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Literature summary for 2.4.2.4 extracted from

  • Reigan, P.; Gbaj, A.; Stratford, I.J.; Bryce, R.A.; Freeman, S.
    Xanthine oxidase-activated prodrugs of thymidine phosphorylase inhibitors (2008), Eur. J. Med. Chem., 43, 1248-1260.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
2-mercapto-7H-pyrrolo[2,3-d]pyrimidin-4(3H)-one 25% inhibition at 0.045 mM Escherichia coli
2-mercapto-7H-pyrrolo[2,3-d]pyrimidin-4(3H)-one
-
Homo sapiens
5-chloro-6-[1-(2-iminopyrrolidinyl)methyl]uracilhydrochloride
-
Escherichia coli
5-chloro-6-[1-(2-iminopyrrolidinyl)methyl]uracilhydrochloride
-
Homo sapiens
6-amino-5-bromouracil
-
Escherichia coli
6-amino-5-bromouracil
-
Homo sapiens
7-deazaxanthine
-
Escherichia coli
7-deazaxanthine
-
Homo sapiens
additional information not inhibited by 5-chloro-6-methyl-3H-pyrimidin-4-one, 5-chloro-6-[1-(2-iminopyrrolidinyl)methyl]-3H-pyrimidin-4-one, 6H-imidazo[1,2-c]pyrimidin-5-one, 7H-pyrrolo[2,3-d]pyrimidin-2(1H)-one, and 7H-pyrrolo[2,3-d]pyrimidine Escherichia coli
xanthine 13% inhibition at 0.158 mM Escherichia coli
xanthine
-
Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.16
-
5-nitro-2'-deoxyuridine in 0.1 M potassium phosphate buffer (pH 7.4), at 25°C Homo sapiens
0.23
-
5-nitro-2'-deoxyuridine in 0.1 M potassium phosphate buffer (pH 7.4), at 25°C Escherichia coli

Organism

Organism UniProt Comment Textmining
Escherichia coli
-
-
-
Homo sapiens P19971
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5-nitro-2'-deoxyuridine + phosphate
-
Escherichia coli 5-nitrouracil + 2-deoxy-D-ribose 1-phosphate
-
?
5-nitro-2'-deoxyuridine + phosphate
-
Homo sapiens 5-nitrouracil + 2-deoxy-D-ribose 1-phosphate
-
?

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
20
-
5-nitro-2'-deoxyuridine in 0.1 M potassium phosphate buffer (pH 7.4), at 25°C Escherichia coli

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00002
-
in 0.1 M potassium phosphate buffer (pH 7.4), at 25°C Escherichia coli 5-chloro-6-[1-(2-iminopyrrolidinyl)methyl]uracilhydrochloride
0.000023
-
in 0.1 M potassium phosphate buffer (pH 7.4), at 25°C Homo sapiens 5-chloro-6-[1-(2-iminopyrrolidinyl)methyl]uracilhydrochloride
0.0016
-
in 0.1 M potassium phosphate buffer (pH 7.4), at 25°C Escherichia coli 6-amino-5-bromouracil
0.0065
-
in 0.1 M potassium phosphate buffer (pH 7.4), at 25°C Escherichia coli 7-deazaxanthine
0.0068
-
in 0.1 M potassium phosphate buffer (pH 7.4), at 25°C Homo sapiens 6-amino-5-bromouracil
0.045
-
in 0.1 M potassium phosphate buffer (pH 7.4), at 25°C Homo sapiens 7-deazaxanthine