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Literature summary for 5.6.1.3 extracted from

  • Parrish, C.A.; Adams, N.D.; Auger, K.R.; Burgess, J.L.; Carson, J.D.; Chaudhari, A.M.; Copeland, R.A.; Diamond, M.A.; Donatelli, C.A.; Duffy, K.J.; Faucette, L.F.; Finer, J.T.; Huffman, W.F.; Hugger, E.D.; Jackson, J.R.; Knight, S.D.; Luo, L.; Moore, M.L.; Newlander, K.A.; Ridgers, L.H.; Sakowicz, R.; Shaw, A.N.; Sung, C.-H.M.
    Novel ATP-competitive kinesin spindle protein inhibitors (2007), J. Med. Chem., 50, 4939-4952.
    View publication on PubMed
Search for more literature for 5.6.1.3

Protein Variants

Protein Variants Comment Organism
D130V mutation in the loop 5 region of the motor domain, screen of inhibitors against this mutant Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-(4'-tert-butylbiphenyl-4-yl)urea
-
 Homo sapiens
1-(4'-[(trifluoromethyl)sulfonyl]biphenyl-4-yl)urea
-
 Homo sapiens
1-[3'-fluoro-4'-(trifluoromethyl)biphenyl-4-yl]urea
-
 Homo sapiens
1-[3'-nitro-4'-(trifluoromethyl)biphenyl-4-yl]urea
-
 Homo sapiens
1-[3-fluoro-4'-(trifluoromethyl)biphenyl-4-yl]urea
-
 Homo sapiens
1-[4'-(propan-2-yl)biphenyl-4-yl]urea
-
 Homo sapiens
1-[4'-(trifluoromethyl)biphenyl-4-yl]thiourea
-
 Homo sapiens
1-[4'-(trifluoromethyl)biphenyl-4-yl]urea
-
 Homo sapiens
1-[4-(1,3-benzodioxol-5-yl)phenyl]urea
-
 Homo sapiens
1-[4-(2,2,3,3-tetrafluoro-2,3-dihydro-1,4-benzodioxin-6-yl)phenyl]urea
-
 Homo sapiens
4'-(trifluoromethyl)biphenyl-4-yl sulfamate
-
 Homo sapiens
N-(3-aminopropyl)-N-[(1R)-1-(3-benzyl-7-chloro-4-oxo-3,4-dihydroquinazolin-2-yl)-2-methylpropyl]-3-fluoro-4-methylbenzamide
-
 Homo sapiens
N-[3-amino-4'-(trifluoromethyl)biphenyl-4-yl]sulfuric diamide
-
 Homo sapiens
N-[3-chloro-4'-(trifluoromethyl)biphenyl-4-yl]sulfuric diamide
-
 Homo sapiens
N-[3-fluoro-4'-(trifluoromethyl)biphenyl-4-yl]sulfuric diamide
-
 Homo sapiens
N-[3-methoxy-4'-(trifluoromethyl)biphenyl-4-yl]sulfuric diamide
-
 Homo sapiens
N-[4'-(trifluoromethyl)biphenyl-4-yl]methanesulfonamide
-
 Homo sapiens
N-[4'-(trifluoromethyl)biphenyl-4-yl]sulfuric diamide
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
 isoform KSP
-

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000001
-
 N-(3-aminopropyl)-N-[(1R)-1-(3-benzyl-7-chloro-4-oxo-3,4-dihydroquinazolin-2-yl)-2-methylpropyl]-3-fluoro-4-methylbenzamide wild-type Homo sapiens
0.0000035
-
 N-[3-fluoro-4'-(trifluoromethyl)biphenyl-4-yl]sulfuric diamide wild-type Homo sapiens
0.000006
-
 N-[3-fluoro-4'-(trifluoromethyl)biphenyl-4-yl]sulfuric diamide mutant D130V Homo sapiens
0.0000062
-
 N-[4'-(trifluoromethyl)biphenyl-4-yl]sulfuric diamide wild-type Homo sapiens
0.000007
-
 N-[4'-(trifluoromethyl)biphenyl-4-yl]sulfuric diamide mutant D130V Homo sapiens
0.00011
-
 N-[4'-(trifluoromethyl)biphenyl-4-yl]methanesulfonamide mutant D130V Homo sapiens
0.00012
-
 N-[4'-(trifluoromethyl)biphenyl-4-yl]methanesulfonamide wild-type Homo sapiens
0.00035
-
 N-(3-aminopropyl)-N-[(1R)-1-(3-benzyl-7-chloro-4-oxo-3,4-dihydroquinazolin-2-yl)-2-methylpropyl]-3-fluoro-4-methylbenzamide mutant D130V Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000005
-
-
 Homo sapiens N-[3-fluoro-4'-(trifluoromethyl)biphenyl-4-yl]sulfuric diamide
0.000011
-
-
 Homo sapiens 1-[4'-(trifluoromethyl)biphenyl-4-yl]thiourea
0.000015
-
-
 Homo sapiens 1-[3'-fluoro-4'-(trifluoromethyl)biphenyl-4-yl]urea
0.000015
-
-
 Homo sapiens 1-[3-fluoro-4'-(trifluoromethyl)biphenyl-4-yl]urea
0.000018
-
-
 Homo sapiens N-[4'-(trifluoromethyl)biphenyl-4-yl]sulfuric diamide
0.000024
-
-
 Homo sapiens N-[3-amino-4'-(trifluoromethyl)biphenyl-4-yl]sulfuric diamide
0.000028
-
-
 Homo sapiens 1-[3'-nitro-4'-(trifluoromethyl)biphenyl-4-yl]urea
0.000031
-
-
 Homo sapiens 1-[4-(1,3-benzodioxol-5-yl)phenyl]urea
0.000039
-
-
 Homo sapiens 1-[4'-(trifluoromethyl)biphenyl-4-yl]urea
0.000054
-
-
 Homo sapiens 1-(4'-tert-butylbiphenyl-4-yl)urea
0.000057
-
-
 Homo sapiens 1-[4'-(propan-2-yl)biphenyl-4-yl]urea
0.000058
-
-
 Homo sapiens 1-(4'-[(trifluoromethyl)sulfonyl]biphenyl-4-yl)urea
0.000064
-
-
 Homo sapiens 4'-(trifluoromethyl)biphenyl-4-yl sulfamate
0.000066
-
-
 Homo sapiens N-[3-methoxy-4'-(trifluoromethyl)biphenyl-4-yl]sulfuric diamide
0.000067
-
-
 Homo sapiens 1-[4-(2,2,3,3-tetrafluoro-2,3-dihydro-1,4-benzodioxin-6-yl)phenyl]urea
0.000067
-
-
 Homo sapiens N-[3-chloro-4'-(trifluoromethyl)biphenyl-4-yl]sulfuric diamide