Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
 

 

Target Validation Information
TTD IDTTDR01395
Target NamemRNA of kinesin-like 1    
Type of TargetResearch target    
Drug Potency against TargetN-[4'-(ethylsulfonyl)-3-fluoro-4-biphenylyl]ureaIC50 = 10904 nM[1]
N-[4'-(trifluoromethyl)-4-biphenylyl]thioureaIC50 = 11 nM[1]
7-tert-butyl-9H-carbazole-3-carboxylic acidIC50 = 11000 nM[2]
methyl 9H-carbazole-2-carboxylateIC50 = 11000 nM[2]
9H-carbazole-2-carbaldehydeIC50 = 13000 nM[2]
N-(4'-methyl-4-biphenylyl)ureaIC50 = 1382 nM[1]
2-tert-butyl-7-(trifluoromethyl)-9H-carbazoleIC50 = 1400 nM[2]
1-tert-butyl-9H-carbazoleIC50 = 14000 nM[2]
2-isopropyl-9H-carbazoleIC50 = 1500 nM[2]
2,3,4,11-tetrahydro-1H-benzo[a]carbazoleIC50 = 1600 nM[2]
4'-trifluoromethyl-biphenyl-4-ylamineIC50 = 1649 nM[1]
9H-carbazole-3-carbaldehydeIC50 = 17000 nM[2]
(S)-dimethylenastronIC50 = 200 nM[3]
(S)-enastronIC50 = 2000 nM[3]
N-(4'-chloro-4-biphenylyl)methanesulfonamideIC50 = 2002 nM[1]
3-tert-butyl-9H-carbazoleIC50 = 240 nM[2]
N-{4'-[(trifluoromethyl)thio]-4-biphenyl}ureaIC50 = 240 nM[1]
N-(4'-bromo-3,3'-difluoro-4-biphenylyl)ureaIC50 = 262 nM[1]
2-ethyl-9H-carbazoleIC50 = 2800 nM[2]
2-tert-butoxy-9H-carbazoleIC50 = 3200 nM[2]
1-(trifluoromethyl)-9H-carbazoleIC50 = 3300 nM[2]
4'-(trifluoromethyl)-4-biphenylsulfonamideIC50 = 345 nM[1]
methyl[4'-(trifluoromethyl)-4-biphenylyl]amineIC50 = 3726 nM[1]
N-[4'-(trifluoromethyl)-4-biphenylyl]ureaIC50 = 39 nM[1]
11H-benzo[a]carbazoleIC50 = 4600 nM[2]
2-(trifluoromethoxy)-9H-carbazoleIC50 = 510 nM[2]
4-(trifluoromethyl)biphenylIC50 = 5320 nM[1]
N-(4'-t-butyl-4-biphenylyl)ureaIC50 = 54 nM[1]
9-methyl-2-(trifluoromethyl)-9H-carbazoleIC50 = 5600 nM[2]
N-(4'-isopropyl-4-biphenylyl)ureaIC50 = 57 nM[1]
N-{4'-[(trifluoromethyl)sulfonyl]-4-biphenyl}ureaIC50 = 58 nM[1]
4'-(trifluoromethyl)-4-biphenylyl sulfamateIC50 = 64 nM[1]
4'-(trifluoromethyl)-4-biphenylolIC50 = 700 nM[1]
4'-(trifluoromethyl)-4-biphenylyl carbamateIC50 = 716 nM[1]
N-[3'-(trifluoromethyl)-4-biphenylyl]ureaIC50 = 7200 nM[1]
adociasulfate-2IC50 = 7300 nM[4]
N-[4-(1,3-benzodioxol-5-yl)phenyl]sulfamideIC50 = 7682 nM[1]
EMD-534085IC50 = 8 nM[5]
2-(difluoromethyl)-9H-carbazoleIC50 = 870 nM[2]
SB-731489Ki < 1 nM[1]
N-[4'-(trifluoromethyl)-4-biphenylyl]sulfamideKi = 6.2 nM[1]
Ref 1J Med Chem. 2007 Oct 4;50(20):4939-52. Epub 2007 Aug 29.Novel ATP-competitive kinesin spindle protein inhibitors. To Reference
Ref 2J Med Chem. 2010 Jul 8;53(13):5054-8.Kinesin spindle protein (KSP) inhibitors with 2,3-fused indole scaffolds. To Reference
Ref 3J Med Chem. 2010 Aug 12;53(15):5676-83.Structural basis for inhibition of Eg5 by dihydropyrimidines: stereoselectivity of antimitotic inhibitors enastron, dimethylenastron and fluorastrol. To Reference
Ref 4J Med Chem. 2006 Aug 10;49(16):4857-60.Inhibition of kinesin motor proteins by adociasulfate-2. To Reference
Ref 5Bioorg Med Chem Lett. 2010 Mar 1;20(5):1491-5. Epub 2010 Jan 25.The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5. To Reference



 

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National University of Singapore, Singapore


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