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Literature summary for 5.6.1.3 extracted from

  • Nagarajan, S.; Skoufias, D.A.; Kozielski, F.; Pae, A.N.
    Receptor-ligand interaction-based virtual screening for novel Eg5/kinesin spindle protein inhibitors (2012), J. Med. Chem., 55, 2561-2573.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
N-terminal part, residues 2-368 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-(2,4-difluorophenyl)-9-(3,4-dimethylphenyl)-8-oxo-8,9-dihydro-7H-purine-6-carboxamide
-
Homo sapiens
2-[1-(4-methoxyphenyl)-5-oxo-3-[2-(thiophen-2-yl)ethyl]-2-thioxoimidazolidin-4-yl]-N-phenylacetamide
-
Homo sapiens
4-[[3-(methoxycarbonyl)-2-methyl-5a,9a-dihydronaphtho[1,2-b]furan-5-yl]sulfamoyl]benzoic acid
-
Homo sapiens
5-(2-fluorophenyl)-2,9-dimethyl-5,6-dihydropyrazolo[1,5-c]quinazoline
-
Homo sapiens
N-(4-fluorophenyl)-2-[1-(4-fluorophenyl)-3-[2-(3-methylthiophen-2-yl)ethyl]-5-oxo-2-thioxoimidazolidin-4-yl]acetamide
-
Homo sapiens
N-(4-methoxyphenyl)-2-[3-[2-(3-methylthiophen-2-yl)ethyl]-5-oxo-1-phenyl-2-thioxoimidazolidin-4-yl]acetamide
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Homo sapiens

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)
-
?

Subunits

Subunits Comment Organism
homotetramer
-
Homo sapiens

Synonyms

Synonyms Comment Organism
Egs5
-
Homo sapiens
HsEgs5
-
Homo sapiens
kinesin spindle protein
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0006
-
inhibition of basal ATPase activity, pH 6.9, 25°C Homo sapiens N-(4-fluorophenyl)-2-[1-(4-fluorophenyl)-3-[2-(3-methylthiophen-2-yl)ethyl]-5-oxo-2-thioxoimidazolidin-4-yl]acetamide
0.001
-
inhibition of basal ATPase activity, pH 6.9, 25°C Homo sapiens 2-[1-(4-methoxyphenyl)-5-oxo-3-[2-(thiophen-2-yl)ethyl]-2-thioxoimidazolidin-4-yl]-N-phenylacetamide
0.0024
-
inhibition of basal ATPase activity, pH 6.9, 25°C Homo sapiens N-(4-methoxyphenyl)-2-[3-[2-(3-methylthiophen-2-yl)ethyl]-5-oxo-1-phenyl-2-thioxoimidazolidin-4-yl]acetamide
0.0063
-
inhibition of basal ATPase activity, pH 6.9, 25°C Homo sapiens 5-(2-fluorophenyl)-2,9-dimethyl-5,6-dihydropyrazolo[1,5-c]quinazoline
0.0415
-
inhibition of basal ATPase activity, pH 6.9, 25°C Homo sapiens 2-(2,4-difluorophenyl)-9-(3,4-dimethylphenyl)-8-oxo-8,9-dihydro-7H-purine-6-carboxamide
0.0791
-
inhibition of basal ATPase activity, pH 6.9, 25°C Homo sapiens 4-[[3-(methoxycarbonyl)-2-methyl-5a,9a-dihydronaphtho[1,2-b]furan-5-yl]sulfamoyl]benzoic acid