Target Validation Information
TTD ID	T63986
Target Name	Kinesin spindle messenger RNA (KIF11 mRNA)
Type of Target	Clinical trial
Drug Potency against Target	(S)-dimethylenastron	Drug Info	IC50 = 200 nM	[5]
	(S)-enastron	Drug Info	IC50 = 2000 nM	[5]
	1-(trifluoromethyl)-9H-carbazole	Drug Info	IC50 = 3300 nM	[4]
	1-tert-butyl-9H-carbazole	Drug Info	IC50 = 14000 nM	[4]
	11H-benzo[a]carbazole	Drug Info	IC50 = 4600 nM	[4]
	2,3,4,11-tetrahydro-1H-benzo[a]carbazole	Drug Info	IC50 = 1600 nM	[4]
	2-(difluoromethyl)-9H-carbazole	Drug Info	IC50 = 870 nM	[4]
	2-(trifluoromethoxy)-9H-carbazole	Drug Info	IC50 = 510 nM	[4]
	2-ethyl-9H-carbazole	Drug Info	IC50 = 2800 nM	[4]
	2-isopropyl-9H-carbazole	Drug Info	IC50 = 1500 nM	[4]
	2-tert-butoxy-9H-carbazole	Drug Info	IC50 = 3200 nM	[4]
	2-tert-butyl-7-(trifluoromethyl)-9H-carbazole	Drug Info	IC50 = 1400 nM	[4]
	3-tert-butyl-9H-carbazole	Drug Info	IC50 = 240 nM	[4]
	4'-(trifluoromethyl)-4-biphenylol	Drug Info	IC50 = 700 nM	[2]
	4'-(trifluoromethyl)-4-biphenylsulfonamide	Drug Info	IC50 = 345 nM	[2]
	4'-(trifluoromethyl)-4-biphenylyl carbamate	Drug Info	IC50 = 716 nM	[2]
	4'-(trifluoromethyl)-4-biphenylyl sulfamate	Drug Info	IC50 = 64 nM	[2]
	4'-trifluoromethyl-biphenyl-4-ylamine	Drug Info	IC50 = 1649 nM	[2]
	4-(trifluoromethyl)biphenyl	Drug Info	IC50 = 5320 nM	[2]
	7-tert-butyl-9H-carbazole-3-carboxylic acid	Drug Info	IC50 = 11000 nM	[4]
	9-methyl-2-(trifluoromethyl)-9H-carbazole	Drug Info	IC50 = 5600 nM	[4]
	9H-carbazole-2-carbaldehyde	Drug Info	IC50 = 13000 nM	[4]
	9H-carbazole-3-carbaldehyde	Drug Info	IC50 = 17000 nM	[4]
	Adociasulfate-2	Drug Info	IC50 = 7300 nM	[1]
	EMD-534085	Drug Info	IC50 = 8 nM	[3]
	Methyl 9H-carbazole-2-carboxylate	Drug Info	IC50 = 11000 nM	[4]
	Methyl[4'-(trifluoromethyl)-4-biphenylyl]amine	Drug Info	IC50 = 3726 nM	[2]
	N-(4'-bromo-3,3'-difluoro-4-biphenylyl)urea	Drug Info	IC50 = 262 nM	[2]
	N-(4'-chloro-4-biphenylyl)methanesulfonamide	Drug Info	IC50 = 2002 nM	[2]
	N-(4'-isopropyl-4-biphenylyl)urea	Drug Info	IC50 = 57 nM	[2]
	N-(4'-methyl-4-biphenylyl)urea	Drug Info	IC50 = 1382 nM	[2]
	N-(4'-t-butyl-4-biphenylyl)urea	Drug Info	IC50 = 54 nM	[2]
	N-[3'-(trifluoromethyl)-4-biphenylyl]urea	Drug Info	IC50 = 7200 nM	[2]
	N-[4'-(ethylsulfonyl)-3-fluoro-4-biphenylyl]urea	Drug Info	IC50 = 10904 nM	[2]
	N-[4'-(trifluoromethyl)-4-biphenylyl]sulfamide	Drug Info	Ki = 6.2 nM	[2]
	N-[4'-(trifluoromethyl)-4-biphenylyl]thiourea	Drug Info	IC50 = 11 nM	[2]
	N-[4'-(trifluoromethyl)-4-biphenylyl]urea	Drug Info	IC50 = 39 nM	[2]
	N-[4-(1,3-benzodioxol-5-yl)phenyl]sulfamide	Drug Info	IC50 = 7682 nM	[2]
	N-{4'-[(trifluoromethyl)sulfonyl]-4-biphenyl}urea	Drug Info	IC50 = 58 nM	[2]
	N-{4'-[(trifluoromethyl)thio]-4-biphenyl}urea	Drug Info	IC50 = 240 nM	[2]
	SB-731489	Drug Info	Ki < 1 nM	[2]
References
REF 1	Inhibition of kinesin motor proteins by adociasulfate-2. J Med Chem. 2006 Aug 10;49(16):4857-60.
REF 2	Novel ATP-competitive kinesin spindle protein inhibitors. J Med Chem. 2007 Oct 4;50(20):4939-52.
REF 3	The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1491-5.
REF 4	Kinesin spindle protein (KSP) inhibitors with 2,3-fused indole scaffolds. J Med Chem. 2010 Jul 8;53(13):5054-8.
REF 5	Structural basis for inhibition of Eg5 by dihydropyrimidines: stereoselectivity of antimitotic inhibitors enastron, dimethylenastron and fluorastrol. J Med Chem. 2010 Aug 12;53(15):5676-83.

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