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Literature summary for 5.6.1.3 extracted from

  • Klein, E.; DeBonis, S.; Thiede, B.; Skoufias, D.A.; Kozielski, F.; Lebeau, L.
    New chemical tools for investigating human mitotic kinesin Eg5 (2007), Bioorg. Med. Chem., 15, 6474-6488.
    View publication on PubMed
Search for more literature for 5.6.1.3

Activating Compound

Activating Compound Comment Organism Structure
microtubule
-
 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-(2-sulfanylethoxy)ethyl 4-(3-hydroxyphenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
 Homo sapiens
2-[2-(acetylsulfanyl)ethoxy]ethyl 4-(3-hydroxyphenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
 Homo sapiens
ethyl 3-acetyl-4-[3-(acetyloxy)phenyl]-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate no inhibition in vitro, inhibitory in cell-based assay Homo sapiens
ethyl 4-(3-hydroxyphenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate i.e. monastrol Homo sapiens
ethyl 4-[3-(acetyloxy)phenyl]-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate no inhibition in vitro, inhibitory in cell-based assay Homo sapiens
furan-2-yl[4-(3-hydroxyphenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl]methanone
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
 isoform Rg5
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + H2O + a kinesin associated with a microtubule at position n
-
 Homo sapiens ADP + phosphate + a kinesin associated with a microtubule at position n+1 (toward the plus end)
-
 ?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0015
-
 22°C, inhibition of basal ATPase activity Homo sapiens furan-2-yl[4-(3-hydroxyphenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl]methanone
0.003
-
 22°C, inhibition of microtubule-stimulated ATPase activity Homo sapiens furan-2-yl[4-(3-hydroxyphenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl]methanone
0.004
-
 22°C, inhibition of basal ATPase activity Homo sapiens 2-(2-sulfanylethoxy)ethyl 4-(3-hydroxyphenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
0.0045
-
 22°C, inhibition of basal ATPase activity Homo sapiens 2-[2-(acetylsulfanyl)ethoxy]ethyl 4-(3-hydroxyphenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
0.0055
-
 22°C, inhibition of microtubule-stimulated ATPase activity Homo sapiens 2-(2-sulfanylethoxy)ethyl 4-(3-hydroxyphenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
0.0061
-
 22°C, inhibition of basal ATPase activity Homo sapiens ethyl 4-(3-hydroxyphenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
0.0092
-
 cell-based assay on monoastral spindles Homo sapiens furan-2-yl[4-(3-hydroxyphenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl]methanone
0.0115
-
 22°C, inhibition of microtubule-stimulated ATPase activity Homo sapiens 2-[2-(acetylsulfanyl)ethoxy]ethyl 4-(3-hydroxyphenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
0.0123
-
 22°C, inhibition of microtubule-stimulated ATPase activity Homo sapiens ethyl 4-(3-hydroxyphenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
0.05
-
 cell-based assay on monoastral spindles Homo sapiens ethyl 4-[3-(acetyloxy)phenyl]-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
0.0513
-
 cell-based assay on monoastral spindles Homo sapiens ethyl 4-(3-hydroxyphenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
0.0625
-
 cell-based assay on monoastral spindles Homo sapiens ethyl 3-acetyl-4-[3-(acetyloxy)phenyl]-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate