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Literature summary for 3.6.1.23 extracted from

  • Miyakoshi, H.; Miyahara, S.; Yokogawa, T.; Chong, K.T.; Taguchi, J.; Endoh, K.; Yano, W.; Wakasa, T.; Ueno, H.; Takao, Y.; Nomura, M.; Shuto, S.; Nagasawa, H.; Fukuoka, M.
    Synthesis and discovery of N-carbonylpyrrolidine- or N-sulfonylpyrrolidine-containing uracil derivatives as potent human deoxyuridine triphosphatase inhibitors (2012), J. Med. Chem., 55, 2960-2969.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(R)-1-(3-(2-(hydroxydiphenylmethyl)-pyrrolidin-1-ylsulfonyl)propyl)pyrimidine-2,4(1H,3H)-dione
-
Homo sapiens
(R)-1-(4-(2-(hydroxydiphenylmethyl)-pyrrolidin-1-yl)-4-oxobutyl)pyrimidine-2,4(1H,3H)-dione
-
Homo sapiens
(S)-1-(4-(2-(hydroxydiphenylmethyl)-pyrrolidin-1-yl)-4-oxobutyl)pyrimidine-2,4(1H,3H)-dione
-
Homo sapiens
1-(3-[[(2S)-2-[hydroxy[bis(2-methoxyphenyl)]methyl]pyrrolidin-1-yl]sulfonyl]propyl)pyrimidine-2,4(1H,3H)-dione
-
Homo sapiens
1-(3-[[(2S)-2-[hydroxy[bis(3-methoxyphenyl)]methyl]pyrrolidin-1-yl]sulfonyl]propyl)pyrimidine-2,4(1H,3H)-dione
-
Homo sapiens
1-(4-[(2S)-2-[bis(3-chlorophenyl)(hydroxy)methyl]pyrrolidin-1-yl]-4-oxobutyl)pyrimidine-2,4(1H,3H)-dione
-
Homo sapiens
1-(4-[(2S)-2-[bis(3-fluorophenyl)(hydroxy)methyl]pyrrolidin-1-yl]-4-oxobutyl)pyrimidine-2,4(1H,3H)-dione
-
Homo sapiens
1-(4-[(2S)-2-[bis(4-chlorophenyl)(hydroxy)methyl]pyrrolidin-1-yl]-4-oxobutyl)pyrimidine-2,4(1H,3H)-dione
-
Homo sapiens
1-(4-[(2S)-2-[bis(4-fluorophenyl)(hydroxy)methyl]pyrrolidin-1-yl]-4-oxobutyl)pyrimidine-2,4(1H,3H)-dione
-
Homo sapiens
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
-
Homo sapiens
1-[3-(4-benzylpiperidin-1-yl)-3-oxopropyl]pyrimidine-2,4(1H,3H)-dione
-
Homo sapiens
1-[3-([(2R)-2-[hydroxy(diphenyl)methyl]pyrrolidin-1-yl]sulfonyl)propyl]pyrimidine-2,4(1H,3H)-dione
-
Homo sapiens
1-[3-([(2S)-2-[bis(3-fluorophenyl)(hydroxy)methyl]pyrrolidin-1-yl]sulfonyl)propyl]pyrimidine-2,4(1H,3H)-dione
-
Homo sapiens
1-[3-([(2S)-2-[bis(4-fluorophenyl)(hydroxy)methyl]pyrrolidin-1-yl]sulfonyl)propyl]pyrimidine-2,4(1H,3H)-dione
-
Homo sapiens
1-[3-[(2S)-2-(diphenylmethyl)pyrrolidin-1-yl]-3-oxopropyl]pyrimidine-2,4(1H,3H)-dione
-
Homo sapiens
1-[4-[(2S)-2-(diphenylmethyl)pyrrolidin-1-yl]-4-oxobutyl]pyrimidine-2,4(1H,3H)-dione
-
Homo sapiens
1-[4-[(2S)-2-[bis[2-(benzyloxy)phenyl](hydroxy)methyl]pyrrolidin-1-yl]-4-oxobutyl]pyrimidine-2,4(1H,3H)-dione
-
Homo sapiens
1-[4-[(2S)-2-[bis[3-(benzyloxy)phenyl](hydroxy)methyl]pyrrolidin-1-yl]-4-oxobutyl]pyrimidine-2,4(1H,3H)-dione
-
Homo sapiens
1-[4-[(2S)-2-[bis[4-(benzyloxy)phenyl](hydroxy)methyl]pyrrolidin-1-yl]-4-oxobutyl]pyrimidine-2,4(1H,3H)-dione
-
Homo sapiens
1-[4-[(2S)-2-[hydroxy[di(thiophen-3-yl)]methyl]pyrrolidin-1-yl]-4-oxobutyl]pyrimidine-2,4(1H,3H)-dione
-
Homo sapiens
1-[[2-(trityloxy)ethoxy]methyl]pyrimidine-2,4(1H,3H)-dione
-
Homo sapiens
2'-deoxy-5'-O-trityluridine
-
Homo sapiens
2'-deoxyuridine 5'-(alpha,beta-imido)triphosphate
-
Homo sapiens
3-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(2,4,4-trimethylpentan-2-yl)propanamide
-
Homo sapiens
3-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(2-methylbutan-2-yl)propanamide
-
Homo sapiens
3-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(2-phenylethyl)propanamide
-
Homo sapiens
3-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(3-ethylhexan-3-yl)propanamide
-
Homo sapiens
3-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(3-phenylpropyl)propanamide
-
Homo sapiens
3-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(diphenylmethyl)propanamide
-
Homo sapiens
4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(1-hydroxy-2-methyl-1,1-diphenylpropan-2-yl)butanamide
-
Homo sapiens
4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(1-hydroxy-2-methylpropan-2-yl)butanamide
-
Homo sapiens
4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(2,2-diphenylethyl)-N-methylbutanamide
-
Homo sapiens
4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(2,2-diphenylethyl)butanamide
-
Homo sapiens
4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(2,4,4-trimethylpentan-2-yl)butanamide
-
Homo sapiens
4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(2-hydroxy-2,2-diphenylethyl)-N-methylbutanamide
-
Homo sapiens
4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(2-methyl-1-phenylpropan-2-yl)butanamide
-
Homo sapiens
4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(2-methyl-4-phenylbutan-2-yl)butanamide
-
Homo sapiens
4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(2-phenylpropan-2-yl)butanamide
-
Homo sapiens
4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(3-ethylpentan-3-yl)butanamide
-
Homo sapiens
4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(diphenylmethyl)butanamide
-
Homo sapiens
4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-phenylbutanamide
-
Homo sapiens
4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-[2-methyl-1-(naphthalen-2-yl)propan-2-yl]butanamide
-
Homo sapiens
5'-(P3-benzyl-alpha,beta-methylene)-2'deoxyuridine
-
Homo sapiens
N,N-dibenzyl-3-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)propanamide
-
Homo sapiens
N-benzyl-4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)butanamide
-
Homo sapiens
N-tert-butyl-4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)butanamide
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P33316
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
dUTP + H2O
-
Homo sapiens dUMP + diphosphate
-
?

Synonyms

Synonyms Comment Organism
deoxyuridine triphosphatase
-
Homo sapiens
dUTPase
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00015
-
in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 1-[4-[(2S)-2-(diphenylmethyl)pyrrolidin-1-yl]-4-oxobutyl]pyrimidine-2,4(1H,3H)-dione
0.00023
-
in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 1-[4-[(2S)-2-[hydroxy[di(thiophen-3-yl)]methyl]pyrrolidin-1-yl]-4-oxobutyl]pyrimidine-2,4(1H,3H)-dione
0.00028
-
in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 1-[3-([(2S)-2-[bis(3-fluorophenyl)(hydroxy)methyl]pyrrolidin-1-yl]sulfonyl)propyl]pyrimidine-2,4(1H,3H)-dione
0.00031
-
in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 1-[3-([(2S)-2-[bis(4-fluorophenyl)(hydroxy)methyl]pyrrolidin-1-yl]sulfonyl)propyl]pyrimidine-2,4(1H,3H)-dione
0.00035
-
in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 1-(4-[(2S)-2-[bis(3-fluorophenyl)(hydroxy)methyl]pyrrolidin-1-yl]-4-oxobutyl)pyrimidine-2,4(1H,3H)-dione
0.00058
-
in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 1-(4-[(2S)-2-[bis(3-chlorophenyl)(hydroxy)methyl]pyrrolidin-1-yl]-4-oxobutyl)pyrimidine-2,4(1H,3H)-dione
0.0006
-
in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 1-(4-[(2S)-2-[bis(4-fluorophenyl)(hydroxy)methyl]pyrrolidin-1-yl]-4-oxobutyl)pyrimidine-2,4(1H,3H)-dione
0.001
-
IC50 above 0.001 mM, in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 1-(4-[(2S)-2-[bis(4-chlorophenyl)(hydroxy)methyl]pyrrolidin-1-yl]-4-oxobutyl)pyrimidine-2,4(1H,3H)-dione
0.001
-
IC50 above 0.001 mM, in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 1-[4-[(2S)-2-[bis[2-(benzyloxy)phenyl](hydroxy)methyl]pyrrolidin-1-yl]-4-oxobutyl]pyrimidine-2,4(1H,3H)-dione
0.001
-
IC50 above 0.001 mM, in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 1-[4-[(2S)-2-[bis[3-(benzyloxy)phenyl](hydroxy)methyl]pyrrolidin-1-yl]-4-oxobutyl]pyrimidine-2,4(1H,3H)-dione
0.001
-
IC50 above 0.001 mM, in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 1-[4-[(2S)-2-[bis[4-(benzyloxy)phenyl](hydroxy)methyl]pyrrolidin-1-yl]-4-oxobutyl]pyrimidine-2,4(1H,3H)-dione
0.001
-
IC50 above 0.001 mM, in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 1-[3-[(2S)-2-(diphenylmethyl)pyrrolidin-1-yl]-3-oxopropyl]pyrimidine-2,4(1H,3H)-dione
0.001
-
IC50 above 0.001 mM, in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 1-(3-[[(2S)-2-[hydroxy[bis(2-methoxyphenyl)]methyl]pyrrolidin-1-yl]sulfonyl]propyl)pyrimidine-2,4(1H,3H)-dione
0.001
-
IC50 above 0.001 mM, in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 1-(3-[[(2S)-2-[hydroxy[bis(3-methoxyphenyl)]methyl]pyrrolidin-1-yl]sulfonyl]propyl)pyrimidine-2,4(1H,3H)-dione
0.0011
-
in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(2-hydroxy-2,2-diphenylethyl)-N-methylbutanamide
0.0013
-
in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(2,2-diphenylethyl)-N-methylbutanamide
0.0025
-
in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(1-hydroxy-2-methyl-1,1-diphenylpropan-2-yl)butanamide
0.0073
-
in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 1-[3-(4-benzylpiperidin-1-yl)-3-oxopropyl]pyrimidine-2,4(1H,3H)-dione
0.0094
-
in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 1-[3-([(2R)-2-[hydroxy(diphenyl)methyl]pyrrolidin-1-yl]sulfonyl)propyl]pyrimidine-2,4(1H,3H)-dione
0.01
-
in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens (R)-1-(4-(2-(hydroxydiphenylmethyl)-pyrrolidin-1-yl)-4-oxobutyl)pyrimidine-2,4(1H,3H)-dione
0.015
-
in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 2'-deoxyuridine 5'-(alpha,beta-imido)triphosphate
0.016
-
in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(2,2-diphenylethyl)butanamide
0.021
-
in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(2-methyl-4-phenylbutan-2-yl)butanamide
0.022
-
in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 3-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(3-ethylhexan-3-yl)propanamide
0.03
-
IC50 above 0.03 mM, in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 1-[3-(4-benzylpiperidin-1-yl)-3-oxopropyl]pyrimidine-2,4(1H,3H)-dione
0.03
-
IC50 above 0.03 mM, in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 3-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(2,4,4-trimethylpentan-2-yl)propanamide
0.03
-
IC50 above 0.03 mM, in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 3-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(2-methylbutan-2-yl)propanamide
0.03
-
IC50 above 0.03 mM, in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens N,N-dibenzyl-3-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)propanamide
0.03
-
IC50 above 0.03 mM, in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 3-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(3-phenylpropyl)propanamide
0.03
-
IC50 above 0.03 mM, in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 3-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(diphenylmethyl)propanamide
0.03
-
IC50 above 0.03 mM, in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-phenylbutanamide
0.03
-
IC50 above 0.03 mM, in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens N-benzyl-4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)butanamide
0.03
-
IC50 above 0.03 mM, in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(2-methyl-1-phenylpropan-2-yl)butanamide
0.03
-
IC50 above 0.03 mM, in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(2-phenylpropan-2-yl)butanamide
0.03
-
IC50 above 0.03 mM, in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(diphenylmethyl)butanamide
0.03
-
IC50 above 0.03 mM, in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-[2-methyl-1-(naphthalen-2-yl)propan-2-yl]butanamide
0.03
-
IC50 above 0.03 mM, in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(1-hydroxy-2-methylpropan-2-yl)butanamide
0.03
-
IC50 above 0.03 mM, in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 3-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(2-phenylethyl)propanamide
0.03
-
IC50 above 0.03 mM, in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(3-ethylpentan-3-yl)butanamide
0.03
-
in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-(2,4,4-trimethylpentan-2-yl)butanamide
0.3
-
IC50 above 0.3 mM, in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 1-[[2-(trityloxy)ethoxy]methyl]pyrimidine-2,4(1H,3H)-dione