymethyl)butyl]uracil
-
-
1-[4-hydroxy-2-(trityloxymethyl)butyl]uracil
-
-
1-[4-hydroxy-3-(tritylaminomethyl)butyl]uracil
-
-
1-[4-hydroxy-3-(tritylaminomethyl)butyl]uracil
-
-
1-[[2-(trityloxy)ethoxy]methyl]pyrimidine-2,4(1H,3H)-dione
-
1-[[2-(trityloxy)ethoxy]methyl]pyrimidine-2,4(1H,3H)-dione
-
-
1-[[2-(trityloxy)ethoxy]methyl]pyrimidine-2,4(1H,3H)-dione
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2',3'-didehydro-2',3'-dideoxyuridine 5'-diphenyl phosphate
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-
2',3'-didehydro-2',3'-dideoxyuridine 5'-diphenyl phosphate
-
-
2',3'-didehydro-2',3'-dideoxyuridine 5'-diphenyl phosphate
-
-
2',3'-didehydro-2',3'-dideoxyuridine 5'-diphenyl phosphate
-
-
2',3'-dideoxy-3'-fluoro-5'-O-trityluridine
-
activity against the parasites with IC50: 0.0020 mM, binding structure involving Tyr112, Ile117, Ile108, and Asn103, overview
2',3'-dideoxy-3'-fluoro-5'-O-trityluridine
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2',5'-dideoxy-5'-(tritylamino)uridine
-
activity against the parasites with IC50: 0.0045 mM
2',5'-dideoxy-5'-(tritylamino)uridine
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2',5'-dideoxyuridine 5'-N-diphenylphosphoramidate
-
-
2',5'-dideoxyuridine 5'-N-diphenylphosphoramidate
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-
2',5'-dideoxyuridine 5'-N-diphenylphosphoramidate
-
-
2',5'-dideoxyuridine 5'-N-diphenylphosphoramidate
-
-
2'-deoxy-5'-O-trityluridine
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2'-deoxy-5'-O-trityluridine
-
activity against the parasites with IC50: 0.006 mM
2'-deoxyuridine 5'-(alpha,beta-imido)triphosphate
-
-
2'-deoxyuridine 5'-(alpha,beta-imido)triphosphate
-
2'-deoxyuridine 5'-(alpha,beta-imido)triphosphate
-
-
2'-deoxyuridine 5'-(alpha,beta-imido)triphosphate
best inhibitor
3'-deoxy-5'-O-(hydroxy{[hydroxy(phosphonooxy)phosphoryl]amino}phosphoryl)uridine
competitive inhibition
3'-deoxy-5'-O-(hydroxy{[hydroxy(phosphonooxy)phosphoryl]amino}phosphoryl)uridine
-
3'-O-tert-butyldimethylsilyl-2',5'-dideoxyuridine 5'-N-diphenylphosphoramidate
-
-
3'-O-tert-butyldimethylsilyl-2',5'-dideoxyuridine 5'-N-diphenylphosphoramidate
-
-
3'-O-tert-butyldimethylsilyl-2',5'-dideoxyuridine 5'-N-diphenylphosphoramidate
-
-
3'-O-tert-butyldimethylsilyl-2',5'-dideoxyuridine 5'-N-diphenylphosphoramidate
-
-
3'-O-tert-butyldimethylsilyl-5'-O-sulfamoyl-2'-deoxyuridine
-
-
3'-O-tert-butyldimethylsilyl-5'-O-sulfamoyl-2'-deoxyuridine
-
-
3'-O-tert-butyldimethylsilyl-5'-O-sulfamoyl-2'-deoxyuridine
-
-
3'-O-tert-butyldimethylsilyl-5'-O-sulfamoyl-2'-deoxyuridine
-
-
5'-O-(1-adamantoyl)-2',3'-didehydro-2',3'-dideoxyuridine
-
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5'-O-(1-adamantoyl)-2',3'-didehydro-2',3'-dideoxyuridine
-
-
5'-O-(1-adamantoyl)-2',3'-didehydro-2',3'-dideoxyuridine
-
-
5'-O-(1-adamantoyl)-2',3'-didehydro-2',3'-dideoxyuridine
-
-
5'-O-sulfamoylcarbamoyl-2',3'-didehydro-2',3'-dideoxyuridine
-
-
5'-O-sulfamoylcarbamoyl-2',3'-didehydro-2',3'-dideoxyuridine
-
-
5'-O-sulfamoylcarbamoyl-2',3'-didehydro-2',3'-dideoxyuridine
-
-
5'-O-sulfamoylcarbamoyl-2',3'-didehydro-2',3'-dideoxyuridine
-
-
5'-O-triphenylsilyl-2',3'-didehydro-2',3'-dideoxyuridine
-
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5'-O-triphenylsilyl-2',3'-didehydro-2',3'-dideoxyuridine
-
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5'-O-triphenylsilyl-2',3'-didehydro-2',3'-dideoxyuridine
-
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5'-O-triphenylsilyl-2',3'-didehydro-2',3'-dideoxyuridine
-
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5'-O-triphenylsilyl-2',3'-dideoxy-3'-fluorouridine
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5'-O-triphenylsilyl-2',3'-dideoxy-3'-fluorouridine
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5'-O-triphenylsilyl-2',3'-dideoxy-3'-fluorouridine
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-
5'-O-triphenylsilyl-2',3'-dideoxy-3'-fluorouridine
-
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5'-O-triphenylsilyl-2'-deoxyuridine
-
-
5'-O-triphenylsilyl-2'-deoxyuridine
-
-
5'-O-triphenylsilyl-2'-deoxyuridine
-
-
5'-O-triphenylsilyl-2'-deoxyuridine
-
-
5'-pentanoylamino-2',5'-dideoxyuridine
-
-
5'-pentanoylamino-2',5'-dideoxyuridine
-
-
5'-pentanoylamino-2',5'-dideoxyuridine
-
-
5'-pentanoylamino-2',5'-dideoxyuridine
-
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5'-tert-butyldiphenylsilyloxy-2',3'-dideoxy-3'-fluorouridine
-
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5'-tert-butyldiphenylsilyloxy-2',3'-dideoxy-3'-fluorouridine
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5'-tert-butyldiphenylsilyloxy-2',3'-dideoxy-3'-fluorouridine
-
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5'-tert-butyldiphenylsilyloxy-2',3'-dideoxy-3'-fluorouridine
-
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5'-tritylamino-2',5'-dideoxyuridine
-
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5'-tritylamino-2',5'-dideoxyuridine
-
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5'-tritylamino-2',5'-dideoxyuridine
-
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5'-tritylamino-2',5'-dideoxyuridine
-
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5'-tritylamino-3'-fluoro-2',3',5'-trideoxyuridine
-
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5'-tritylamino-3'-fluoro-2',3',5'-trideoxyuridine
-
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5'-tritylamino-3'-fluoro-2',3',5'-trideoxyuridine
-
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5'-tritylamino-3'-fluoro-2',3',5'-trideoxyuridine
-
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alpha,beta-imido-dUDP
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potent inhibition
alpha,beta-imido-dUDP
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-
alpha,beta-imido-dUTP
substrate analogue, inhibits the wild-type enzyme, not mutant S72A
alpha,beta-imido-dUTP
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alpha,beta-imido-dUTP
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alpha,beta-imido-dUTP
-
competitive inhibition
Ca2+
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-
Ca2+
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5 mM, 69% inhibition
Ca2+
Spbetavirus SPbeta
-
-
Cu2+
-
0.5 mM, 50% inhibition
dTMP
-
-
dTTP
-
-
dTTP
competitive feedback inhibition
dUDP
-
-
dUDP
-
competitive inhibition
dUMP
-
product inhibition
dUMP
-
product inhibition
dUMP
-
product, competitive inhibition
dUMP
-
product inhibition
dUTP
-
substrate inhibition at higher concentrations
EDTA
-
reversed by Mg2+, Mn2+, Zn2+, Co2+ and Ca2+
EDTA
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1 mM, 65% loss of activity
EDTA
-
2 mM, complete inhibition
EDTA
-
reversed by Mg2+ or Zn2+
EDTA
-
0.5 mM, more than 90% inhibition
EDTA
-
dissociation of the enzyme into its monomeric form
EDTA
-
reversed by Mg2+, Co2+ or Mn2+
EDTA
-
reversed by Co2+ or Mg2+
EDTA
-
causes a 105fold decrease and a 12fold increase of the kcat and Km values for dUTP hydrolysis, respectively, compared to the dUTP-Mg2+ complex
EDTA
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1 mM, 91% inhibition
EDTA
less than 10% residual activity at 1 mM
EDTA
-
reversed by Mg2+, Mn2+ or Zn2+
EGTA
-
-
EGTA
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10 mM, more than 90% inhibition
fluorodeoxy-UMP
-
-
Hg2+
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10 mM HgCl2, 50% inhibition in absence of mercaptoethanol
Mn2+
-
-
Mn2+
-
5 mM, 26% inhibition
Stl protein
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-
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Uracil
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5 mM, 30% loss of activity
Zn2+
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-
Zn2+
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5 mM, 23% inhibition
additional information
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several dUMP analogues with substituents at the 3'- or 5'-positions show poor inhibitory activity
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additional information
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the enzyme possesses a specific tryptic cleavage site Arg132-Ile133 20 A far from the active site of the enzyme, the enzyme is protected against tryptic digestion by binding alpha,beta-imino-dUTP which induces an allosteric conformational change within the central threefold channel of the homotrimer
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additional information
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the enzyme is not inhibited by 3'-azido-2',3'-dideoxy-UTP
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additional information
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binding of alpha,beta-imino-dUTP does not induce allosteric conformational changes and does not protect the enzyme against tryptic digestion
-
additional information
the wild type enzyme is not inhibited by staphylococcal repressor StlSaPIbov1 protein
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additional information
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the wild type enzyme is not inhibited by staphylococcal repressor StlSaPIbov1 protein
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additional information
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inhibitor in vivo activity against the parasite, overview
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additional information
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programmed cell death protein 4 downregulates dUTPase in certain cell types, overview
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additional information
-
enzyme inhibitor development by high-throughput screening of triskelion libraries, a uracil-aldehyde ligand is covalently tethered to one position of a trivalent alkyloxyamine linker via an oxime linkage, and then the vacant linker positions are derivatized with a library of aldehydes, screening of triskelion oximes for inhibitory potency, overview
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additional information
-
the enzyme is not inhibited by 3'-azido-2',3'-dideoxy-UTP
-
additional information
-
inhibitor in vivo activity against the parasite, overview
-
additional information
-
diphosphate has no effect on activity
-
additional information
-
inhibitor in vivo activity against the parasite, overview
-
additional information
fast screening for binding of potential inhibitors to the active site
-
additional information
-
fast screening for binding of potential inhibitors to the active site
-
additional information
-
no inhibition by dTTp, dGTP, dATP, and dCTP
-
additional information
-
inhibitor in vivo activity against the parasite, overview
-
additional information
-
growth inhibition potency in vitro, overview, molecular docking modeling study
-
additional information
-
design and synthesis of tert-butyl diphenyl silyl uracil acetamides inhibitors, molecular modelling, overview
-
additional information
-
computational docking of small molecules structures to the enzyme for inhibitor development, overview
-