Literature summary for 5.6.1.3 extracted from

Rickert, K.W.; Schaber, M.; Torrent, M.; Neilson, L.A.; Tasber, E.S.; Garbaccio, R.; Coleman, P.J.; Harvey, D.; Zhang, Y.; Yang, Y.; Marshall, G.; Lee, L.; Walsh, E.S.; Hamilton, K.; Buser, C.A.
Discovery and biochemical characterization of selective ATP competitive inhibitors of the human mitotic kinesin KSP (2008), Arch. Biochem. Biophys., 469, 220-231.

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Inhibitors

Inhibitors	Comment	Organism	Structure
4-(2-[1-(2,4,6-trifluorophenyl)cyclopropyl]-1,3-thiazol-4-yl)pyridine	-	Homo sapiens
4-(2-[1-(2,4-difluorophenyl)cyclopropyl]-1,3-thiazol-4-yl)pyridine	-	Homo sapiens
4-(2-[1-(2,6-difluorophenyl)cyclopropyl]-1,3-thiazol-4-yl)pyridine	-	Homo sapiens
4-(2-[1-(2-fluorophenyl)cyclopropyl]-1,3-thiazol-4-yl)pyridine	-	Homo sapiens
4-(2-[1-(4-chlorophenyl)cyclopropyl]-1,3-thiazol-4-yl)pyridine	-	Homo sapiens
4-(2-[1-(4-fluorophenyl)cyclopropyl]-1,3-thiazol-4-yl)pyridine	treatmebnt of cells results in inhibition of proliferation and induction of caspase 3 activity with EC50 values of 0.0017 and 0.0011 mM, respectively. Compound induces monoastral spindles in A2780 cells when incubated at concentrations above that required to induce a full mitotic arrest	Homo sapiens
4-[2-(1-phenylcyclopropyl)-1,3-thiazol-4-yl]pyridine 1-oxide	-	Homo sapiens
5-[2-(1-phenylcyclopropyl)-1,3-thiazol-4-yl]pyridine-2-carbonitrile	-	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	P52732	-	-

Synonyms

Synonyms	Comment	Organism
kinesin spindle protein	-	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.00023	-	-	Homo sapiens	4-(2-[1-(2,4,6-trifluorophenyl)cyclopropyl]-1,3-thiazol-4-yl)pyridine
0.00028	-	-	Homo sapiens	4-(2-[1-(2,6-difluorophenyl)cyclopropyl]-1,3-thiazol-4-yl)pyridine
0.00029	-	-	Homo sapiens	4-(2-[1-(4-chlorophenyl)cyclopropyl]-1,3-thiazol-4-yl)pyridine
0.0003	-	-	Homo sapiens	4-(2-[1-(2-fluorophenyl)cyclopropyl]-1,3-thiazol-4-yl)pyridine
0.00033	-	-	Homo sapiens	4-(2-[1-(2,4-difluorophenyl)cyclopropyl]-1,3-thiazol-4-yl)pyridine
0.00047	-	-	Homo sapiens	4-[2-(1-phenylcyclopropyl)-1,3-thiazol-4-yl]pyridine 1-oxide
0.000532	-	-	Homo sapiens	5-[2-(1-phenylcyclopropyl)-1,3-thiazol-4-yl]pyridine-2-carbonitrile
0.00054	-	pH 6.8, 22°C	Homo sapiens	4-(2-[1-(4-fluorophenyl)cyclopropyl]-1,3-thiazol-4-yl)pyridine

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Release 2023.1 (January 2023)