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Literature summary for 5.6.1.3 extracted from

  • Braun, J.; Moeckel, M.M.; Strittmatter, T.; Marx, A.; Groth, U.; Mayer, T.U.
    Synthesis and biological evaluation of optimized inhibitors of the mitotic kinesin Kif18A (2015), ACS Chem. Biol., 10, 554-560.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
1-(benzenesulfinyl)-2,4-dinitrobenzene
-
Homo sapiens
1-(benzenesulfinyl)-2-nitrobenzene
-
Homo sapiens
1-(benzenesulfonyl)-2,4-dinitrobenzene
-
Homo sapiens
1-(benzenesulfonyl)-2-nitro-4-(trifluoromethyl)benzene
-
Homo sapiens
1-(benzenesulfonyl)-2-nitrobenzene
-
Homo sapiens
1-(benzenesulfonyl)-4-chloro-2-nitrobenzene i.e. BTB-1, reversibly inhibits the microtubule-stimulated ATPase activity of Kif18A Homo sapiens
1-(benzenesulfonyl)-4-fluoro-2-nitrobenzene
-
Homo sapiens
1-[(4-chlorophenyl)methanesulfonyl]-2,4-dinitrobenzene
-
Homo sapiens
1-[(4-methoxyphenyl)methanesulfinyl]-2-nitrobenzene
-
Homo sapiens
1-[(4-methoxyphenyl)methanesulfonyl]-2-nitrobenzene
-
Homo sapiens
1-[(4-methylphenyl)methanesulfinyl]-2,4-dinitrobenzene
-
Homo sapiens
1-[(4-methylphenyl)methanesulfonyl]-2,4-dinitrobenzene
-
Homo sapiens
2-(4-chloro-2-nitrobenzene-1-sulfinyl)naphthalene
-
Homo sapiens
2-(4-chloro-2-nitrobenzene-1-sulfonyl)thiophene
-
Homo sapiens
4-(benzenesulfonyl)-1-chloro-2-nitrobenzene
-
Homo sapiens
4-chloro-1-(4-methoxybenzene-1-sulfinyl)-2-nitrobenzene
-
Homo sapiens
4-chloro-1-[(4-chlorophenyl)methanesulfonyl]-2-nitrobenzene
-
Homo sapiens
4-chloro-1-[(4-methoxyphenyl)methanesulfonyl]-2-nitrobenzene
-
Homo sapiens
4-chloro-1-[(4-methylphenyl)methanesulfonyl]-2-nitrobenzene
-
Homo sapiens
4-chloro-2-nitro-1-phenoxybenzene
-
Homo sapiens
6-(4-chloro-2-nitrobenzene-1-sulfonyl)-1,4-dihydronaphthalene
-
Homo sapiens
additional information identification of optimized small molecule inhibitors of the mitotic kinesin Kif18A, usage of BTB-1 as a lead compound, structure-activity relationship studies and inhibition mechanism of BTB-1 and its analogues, overview Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ required Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) 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)
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q8NI77
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HeLa cell
-
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)
-
?

Synonyms

Synonyms Comment Organism
KIF18A
-
Homo sapiens
mitotic kinesin
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0017
-
pH and temperature not specified in the publication Homo sapiens 1-(benzenesulfonyl)-4-chloro-2-nitrobenzene
0.003
-
pH and temperature not specified in the publication Homo sapiens 1-(benzenesulfonyl)-2-nitrobenzene
0.0048
-
pH and temperature not specified in the publication Homo sapiens 1-(benzenesulfonyl)-4-fluoro-2-nitrobenzene
0.0064
-
pH and temperature not specified in the publication Homo sapiens 2-(4-chloro-2-nitrobenzene-1-sulfonyl)thiophene
0.0102
-
pH and temperature not specified in the publication Homo sapiens 1-(benzenesulfonyl)-2,4-dinitrobenzene
0.0103
-
pH and temperature not specified in the publication Homo sapiens 1-(benzenesulfonyl)-2-nitro-4-(trifluoromethyl)benzene