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Literature summary for 2.7.1.21 extracted from

  • Lin, J.; Roy, V.; Wang, L.; You, L.; Agrofoglio, L.A.; Deville-Bonne, D.; McBrayer, T.R.; Coats, S.J.; Schinazi, R.F.; Eriksson, S.
    3-(1,2,3-Triazol-1-yl)-3-deoxythymidine analogs as substrates for human and Ureaplasma parvum thymidine kinase for structure-activity investigations (2010), Bioorg. Med. Chem., 18, 3261-3269.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
3'-(4-(2-phenyl-ethyl)-1,2,3-triazole-1-yl)-3'-deoxythymidine
-
Homo sapiens
3'-(4-(2-phenyl-ethyl)-1,2,3-triazole-1-yl)-3'-deoxythymidine
-
Ureaplasma parvum
3'-(4-(2-pyridine)-1,2,3-triazole-1-yl)-3'-deoxythymidine
-
Homo sapiens
3'-(4-(2-pyridine)-1,2,3-triazole-1-yl)-3'-deoxythymidine
-
Ureaplasma parvum
3'-(4-(3-chloro-propyl)-1,2,3-triazol-1-yl)-3'-deoxythymidine
-
Homo sapiens
3'-(4-(3-chloro-propyl)-1,2,3-triazol-1-yl)-3'-deoxythymidine
-
Ureaplasma parvum
3'-(4-(4-fluorophenyl)-1,2,3-triazole-1-yl)-3'-deoxythymidine
-
Homo sapiens
3'-(4-(4-fluorophenyl)-1,2,3-triazole-1-yl)-3'-deoxythymidine
-
Ureaplasma parvum
3'-(4-benzyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
-
Homo sapiens
3'-(4-benzyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
-
Ureaplasma parvum
3'-(4-pentyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
-
Homo sapiens
3'-(4-pentyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
-
Ureaplasma parvum
3'-(4-phenyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
-
Homo sapiens
3'-(4-phenyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
-
Ureaplasma parvum
3'-(4-propyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
-
Homo sapiens
3'-(4-propyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
-
Ureaplasma parvum
3'-(4-tert-butyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
-
Homo sapiens
3'-(4-tert-butyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
-
Ureaplasma parvum
3'-azido-3'-deoxythymidine
-
Homo sapiens
3'-azido-3'-deoxythymidine
-
Ureaplasma parvum

Organism

Organism UniProt Comment Textmining
Homo sapiens P04183
-
-
Ureaplasma parvum Q9PPP5
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Homo sapiens
-
Ureaplasma parvum

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + 3'-(4-(2-phenylethyl)-1,2,3-triazole-1-yl)-3'-deoxythymidine 12.3% activity compared to thymidine Ureaplasma parvum ADP + 3'-(4-(2-phenylethyl)-1,2,3-triazole-1-yl)-3'-deoxythymidine 5'-phosphate
-
?
ATP + 3'-(4-(2-phenylethyl)-1,2,3-triazole-1-yl)-3'-deoxythymidine 2.4% activity compared to thymidine Homo sapiens ADP + 3'-(4-(2-phenylethyl)-1,2,3-triazole-1-yl)-3'-deoxythymidine 5'-phosphate
-
?
ATP + 3'-(4-(2-pyridine)-1,2,3-triazole-1-yl)-3'-deoxythymidine 3.1% activity compared to thymidine Homo sapiens ADP + 3'-(4-(2-pyridine)-1,2,3-triazole-1-yl)-3'-deoxythymidine 5'-phosphate
-
?
ATP + 3'-(4-(2-pyridine)-1,2,3-triazole-1-yl)-3'-deoxythymidine 7.1% activity compared to thymidine Ureaplasma parvum ADP + 3'-(4-(2-pyridine)-1,2,3-triazole-1-yl)-3'-deoxythymidine 5'-phosphate
-
?
ATP + 3'-(4-(3-chloropropyl)-1,2,3-triazol-1-yl)-3'-deoxythymidine 2.7% activity compared to thymidine Homo sapiens ADP + 3'-(4-(3-chloropropyl)-1,2,3-triazol-1-yl)-3'-deoxythymidine 5'-phosphate
-
?
ATP + 3'-(4-(3-chloropropyl)-1,2,3-triazol-1-yl)-3'-deoxythymidine 6.5% activity compared to thymidine Ureaplasma parvum ADP + 3'-(4-(3-chloropropyl)-1,2,3-triazol-1-yl)-3'-deoxythymidine 5'-phosphate
-
?
ATP + 3'-(4-(4-fluorophenyl)-1,2,3-triazole-1-yl)-3'-deoxythymidine 13.7% activity compared to thymidine Ureaplasma parvum ADP + 3'-(4-(4-fluorophenyl)-1,2,3-triazole-1-yl)-3'-deoxythymidine 5'-phosphate
-
?
ATP + 3'-(4-(4-fluorophenyl)-1,2,3-triazole-1-yl)-3'-deoxythymidine 2.6% activity compared to thymidine Homo sapiens ADP + 3'-(4-(4-fluorophenyl)-1,2,3-triazole-1-yl)-3'-deoxythymidine 5'-phosphate
-
?
ATP + 3'-(4-benzyl-1,2,3-triazol-1-yl)-3'-deoxythymidine 11.6% activity compared to thymidine Ureaplasma parvum ADP + 3'-(4-benzyl-1,2,3-triazol-1-yl)-3'-deoxythymidine 5'-phosphate
-
?
ATP + 3'-(4-benzyl-1,2,3-triazol-1-yl)-3'-deoxythymidine 4.8% activity compared to thymidine Homo sapiens ADP + 3'-(4-benzyl-1,2,3-triazol-1-yl)-3'-deoxythymidine 5'-phosphate
-
?
ATP + 3'-(4-pentyl-1,2,3-triazol-1-yl)-3'-deoxythymidine 2.9% activity compared to thymidine Homo sapiens ADP + 3'-(4-pentyl-1,2,3-triazol-1-yl)-3'-deoxythymidine 5'-phosphate
-
?
ATP + 3'-(4-pentyl-1,2,3-triazol-1-yl)-3'-deoxythymidine 8.7% activity compared to thymidine Ureaplasma parvum ADP + 3'-(4-pentyl-1,2,3-triazol-1-yl)-3'-deoxythymidine 5'-phosphate
-
?
ATP + 3'-(4-phenyl-1,2,3-triazol-1-yl)-3'-deoxythymidine 2.1% activity compared to thymidine Homo sapiens ADP + 3'-(4-phenyl-1,2,3-triazol-1-yl)-3'-deoxythymidine 5'-phosphate
-
?
ATP + 3'-(4-phenyl-1,2,3-triazol-1-yl)-3'-deoxythymidine 5.5% activity compared to thymidine Ureaplasma parvum ADP + 3'-(4-phenyl-1,2,3-triazol-1-yl)-3'-deoxythymidine 5'-phosphate
-
?
ATP + 3'-(4-propyl-1,2,3-triazol-1-yl)-3'-deoxythymidine 1.9% activity compared to thymidine Homo sapiens ADP + 3'-(4-propyl-1,2,3-triazol-1-yl)-3'-deoxythymidine 5'-phosphate
-
?
ATP + 3'-(4-propyl-1,2,3-triazol-1-yl)-3'-deoxythymidine 7.2% activity compared to thymidine Ureaplasma parvum ADP + 3'-(4-propyl-1,2,3-triazol-1-yl)-3'-deoxythymidine 5'-phosphate
-
?
ATP + 3'-(4-tert-butyl-1,2,3-triazol-1-yl)-3'-deoxythymidine 2.2% activity compared to thymidine Homo sapiens ADP + 3'-(4-tert-butyl-1,2,3-triazol-1-yl)-3'-deoxythymidine 5'-phosphate
-
?
ATP + 3'-(4-tert-butyl-1,2,3-triazol-1-yl)-3'-deoxythymidine 4.7% activity compared to thymidine Ureaplasma parvum ADP + 3'-(4-tert-butyl-1,2,3-triazol-1-yl)-3'-deoxythymidine 5'-phosphate
-
?
ATP + 3'-azido-3'-deoxythymidine 27.8% activity compared to thymidine Ureaplasma parvum ADP + 3'-azido-3'-deoxythymidine 5'-phosphate
-
?
ATP + 3'-azido-3'-deoxythymidine 47.3% activity compared to thymidine Homo sapiens ADP + 3'-azido-3'-deoxythymidine 5'-phosphate
-
?
ATP + thymidine 100% activity Homo sapiens ADP + dTMP
-
?
ATP + thymidine 100% activity Ureaplasma parvum ADP + dTMP
-
?

Synonyms

Synonyms Comment Organism
thymidine kinase 1
-
Homo sapiens
thymidine kinase 1
-
Ureaplasma parvum
TK1
-
Homo sapiens
TK1
-
Ureaplasma parvum

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.003
-
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37°C Homo sapiens 3'-azido-3'-deoxythymidine
0.0125
-
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37°C Ureaplasma parvum 3'-azido-3'-deoxythymidine
0.044
-
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37°C Homo sapiens 3'-(4-(4-fluorophenyl)-1,2,3-triazole-1-yl)-3'-deoxythymidine
0.053
-
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37°C Homo sapiens 3'-(4-(2-pyridine)-1,2,3-triazole-1-yl)-3'-deoxythymidine
0.06
-
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37°C Homo sapiens 3'-(4-(2-phenyl-ethyl)-1,2,3-triazole-1-yl)-3'-deoxythymidine
0.071
-
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37°C Ureaplasma parvum 3'-(4-(4-fluorophenyl)-1,2,3-triazole-1-yl)-3'-deoxythymidine
0.073
-
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37°C Ureaplasma parvum 3'-(4-benzyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
0.078
-
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37°C Homo sapiens 3'-(4-benzyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
0.086
-
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37°C Homo sapiens 3'-(4-pentyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
0.099
-
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37°C Homo sapiens 3'-(4-phenyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
0.105
-
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37°C Homo sapiens 3'-(4-(3-chloro-propyl)-1,2,3-triazol-1-yl)-3'-deoxythymidine
0.114
-
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37°C Homo sapiens 3'-(4-tert-butyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
0.12
-
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37°C Ureaplasma parvum 3'-(4-(2-phenyl-ethyl)-1,2,3-triazole-1-yl)-3'-deoxythymidine
0.15
-
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37°C Ureaplasma parvum 3'-(4-pentyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
0.189
-
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37°C Ureaplasma parvum 3'-(4-propyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
0.2
-
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37°C Ureaplasma parvum 3'-(4-phenyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
0.208
-
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37°C Ureaplasma parvum 3'-(4-(3-chloro-propyl)-1,2,3-triazol-1-yl)-3'-deoxythymidine
0.211
-
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37°C Ureaplasma parvum 3'-(4-(2-pyridine)-1,2,3-triazole-1-yl)-3'-deoxythymidine
0.311
-
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37°C Homo sapiens 3'-(4-propyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
0.318
-
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37°C Ureaplasma parvum 3'-(4-tert-butyl-1,2,3-triazol-1-yl)-3'-deoxythymidine