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Literature summary extracted from

  • Bera, H.; Dolzhenko, A.V.; Sun, L.; Dutta Gupta, S.; Chui, W.K.
    Synthesis and in vitro evaluation of 1,2,4-triazolo[1,5-a][1,3,5]triazine derivatives as thymidine phosphorylase inhibitors (2013), Chem. Biol. Drug Des., 82, 351-360.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.2.4 2,7-bis(methylsulfanyl)[1,2,4]triazolo[1,5-a][1,3,5]triazin-5(4H)-one
-
 Homo sapiens
2.4.2.4 2-(3-bromophenyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
 Homo sapiens
2.4.2.4 2-(3-methylphenyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
 Homo sapiens
2.4.2.4 2-(4-bromo-3-methylphenyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
 Homo sapiens
2.4.2.4 2-(4-bromophenyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
 Homo sapiens
2.4.2.4 2-(4-methylphenyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
 Homo sapiens
2.4.2.4 2-(benzylsulfanyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
 Homo sapiens
2.4.2.4 2-(furan-2-yl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
 Homo sapiens
2.4.2.4 2-(methylsulfanyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
 Homo sapiens
2.4.2.4 2-(methylsulfanyl)-7-sulfanylidene-6,7-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-5(4H)-one
-
 Homo sapiens
2.4.2.4 2-(methylsulfanyl)[1,2,4]triazolo[1,5-a][1,3,5]triazine-5,7(4H,6H)-dione
-
 Homo sapiens
2.4.2.4 2-(pyridin-2-yl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
 Homo sapiens
2.4.2.4 2-benzyl-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
 Homo sapiens
2.4.2.4 2-phenyl-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
 Homo sapiens
2.4.2.4 2-phenyl-7-sulfanylidene-6,7-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-5(4H)-one
-
 Homo sapiens
2.4.2.4 2-phenyl[1,2,4]triazolo[1,5-a][1,3,5]triazine-5,7(4H,6H)-dione
-
 Homo sapiens
2.4.2.4 2-[(2-phenylethyl)sulfanyl]-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
 Homo sapiens
2.4.2.4 2-[(3-phenylpropyl)sulfanyl]-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
 Homo sapiens
2.4.2.4 5-chloro-6-[1-(2-iminopyrrolidinyl)methyl] uracil hydrochloride
-
 Homo sapiens
2.4.2.4 5-sulfanylidene-2-(thiophen-2-yl)-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
 Homo sapiens
2.4.2.4 5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
 Homo sapiens
2.4.2.4 7-(methylsulfanyl)-2-phenyl[1,2,4]triazolo[1,5-a][1,3,5]triazin-5(4H)-one
-
 Homo sapiens
2.4.2.4 7-deazaxanthine
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.4.2.4 thymidine + phosphate Homo sapiens
-
 thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.4.2.4 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.4.2.4 MDA-MB-231 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

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

Synonyms

EC Number Synonyms Comment Organism
2.4.2.4 gliostatin
-
 Homo sapiens
2.4.2.4 PD-ECGF
-
 Homo sapiens
2.4.2.4 platelet derived-endothelial cell growth factor
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.4.2.4 0.01309
-
 pH and temperature not specified in the publication Homo sapiens 2-(4-bromo-3-methylphenyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
2.4.2.4 0.02206
-
 pH and temperature not specified in the publication Homo sapiens 2-(4-bromophenyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
2.4.2.4 0.02453
-
 pH and temperature not specified in the publication Homo sapiens 2-(pyridin-2-yl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
2.4.2.4 0.03095
-
 pH and temperature not specified in the publication Homo sapiens 5-sulfanylidene-2-(thiophen-2-yl)-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
2.4.2.4 0.03154
-
 pH and temperature not specified in the publication Homo sapiens 2-(furan-2-yl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
2.4.2.4 0.03158
-
 pH and temperature not specified in the publication Homo sapiens 2-(4-methylphenyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
2.4.2.4 0.03178
-
 pH and temperature not specified in the publication Homo sapiens 2-(3-bromophenyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
2.4.2.4 0.03442
-
 pH and temperature not specified in the publication Homo sapiens 2-(3-methylphenyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
2.4.2.4 0.03956
-
 pH and temperature not specified in the publication Homo sapiens 2-phenyl-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
2.4.2.4 0.04263
-
 pH and temperature not specified in the publication Homo sapiens 7-deazaxanthine
2.4.2.4 0.04332
-
 pH and temperature not specified in the publication Homo sapiens 2-benzyl-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
2.4.2.4 0.05167
-
 pH and temperature not specified in the publication Homo sapiens 2-(methylsulfanyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
2.4.2.4 0.05538
-
 pH and temperature not specified in the publication Homo sapiens 2-(benzylsulfanyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
2.4.2.4 0.05813
-
 pH and temperature not specified in the publication Homo sapiens 5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
2.4.2.4 0.05925
-
 pH and temperature not specified in the publication Homo sapiens 2-[(3-phenylpropyl)sulfanyl]-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
2.4.2.4 0.05988
-
 pH and temperature not specified in the publication Homo sapiens 2-[(2-phenylethyl)sulfanyl]-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
2.4.2.4 0.1
-
 IC50 above 0.1 mM, pH and temperature not specified in the publication Homo sapiens 2-(methylsulfanyl)[1,2,4]triazolo[1,5-a][1,3,5]triazine-5,7(4H,6H)-dione
2.4.2.4 0.1
-
 IC50 above 0.1 mM, pH and temperature not specified in the publication Homo sapiens 2-phenyl[1,2,4]triazolo[1,5-a][1,3,5]triazine-5,7(4H,6H)-dione
2.4.2.4 0.1
-
 IC50 above 0.1 mM, pH and temperature not specified in the publication Homo sapiens 2-(methylsulfanyl)-7-sulfanylidene-6,7-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-5(4H)-one
2.4.2.4 0.1
-
 IC50 above 0.1 mM, pH and temperature not specified in the publication Homo sapiens 2-phenyl-7-sulfanylidene-6,7-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-5(4H)-one
2.4.2.4 0.1
-
 IC50 above 0.1 mM, pH and temperature not specified in the publication Homo sapiens 2,7-bis(methylsulfanyl)[1,2,4]triazolo[1,5-a][1,3,5]triazin-5(4H)-one
2.4.2.4 0.1
-
 IC50 above 0.1 mM, pH and temperature not specified in the publication Homo sapiens 7-(methylsulfanyl)-2-phenyl[1,2,4]triazolo[1,5-a][1,3,5]triazin-5(4H)-one