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Literature summary for 2.4.2.4 extracted from

  • McNally, V.A.; Rajabi, M.; Gbaj, A.; Stratford, I.J.; Edwards, P.N.; Douglas, K.T.; Bryce, R.A.; Jaffar, M.; Freeman, S.
    Design, synthesis and enzymatic evaluation of 6-bridged imidazolyluracil derivatives as inhibitors of human thymidine phosphorylase (2007), J. Pharm. Pharmacol., 59, 537-547.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
5-bromo-6-(3'-methylimidazol-1-yl)uracil IC50: 0.038 mM Homo sapiens
5-bromo-6-[(3-methylimidazol-1-yl)methyl]uracil IC50: 0.017 mM Homo sapiens
5-chloro-6-(3'-methylimidazol-1-yl)uracil IC50: 0.035 mM Homo sapiens
5-chloro-6-[(3-methylimidazol-1-yl)methyl]uracil IC50: 0.018 mM Homo sapiens
6-(3-methylimidazol-1-yl)uracil IC50: 0.110 mM Homo sapiens
6-[(3-methylimidazol-1-yl)methyl]thymine IC50: 0.06 mM Homo sapiens
6-[(3-methylimidazol-1-yl)methyl]uracil IC50: 0.042 mM Homo sapiens

Organism

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

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
thymidine + phosphate
-
Homo sapiens thymine + 2-deoxy-D-ribose 1-phosphate
-
?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.017
-
IC50: 0.017 mM Homo sapiens 5-bromo-6-[(3-methylimidazol-1-yl)methyl]uracil
0.018
-
IC50: 0.018 mM Homo sapiens 5-chloro-6-[(3-methylimidazol-1-yl)methyl]uracil
0.035
-
IC50: 0.035 mM Homo sapiens 5-chloro-6-(3'-methylimidazol-1-yl)uracil
0.038
-
IC50: 0.038 mM Homo sapiens 5-bromo-6-(3'-methylimidazol-1-yl)uracil
0.042
-
IC50: 0.042 mM Homo sapiens 6-[(3-methylimidazol-1-yl)methyl]uracil
0.06
-
IC50: 0.06 mM Homo sapiens 6-[(3-methylimidazol-1-yl)methyl]thymine
0.11
-
IC50: 0.110 mM Homo sapiens 6-(3-methylimidazol-1-yl)uracil