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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