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Literature summary extracted from

  • Miyahara, S.; Miyakoshi, H.; Yokogawa, T.; Chong, K.T.; Taguchi, J.; Muto, T.; Endoh, K.; Yano, W.; Wakasa, T.; Ueno, H.; Takao, Y.; Fujioka, A.; Hashimoto, A.; Itou, K.; Yamamura, K.; Nomura, M.; Nagasawa, H.; Shuto, S.; Fukuoka, M.
    Discovery of highly potent human deoxyuridine triphosphatase inhibitors based on the conformation restriction strategy (2012), J. Med. Chem., 55, 5483-5496.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.6.1.23 (E)-3-(2,2-difluoroethoxy)-N-(7-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2-methylhept-5-en-2-yl)benzenesulfonamide
-
 Homo sapiens
3.6.1.23 (E)-3-(cyclopentyloxy)-N-(7-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2-methylhept-5-en-2-yl)benzenesulfonamide
-
 Homo sapiens
3.6.1.23 (E)-3-(cyclopropylmethoxy)-N-(7-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2-methylhept-5-en-2-yl)benzenesulfonamide
-
 Homo sapiens
3.6.1.23 (E)-N-(7-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2-methylhept-5-en-2-yl)-3-methoxybenzenesulfonamide
-
 Homo sapiens
3.6.1.23 (E)-N-(7-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2-methylhept-5-en-2-yl)benzenesulfonamide
-
 Homo sapiens
3.6.1.23 (R)-N-(1-(3-(2,2-difluoroethoxy)phenyl)ethyl)-4-((2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)benzenesulfonamide
-
 Homo sapiens
3.6.1.23 (R)-N-(1-(3-(cyclopentyloxy)phenyl)ethyl)-4-((2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)benzenesulfonamide
-
 Homo sapiens
3.6.1.23 (R)-N-(1-(3-(cyclopropylmethoxy)phenyl)ethyl)-4-((2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-benzenesulfonamide
-
 Homo sapiens
3.6.1.23 (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
-
 Homo sapiens
3.6.1.23 (R,E)-N-(1-(3-(cyclopentyloxy)phenyl)ethyl)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)pent-3-ene-1-sulfonamide
-
 Homo sapiens
3.6.1.23 (R,E)-N-(1-(3-(cyclopropylmethoxy)phenyl)ethyl)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)pent-3-ene-1-sulfonamide
-
 Homo sapiens
3.6.1.23 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
-
 Homo sapiens
3.6.1.23 1-[[2-(trityloxy)ethoxy]methyl]pyrimidine-2,4(1H,3H)-dione
-
 Homo sapiens
3.6.1.23 2'-deoxyuridine 5'-(alpha,beta-imido)triphosphate
-
 Homo sapiens
3.6.1.23 3-(2,2-difluoroethoxy)-N-(2-(4-((2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)phenyl)propan-2-yl)-benzenesulfonamide
-
 Homo sapiens
3.6.1.23 3-(cyclopentyloxy)-N-(2-(4-((2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)phenyl)propan-2-yl)-benzenesulfonamide
-
 Homo sapiens
3.6.1.23 3-(cyclopropylmethoxy)-N-(2-(4-((2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)phenyl)propan-2-yl)-benzenesulfonamide
-
 Homo sapiens
3.6.1.23 3-(cyclopropylmethoxy)-N-[5-[(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methoxy]-2-methylpentan-2-yl]benzenesulfonamide
-
 Homo sapiens
3.6.1.23 N-(2-(4-((2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-phenyl)propan-2-yl)-3-methoxybenzenesulfonamide
-
 Homo sapiens
3.6.1.23 N-(2-(4-((2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-phenyl)propan-2-yl)benzenesulfonamide
-
 Homo sapiens
3.6.1.23 N-[(1R)-1-[3-(cyclopropylmethoxy)-4-fluorophenyl]ethyl]-3-[(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methoxy]propane-1-sulfonamide
-
 Homo sapiens
3.6.1.23 N-[(1R)-1-[3-(cyclopropylmethoxy)phenyl]ethyl]-3-[(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methoxy]propane-1-sulfonamide
-
 Homo sapiens
3.6.1.23 N-[2-[3-(cyclopropylmethoxy)phenyl]propan-2-yl]-3-[(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methoxy]propane-1-sulfonamide
-
 Homo sapiens
3.6.1.23 N-[5-[(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methoxy]-2-methylpentan-2-yl]benzenesulfonamide
-
 Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
3.6.1.23 Homo sapiens P33316
-
-

Substrates and Products (Substrate)

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

Synonyms

EC Number Synonyms Comment Organism
3.6.1.23 deoxyuridine triphosphatase
-
 Homo sapiens
3.6.1.23 dUTPase
-
 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.6.1.23 0.000021
-
 N-[(1R)-1-[3-(cyclopropylmethoxy)-4-fluorophenyl]ethyl]-3-[(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methoxy]propane-1-sulfonamide in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens
3.6.1.23 0.0033
-
 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 in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens
3.6.1.23 0.017
-
 1-[[2-(trityloxy)ethoxy]methyl]pyrimidine-2,4(1H,3H)-dione in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens
3.6.1.23 0.018
-
 2'-deoxyuridine 5'-(alpha,beta-imido)triphosphate in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.6.1.23 0.000026
-
 in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens (E)-3-(2,2-difluoroethoxy)-N-(7-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2-methylhept-5-en-2-yl)benzenesulfonamide
3.6.1.23 0.000028
-
 in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens (E)-3-(cyclopropylmethoxy)-N-(7-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2-methylhept-5-en-2-yl)benzenesulfonamide
3.6.1.23 0.000031
-
 in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 3-(cyclopentyloxy)-N-(2-(4-((2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)phenyl)propan-2-yl)-benzenesulfonamide
3.6.1.23 0.000033
-
 in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens (E)-3-(cyclopentyloxy)-N-(7-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2-methylhept-5-en-2-yl)benzenesulfonamide
3.6.1.23 0.000035
-
 in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 3-(cyclopropylmethoxy)-N-[5-[(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methoxy]-2-methylpentan-2-yl]benzenesulfonamide
3.6.1.23 0.000039
-
 in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens (R,E)-N-(1-(3-(cyclopropylmethoxy)phenyl)ethyl)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)pent-3-ene-1-sulfonamide
3.6.1.23 0.00004
-
 in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens N-[(1R)-1-[3-(cyclopropylmethoxy)phenyl]ethyl]-3-[(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methoxy]propane-1-sulfonamide
3.6.1.23 0.000041
-
 in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens (R,E)-N-(1-(3-(cyclopentyloxy)phenyl)ethyl)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)pent-3-ene-1-sulfonamide
3.6.1.23 0.000073
-
 in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 3-(cyclopropylmethoxy)-N-(2-(4-((2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)phenyl)propan-2-yl)-benzenesulfonamide
3.6.1.23 0.000073
-
 in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens 3-(2,2-difluoroethoxy)-N-(2-(4-((2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)phenyl)propan-2-yl)-benzenesulfonamide
3.6.1.23 0.000082
-
 in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens (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
3.6.1.23 0.00034
-
 in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens N-[2-[3-(cyclopropylmethoxy)phenyl]propan-2-yl]-3-[(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methoxy]propane-1-sulfonamide
3.6.1.23 0.00034
-
 in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens (E)-N-(7-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2-methylhept-5-en-2-yl)-3-methoxybenzenesulfonamide
3.6.1.23 0.00041
-
 in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens (R)-N-(1-(3-(2,2-difluoroethoxy)phenyl)ethyl)-4-((2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)benzenesulfonamide
3.6.1.23 0.00043
-
 in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens (R)-N-(1-(3-(cyclopentyloxy)phenyl)ethyl)-4-((2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)benzenesulfonamide
3.6.1.23 0.00082
-
 in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens (R)-N-(1-(3-(cyclopropylmethoxy)phenyl)ethyl)-4-((2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-benzenesulfonamide
3.6.1.23 0.00127
-
 in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens N-(2-(4-((2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-phenyl)propan-2-yl)-3-methoxybenzenesulfonamide
3.6.1.23 0.0016
-
 in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens (E)-N-(7-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2-methylhept-5-en-2-yl)benzenesulfonamide
3.6.1.23 0.0018
-
 in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens N-(2-(4-((2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-phenyl)propan-2-yl)benzenesulfonamide
3.6.1.23 0.0039
-
 in 0.2 M Tris buffer (pH 7.4), 16 mM MgCl2, at 37°C Homo sapiens N-[5-[(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methoxy]-2-methylpentan-2-yl]benzenesulfonamide