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5,5'-dithiobis(2-nitrobenzoic acid)
-
adenosine
competitive with MgATP2-
Choline analogues
several compounds tested and found to be inhibitory
choline kinase inhibitor Mn58b
-
-
(1-azabicyclo[2.2.2]octan-3-yl)bis(5-chlorothiophen-2-yl)methanol
(1S)-1-[(3R)-1-azabicyclo[2.2.2]octan-3-yl]-3-[2-[(oxan-4-yl)oxy]phenyl]-1-phenylpropan-1-ol
(4-methyl-1,4-diazepan-1-yl)(4'-((4-methyl-1,4-diazepan-1-yl)-methyl)-[1,1'-biphenyl]-4-yl)methanone
(azepan-1-yl)(piperazin-1-yl)methanone
-
1,1',1''-(benzene-1,3,5-triylmethylene)tris[(4-dimethylamino)pyridinium] tribromide
-
1,1',1''-(benzene-1,3,5-triylmethylene)tris[4-(3,5-dichloro-N-methylanilino)pyridinium] tribromide
-
1,1',1''-(benzene-1,3,5-triylmethylene)tris[4-(4-chloro-N-methylanilino)pyridinium] tribromide
-
1,1',1''-(benzene-1,3,5-triylmethylene)tris[4-(N-methylanilino)pyridinium] tribromide
-
1,1',1''-(benzene-1,3,5-triylmethylene)tris[4-(piperidino)pyridinium] tribromide
-
1,1',1''-(benzene-1,3,5-triylmethylene)tris[4-(pyrrolidino)pyridinium] tribromide
-
1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(3-hydroxyquinuclidinium) bromide
-
1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(4-((4-chlorophenyl)(methyl)amino)pyridinium) bromide
-
1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(4-((4-chlorophenyl)(methyl)amino)quinolinium) bromide
-
1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(4-(azepan-1-yl)-7-chloroquinolinium) bromide
-
1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(4-(azepan-1-yl)quinolinium) bromide
-
1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(4-(dimethylamino)pyridinium) bromide
-
1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(4-(methyl(phenyl)amino)quinolinium) bromide
-
1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(4-(pyrrolidin-1-yl)pyridinium) bromide
-
1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(7-chloro-4-((4-chlorophenyl)(methyl)amino)quinolinium) bromide
-
1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(7-chloro-4-(methyl(phenyl)amino)quinolinium) bromide
-
1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(7-chloro-4-(pyrrolidin-1-yl)quinolinium) bromide
-
1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(quinuclidinium) bromide
-
1,1'-(benzene-1,3-diyldimethanediyl)bis(4-piperidin-1-ylpyridinium) dibromide
-
IC50: 0.0528 mM
1,1'-(benzene-1,3-diyldimethanediyl)bis(4-pyrrolidin-1-ylpyridinium) dibromide
-
IC50: 0.0842 mM
1,1'-(benzene-1,3-diyldimethanediyl)bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide
-
IC50: 0.0084 mM
1,1'-(benzene-1,3-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]pyridinium) dibromide
-
IC50: 0.0072 mM
1,1'-(benzene-1,3-diyldimethanediyl)bis[4-[(phenylamino)methyl]pyridinium] dibromide
-
IC50: 0.0375 mM
1,1'-(benzene-1,3-diylmethylene)bis[(4-dimethylamino)pyridinium] dibromide
-
1,1'-(benzene-1,3-diylmethylene)bis[4-(N-methylanilino)pyridinium] dibromide
-
1,1'-(benzene-1,3-diylmethylene)bis[4-(piperidino)pyridinium] dibromide
-
1,1'-(benzene-1,3-diylmethylene)bis[4-(pyrrolidino)pyridinium] dibromide
-
1,1'-(benzene-1,4-diyldimethanediyl)bis(4-piperidin-1-ylpyridinium) dibromide
-
IC50: 0.0377 mM
1,1'-(benzene-1,4-diyldimethanediyl)bis(4-pyrrolidin-1-ylpyridinium) dibromide
-
IC50: 0.024 mM
1,1'-(benzene-1,4-diyldimethanediyl)bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide
-
IC50: 0.0097 mM
1,1'-(benzene-1,4-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]pyridinium) dibromide
-
IC50: 0.0029 mM
1,1'-(benzene-1,4-diyldimethanediyl)bis[4-[(phenylamino)methyl]pyridinium] dibromide
-
IC50: 0.015 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-amino-3-methylquinolinium) dibromide
-
IC50: 0.0119 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-amino-7-chloroquinolinium) dibromide
-
IC50: 0.0206 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-aminoquinolinium) dibromide
-
IC50: 0.0012 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-azepan-1-ylquinolinium) dibromide
-
IC50: 0.0005 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-piperidin-1-ylpyridinium) dibromide
-
IC50: 0.0019 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-pyrrolidin-1-ylpyridinium) dibromide
-
IC50: 0.0058 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide
-
IC50: 0.0026 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]pyridinium) dibromide
-
IC50: 0.0015 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide
-
IC50: 0.0021 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(7-amino-4-[[(4-chlorophenyl)amino]methyl]-8-methylquinolinium) dibromide
-
IC50: 0.147 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(7-chloro-4-pyrrolidin-1-ylquinolinium) dibromide
-
IC50: 0.0012 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(7-chloro-4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide
-
IC50: 0.0057 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[4-(dimethylamino)quinolinium] dibromide
-
IC50: 0.0044 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[4-(phenylamino)quinolinium] dibromide
-
IC50: 0.0013 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[4-[(phenylamino)methyl]pyridinium] dibromide
-
IC50: 0.00043 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[4-[(phenylamino)methyl]quinolinium] dibromide
-
IC50: 0.0004 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[7-amino-8-methyl-4-[(phenylamino)methyl]quinolinium] dibromide
-
IC50: 0.0568 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[7-chloro-4-(dimethylamino)quinolinium] dibromide
-
IC50: 0.0096 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[7-chloro-4-[(phenylamino)methyl]quinolinium] dibromide
-
IC50: 0.0031 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-amino-3-methylquinolinium) dibromide
-
IC50: above 0.2 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-amino-7-chloroquinolinium) dibromide
-
IC50: 0.0633 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-aminoquinolinium) dibromide
-
IC50: 0.0811 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-azepan-1-ylquinolinium) dibromide
-
IC50: 0.0022 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-piperidin-1-ylpyridinium) dibromide
-
IC50: 0.0088 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-pyrrolidin-1-ylpyridinium) dibromide
-
IC50: 0.0111 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide
-
IC50: 0.0034 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]pyridinium) dibromide
-
IC50: 0.0018 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide
-
IC50: 0.002 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(7-amino-4-[[(4-chlorophenyl)amino]methyl]-8-methylquinolinium) dibromide
-
IC50: 0.0461 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(7-chloro-4-pyrrolidin-1-ylquinolinium) dibromide
-
IC50: 0.0198 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(7-chloro-4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide
-
IC50: 0.0114 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[4-(dimethylamino)quinolinium] dibromide
-
IC50: 0.0397 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[4-(phenylamino)quinolinium] dibromide
-
IC50: 0.0178 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[4-[(phenylamino)methyl]pyridinium] dibromide
-
IC50: 0.0043 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[4-[(phenylamino)methyl]quinolinium] dibromide
-
IC50: 0.003 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[7-amino-8-methyl-4-[(phenylamino)methyl]quinolinium] dibromide
-
IC50: 0.0961 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[7-chloro-4-(dimethylamino)quinolinium] dibromide
-
IC50: 0.0206 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[7-chloro-4-[(phenylamino)methyl]quinolinium] dibromide
-
IC50: 0.0114 mM
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis(4-aminoquinolinium)
-
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis(4-azepan-1-ylquinolinium)
-
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[4-(dimethylamino)quinolinium]
-
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[4-(phenylamino)quinolinium]
-
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[4-[(4-chlorophenyl)(methyl)amino]quinolinium]
-
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[4-[methyl(phenyl)amino]quinolinium]
-
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[7-amino-4-[(4-chlorophenyl)(methyl)amino]-8-methylquinolinium]
-
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[7-amino-8-methyl-4-[methyl(phenyl)amino]quinolinium]
-
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[7-chloro-4-(dimethylamino)quinolinium]
-
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[7-chloro-4-[(4-chlorophenyl)(methyl)amino]quinolinium]
-
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[7-chloro-4-[methyl(phenyl)amino]quinolinium]
-
1,1'-biphenyl-3,3'-diylbis(4-amino-3-methylquinolinium)
-
1,1'-biphenyl-3,3'-diylbis(4-amino-7-chloroquinolinium)
-
1,1'-biphenyl-3,3'-diylbis(4-aminoquinolinium)
-
1,1'-biphenyl-3,3'-diylbis(4-azepan-1-ylquinolinium)
-
1,1'-biphenyl-3,3'-diylbis(7-chloro-4-pyrrolidin-1-ylquinolinium)
-
1,1'-biphenyl-3,3'-diylbis[4-(dimethylamino)quinolinium]
-
1,1'-biphenyl-3,3'-diylbis[4-(phenylamino)quinolinium]
-
1,1'-biphenyl-3,3'-diylbis[4-[(4-chlorophenyl)(methyl)amino]quinolinium]
-
1,1'-biphenyl-3,3'-diylbis[4-[methyl(phenyl)amino]quinolinium]
-
1,1'-biphenyl-3,3'-diylbis[7-amino-4-[(4-chlorophenyl)(methyl)amino]-8-methylquinolinium]
-
1,1'-biphenyl-3,3'-diylbis[7-amino-8-methyl-4-[methyl(phenyl)amino]quinolinium]
-
1,1'-biphenyl-3,3'-diylbis[7-chloro-4-(dimethylamino)quinolinium]
-
1,1'-biphenyl-3,3'-diylbis[7-chloro-4-[(4-chlorophenyl)(methyl)amino]quinolinium]
-
1,1'-biphenyl-3,3'-diylbis[7-chloro-4-[methyl(phenyl)amino]quinolinium]
-
1,1'-biphenyl-4,4'-diylbis(4-amino-7-chloroquinolinium)
-
1,1'-biphenyl-4,4'-diylbis(4-aminoquinolinium)
-
1,1'-biphenyl-4,4'-diylbis(4-azepan-1-ylquinolinium)
-
1,1'-biphenyl-4,4'-diylbis(7-chloro-4-pyrrolidin-1-ylquinolinium)
-
1,1'-biphenyl-4,4'-diylbis[4-(dimethylamino)quinolinium]
-
1,1'-biphenyl-4,4'-diylbis[4-(phenylamino)quinolinium]
-
1,1'-biphenyl-4,4'-diylbis[4-[(4-chlorophenyl)(methyl)amino]quinolinium]
-
1,1'-biphenyl-4,4'-diylbis[4-[methyl(phenyl)amino]quinolinium]
-
1,1'-biphenyl-4,4'-diylbis[7-amino-4-[(4-chlorophenyl)(methyl)amino]-8-methylquinolinium]
-
1,1'-biphenyl-4,4'-diylbis[7-amino-8-methyl-4-[methyl(phenyl)amino]quinolinium]
-
1,1'-biphenyl-4,4'-diylbis[7-chloro-4-(dimethylamino)quinolinium]
-
1,1'-biphenyl-4,4'-diylbis[7-chloro-4-[(4-chlorophenyl)(methyl)amino]quinolinium]
-
1,1'-biphenyl-4,4'-diylbis[7-chloro-4-[methyl(phenyl)amino]quinolinium]
-
1,1'-[(1S,2S)-cyclopropane-1,2-diyldiethane-2,1-diyl]bis(4-piperidin-1-ylpyridinium) dibromide
-
IC50: 0.098 mM
1,1'-[(1S,2S)-cyclopropane-1,2-diyldiethane-2,1-diyl]bis(4-pyrrolidin-1-ylpyridinium) dibromide
-
IC50: above 0.1 mM
1,1'-[(1S,2S)-cyclopropane-1,2-diyldiethane-2,1-diyl]bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide
1,1'-[(1S,2S)-cyclopropane-1,2-diyldiethane-2,1-diyl]bis[4-[(phenylamino)methyl]pyridinium] dibromide
-
IC50: above 0.1 mM
1,1'-[butane-1,4-diylbis[(4,1-phenylene)methylene]]bis[4-(dimethylamino)pyridin-1-ium]
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(4-amino-7-chloroquinolinium) dibromide
-
IC50: above 0.2 mM
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(4-aminoquinolinium) dibromide
-
IC50: 0.08 mM
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(4-azepan-1-ylquinolinium) dibromide
-
IC50: 0.006 mM
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide
-
IC50: 0.0048 mM
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(7-amino-4-[[(4-chlorophenyl)amino]methyl]-8-methylquinolinium) dibromide
-
IC50: 0.0575 mM
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(7-chloro-4-pyrrolidin-1-ylquinolinium) dibromide
-
IC50: 0.001 mM
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(7-chloro-4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide
-
IC50: 0.0057 mM
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[4-(dimethylamino)quinolinium] dibromide
-
IC50: 0.0102 mM
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[4-(phenylamino)quinolinium] dibromide
-
IC50: 0.0023 mM
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[4-[(phenylamino)methyl]quinolinium] dibromide
-
IC50: 0.0014 mM
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[7-amino-8-methyl-4-[(phenylamino)methyl]quinolinium] dibromide
-
IC50: 0.133 mM
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[7-chloro-4-(dimethylamino)quinolinium] dibromide
-
IC50: 0.009 mM
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[7-chloro-4-[(phenylamino)methyl]quinolinium] dibromide
-
IC50: 0.0035 mM
1,1'-[[1,1'-biphenyl]-4,4'-diylbis(methylene)]bis[4-[(4-chlorophenyl)(methyl)amino]quinolin-1-ium]
RSM-932A or TDC-717, a potential cancer therapeutic agent targeting choline metabolism, strong inhibition
1-((4'-methoxy-[1,1'-biphenyl]-4-yl)methyl)-4-methyl-1,4-diazepane
1-(4-(4-[(3-aminophenoxy)methyl]phenethyl)benzyl)-4-(dimethylamino)pyridinium bromide
21.9% inhibition at 0.05 mM
1-(4-[4-[(3-hydroxyphenylamino)methyl]phenethyl]-benzyl)-4-(pyrrolidin-1-yl)pyridinium bromide
13.6% inhibition at 0.05 mM
1-(4-[4-[(6-amino-3H-purin-3-yl)methyl]phenethyl]benzyl)-4-pyrrolidinopyridinium bromide
0.1% inhibition at 0.01 mM, 24.8% inhibition at 0.05 mM
1-(4-[4-[(6-amino-3H-purin-3-yl)methyl]phenyl]benzyl)-4-(dimethylamino)pyridinium bromide
62.3% inhibition at 0.01 mM, 71.4% inhibition at 0.05 mM
1-(4-[4-[(6-amino-9H-purin-9-yl)methyl]phenethyl]benzyl)-4-(dimethylamino)pyridinium bromide
38.6% inhibition at 0.01 mM, 81% inhibition at 0.05 mM
1-(4-[4-[(6-amino-9H-purin-9-yl)methyl]phenethyl]benzyl)-4-pyrrolidinopyridinium bromide
28.6% inhibition at 0.01 mM, 46.9% inhibition at 0.05 mM
1-(4-[4-[(6-amino-9H-purin-9-yl)methyl]phenyl]benzyl)-4-(dimethylamino)pyridinium bromide
37.6% inhibition at 0.01 mM, 51% inhibition at 0.05 mM
1-(4-[4-[(6-amino-9H-purin-9-yl)methyl]phenyl]benzyl)-4-pyrrolidinopyridinium bromide
50.2% inhibition at 0.01 mM, 72.8% inhibition at 0.05 mM
1-([1,1'-biphenyl]-4-ylmethyl)-4-methyl-1,4-diazepane
-
1-([4'-[(3-aminophenoxy)methyl]biphenyl-4-yl]methyl)-4-(dimethylamino)pyridinium bromide
79.8% inhibition at 0.05 mM
1-([4'-[(3-aminophenoxy)methyl]biphenyl-4-yl]methyl)-4-(pyrrolidin-1-yl)pyridinium bromide
20.8% inhibition at 0.05 mM
1-([4'-[(3-hydroxyphenylamino)methyl]biphenyl-4-yl]-methyl)-4-(pyrrolidin-1-yl)-pyridinium bromide
28.2% inhibition at 0.05 mM
1-([4'-[(6-amino-9H-purin-9-yl)methyl][1,1'-biphenyl]-4-yl]methyl)-4-(dimethylamino)pyridin-1-ium bromide
-
1-([4'-[(6-amino-9H-purin-9-yl)methyl][1,1'-biphenyl]-4-yl]methyl)-4-(pyrrolidin-1-yl)pyridin-1-ium bromide
-
1-([4-[(6-amino-9H-purin-9-yl)methyl]phenyl]methyl)-4-(dimethylamino)pyridin-1-ium bromide
-
1-([4-[(6-amino-9H-purin-9-yl)methyl]phenyl]methyl)-4-(pyrrolidin-1-yl)pyridin-1-ium bromide
-
1-([4-[2-(4-[[6-(benzylsulfanyl)-9H-purin-9-yl]methyl]phenyl)ethyl]phenyl]methyl)-4-(dimethylamino)pyridin-1-ium bromide
-
1-([4-[2-(4-[[6-(benzylsulfanyl)-9H-purin-9-yl]methyl]phenyl)ethyl]phenyl]methyl)-4-(pyrrolidin-1-yl)pyridin-1-ium bromide
-
1-([4-[4-(4-[[6-(benzylsulfanyl)-9H-purin-9-yl]methyl]phenyl)butyl]phenyl]methyl)-4-(dimethylamino)pyridin-1-ium bromide
-
1-([4-[4-(4-[[6-(benzylsulfanyl)-9H-purin-9-yl]methyl]phenyl)butyl]phenyl]methyl)-4-(pyrrolidin-1-yl)pyridin-1-ium bromide
-
1-methyl-4-((4'-(4-methylpiperazin-1-yl)-[1,1'-biphenyl]-4-yl)-methyl)-1,4-diazepane
1-methyl-4-((4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)methyl)-1,4-diazepane
1-methyl-4-(naphthalen-2-ylmethyl)-1,4-diazepane
1-[(4'-[[6-(benzylsulfanyl)-9H-purin-9-yl]methyl][1,1'-biphenyl]-4-yl)methyl]-4-(dimethylamino)pyridin-1-ium bromide
-
1-[(4'-[[6-(benzylsulfanyl)-9H-purin-9-yl]methyl][1,1'-biphenyl]-4-yl)methyl]-4-(pyrrolidin-1-yl)pyridin-1-ium bromide
-
1-[(4-[4-[4-([4-[(4-chlorophenyl)(methyl)amino]pyridin-1-ium-1-yl]methyl)phenyl]butyl]phenyl)methyl]-4-(dimethylamino)pyridin-1-ium
-
1-[(4-[4-[4-([4-[(4-chlorophenyl)(methyl)amino]pyridin-1-ium-1-yl]methyl)phenyl]butyl]phenyl)methyl]-4-(dimethylamino)pyridin-1-ium dibromide
-
1-[(4-[[6-(benzylsulfanyl)-9H-purin-9-yl]methyl]phenyl)methyl]-4-(dimethylamino)pyridin-1-ium bromide
-
1-[(4-[[6-(benzylsulfanyl)-9H-purin-9-yl]methyl]phenyl)methyl]-4-(pyrrolidin-1-yl)pyridin-1-ium bromide
-
1-[4'-[(6-amino-9H-purin-9-yl)methyl][1,1'-biphenyl]-4-yl]-4-(dimethylamino)pyridin-1-ium bromide
-
1-[4-(4-[4-[(3-aminophenoxy)methyl]phenyl]butyl)-benzyl]-4-(pyrrolidin-1-yl)pyridinium bromide
21.6% inhibition at 0.05 mM
1-[4-(4-[4-[(3-hydroxyphenylamino)methyl]phenyl]-butyl)benzyl]-4-(pyrrolidin-1-yl)pyridinium bromide
18% inhibition at 0.05 mM
1-[4-(4-[4-[(6-amino-3H-purin-3-yl)methyl]phenyl]butyl)benzyl]-4-(dimethylamino)pyridinium bromide
61.3% inhibition at 0.01 mM, 68.2% inhibition at 0.05 mM
1-[4-(4-[4-[(6-amino-3H-purin-3-yl)methyl]phenyl]butyl)benzyl]-4-pyrrolidinopyridinium bromide
22.6% inhibition at 0.01 mM, 59.9% inhibition at 0.05 mM
1-[4-(4-[4-[(6-amino-9H-purin-9-yl)methyl]phenyl]butyl)benzyl]-4-(dimethylamino)pyridinium bromide
66.7% inhibition at 0.01 mM, 89.7% inhibition at 0.05 mM
1-[4-(4-[4-[(6-amino-9H-purin-9-yl)methyl]phenyl]butyl)benzyl]-4-pyrrolidinopyridinium bromide
36.9% inhibition at 0.01 mM, 41.9% inhibition at 0.05 mM
1-[4-[(3-aminophenoxy)methyl]benzyl]-4-(dimethylamino)pyridinium bromide
37.7% inhibition at 0.05 mM
1-[4-[(3-aminophenoxy)methyl]benzyl]-4-(pyrrolidin-1-yl)pyridinium bromide
12.9% inhibition at 0.05 mM
1-[4-[(3-hydroxyphenylamino)methyl]benzyl]-4-(pyrrolidin-1-yl)pyridinium bromide
41.3% inhibition at 0.05 mM
1-[4-[(4-methyl-1,4-diazepan-1-yl)methyl]phenyl]methanamine
analysis of the enzyme bound structure, PDB ID 5EQE
1-[4-[(6-amino-3H-purin-3-yl)methyl]benzyl]-4-(dimethylamino)pyridinium bromide
25% inhibition at 0.01 mM, 50.2% inhibition at 0.05 mM
1-[4-[(6-amino-9H-purin-9-yl)methyl]benzyl]-4-(dimethylamino)pyridinium bromide
46.7% inhibition at 0.01 mM, 54.1% inhibition at 0.05 mM
1-[4-[(6-amino-9H-purin-9-yl)methyl]benzyl]-4-pyrrolidinopyridinium bromide
27% inhibition at 0.05 mM
1-[[4-(2-[4-[(6-amino-9H-purin-9-yl)methyl]phenyl]ethyl)phenyl]methyl]-4-(dimethylamino)pyridin-1-ium bromide
-
1-[[4-(2-[4-[(6-amino-9H-purin-9-yl)methyl]phenyl]ethyl)phenyl]methyl]-4-(pyrrolidin-1-yl)pyridin-1-ium bromide
-
1-[[4-(4-[4-[(6-amino-9H-purin-9-yl)methyl]phenyl]butyl)phenyl]methyl]-4-(dimethylamino)pyridin-1-ium bromide
1-[[4-(4-[4-[(6-amino-9H-purin-9-yl)methyl]phenyl]butyl)phenyl]methyl]-4-(pyrrolidin-1-yl)pyridin-1-ium bromide
-
1-[[4-[4-[[4-(4-chloro-N-methylanilino)quinolin-1-ium-1-yl]methyl]phenyl]phenyl]methyl]-N-(4-chlorophenyl)-N-methylquinolin-1-ium-4-amine
i.e. TCD-717 or RSM-932A, strong inhibition of ChoKalpha, TCD-717 does not bind directly in the choline pocket but rather in a proximal location near the surface of the enzyme. Most notably, residues Tyr148, Ala176, Met177, Glu180, Phe200, Pro201, Trp248, Thr252, Tyr256, Glu332, Tyr333, Phe341, and Leu419 serve to orient and hold TCD-717 in place. Interaction of TCD-717 with ChoKalpha is driven by hydrophobic interactions across the N- and C-terminal domains. Binding of TCD-717 induces conformational changes compared to the unbound ChoKalpha structure. TCD-717 has completed phase I clinical trials
12,19-diaza-1,8-diazoniapentacyclo[18.2.2.23,6.28,11.214,17]triaconta-1(22),3,5,8,10,14,16,20,23,25,27,29-dodecaene dibromide
-
IC50: 0.0132 mM
12,21-diaza-1,8-diazoniapentacyclo[20.2.2.23,6.28,11.014,19]triaconta-1(24),3,5,8,10,14,16,18,22,25,27,29-dodecaene dibromide
-
IC50: 0.0021 mM
14,21-diaza-1,10-diazoniapentacyclo[20.2.2.210,13.216,19.03,8]triaconta-1(24),3,5,7,10,12,16,18,22,25,27,29-dodecaene dibromide
2'-fluoro-4,4'-bis((4-methyl-1,4-diazepan-1-yl)methyl)-[1,1'-biphenyl]-2-carbonitrile
4'-bispyridyl-5,5'-perfluoroalkyl-2,2'-bisoxazol
-
-
-
4,4'-((2,3-difluoro-[1,1'-biphenyl]-4,4'-diyl)bis(methylene))bis-(1-methyl-1,4-diazepane)
4,4'-((2-fluoro-[1,1'-biphenyl]-4,4'-diyl)bis(methylene))bis(1-methyl-1,4-diazepane)
4,4'-((3,5-difluoro-[1,1'-biphenyl]-4,4'-diyl)bis(methylene))bis-(1-methyl-1,4-diazepane)
4,4'-((3-chloro-[1,1'-biphenyl]-4,4'-diyl)bis(methylene))bis(1-methyl-1,4-diazepane)
4,4'-bis((4-methyl-1,4-diazepan-1-yl)methyl)-1,1'-biphenyl
4,4'-bis((4-methyl-1,4-diazepan-1-yl)methyl)-[1,1'-biphenyl]-2-carbonitrile
4-(4-chloro-N-methylanilino)-1-(4-[4-[(4-dimethylaminopyridinium-1-yl)methyl]phenethyl]benzyl)pyridinium dibromide
-
4-(4-chloro-N-methylanilino)-1-(4-[4-[(4-dimethylaminopyridinium-1-yl)methyl]phenyl]benzyl)pyridinium dibromide
-
4-(4-chloro-N-methylanilino)-1-(4-[4-[(4-pyrrolidinopyridinium-1-yl)methyl]phenethyl]benzyl)pyridinium dibromide
-
4-(4-chloro-N-methylanilino)-1-(4-[4-[(4-pyrrolidinopyridinium-1-yl)methyl]phenyl]benzyl)pyridinium dibromide
-
4-(4-chloro-N-methylanilino)-1-[4-(4-[4-[(4-dimethylaminopyridinium-1-yl)methyl]phenyl]butyl)benzyl]pyridinium dibromide
-
4-(4-chloro-N-methylanilino)-1-[4-(4-[4-[(4-pyrrolidinopyridinium-1-yl)methyl]phenyl]butyl)benzyl]pyridinium dibromide
-
4-(4-chloro-N-methylanilino)-1-[4-[(4-dimethylaminopyridinium-1-yl)methyl]benzyl]pyridinium dibromide
-
4-(4-chloro-N-methylanilino)-1-[4-[(4-pyrrolidinopyridinium-1-yl)methyl]benzyl]pyridinium dibromide
-
4-(dimethylamino)-1-(4-(3-(4-(((3-hydroxyphenyl)amino)methyl)phenyl)propyl)benzyl)pyridin-1-ium bromide
12.9% inhibition at 0.05 mM
4-(dimethylamino)-1-(4-(4-(((3-hydroxyphenyl)amino)methyl)benzyl)benzyl)pyridin-1-ium bromide
39.5% inhibition at 0.05 mM
4-(dimethylamino)-1-(4-[4-[(4-pyrrolidinopyridinium-1-yl)-methyl]phenethyl]benzyl)pyridinium dibromide
-
4-(dimethylamino)-1-(4-[4-[(4-pyrrolidinopyridinium-1-yl)-methyl]phenyl]benzyl)pyridinium dibromide
-
4-(dimethylamino)-1-({4-[(3-hydroxyphenylamino)-methyl]biphenyl-4-yl}methyl)pyridinium bromide
66.2% inhibition at 0.05 mM
4-(dimethylamino)-1-[4-(4-[4-[(4-pyrrolidinopyridinium-1-yl)-methyl]phenyl]butyl)benzyl]pyridinium dibromide
-
4-(dimethylamino)-1-[4-[(3-hydroxyphenylamino)-methyl]benzyl]pyridinium bromide
52.4% inhibition at 0.05 mM
4-(dimethylamino)-1-[4-[(4-pyrrolidinopyridinium-1-yl)methyl]-benzyl]pyridinium dibromide
-
4-chloro-N-methylanilino
-
IC50: 0.0014 mM
4-[(4-chlorophenyl)(methyl)amino]-1-[(4'-[[4-(dimethylamino)phenyl]methyl][1,1'-biphenyl]-4-yl)methyl]pyridin-1-ium bromide
-
5'-dithio-bis-(2-nitrobenzoic acid)
-
modest inhibitory activity
5,10,11,16,17,22-hexahydro-6,9:18,21-diethenodibenzo[g,p][1,5,10,14]tetraazacyclooctadecine-6,21-diium dibromide
-
IC50: 0.0248 mM
5-fluorouracil
-
Investigation of the effect of combining transient siRNA-chk transfection with the anticancer drug 5-fluorouracil on cell viability and proliferation. Choline kinase down-regulation with 5-fluorouracil treatment increased cell kill in cancer cells.
6-(trifluoromethyl)pyrimidin-4-amine
-
6-amino-3-([4-[4-(4-[[4-(dimethylamino)pyridin-1-ium-1-yl]methyl]phenyl)butyl]phenyl]methyl)-9H-purin-3-ium
-
6-amino-3-([4-[4-(4-[[4-(pyrrolidin-1-yl)pyridin-1-ium-1-yl]methyl]phenyl)butyl]phenyl]methyl)-9H-purin-3-ium
-
6-amino-3-[(4'-[[4-(dimethylamino)pyridin-1-ium-1-yl]methyl][1,1'-biphenyl]-4-yl)methyl]-9H-purin-3-ium
6-amino-3-[(4-[[4-(dimethylamino)pyridin-1-ium-1-yl]methyl]phenyl)methyl]-9H-purin-3-ium
-
6-[(1-methyl-1,4-diazepan-6-yl)methyl]quinoline
-
7-((4-methyl-1,4-diazepan-1-yl)methyl)quinolone
7-chloro-1-(4-[2-[4-(7-chloro-5-pyrrolidin-1-ylquinolinium-1-yl)phenyl]ethyl]phenyl)-4-pyrrolidin-1-ylquinolinium
-
choline kinase inhibitor Mn58b
-
choline kinase inhibitor TCD828
-
-
-
methyl 4'-((4-methyl-1,4-diazepan-1-yl)methyl)-[1,1'-biphenyl]-4-carboxylate
N-(3,5-dimethylphenyl)-2-[[5-(4-ethylphenyl)-1H-1,2,4-triazol-3-yl]sulfanyl]acetamide
CK37, identified through computational virtual screening, inhibits ChoKalpha activity both in enzymatic and in cellular assays, is able to suppress pCho production and tumor growth in vivo
N-ethylmaleimide
-
modest inhibitory activity
N-[2-bromocinnamyl(amino)ethyl]-5-isoquinoline sulfonamide
-
-
piperazine
-
modest inhibitory activity
purinyl-6-histamine
-
modest inhibitory activity
Quinacrine
-
indirect inhibitor
RSM932A
also called TCD-717
[4-(4-methyl-1,4-diazepan-1-yl)phenyl]methanol
-
hemicholinium-3
-
hemicholinium-3
competitive inhibitor, the inhibitory effect of hemicholinium-3 is about 500times higher toward the ChoKalpha isoforms than ChoKbeta isoform
(1-azabicyclo[2.2.2]octan-3-yl)bis(5-chlorothiophen-2-yl)methanol
-
(1-azabicyclo[2.2.2]octan-3-yl)bis(5-chlorothiophen-2-yl)methanol
precursor of (1S)-1-[(3R)-1-azabicyclo[2.2.2]octan-3-yl]-3-[2-[(oxan-4-yl)oxy]phenyl]-1-phenylpropan-1-ol, inhibits competitively against ATP, but not against choline
(1S)-1-[(3R)-1-azabicyclo[2.2.2]octan-3-yl]-3-[2-[(oxan-4-yl)oxy]phenyl]-1-phenylpropan-1-ol
-
(1S)-1-[(3R)-1-azabicyclo[2.2.2]octan-3-yl]-3-[2-[(oxan-4-yl)oxy]phenyl]-1-phenylpropan-1-ol
a structure-directed, selective ChoKalpha inhibitor. Treatment of HeLa cells and other cancer cells with the compound leads to a substantial reduction in the pCho level, and causes a reversible growth arrest but not cell death
(4-methyl-1,4-diazepan-1-yl)(4'-((4-methyl-1,4-diazepan-1-yl)-methyl)-[1,1'-biphenyl]-4-yl)methanone
-
(4-methyl-1,4-diazepan-1-yl)(4'-((4-methyl-1,4-diazepan-1-yl)-methyl)-[1,1'-biphenyl]-4-yl)methanone
-
1,1'-[(1S,2S)-cyclopropane-1,2-diyldiethane-2,1-diyl]bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide
-
IC50: above 0.1 mM
1,1'-[(1S,2S)-cyclopropane-1,2-diyldiethane-2,1-diyl]bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide
-
IC50: 0.0482 mM
1,1'-[butane-1,4-diylbis[(4,1-phenylene)methylene]]bis[4-(dimethylamino)pyridin-1-ium]
-
1,1'-[butane-1,4-diylbis[(4,1-phenylene)methylene]]bis[4-(dimethylamino)pyridin-1-ium]
a less toxic derivative of hemicholinium-3, it inhibits endogenous ChoKbeta activity and suppress breast cancer, colon cancer, and epidermoid carcinoma xenograft growth in vivo
1-((4'-methoxy-[1,1'-biphenyl]-4-yl)methyl)-4-methyl-1,4-diazepane
-
1-((4'-methoxy-[1,1'-biphenyl]-4-yl)methyl)-4-methyl-1,4-diazepane
-
1-methyl-4-((4'-(4-methylpiperazin-1-yl)-[1,1'-biphenyl]-4-yl)-methyl)-1,4-diazepane
-
1-methyl-4-((4'-(4-methylpiperazin-1-yl)-[1,1'-biphenyl]-4-yl)-methyl)-1,4-diazepane
-
1-methyl-4-((4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)methyl)-1,4-diazepane
-
1-methyl-4-((4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)methyl)-1,4-diazepane
-
1-methyl-4-(naphthalen-2-ylmethyl)-1,4-diazepane
-
1-methyl-4-(naphthalen-2-ylmethyl)-1,4-diazepane
-
1-[[4-(4-[4-[(6-amino-9H-purin-9-yl)methyl]phenyl]butyl)phenyl]methyl]-4-(dimethylamino)pyridin-1-ium bromide
-
1-[[4-(4-[4-[(6-amino-9H-purin-9-yl)methyl]phenyl]butyl)phenyl]methyl]-4-(dimethylamino)pyridin-1-ium bromide
-
14,21-diaza-1,10-diazoniapentacyclo[20.2.2.210,13.216,19.03,8]triaconta-1(24),3,5,7,10,12,16,18,22,25,27,29-dodecaene dibromide
-
IC50: 0.0003 mM
14,21-diaza-1,10-diazoniapentacyclo[20.2.2.210,13.216,19.03,8]triaconta-1(24),3,5,7,10,12,16,18,22,25,27,29-dodecaene dibromide
-
IC50: 0.0003 mM, most potent inhibitor
2'-fluoro-4,4'-bis((4-methyl-1,4-diazepan-1-yl)methyl)-[1,1'-biphenyl]-2-carbonitrile
-
2'-fluoro-4,4'-bis((4-methyl-1,4-diazepan-1-yl)methyl)-[1,1'-biphenyl]-2-carbonitrile
-
4,4'-((2,3-difluoro-[1,1'-biphenyl]-4,4'-diyl)bis(methylene))bis-(1-methyl-1,4-diazepane)
-
4,4'-((2,3-difluoro-[1,1'-biphenyl]-4,4'-diyl)bis(methylene))bis-(1-methyl-1,4-diazepane)
-
4,4'-((2-fluoro-[1,1'-biphenyl]-4,4'-diyl)bis(methylene))bis(1-methyl-1,4-diazepane)
-
4,4'-((2-fluoro-[1,1'-biphenyl]-4,4'-diyl)bis(methylene))bis(1-methyl-1,4-diazepane)
-
4,4'-((3,5-difluoro-[1,1'-biphenyl]-4,4'-diyl)bis(methylene))bis-(1-methyl-1,4-diazepane)
-
4,4'-((3,5-difluoro-[1,1'-biphenyl]-4,4'-diyl)bis(methylene))bis-(1-methyl-1,4-diazepane)
-
4,4'-((3-chloro-[1,1'-biphenyl]-4,4'-diyl)bis(methylene))bis(1-methyl-1,4-diazepane)
-
4,4'-((3-chloro-[1,1'-biphenyl]-4,4'-diyl)bis(methylene))bis(1-methyl-1,4-diazepane)
-
4,4'-bis((4-methyl-1,4-diazepan-1-yl)methyl)-1,1'-biphenyl
-
4,4'-bis((4-methyl-1,4-diazepan-1-yl)methyl)-1,1'-biphenyl
-
4,4'-bis((4-methyl-1,4-diazepan-1-yl)methyl)-[1,1'-biphenyl]-2-carbonitrile
-
4,4'-bis((4-methyl-1,4-diazepan-1-yl)methyl)-[1,1'-biphenyl]-2-carbonitrile
-
6-amino-3-[(4'-[[4-(dimethylamino)pyridin-1-ium-1-yl]methyl][1,1'-biphenyl]-4-yl)methyl]-9H-purin-3-ium
-
6-amino-3-[(4'-[[4-(dimethylamino)pyridin-1-ium-1-yl]methyl][1,1'-biphenyl]-4-yl)methyl]-9H-purin-3-ium
-
7-((4-methyl-1,4-diazepan-1-yl)methyl)quinolone
-
7-((4-methyl-1,4-diazepan-1-yl)methyl)quinolone
-
choline kinase inhibitor Mn58b
-
-
-
choline kinase inhibitor Mn58b
-
-
hemicholinium
-
-
hemicholinium-3
-
-
hemicholinium-3
-
weak inhibitor, IC50: 0.057 mM
hemicholinium-3
competitive inhibitor, the inhibitory effect of hemicholinium-3 is about 500times higher toward the ChoKalpha isoforms than ChoKbeta isoform
hemicholinium-3
HC-3, a substrate site inhibitor that bears structural homology to choline, which contributes to its toxicity
methyl 4'-((4-methyl-1,4-diazepan-1-yl)methyl)-[1,1'-biphenyl]-4-carboxylate
-
methyl 4'-((4-methyl-1,4-diazepan-1-yl)methyl)-[1,1'-biphenyl]-4-carboxylate
-
MN58b
-
MN58b
-
specific inhibitor, IC50: 0.0005-0.072 mM depending on cell type
MN58b
-
specific for choline kinase
additional information
not inhibited by 1-[4-(4-[4-[(3-aminophenoxy)methyl]phenyl]butyl)-benzyl]-4-(dimethylamino)pyridinium bromide
-
additional information
chemotherapeutic drug design has centered on stopping the catalytic activity of choline kinase and reducing the downstream metabolites it produces
-
additional information
-
chemotherapeutic drug design has centered on stopping the catalytic activity of choline kinase and reducing the downstream metabolites it produces
-
additional information
choline kinase inhibition and docking studies of a series of 6-(benzylthio)-9H-purin-9-yl-pyridinium derivatives using native ChoK from the cytosol of Hep-G2 cells and recombinantly expressed ChoKalpha, overview
-
additional information
small molecule inhibitors of choline kinase identified by fragment-based drug discovery (NMR fragment screening and competition experiments), quantification of protein-ligand affinities, overview
-
additional information
-
small molecule inhibitors of choline kinase identified by fragment-based drug discovery (NMR fragment screening and competition experiments), quantification of protein-ligand affinities, overview
-
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acylglycerol kinase deficiency
Disorders of phospholipids, sphingolipids and fatty acids biosynthesis: toward a new category of inherited metabolic diseases.
Adenocarcinoma
Choline Kinase Alpha (CHK?) as a Therapeutic Target in Pancreatic Ductal Adenocarcinoma: Expression, Predictive Value, and Sensitivity to Inhibitors.
Adenocarcinoma
Generation and characterization of monoclonal antibodies against choline kinase alpha and their potential use as diagnostic tools in cancer.
Adenoma
Increased choline kinase activity and elevated phosphocholine levels in human colon cancer.
Alzheimer Disease
Alterations of selected enzymes of phospholipid metabolism in Alzheimer's disease brain tissue as compared to non-Alzheimer's demented controls.
Arthritis, Rheumatoid
Choline kinase inhibition in rheumatoid arthritis.
Barth Syndrome
Disorders of phospholipids, sphingolipids and fatty acids biosynthesis: toward a new category of inherited metabolic diseases.
Brain Neoplasms
Fully automated SPE-based synthesis and purification of 2-[18F]fluoroethyl-choline for human use.
Brain Neoplasms
Magnetic resonance spectroscopy for detection of choline kinase inhibition in the treatment of brain tumors.
Breast Neoplasms
Activation of choline kinase by extracellular Ca2+ is Ca(2+)-sensing receptor, Galpha12 and Rho-dependent in breast cancer cells.
Breast Neoplasms
Characterization of breast cancers and therapy response by MRS and quantitative gene expression profiling in the choline pathway.
Breast Neoplasms
Choline kinase activation is a critical requirement for the proliferation of primary human mammary epithelial cells and breast tumor progression.
Breast Neoplasms
Choline Kinase Alpha Inhibition by EB-3D Triggers Cellular Senescence, Reduces Tumor Growth and Metastatic Dissemination in Breast Cancer.
Breast Neoplasms
Choline kinase down-regulation increases the effect of 5-fluorouracil in breast cancer cells.
Breast Neoplasms
Choline kinase overexpression increases invasiveness and drug resistance of human breast cancer cells.
Breast Neoplasms
Correlation between Choline Peak at MR Spectroscopy and Calcium-Sensing Receptor Expression Level in Breast Cancer: A Preliminary Clinical Study.
Breast Neoplasms
Direct inhibition of choline kinase by a near-infrared fluorescent carbocyanine.
Breast Neoplasms
Downregulation of Choline Kinase-Alpha Enhances Autophagy in Tamoxifen-Resistant Breast Cancer Cells.
Breast Neoplasms
Functional interactions between Choline kinase ?, epidermal growth factor receptor and c-Src in breast cancer cell proliferation.
Breast Neoplasms
Increased choline kinase activity in human breast carcinomas: clinical evidence for a potential novel antitumor strategy.
Breast Neoplasms
Kinetics of choline transport and phosphorylation in human breast cancer cells; NMR application of the zero trans method.
Breast Neoplasms
Molecular causes of the aberrant choline phospholipid metabolism in breast cancer.
Breast Neoplasms
Near infrared fluorescent imaging of choline kinase alpha expression and inhibition in breast tumors.
Breast Neoplasms
Noninvasive detection of lentiviral-mediated choline kinase targeting in a human breast cancer xenograft.
Breast Neoplasms
Novel 4-Amino Bis-pyridinium and Bis-quinolinium Derivatives as Choline Kinase Inhibitors with Antiproliferative Activity against the Human Breast Cancer SKBR-3 Cell Line.
Breast Neoplasms
Pharmacodynamic markers for choline kinase down-regulation in breast cancer cells.
Breast Neoplasms
Phosphocholine as a biomarker of breast cancer: molecular and biochemical studies.
Breast Neoplasms
Phospholipid metabolism in cancer cells monitored by 31P NMR spectroscopy.
Breast Neoplasms
Regulation of Akt(ser473) phosphorylation by choline kinase in breast carcinoma cells.
Breast Neoplasms
RNA interference-mediated choline kinase suppression in breast cancer cells induces differentiation and reduces proliferation.
Breast Neoplasms
[Increased activity of choline kinase in human breast cancer and 7, 12-dimethylbenz[a]anthracene (DMBA)-induced rat mammary carcinoma, and activated by 17 beta-estradiol: preliminary report]
Breast Neoplasms
[Methyl-3H]-choline incorporation into MCF-7 cells: correlation with proliferation, choline kinase and phospholipase D assay.
Carcinogenesis
CHKA mediates the poor prognosis of lung adenocarcinoma and acts as a prognostic indicator.
Carcinogenesis
Choline Kinase ? Mediates Interactions Between the Epidermal Growth Factor Receptor and Mechanistic Target of Rapamycin Complex 2 in Hepatocellular Carcinoma Cells to Promote Drug Resistance and Xenograft Tumor Progression.
Carcinogenesis
Choline kinase as a link connecting phospholipid metabolism and cell cycle regulation: implications in cancer therapy.
Carcinogenesis
Choline kinase is a novel oncogene that potentiates RhoA-induced carcinogenesis.
Carcinogenesis
Differential role of human choline kinase alpha and beta enzymes in lipid metabolism: implications in cancer onset and treatment.
Carcinogenesis
EB-3D a novel choline kinase inhibitor induces deregulation of the AMPK-mTOR pathway and apoptosis in leukemia T-cells.
Carcinogenesis
Increased choline kinase activity and elevated phosphocholine levels in human colon cancer.
Carcinogenesis
Increased choline kinase activity in human breast carcinomas: clinical evidence for a potential novel antitumor strategy.
Carcinogenesis
Involvement of human choline kinase alpha and beta in carcinogenesis: A different role in lipid metabolism and biological functions.
Carcinogenesis
Novel Small Molecule Inhibitors of Choline Kinase Identified by Fragment-Based Drug Discovery.
Carcinoma
A critical role for choline kinase-alpha in the aggressiveness of bladder carcinomas.
Carcinoma
Activation of choline kinase drives aberrant choline metabolism in esophageal squamous cell carcinomas.
Carcinoma
Choline kinase alpha depletion selectively kills tumoral cells.
Carcinoma
Global metabolic profile identifies choline kinase alpha as a key regulator of glutathione-dependent antioxidant cell defense in ovarian carcinoma.
Carcinoma
Noninvasive magnetic resonance spectroscopic pharmacodynamic markers of the choline kinase inhibitor MN58b in human carcinoma models.
Carcinoma
[Increased activity of choline kinase in human breast cancer and 7, 12-dimethylbenz[a]anthracene (DMBA)-induced rat mammary carcinoma, and activated by 17 beta-estradiol: preliminary report]
Carcinoma, Hepatocellular
Choline Kinase ? Mediates Interactions Between the Epidermal Growth Factor Receptor and Mechanistic Target of Rapamycin Complex 2 in Hepatocellular Carcinoma Cells to Promote Drug Resistance and Xenograft Tumor Progression.
Carcinoma, Hepatocellular
Choline kinase alpha and hexokinase-2 protein expression in hepatocellular carcinoma: association with survival.
Carcinoma, Hepatocellular
The effect of polycyclic aromatic hydrocarbons on choline kinase activity in mouse hepatoma cells.
Carcinoma, Ovarian Epithelial
Choline kinase-alpha by regulating cell aggressiveness and drug sensitivity is a potential druggable target for ovarian cancer.
Carcinoma, Ovarian Epithelial
Global metabolic profile identifies choline kinase alpha as a key regulator of glutathione-dependent antioxidant cell defense in ovarian carcinoma.
Carcinoma, Squamous Cell
Activation of choline kinase drives aberrant choline metabolism in esophageal squamous cell carcinomas.
Cardiomyopathies
Disorders of phospholipids, sphingolipids and fatty acids biosynthesis: toward a new category of inherited metabolic diseases.
Cardiomyopathy, Dilated
Clinical characteristics of megaconial congenital muscular dystrophy due to choline kinase beta gene defects in a series of 15 patients.
Cataract
Effects of cataractogenesis on the CDP-choline pathway: changes in ATP concentration and phosphocholine synthesis during and after exposure of rat lenses to sugars in vitro and in vivo.
Cholangiocarcinoma
Synergistic antiproliferative effects of an mTOR inhibitor (rad001) plus gemcitabine on cholangiocarcinoma by decreasing choline kinase activity.
Choline Deficiency
Effect of choline deficiency on CTP: phosphocholine cytidylyltransferase and choline kinase activities in rat liver subcellular fractions.
choline kinase deficiency
Disorders of phospholipids, sphingolipids and fatty acids biosynthesis: toward a new category of inherited metabolic diseases.
choline kinase deficiency
[Treatment of choline kinase beta deficiency with citicoline].
Colonic Neoplasms
Increased choline kinase activity and elevated phosphocholine levels in human colon cancer.
Colonic Neoplasms
Increased choline kinase activity in 1,2-dimethylhydrazine-induced rat colon cancer.
Colonic Neoplasms
Synthesis and biological activity of new bispyridinium salts of 4,4'-bispyridyl-5,5'-perfluoroalkyl-2,2'-bisoxazoles.
Colorectal Neoplasms
Combined 5-FU and ChoK? inhibitors as a new alternative therapy of colorectal cancer: evidence in human tumor-derived cell lines and mouse xenografts.
Colorectal Neoplasms
Overexpression of CHKA contributes to tumor progression and metastasis and predicts poor prognosis in colorectal carcinoma.
Congenital Abnormalities
Choline kinase and its function.
Congenital Abnormalities
Molecular structure and differential function of choline kinases CHK? and CHK? in musculoskeletal system and cancer.
Endometrial Neoplasms
Alterations of choline phospholipid metabolism in endometrial cancer are caused by choline kinase alpha overexpression and a hyperactivated deacylation pathway.
Glioblastoma
Cloning of a human choline kinase cDNA by complementation of the yeast cki mutation.
Glioma
(1)H HR-MAS and genomic analysis of human tumor biopsies discriminate between high and low grade astrocytomas.
Glioma
Imaging and Tissue Biomarkers of Choline Metabolism in Diffuse Adult Glioma: 18F-Fluoromethylcholine PET/CT, Magnetic Resonance Spectroscopy, and Choline Kinase ?.
Glioma
[Knockdown of choline kinase ? (CHKA) inhibits the proliferation, invasion and migration of human U87MG glioma cells].
Hyperparathyroidism, Secondary
Altered acetylcholine metabolism of brain in uremia: role of secondary hyperparathyroidism.
Hyperparathyroidism, Secondary
Derangements in acetylcholine metabolism in brain synaptosomes in chronic renal failure.
Infections
In Vitro Hepatitis C Virus Infection and Hepatic Choline Metabolism.
Infections
Inhibition of giant cell formation by Compound 48-80 after infection with herpesvirus hominis. IV. Compound 48-80, an inhibitor of choline kinase activity.
Infections
The metabolic responses to hepatitis B virus infection shed new light on pathogenesis and targets for treatment.
Intellectual Disability
A congenital muscular dystrophy with mitochondrial structural abnormalities caused by defective de novo phosphatidylcholine biosynthesis.
Intellectual Disability
Clinical characteristics of megaconial congenital muscular dystrophy due to choline kinase beta gene defects in a series of 15 patients.
Leukemia
A genetic database can be utilized to identify potential biomarkers for biphenotypic hepatocellular carcinoma-cholangiocarcinoma.
Leukemia
EB-3D a novel choline kinase inhibitor induces deregulation of the AMPK-mTOR pathway and apoptosis in leukemia T-cells.
Liver Neoplasms
The emerging role of positron emission tomography in hepatocellular carcinoma.
Lung Neoplasms
Acid ceramidase as a chemotherapeutic target to overcome resistance to the antitumoral effect of choline kinase ? inhibition.
Lung Neoplasms
Differential role of human choline kinase alpha and beta enzymes in lipid metabolism: implications in cancer onset and treatment.
Lung Neoplasms
Disease-specific target gene expression profiling of molecular imaging probes: database development and clinical validation.
Lung Neoplasms
Disease-Specific Target Gene Expression Profiling of Molecular Imaging Probes: Database Development and Clinical Validation.
Lung Neoplasms
Expression of choline kinase alpha to predict outcome in patients with early-stage non-small-cell lung cancer: a retrospective study.
Lung Neoplasms
Value of 11C-choline PET/CT for lung cancer diagnosis and the relation between choline metabolism and proliferation of cancer cells.
Malaria
Effect of choline kinase inhibitor hexadecyltrimethylammonium bromide on Plasmodium falciparum gene expression.
Malaria
Inhibition of Plasmodium falciparum choline kinase by hexadecyltrimethylammonium bromide: a possible antimalarial mechanism.
Malaria
Molecular characterization and localization of Plasmodium falciparum choline kinase.
Mitochondrial Myopathies
Congenital megaconial myopathy due to a novel defect in the choline kinase Beta gene.
Muscular Diseases
Late-onset megaconial myopathy in mice lacking group I Paks.
Muscular Dystrophies
A congenital muscular dystrophy with mitochondrial structural abnormalities caused by defective de novo phosphatidylcholine biosynthesis.
Muscular Dystrophies
A rostrocaudal muscular dystrophy caused by a defect in choline kinase Beta, the first enzyme in phosphatidylcholine biosynthesis.
Muscular Dystrophies
Choline kinase and its function.
Muscular Dystrophies
Choline Kinase Beta-Related Muscular Dystrophy, Appearance of Muscle Involvement on Magnetic Resonance Imaging.
Muscular Dystrophies
Clinical characteristics of megaconial congenital muscular dystrophy due to choline kinase beta gene defects in a series of 15 patients.
Muscular Dystrophies
Congenital neurogenic muscular atrophy in megaconial myopathy due to a mutation in CHKB gene.
Muscular Dystrophies
Differential expression of choline kinase isoforms in skeletal muscle explains the phenotypic variability in the rostrocaudal muscular dystrophy mouse.
Muscular Dystrophies
Disorders of phospholipids, sphingolipids and fatty acids biosynthesis: toward a new category of inherited metabolic diseases.
Muscular Dystrophies
Exome sequencing identifies a CHKB mutation in Spanish patient with Megaconial Congenital Muscular Dystrophy and mtDNA depletion.
Muscular Dystrophies
Late-onset megaconial myopathy in mice lacking group I Paks.
Muscular Dystrophies
Megaconial congenital muscular dystrophy due to loss-of-function mutations in choline kinase ?.
Muscular Dystrophies
Megaconial muscular dystrophy caused by mitochondrial membrane homeostasis defect, new insights from skeletal and heart muscle analyses.
Muscular Dystrophies
Molecular structure and differential function of choline kinases CHK? and CHK? in musculoskeletal system and cancer.
Muscular Dystrophies
Muscle choline kinase beta defect causes mitochondrial dysfunction and increased mitophagy.
Muscular Dystrophies
New splicing mutation in the choline kinase beta (CHKB) gene causing a muscular dystrophy detected by whole-exome sequencing.
Muscular Dystrophies
Novel CHKB mutation expands the megaconial muscular dystrophy phenotype.
Muscular Dystrophies
Phosphatidylcholine and choline homeostasis.
Muscular Dystrophies
Phospholipid synthetic defect and mitophagy in muscle disease.
Muscular Dystrophies
Reduced mitochondrial fission and impaired energy metabolism in human primary skeletal muscle cells of Megaconial Congenital Muscular Dystrophy.
Muscular Dystrophies
Understanding the muscular dystrophy caused by deletion of choline kinase beta in mice.
Myoglobinuria
Disorders of phospholipids, sphingolipids and fatty acids biosynthesis: toward a new category of inherited metabolic diseases.
Neoplasm Metastasis
Pharmacodynamic markers for choline kinase down-regulation in breast cancer cells.
Neoplasm Metastasis
Regulation of Akt(ser473) phosphorylation by choline kinase in breast carcinoma cells.
Neoplasms
A Conserved MicroRNA Regulatory Circuit Is Differentially Controlled during Limb/Appendage Regeneration.
Neoplasms
A critical role for choline kinase-alpha in the aggressiveness of bladder carcinomas.
Neoplasms
A moonlighting function of choline kinase alpha 2 in the initiation of lipid droplet lipolysis in cancer cells.
Neoplasms
A non-catalytic role of choline kinase alpha is important in promoting cancer cell survival.
Neoplasms
Acid ceramidase as a chemotherapeutic target to overcome resistance to the antitumoral effect of choline kinase ? inhibition.
Neoplasms
Activation of Phosphatidylcholine-Specific Phospholipase C in Breast and Ovarian Cancer: Impact on MRS-Detected Choline Metabolic Profile and Perspectives for Targeted Therapy.
Neoplasms
An evaluation of motion compensation strategies and repeatability for abdominal (1) H MR spectroscopy measurements in volunteer studies and clinical trials.
Neoplasms
An illustration of the potential for mapping MRI/MRS parameters with genetic over-expression profiles in human prostate cancer.
Neoplasms
Association of CHKA polymorphism (rs3794186) with ?-fetoprotein levels in hepatocellular carcinoma.
Neoplasms
Balance of human choline kinase isoforms is critical for cell cycle regulation: implications for the development of choline kinase-targeted cancer therapy.
Neoplasms
Biochemical and Pathophysiological Premises to Positron Emission Tomography With Choline Radiotracers.
Neoplasms
Biomimetic Magnetic Nanocarriers Drive Choline Kinase Alpha Inhibitor inside Cancer Cells for Combined Chemo-Hyperthermia Therapy.
Neoplasms
Cancer imaging with fluorine-18-labeled choline derivatives.
Neoplasms
ChoK-Full of Potential: Choline Kinase in B Cell and T Cell Malignancies.
Neoplasms
Choline Kinase ? Mediates Interactions Between the Epidermal Growth Factor Receptor and Mechanistic Target of Rapamycin Complex 2 in Hepatocellular Carcinoma Cells to Promote Drug Resistance and Xenograft Tumor Progression.
Neoplasms
Choline kinase activation is a critical requirement for the proliferation of primary human mammary epithelial cells and breast tumor progression.
Neoplasms
Choline kinase alpha and hexokinase-2 protein expression in hepatocellular carcinoma: association with survival.
Neoplasms
Choline Kinase Alpha as an Androgen Receptor Chaperone and Prostate Cancer Therapeutic Target.
Neoplasms
Choline kinase alpha depletion selectively kills tumoral cells.
Neoplasms
Choline kinase alpha in cancer prognosis and treatment.
Neoplasms
Choline Kinase Alpha Inhibition by EB-3D Triggers Cellular Senescence, Reduces Tumor Growth and Metastatic Dissemination in Breast Cancer.
Neoplasms
Choline kinase alpha-Putting the ChoK-hold on tumor metabolism.
Neoplasms
Choline kinase as a link connecting phospholipid metabolism and cell cycle regulation: implications in cancer therapy.
Neoplasms
Choline kinase down-regulation increases the effect of 5-fluorouracil in breast cancer cells.
Neoplasms
Choline kinase inhibition in rheumatoid arthritis.
Neoplasms
Choline kinase inhibition induces exacerbated endoplasmic reticulum stress and triggers apoptosis via CHOP in cancer cells.
Neoplasms
Choline kinase inhibition induces the increase in ceramides resulting in a highly specific and selective cytotoxic antitumoral strategy as a potential mechanism of action.
Neoplasms
Choline kinase inhibitors EB-3D and EB-3P interferes with lipid homeostasis in HepG2 cells.
Neoplasms
Choline kinase is a novel oncogene that potentiates RhoA-induced carcinogenesis.
Neoplasms
Choline kinase overexpression increases invasiveness and drug resistance of human breast cancer cells.
Neoplasms
Choline kinase: an important target for cancer.
Neoplasms
Choline metabolism in malignant transformation.
Neoplasms
Choline transporter-like proteins CTLs/SLC44 family as a novel molecular target for cancer therapy.
Neoplasms
Combined 5-FU and ChoK? inhibitors as a new alternative therapy of colorectal cancer: evidence in human tumor-derived cell lines and mouse xenografts.
Neoplasms
Degradable Dextran Nanopolymer as a Carrier for Choline Kinase (ChoK) siRNA Cancer Therapy.
Neoplasms
Design of symmetrical and nonsymmetrical N,N-dimethylaminopyridine derivatives as highly potent choline kinase alpha inhibitors.
Neoplasms
Design, synthesis, theoretical calculations and biological evaluation of new non-symmetrical choline kinase inhibitors.
Neoplasms
Differential role of human choline kinase alpha and beta enzymes in lipid metabolism: implications in cancer onset and treatment.
Neoplasms
Discovery of a new binding site on human choline kinase ?1: design, synthesis, crystallographic studies, and biological evaluation of asymmetrical bispyridinium derivatives.
Neoplasms
EB-3D a novel choline kinase inhibitor induces deregulation of the AMPK-mTOR pathway and apoptosis in leukemia T-cells.
Neoplasms
Epigenetic footprint enables molecular risk stratification of hepatoblastoma with clinical implications.
Neoplasms
Expression of choline kinase alpha to predict outcome in patients with early-stage non-small-cell lung cancer: a retrospective study.
Neoplasms
Functional expression of choline transporter-like protein 1 (CTL1) in small cell lung carcinoma cells: A target molecule for lung cancer therapy.
Neoplasms
Generation and characterization of monoclonal antibodies against choline kinase alpha and their potential use as diagnostic tools in cancer.
Neoplasms
Glycerophosphodiester phosphodiesterase domain containing 5 (GDPD5) expression correlates with malignant choline phospholipid metabolite profiles in human breast cancer.
Neoplasms
Histone Deacetylase Inhibition Increases Levels of Choline Kinase ? and Phosphocholine Facilitating Noninvasive Imaging in Human Cancers.
Neoplasms
Identification of a Unique Inhibitor-Binding Site on Choline Kinase ?.
Neoplasms
Increased choline kinase activity in 1,2-dimethylhydrazine-induced rat colon cancer.
Neoplasms
Inhibition of choline kinase renders a highly selective cytotoxic effect in tumour cells through a mitochondrial independent mechanism.
Neoplasms
Kinetics from Indirectly Detected Hyperpolarized NMR Spectroscopy by Using Spatially Selective Coherence Transfers.
Neoplasms
Kinetics from indirectly detected hyperpolarized NMR spectroscopy by using spatially selective coherence transfers.
Neoplasms
Lead optimization-hit expansion of new asymmetrical pyridinium/quinolinium compounds as choline kinase ?1 inhibitors.
Neoplasms
Magnetic Resonance Spectroscopy of siRNA-Based Cancer Therapy.
Neoplasms
Metabolic profiling of transgenic adenocarcinoma of mouse prostate (TRAMP) tissue by 1H-NMR analysis: evidence for unusual phospholipid metabolism.
Neoplasms
Metabolomics analysis uncovers that dietary restriction buffers metabolic changes associated with aging in Caenorhabditis elegans.
Neoplasms
Modulation of choline kinase activity in human cancer cells observed by dynamic 31P NMR.
Neoplasms
Molecular structure and differential function of choline kinases CHK? and CHK? in musculoskeletal system and cancer.
Neoplasms
Multimodal Mass Spectrometric Imaging of Small Molecules Reveals Distinct Spatio-Molecular Signatures in Differentially Metastatic Breast Tumor Models.
Neoplasms
Near infrared fluorescent imaging of choline kinase alpha expression and inhibition in breast tumors.
Neoplasms
Noninvasive detection of lentiviral-mediated choline kinase targeting in a human breast cancer xenograft.
Neoplasms
Noninvasive magnetic resonance spectroscopic pharmacodynamic markers of the choline kinase inhibitor MN58b in human carcinoma models.
Neoplasms
Novel Non-Congeneric Derivatives of the Choline Kinase Alpha Inhibitor ICL-CCIC-0019.
Neoplasms
Overexpression of CHKA contributes to tumor progression and metastasis and predicts poor prognosis in colorectal carcinoma.
Neoplasms
Overexpression of choline kinase is a frequent feature in human tumor-derived cell lines and in lung, prostate, and colorectal human cancers.
Neoplasms
Phosphocholine as a biomarker of breast cancer: molecular and biochemical studies.
Neoplasms
Phospholipase D and choline kinase: their role in cancer development and their potential as drug targets.
Neoplasms
Preclinical characterization of RSM-932A, a novel anticancer drug targeting the human choline kinase alpha, an enzyme involved in increased lipid metabolism of cancer cells.
Neoplasms
Preclinical development of a non-toxic oral formulation of monoethanolamine, a lipid precursor, for prostate cancer treatment.
Neoplasms
Radiolabeled choline as a proliferation marker: comparison with radiolabeled acetate.
Neoplasms
Recent advances in the design of choline kinase ? inhibitors and the molecular basis of their inhibition.
Neoplasms
Regulation of Akt(ser473) phosphorylation by choline kinase in breast carcinoma cells.
Neoplasms
RNA interference-mediated choline kinase suppression in breast cancer cells induces differentiation and reduces proliferation.
Neoplasms
Sensitization of (colon) cancer cells to death receptor related therapies: A report from the FP6-ONCODEATH research consortium.
Neoplasms
Significantly increased monounsaturated lipids relative to polyunsaturated lipids in six types of cancer microenvironment are observed by mass spectrometry imaging.
Neoplasms
Synthesis and evaluation of (18)F-labeled choline analogs as oncologic PET tracers.
Neoplasms
Synthesis and preclinical evaluation of the choline transport tracer deshydroxy-[18F]fluorocholine ([18F]dOC).
Neoplasms
Targeted therapies in bladder cancer: an overview of in vivo research.
Neoplasms
Targeting Phospholipid Metabolism in Cancer.
Neoplasms
The novel choline kinase inhibitor ICL-CCIC-0019 reprograms cellular metabolism and inhibits cancer cell growth.
Neoplasms
[18F]fluoromethyl-[1,2-2H4]-choline: a novel radiotracer for imaging choline metabolism in tumors by positron emission tomography.
Neuroblastoma
KDM2B regulates choline kinase expression and neuronal differentiation of neuroblastoma cells.
Ovarian Neoplasms
Choline kinase alpha impairment overcomes TRAIL resistance in ovarian cancer cells.
Ovarian Neoplasms
Choline kinase-alpha by regulating cell aggressiveness and drug sensitivity is a potential druggable target for ovarian cancer.
Paraplegia
Disorders of phospholipids, sphingolipids and fatty acids biosynthesis: toward a new category of inherited metabolic diseases.
Peripheral Nervous System Diseases
Disorders of phospholipids, sphingolipids and fatty acids biosynthesis: toward a new category of inherited metabolic diseases.
Prostatic Intraepithelial Neoplasia
Choline Kinase Alpha as an Androgen Receptor Chaperone and Prostate Cancer Therapeutic Target.
Prostatic Neoplasms
An illustration of the potential for mapping MRI/MRS parameters with genetic over-expression profiles in human prostate cancer.
Prostatic Neoplasms
Choline Kinase Alpha as an Androgen Receptor Chaperone and Prostate Cancer Therapeutic Target.
Prostatic Neoplasms
Choline phosphorylation and regulation of transcription of choline kinase ? in hypoxia.
Prostatic Neoplasms
Circulating androgen receptor combined with 18F-fluorocholine PET/CT metabolic activity and outcome to androgen receptor signalling-directed therapies in castration-resistant prostate cancer.
Prostatic Neoplasms
Exploiting altered patterns of choline kinase-alpha expression on human prostate tissue to prognosticate prostate cancer.
Prostatic Neoplasms
Fully automated SPE-based synthesis and purification of 2-[18F]fluoroethyl-choline for human use.
Prostatic Neoplasms
Hypoxia regulates choline kinase expression through hypoxia-inducible factor-1 alpha signaling in a human prostate cancer model.
Prostatic Neoplasms
Kinase joins the chaperone club: Androgen-regulated kinome reveals choline kinase alpha as a potential drug target in prostate cancer.
Prostatic Neoplasms
Metabolic profiling of transgenic adenocarcinoma of mouse prostate (TRAMP) tissue by 1H-NMR analysis: evidence for unusual phospholipid metabolism.
Prostatic Neoplasms
Quantification of 18F-Fluorocholine Kinetics in Patients with Prostate Cancer.
Prostatic Neoplasms
Role of p115RhoGEF in the regulation of extracellular Ca(2+)-induced choline kinase activation and prostate cancer cell proliferation.
Prostatic Neoplasms
Sci-Fri AM: Imaging - 01: Feasibility of estimating choline kinase activity with kinetic modeling of 18F-fluorocholine pet imaging of prostate cancer.
Prostatic Neoplasms
Use of [11C]choline PET-CT as a noninvasive method for detecting pelvic lymph node status from prostate cancer and relationship with choline kinase expression.
Renal Insufficiency
Derangements in acetylcholine metabolism in brain synaptosomes in chronic renal failure.
Sepsis
Influence of a beta-adrenergic agonist on septic shock-induced alterations of phosphatidylcholine metabolism in rat lung.
Sepsis
Influence of a?-adrenergic agonist on septic shock-induced alterations of phosphatidylcholine metabolism in rat lung.
Small Cell Lung Carcinoma
Acid ceramidase as a chemotherapeutic target to overcome resistance to the antitumoral effect of choline kinase ? inhibition.
Spinal Dysraphism
CHKA and PCYT1A gene polymorphisms, choline intake and spina bifida risk in a California population.
Starvation
Appropriate leucine supplementation promotes glucose metabolism and enhances energy homeostasis in juvenile crucian carp (Carassius auratus gibelio var. CAS III).
Urinary Bladder Neoplasms
A critical role for choline kinase-alpha in the aggressiveness of bladder carcinomas.
Uterine Cervical Neoplasms
Modulation of choline kinase activity in human cancer cells observed by dynamic 31P NMR.
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0.1075
choline kinase inhibitor Mn58b
Homo sapiens
-
-
0.00002
(1S)-1-[(3R)-1-azabicyclo[2.2.2]octan-3-yl]-3-[2-[(oxan-4-yl)oxy]phenyl]-1-phenylpropan-1-ol
Homo sapiens
pH 7.0, 25°C, recombinant enzyme
0.000251
(4-methyl-1,4-diazepan-1-yl)(4'-((4-methyl-1,4-diazepan-1-yl)-methyl)-[1,1'-biphenyl]-4-yl)methanone
0.00951
1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(3-hydroxyquinuclidinium) bromide
Homo sapiens
at pH 8.5 and 37°C
0.00163
1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(4-((4-chlorophenyl)(methyl)amino)pyridinium) bromide
Homo sapiens
at pH 8.5 and 37°C
0.00327
1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(4-((4-chlorophenyl)(methyl)amino)quinolinium) bromide
Homo sapiens
at pH 8.5 and 37°C
0.00202
1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(4-(azepan-1-yl)-7-chloroquinolinium) bromide
Homo sapiens
at pH 8.5 and 37°C
0.00166
1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(4-(azepan-1-yl)quinolinium) bromide
Homo sapiens
at pH 8.5 and 37°C
0.001
1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(4-(dimethylamino)pyridinium) bromide
Homo sapiens
at pH 8.5 and 37°C
0.00685
1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(4-(methyl(phenyl)amino)quinolinium) bromide
Homo sapiens
at pH 8.5 and 37°C
0.00956
1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(4-(pyrrolidin-1-yl)pyridinium) bromide
Homo sapiens
at pH 8.5 and 37°C
0.01622
1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(7-chloro-4-((4-chlorophenyl)(methyl)amino)quinolinium) bromide
Homo sapiens
at pH 8.5 and 37°C
0.00279
1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(7-chloro-4-(methyl(phenyl)amino)quinolinium) bromide
Homo sapiens
at pH 8.5 and 37°C
0.00092
1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(7-chloro-4-(pyrrolidin-1-yl)quinolinium) bromide
Homo sapiens
at pH 8.5 and 37°C
0.03754
1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(quinuclidinium) bromide
Homo sapiens
at pH 8.5 and 37°C
0.0528
1,1'-(benzene-1,3-diyldimethanediyl)bis(4-piperidin-1-ylpyridinium) dibromide
Homo sapiens
-
IC50: 0.0528 mM
0.0842
1,1'-(benzene-1,3-diyldimethanediyl)bis(4-pyrrolidin-1-ylpyridinium) dibromide
Homo sapiens
-
IC50: 0.0842 mM
0.0084
1,1'-(benzene-1,3-diyldimethanediyl)bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide
Homo sapiens
-
IC50: 0.0084 mM
0.0072
1,1'-(benzene-1,3-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]pyridinium) dibromide
Homo sapiens
-
IC50: 0.0072 mM
0.0375
1,1'-(benzene-1,3-diyldimethanediyl)bis[4-[(phenylamino)methyl]pyridinium] dibromide
Homo sapiens
-
IC50: 0.0375 mM
0.0377
1,1'-(benzene-1,4-diyldimethanediyl)bis(4-piperidin-1-ylpyridinium) dibromide
Homo sapiens
-
IC50: 0.0377 mM
0.024
1,1'-(benzene-1,4-diyldimethanediyl)bis(4-pyrrolidin-1-ylpyridinium) dibromide
Homo sapiens
-
IC50: 0.024 mM
0.0097
1,1'-(benzene-1,4-diyldimethanediyl)bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide
Homo sapiens
-
IC50: 0.0097 mM
0.0029
1,1'-(benzene-1,4-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]pyridinium) dibromide
Homo sapiens
-
IC50: 0.0029 mM
0.015
1,1'-(benzene-1,4-diyldimethanediyl)bis[4-[(phenylamino)methyl]pyridinium] dibromide
Homo sapiens
-
IC50: 0.015 mM
0.0119
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-amino-3-methylquinolinium) dibromide
Homo sapiens
-
IC50: 0.0119 mM
0.0206
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-amino-7-chloroquinolinium) dibromide
Homo sapiens
-
IC50: 0.0206 mM
0.0012
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-aminoquinolinium) dibromide
Homo sapiens
-
IC50: 0.0012 mM
0.0005
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-azepan-1-ylquinolinium) dibromide
Homo sapiens
-
IC50: 0.0005 mM
0.0019
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-piperidin-1-ylpyridinium) dibromide
Homo sapiens
-
IC50: 0.0019 mM
0.0058
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-pyrrolidin-1-ylpyridinium) dibromide
Homo sapiens
-
IC50: 0.0058 mM
0.0026
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide
Homo sapiens
-
IC50: 0.0026 mM
0.0015
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]pyridinium) dibromide
Homo sapiens
-
IC50: 0.0015 mM
0.0021
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide
Homo sapiens
-
IC50: 0.0021 mM
0.147
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(7-amino-4-[[(4-chlorophenyl)amino]methyl]-8-methylquinolinium) dibromide
Homo sapiens
-
IC50: 0.147 mM
0.0012
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(7-chloro-4-pyrrolidin-1-ylquinolinium) dibromide
Homo sapiens
-
IC50: 0.0012 mM
0.0057
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(7-chloro-4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide
Homo sapiens
-
IC50: 0.0057 mM
0.0044
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[4-(dimethylamino)quinolinium] dibromide
Homo sapiens
-
IC50: 0.0044 mM
0.0013
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[4-(phenylamino)quinolinium] dibromide
Homo sapiens
-
IC50: 0.0013 mM
0.00043
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[4-[(phenylamino)methyl]pyridinium] dibromide
Homo sapiens
-
IC50: 0.00043 mM
0.0004
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[4-[(phenylamino)methyl]quinolinium] dibromide
Homo sapiens
-
IC50: 0.0004 mM
0.0568
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[7-amino-8-methyl-4-[(phenylamino)methyl]quinolinium] dibromide
Homo sapiens
-
IC50: 0.0568 mM
0.0096
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[7-chloro-4-(dimethylamino)quinolinium] dibromide
Homo sapiens
-
IC50: 0.0096 mM
0.0031
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[7-chloro-4-[(phenylamino)methyl]quinolinium] dibromide
Homo sapiens
-
IC50: 0.0031 mM
0.2
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-amino-3-methylquinolinium) dibromide
Homo sapiens
-
IC50: above 0.2 mM
0.0633
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-amino-7-chloroquinolinium) dibromide
Homo sapiens
-
IC50: 0.0633 mM
0.0811
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-aminoquinolinium) dibromide
Homo sapiens
-
IC50: 0.0811 mM
0.0022
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-azepan-1-ylquinolinium) dibromide
Homo sapiens
-
IC50: 0.0022 mM
0.0088
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-piperidin-1-ylpyridinium) dibromide
Homo sapiens
-
IC50: 0.0088 mM
0.0111
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-pyrrolidin-1-ylpyridinium) dibromide
Homo sapiens
-
IC50: 0.0111 mM
0.0034
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide
Homo sapiens
-
IC50: 0.0034 mM
0.0018
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]pyridinium) dibromide
Homo sapiens
-
IC50: 0.0018 mM
0.002
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide
Homo sapiens
-
IC50: 0.002 mM
0.0461
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(7-amino-4-[[(4-chlorophenyl)amino]methyl]-8-methylquinolinium) dibromide
Homo sapiens
-
IC50: 0.0461 mM
0.0198
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(7-chloro-4-pyrrolidin-1-ylquinolinium) dibromide
Homo sapiens
-
IC50: 0.0198 mM
0.0114
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(7-chloro-4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide
Homo sapiens
-
IC50: 0.0114 mM
0.0397
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[4-(dimethylamino)quinolinium] dibromide
Homo sapiens
-
IC50: 0.0397 mM
0.0178
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[4-(phenylamino)quinolinium] dibromide
Homo sapiens
-
IC50: 0.0178 mM
0.0043
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[4-[(phenylamino)methyl]pyridinium] dibromide
Homo sapiens
-
IC50: 0.0043 mM
0.003
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[4-[(phenylamino)methyl]quinolinium] dibromide
Homo sapiens
-
IC50: 0.003 mM
0.0961
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[7-amino-8-methyl-4-[(phenylamino)methyl]quinolinium] dibromide
Homo sapiens
-
IC50: 0.0961 mM
0.0206
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[7-chloro-4-(dimethylamino)quinolinium] dibromide
Homo sapiens
-
IC50: 0.0206 mM
0.0114
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[7-chloro-4-[(phenylamino)methyl]quinolinium] dibromide
Homo sapiens
-
IC50: 0.0114 mM
0.08
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis(4-aminoquinolinium)
Homo sapiens
-
0.0006
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis(4-azepan-1-ylquinolinium)
Homo sapiens
-
0.0102
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[4-(dimethylamino)quinolinium]
Homo sapiens
-
0.0023
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[4-(phenylamino)quinolinium]
Homo sapiens
-
0.0048
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[4-[(4-chlorophenyl)(methyl)amino]quinolinium]
Homo sapiens
-
0.0014
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[4-[methyl(phenyl)amino]quinolinium]
Homo sapiens
-
0.0575
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[7-amino-4-[(4-chlorophenyl)(methyl)amino]-8-methylquinolinium]
Homo sapiens
-
0.133
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[7-amino-8-methyl-4-[methyl(phenyl)amino]quinolinium]
Homo sapiens
-
0.009
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[7-chloro-4-(dimethylamino)quinolinium]
Homo sapiens
-
0.0057
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[7-chloro-4-[(4-chlorophenyl)(methyl)amino]quinolinium]
Homo sapiens
-
0.0035
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[7-chloro-4-[methyl(phenyl)amino]quinolinium]
Homo sapiens
-
0.01109
1,1'-biphenyl-3,3'-diylbis(4-amino-3-methylquinolinium)
Homo sapiens
-
0.0206
1,1'-biphenyl-3,3'-diylbis(4-amino-7-chloroquinolinium)
Homo sapiens
-
0.0012
1,1'-biphenyl-3,3'-diylbis(4-aminoquinolinium)
Homo sapiens
-
0.0005
1,1'-biphenyl-3,3'-diylbis(4-azepan-1-ylquinolinium)
Homo sapiens
-
0.0012
1,1'-biphenyl-3,3'-diylbis(7-chloro-4-pyrrolidin-1-ylquinolinium)
Homo sapiens
-
0.0044
1,1'-biphenyl-3,3'-diylbis[4-(dimethylamino)quinolinium]
Homo sapiens
-
0.0013
1,1'-biphenyl-3,3'-diylbis[4-(phenylamino)quinolinium]
Homo sapiens
-
0.0021
1,1'-biphenyl-3,3'-diylbis[4-[(4-chlorophenyl)(methyl)amino]quinolinium]
Homo sapiens
-
0.0004
1,1'-biphenyl-3,3'-diylbis[4-[methyl(phenyl)amino]quinolinium]
Homo sapiens
-
0.147
1,1'-biphenyl-3,3'-diylbis[7-amino-4-[(4-chlorophenyl)(methyl)amino]-8-methylquinolinium]
Homo sapiens
-
0.0568
1,1'-biphenyl-3,3'-diylbis[7-amino-8-methyl-4-[methyl(phenyl)amino]quinolinium]
Homo sapiens
-
0.0096
1,1'-biphenyl-3,3'-diylbis[7-chloro-4-(dimethylamino)quinolinium]
Homo sapiens
-
0.0057
1,1'-biphenyl-3,3'-diylbis[7-chloro-4-[(4-chlorophenyl)(methyl)amino]quinolinium]
Homo sapiens
-
0.0031
1,1'-biphenyl-3,3'-diylbis[7-chloro-4-[methyl(phenyl)amino]quinolinium]
Homo sapiens
-
0.0633
1,1'-biphenyl-4,4'-diylbis(4-amino-7-chloroquinolinium)
Homo sapiens
-
0.0811
1,1'-biphenyl-4,4'-diylbis(4-aminoquinolinium)
Homo sapiens
-
0.0022
1,1'-biphenyl-4,4'-diylbis(4-azepan-1-ylquinolinium)
Homo sapiens
-
0.0198
1,1'-biphenyl-4,4'-diylbis(7-chloro-4-pyrrolidin-1-ylquinolinium)
Homo sapiens
-
0.0397
1,1'-biphenyl-4,4'-diylbis[4-(dimethylamino)quinolinium]
Homo sapiens
-
0.0178
1,1'-biphenyl-4,4'-diylbis[4-(phenylamino)quinolinium]
Homo sapiens
-
0.002
1,1'-biphenyl-4,4'-diylbis[4-[(4-chlorophenyl)(methyl)amino]quinolinium]
Homo sapiens
-
0.003
1,1'-biphenyl-4,4'-diylbis[4-[methyl(phenyl)amino]quinolinium]
Homo sapiens
-
0.0461
1,1'-biphenyl-4,4'-diylbis[7-amino-4-[(4-chlorophenyl)(methyl)amino]-8-methylquinolinium]
Homo sapiens
-
0.0961
1,1'-biphenyl-4,4'-diylbis[7-amino-8-methyl-4-[methyl(phenyl)amino]quinolinium]
Homo sapiens
-
0.0206
1,1'-biphenyl-4,4'-diylbis[7-chloro-4-(dimethylamino)quinolinium]
Homo sapiens
-
0.0114
1,1'-biphenyl-4,4'-diylbis[7-chloro-4-[(4-chlorophenyl)(methyl)amino]quinolinium]
Homo sapiens
-
0.0114
1,1'-biphenyl-4,4'-diylbis[7-chloro-4-[methyl(phenyl)amino]quinolinium]
Homo sapiens
-
0.098
1,1'-[(1S,2S)-cyclopropane-1,2-diyldiethane-2,1-diyl]bis(4-piperidin-1-ylpyridinium) dibromide
Homo sapiens
-
IC50: 0.098 mM
0.1
1,1'-[(1S,2S)-cyclopropane-1,2-diyldiethane-2,1-diyl]bis(4-pyrrolidin-1-ylpyridinium) dibromide
Homo sapiens
-
IC50: above 0.1 mM
0.0482 - 0.1
1,1'-[(1S,2S)-cyclopropane-1,2-diyldiethane-2,1-diyl]bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide
0.1
1,1'-[(1S,2S)-cyclopropane-1,2-diyldiethane-2,1-diyl]bis[4-[(phenylamino)methyl]pyridinium] dibromide
Homo sapiens
-
IC50: above 0.1 mM
0.2
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(4-amino-7-chloroquinolinium) dibromide
Homo sapiens
-
IC50: above 0.2 mM
0.08
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(4-aminoquinolinium) dibromide
Homo sapiens
-
IC50: 0.08 mM
0.006
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(4-azepan-1-ylquinolinium) dibromide
Homo sapiens
-
IC50: 0.006 mM
0.0048
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide
Homo sapiens
-
IC50: 0.0048 mM
0.0575
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(7-amino-4-[[(4-chlorophenyl)amino]methyl]-8-methylquinolinium) dibromide
Homo sapiens
-
IC50: 0.0575 mM
0.001
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(7-chloro-4-pyrrolidin-1-ylquinolinium) dibromide
Homo sapiens
-
IC50: 0.001 mM
0.0057
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(7-chloro-4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide
Homo sapiens
-
IC50: 0.0057 mM
0.0102
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[4-(dimethylamino)quinolinium] dibromide
Homo sapiens
-
IC50: 0.0102 mM
0.0023
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[4-(phenylamino)quinolinium] dibromide
Homo sapiens
-
IC50: 0.0023 mM
0.0014
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[4-[(phenylamino)methyl]quinolinium] dibromide
Homo sapiens
-
IC50: 0.0014 mM
0.133
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[7-amino-8-methyl-4-[(phenylamino)methyl]quinolinium] dibromide
Homo sapiens
-
IC50: 0.133 mM
0.009
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[7-chloro-4-(dimethylamino)quinolinium] dibromide
Homo sapiens
-
IC50: 0.009 mM
0.0035
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[7-chloro-4-[(phenylamino)methyl]quinolinium] dibromide
Homo sapiens
-
IC50: 0.0035 mM
0.00143
1-((4'-methoxy-[1,1'-biphenyl]-4-yl)methyl)-4-methyl-1,4-diazepane
0.00621
1-(4-[4-[(6-amino-3H-purin-3-yl)methyl]phenyl]benzyl)-4-(dimethylamino)pyridinium bromide
Homo sapiens
in 100 mM Tris (pH 8.5), 10 mM MgCl2, at 37°C
0.0015
1-([1,1'-biphenyl]-4-ylmethyl)-4-methyl-1,4-diazepane
Homo sapiens
at pH 7.0, temperature not specified in the publication
0.00232
1-([4-[2-(4-[[6-(benzylsulfanyl)-9H-purin-9-yl]methyl]phenyl)ethyl]phenyl]methyl)-4-(dimethylamino)pyridin-1-ium bromide
Homo sapiens
pH and temperature not specified in the publication, recombinant ChoKalpha
0.01836
1-([4-[2-(4-[[6-(benzylsulfanyl)-9H-purin-9-yl]methyl]phenyl)ethyl]phenyl]methyl)-4-(pyrrolidin-1-yl)pyridin-1-ium bromide
Homo sapiens
pH and temperature not specified in the publication, recombinant ChoKalpha
0.01883
1-([4-[4-(4-[[6-(benzylsulfanyl)-9H-purin-9-yl]methyl]phenyl)butyl]phenyl]methyl)-4-(dimethylamino)pyridin-1-ium bromide
Homo sapiens
pH and temperature not specified in the publication, recombinant ChoKalpha
0.05
1-([4-[4-(4-[[6-(benzylsulfanyl)-9H-purin-9-yl]methyl]phenyl)butyl]phenyl]methyl)-4-(pyrrolidin-1-yl)pyridin-1-ium bromide
Homo sapiens
above, pH and temperature not specified in the publication, recombinant ChoKalpha
0.0013 - 0.0015
1-methyl-4-((4'-(4-methylpiperazin-1-yl)-[1,1'-biphenyl]-4-yl)-methyl)-1,4-diazepane
0.0026
1-methyl-4-((4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)methyl)-1,4-diazepane
0.0026
1-methyl-4-(naphthalen-2-ylmethyl)-1,4-diazepane
0.0015
1-[(4'-[[6-(benzylsulfanyl)-9H-purin-9-yl]methyl][1,1'-biphenyl]-4-yl)methyl]-4-(dimethylamino)pyridin-1-ium bromide
Homo sapiens
pH and temperature not specified in the publication, recombinant ChoKalpha
0.05
1-[(4'-[[6-(benzylsulfanyl)-9H-purin-9-yl]methyl][1,1'-biphenyl]-4-yl)methyl]-4-(pyrrolidin-1-yl)pyridin-1-ium bromide
Homo sapiens
above, pH and temperature not specified in the publication, recombinant ChoKalpha
0.0004
1-[(4-[[6-(benzylsulfanyl)-9H-purin-9-yl]methyl]phenyl)methyl]-4-(dimethylamino)pyridin-1-ium bromide
Homo sapiens
pH and temperature not specified in the publication, recombinant ChoKalpha
0.00791
1-[(4-[[6-(benzylsulfanyl)-9H-purin-9-yl]methyl]phenyl)methyl]-4-(pyrrolidin-1-yl)pyridin-1-ium bromide
Homo sapiens
pH and temperature not specified in the publication, recombinant ChoKalpha
0.0389
1-[4-(4-[4-[(6-amino-3H-purin-3-yl)methyl]phenyl]butyl)benzyl]-4-(dimethylamino)pyridinium bromide
Homo sapiens
in 100 mM Tris (pH 8.5), 10 mM MgCl2, at 37°C
0.0107
1-[4-(4-[4-[(6-amino-9H-purin-9-yl)methyl]phenyl]butyl)benzyl]-4-(dimethylamino)pyridinium bromide
Homo sapiens
in 100 mM Tris (pH 8.5), 10 mM MgCl2, at 37°C
0.087
1-[4-[(4-methyl-1,4-diazepan-1-yl)methyl]phenyl]methanamine
Homo sapiens
pH 7.5, 25°C, recombinant enzyme
0.0107
1-[[4-(4-[4-[(6-amino-9H-purin-9-yl)methyl]phenyl]butyl)phenyl]methyl]-4-(dimethylamino)pyridin-1-ium bromide
Homo sapiens
pH and temperature not specified in the publication, recombinant ChoKalpha
0.00052
1-[[4-[4-[[4-(4-chloro-N-methylanilino)quinolin-1-ium-1-yl]methyl]phenyl]phenyl]methyl]-N-(4-chlorophenyl)-N-methylquinolin-1-ium-4-amine
Homo sapiens
wild-type enzyme ChoKalpha, pH 7.5, 37°C
0.0132
12,19-diaza-1,8-diazoniapentacyclo[18.2.2.23,6.28,11.214,17]triaconta-1(22),3,5,8,10,14,16,20,23,25,27,29-dodecaene dibromide
Homo sapiens
-
IC50: 0.0132 mM
0.0021
12,21-diaza-1,8-diazoniapentacyclo[20.2.2.23,6.28,11.014,19]triaconta-1(24),3,5,8,10,14,16,18,22,25,27,29-dodecaene dibromide
Homo sapiens
-
IC50: 0.0021 mM
0.0003
14,21-diaza-1,10-diazoniapentacyclo[20.2.2.210,13.216,19.03,8]triaconta-1(24),3,5,7,10,12,16,18,22,25,27,29-dodecaene dibromide
0.000085
2'-fluoro-4,4'-bis((4-methyl-1,4-diazepan-1-yl)methyl)-[1,1'-biphenyl]-2-carbonitrile
0.000233
4,4'-((2,3-difluoro-[1,1'-biphenyl]-4,4'-diyl)bis(methylene))bis-(1-methyl-1,4-diazepane)
0.000165
4,4'-((2-fluoro-[1,1'-biphenyl]-4,4'-diyl)bis(methylene))bis(1-methyl-1,4-diazepane)
0.000255
4,4'-((3,5-difluoro-[1,1'-biphenyl]-4,4'-diyl)bis(methylene))bis-(1-methyl-1,4-diazepane)
0.000268
4,4'-((3-chloro-[1,1'-biphenyl]-4,4'-diyl)bis(methylene))bis(1-methyl-1,4-diazepane)
0.000457
4,4'-bis((4-methyl-1,4-diazepan-1-yl)methyl)-1,1'-biphenyl
0.000066
4,4'-bis((4-methyl-1,4-diazepan-1-yl)methyl)-[1,1'-biphenyl]-2-carbonitrile
0.0007
4-(4-chloro-N-methylanilino)-1-(4-[4-[(4-dimethylaminopyridinium-1-yl)methyl]phenethyl]benzyl)pyridinium dibromide
Homo sapiens
at pH 8.5 and 37°C
0.0015
4-(4-chloro-N-methylanilino)-1-(4-[4-[(4-dimethylaminopyridinium-1-yl)methyl]phenyl]benzyl)pyridinium dibromide
Homo sapiens
at pH 8.5 and 37°C
0.0025
4-(4-chloro-N-methylanilino)-1-(4-[4-[(4-pyrrolidinopyridinium-1-yl)methyl]phenethyl]benzyl)pyridinium dibromide
Homo sapiens
at pH 8.5 and 37°C
0.0022
4-(4-chloro-N-methylanilino)-1-(4-[4-[(4-pyrrolidinopyridinium-1-yl)methyl]phenyl]benzyl)pyridinium dibromide
Homo sapiens
at pH 8.5 and 37°C
0.0012
4-(4-chloro-N-methylanilino)-1-[4-(4-[4-[(4-dimethylaminopyridinium-1-yl)methyl]phenyl]butyl)benzyl]pyridinium dibromide
Homo sapiens
at pH 8.5 and 37°C
0.0015
4-(4-chloro-N-methylanilino)-1-[4-(4-[4-[(4-pyrrolidinopyridinium-1-yl)methyl]phenyl]butyl)benzyl]pyridinium dibromide
Homo sapiens
at pH 8.5 and 37°C
0.0009
4-(4-chloro-N-methylanilino)-1-[4-[(4-dimethylaminopyridinium-1-yl)methyl]benzyl]pyridinium dibromide
Homo sapiens
at pH 8.5 and 37°C
0.0006
4-(4-chloro-N-methylanilino)-1-[4-[(4-pyrrolidinopyridinium-1-yl)methyl]benzyl]pyridinium dibromide
Homo sapiens
at pH 8.5 and 37°C
0.0012
4-(dimethylamino)-1-(4-[4-[(4-pyrrolidinopyridinium-1-yl)-methyl]phenethyl]benzyl)pyridinium dibromide
Homo sapiens
at pH 8.5 and 37°C
0.0008
4-(dimethylamino)-1-(4-[4-[(4-pyrrolidinopyridinium-1-yl)-methyl]phenyl]benzyl)pyridinium dibromide
Homo sapiens
at pH 8.5 and 37°C
0.0009
4-(dimethylamino)-1-[4-(4-[4-[(4-pyrrolidinopyridinium-1-yl)-methyl]phenyl]butyl)benzyl]pyridinium dibromide
Homo sapiens
at pH 8.5 and 37°C
0.008
4-(dimethylamino)-1-[4-[(4-pyrrolidinopyridinium-1-yl)methyl]-benzyl]pyridinium dibromide
Homo sapiens
at pH 8.5 and 37°C
0.0014
4-chloro-N-methylanilino
Homo sapiens
-
IC50: 0.0014 mM
0.0248
5,10,11,16,17,22-hexahydro-6,9:18,21-diethenodibenzo[g,p][1,5,10,14]tetraazacyclooctadecine-6,21-diium dibromide
Homo sapiens
-
IC50: 0.0248 mM
0.0172
6-[(1-methyl-1,4-diazepan-6-yl)methyl]quinoline
Homo sapiens
pH 7.5, 25°C, recombinant enzyme
0.0015 - 0.0039
7-((4-methyl-1,4-diazepan-1-yl)methyl)quinolone
0.001
7-chloro-1-(4-[2-[4-(7-chloro-5-pyrrolidin-1-ylquinolinium-1-yl)phenyl]ethyl]phenyl)-4-pyrrolidin-1-ylquinolinium
Homo sapiens
-
0.005
choline kinase inhibitor Mn58b
Homo sapiens
-
-
0.057
hemicholinium-3
Homo sapiens
-
weak inhibitor, IC50: 0.057 mM
0.00495
methyl 4'-((4-methyl-1,4-diazepan-1-yl)methyl)-[1,1'-biphenyl]-4-carboxylate
0.00192
RSM932A
Homo sapiens
at pH 8.5 and 37°C
0.00047
V-11-023907
Homo sapiens
in 100 mM Tris-HCl pH 7.5, 100 mM KCl, 10 mM MgCl2, at 25°C
2
[4-(4-methyl-1,4-diazepan-1-yl)phenyl]methanol
Homo sapiens
pH 7.5, 25°C, recombinant enzyme
additional information
additional information
Homo sapiens
IC50 values for inhibitors with HepG2 cell and the cytosolic fraction of HepG2 cells, overview
-
0.000251
(4-methyl-1,4-diazepan-1-yl)(4'-((4-methyl-1,4-diazepan-1-yl)-methyl)-[1,1'-biphenyl]-4-yl)methanone
Homo sapiens
pH 7.5, 25°C, recombinant enzyme
0.000251
(4-methyl-1,4-diazepan-1-yl)(4'-((4-methyl-1,4-diazepan-1-yl)-methyl)-[1,1'-biphenyl]-4-yl)methanone
Homo sapiens
at pH 7.0, temperature not specified in the publication
0.0482
1,1'-[(1S,2S)-cyclopropane-1,2-diyldiethane-2,1-diyl]bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide
Homo sapiens
-
IC50: 0.0482 mM
0.1
1,1'-[(1S,2S)-cyclopropane-1,2-diyldiethane-2,1-diyl]bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide
Homo sapiens
-
IC50: above 0.1 mM
0.00143
1-((4'-methoxy-[1,1'-biphenyl]-4-yl)methyl)-4-methyl-1,4-diazepane
Homo sapiens
pH 7.5, 25°C, recombinant enzyme
0.00143
1-((4'-methoxy-[1,1'-biphenyl]-4-yl)methyl)-4-methyl-1,4-diazepane
Homo sapiens
at pH 7.0, temperature not specified in the publication
0.0013
1-methyl-4-((4'-(4-methylpiperazin-1-yl)-[1,1'-biphenyl]-4-yl)-methyl)-1,4-diazepane
Homo sapiens
pH 7.5, 25°C, recombinant enzyme
0.0013
1-methyl-4-((4'-(4-methylpiperazin-1-yl)-[1,1'-biphenyl]-4-yl)-methyl)-1,4-diazepane
Homo sapiens
at pH 7.0, temperature not specified in the publication
0.0015
1-methyl-4-((4'-(4-methylpiperazin-1-yl)-[1,1'-biphenyl]-4-yl)-methyl)-1,4-diazepane
Homo sapiens
pH 7.5, 25°C, recombinant enzyme
0.0026
1-methyl-4-((4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)methyl)-1,4-diazepane
Homo sapiens
pH 7.5, 25°C, recombinant enzyme
0.0026
1-methyl-4-((4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)methyl)-1,4-diazepane
Homo sapiens
at pH 7.0, temperature not specified in the publication
0.0026
1-methyl-4-(naphthalen-2-ylmethyl)-1,4-diazepane
Homo sapiens
pH 7.5, 25°C, recombinant enzyme
0.0026
1-methyl-4-(naphthalen-2-ylmethyl)-1,4-diazepane
Homo sapiens
at pH 7.0, temperature not specified in the publication
0.0003
14,21-diaza-1,10-diazoniapentacyclo[20.2.2.210,13.216,19.03,8]triaconta-1(24),3,5,7,10,12,16,18,22,25,27,29-dodecaene dibromide
Homo sapiens
-
IC50: 0.0003 mM
0.0003
14,21-diaza-1,10-diazoniapentacyclo[20.2.2.210,13.216,19.03,8]triaconta-1(24),3,5,7,10,12,16,18,22,25,27,29-dodecaene dibromide
Homo sapiens
-
IC50: 0.0003 mM, most potent inhibitor
0.000085
2'-fluoro-4,4'-bis((4-methyl-1,4-diazepan-1-yl)methyl)-[1,1'-biphenyl]-2-carbonitrile
Homo sapiens
pH 7.5, 25°C, recombinant enzyme
0.000085
2'-fluoro-4,4'-bis((4-methyl-1,4-diazepan-1-yl)methyl)-[1,1'-biphenyl]-2-carbonitrile
Homo sapiens
at pH 7.0, temperature not specified in the publication
0.000233
4,4'-((2,3-difluoro-[1,1'-biphenyl]-4,4'-diyl)bis(methylene))bis-(1-methyl-1,4-diazepane)
Homo sapiens
pH 7.5, 25°C, recombinant enzyme
0.000233
4,4'-((2,3-difluoro-[1,1'-biphenyl]-4,4'-diyl)bis(methylene))bis-(1-methyl-1,4-diazepane)
Homo sapiens
at pH 7.0, temperature not specified in the publication
0.000165
4,4'-((2-fluoro-[1,1'-biphenyl]-4,4'-diyl)bis(methylene))bis(1-methyl-1,4-diazepane)
Homo sapiens
pH 7.5, 25°C, recombinant enzyme
0.000165
4,4'-((2-fluoro-[1,1'-biphenyl]-4,4'-diyl)bis(methylene))bis(1-methyl-1,4-diazepane)
Homo sapiens
at pH 7.0, temperature not specified in the publication
0.000255
4,4'-((3,5-difluoro-[1,1'-biphenyl]-4,4'-diyl)bis(methylene))bis-(1-methyl-1,4-diazepane)
Homo sapiens
pH 7.5, 25°C, recombinant enzyme
0.000255
4,4'-((3,5-difluoro-[1,1'-biphenyl]-4,4'-diyl)bis(methylene))bis-(1-methyl-1,4-diazepane)
Homo sapiens
at pH 7.0, temperature not specified in the publication
0.000268
4,4'-((3-chloro-[1,1'-biphenyl]-4,4'-diyl)bis(methylene))bis(1-methyl-1,4-diazepane)
Homo sapiens
pH 7.5, 25°C, recombinant enzyme
0.000268
4,4'-((3-chloro-[1,1'-biphenyl]-4,4'-diyl)bis(methylene))bis(1-methyl-1,4-diazepane)
Homo sapiens
at pH 7.0, temperature not specified in the publication
0.000457
4,4'-bis((4-methyl-1,4-diazepan-1-yl)methyl)-1,1'-biphenyl
Homo sapiens
pH 7.5, 25°C, recombinant enzyme
0.000457
4,4'-bis((4-methyl-1,4-diazepan-1-yl)methyl)-1,1'-biphenyl
Homo sapiens
at pH 7.0, temperature not specified in the publication
0.000066
4,4'-bis((4-methyl-1,4-diazepan-1-yl)methyl)-[1,1'-biphenyl]-2-carbonitrile
Homo sapiens
pH 7.5, 25°C, recombinant enzyme
0.000066
4,4'-bis((4-methyl-1,4-diazepan-1-yl)methyl)-[1,1'-biphenyl]-2-carbonitrile
Homo sapiens
at pH 7.0, temperature not specified in the publication
0.0015
7-((4-methyl-1,4-diazepan-1-yl)methyl)quinolone
Homo sapiens
at pH 7.0, temperature not specified in the publication
0.0039
7-((4-methyl-1,4-diazepan-1-yl)methyl)quinolone
Homo sapiens
pH 7.5, 25°C, recombinant enzyme
0.00495
methyl 4'-((4-methyl-1,4-diazepan-1-yl)methyl)-[1,1'-biphenyl]-4-carboxylate
Homo sapiens
pH 7.5, 25°C, recombinant enzyme
0.00495
methyl 4'-((4-methyl-1,4-diazepan-1-yl)methyl)-[1,1'-biphenyl]-4-carboxylate
Homo sapiens
at pH 7.0, temperature not specified in the publication
0.0001
MN58b
Homo sapiens
-
H510 cell, 144 h
0.00027
MN58b
Homo sapiens
-
H82 cell, 144 h
0.0004
MN58b
Homo sapiens
-
H510 cell, 72 h
0.0005 - 0.072
MN58b
Homo sapiens
-
specific inhibitor, IC50: 0.0005-0.072 mM depending on cell type
0.00078
MN58b
Homo sapiens
at pH 8.5 and 37°C
0.0008
MN58b
Homo sapiens
-
H82 cell, 72 h
0.0009
MN58b
Homo sapiens
-
H1299 cell, 144 h
0.0011
MN58b
Homo sapiens
-
H460 cell, 144 h
0.0011
MN58b
Homo sapiens
-
H510 cell, 48 h
0.0019
MN58b
Homo sapiens
-
H82 cell, 48 h
0.0026
MN58b
Homo sapiens
-
H460 cell, 72 h
0.0027
MN58b
Homo sapiens
-
H1299 cell, 72 h
0.0034
MN58b
Homo sapiens
-
primary HMEC cell, 144 h
0.0042
MN58b
Homo sapiens
-
primary BEC cell, 144 h
0.00703
MN58b
Homo sapiens
-
H460 cell, 48 h
0.0103
MN58b
Homo sapiens
-
H1299 cell, 48 h
0.0183
MN58b
Homo sapiens
-
primary BEC cell, 72 h
0.0209
MN58b
Homo sapiens
-
primary HMEC cell, 72 h
0.0405
MN58b
Homo sapiens
-
primary BEC cell, 48 h
0.0447
MN58b
Homo sapiens
-
primary HMEC cell, 48 h
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Hosaka, K.; Tanaka, S.; Nikawa, J.; Yamashita, S.
Cloning of a human choline kinase cDNA by complementation of the yeast cki mutation
FEBS Lett.
304
229-232
1992
Homo sapiens
brenda
Hernandez-Alcoceba, R.; Fernandez, F.; Lacal, J.C.
In vivo antitumor activity of choline kinase inhibitors: a novel target for anticancer drug discovery
Cancer Res.
59
3112-3118
1999
Homo sapiens
brenda
Ishidate, K.
Choline/ethanolamine kinase from mammalian tissues
Biochim. Biophys. Acta
1348
70-78
1997
Homo sapiens, Rattus norvegicus
brenda
Rodriguez-Gonzalez, A.; Ramirez de Molina, A.; Benitez-Rajal, J.; Lacal, J.C.
Phospholipase D and choline kinase: their role in cancer development and their potential as drug targets
Prog. Cell Cycle Res.
5
191-201
2003
Mus musculus (Q54AG5), Homo sapiens (Q9Y259)
brenda
Aoyama, C.; Liao, H.; Ishidate, K.
Structure and function of choline kinase isoforms in mammalian cells
Prog. Lipid Res.
43
266-281
2004
Saccharomyces cerevisiae, Caenorhabditis elegans, Homo sapiens, Mus musculus, Rattus norvegicus
brenda
Al-Saeedi, F.; Smith, T.; Welch, A.
[Methyl-3H]-choline incorporation into MCF-7 cells: correlation with proliferation, choline kinase and phospholipase D assay
Anticancer Res.
27
901-906
2007
Homo sapiens
brenda
Glunde, K.; Raman, V.; Mori, N.; Bhujwalla, Z.M.
RNA interference-mediated choline kinase suppression in breast cancer cells induces differentiation and reduces proliferation
Cancer Res.
65
11034-11043
2005
Homo sapiens
brenda
Milanese, L.; Espinosa, A.; Campos, J.M.; Gallo, M.A.; Entrena, A.
Insight into the inhibition of human choline kinase: homology modeling and molecular dynamics simulations
ChemMedChem
1
1216-1228
2006
Caenorhabditis elegans, Homo sapiens
brenda
Janardhan, S.; Srivani, P.; Sastry, G.N.
Choline kinase: an important target for cancer
Curr. Med. Chem.
13
1169-1186
2006
Saccharomyces cerevisiae, Caenorhabditis elegans, Homo sapiens, Mus musculus, Rattus norvegicus, Schizosaccharomyces pombe
brenda
Campos, J.M.; Sanchez-Martin, R.M.; Conejo-Garcia, A.; Entrena, A.; Gallo, M.A.; Espinosa, A.
(Q)SAR studies to design new human choline kinase inhibitors as antiproliferative drugs
Curr. Med. Chem.
13
1231-1248
2006
Homo sapiens
brenda
Conejo-Garcia, A.; Entrena, A.; Campos, J.M.; Sanchez-Martin, R.M.; Gallo, M.A.; Espinosa, A.
Towards a model for the inhibition of choline kinase by a new type of inhibitor
Eur. J. Med. Chem.
40
315-319
2005
Homo sapiens
brenda
Rodriguez-Gonzalez, A.; Ramirez de Molina, A.; Banez-Coronel, M.; Megias, D.; Lacal, J.C.
Inhibition of choline kinase renders a highly selective cytotoxic effect in tumour cells through a mitochondrial independent mechanism
Int. J. Oncol.
26
999-1008
2005
Homo sapiens
brenda
Malito, E.; Sekulic, N.; Too, W.C.; Konrad, M.; Lavie, A.
Elucidation of human choline kinase crystal structures in complex with the products ADP or phosphocholine
J. Mol. Biol.
364
136-151
2006
Homo sapiens (P35790), Homo sapiens
brenda
Mori, N.; Glunde, K.; Takagi, T.; Raman, V.; Bhujwalla, Z.M.
Choline kinase down-regulation increases the effect of 5-fluorouracil in breast cancer cells
Cancer Res.
67
11284-11290
2007
Homo sapiens
brenda
Glunde, K.; Shah, T.; Winnard, P.T.; Raman, V.; Takagi, T.; Vesuna, F.; Artemov, D.; Bhujwalla, Z.M.
Hypoxia regulates choline kinase expression through hypoxia-inducible factor-1 alpha signaling in a human prostate cancer model
Cancer Res.
68
172-180
2008
Homo sapiens
brenda
Ramirez de Molina, A.; Gallego-Ortega, D.; Sarmentero-Estrada, J.; Lagares, D.; Gomez Del Pulgar, T.; Bandres, E.; Garcia-Foncillas, J.; Lacal, J.C.
Choline kinase as a link connecting phospholipid metabolism and cell cycle regulation: implications in cancer therapy
Int. J. Biochem. Cell Biol.
40
1753-1763
2008
Homo sapiens
brenda
Ramirez de Molina, A.; Sarmentero-Estrada, J.; Belda-Iniesta, C.; Taron, M.; Ramirez de Molina, V.; Cejas, P.; Skrzypski, M.; Gallego-Ortega, D.; de Castro, J.; Casado, E.; Garcia-Cabezas, M.A.; Sanchez, J.J.; Nistal, M.; Rosell, R.; Gonzalez-Baron, M.; Lacal, J.C.
Expression of choline kinase alpha to predict outcome in patients with early-stage non-small-cell lung cancer: a retrospective study
Lancet Oncol.
8
889-897
2007
Homo sapiens
brenda
Srivani, P.; Sastry, G.N.
Potential choline kinase inhibitors: a molecular modeling study of bis-quinolinium compounds
J. Mol. Graph. Model.
27
676-688
2009
Homo sapiens (P35790)
brenda
Ross, J.; Najjar, A.M.; Sankaranarayanapillai, M.; Tong, W.P.; Kaluarachchi, K.; Ronen, S.M.
Fatty acid synthase inhibition results in a magnetic resonance-detectable drop in phosphocholine
Mol. Cancer Ther.
7
2556-2565
2008
Homo sapiens
brenda
Chua, B.T.; Gallego-Ortega, D.; Ramirez de Molina, A.; Ullrich, A.; Lacal, J.C.; Downward, J.
Regulation of Akt(ser473)phosphorylation by Choline kinase in breast carcinoma cells
Mol. Cancer
8
131
2009
Homo sapiens
brenda
Nimmagadda, S.; Glunde, K.; Pomper, M.G.; Bhujwalla, Z.M.
Pharmacodynamic markers for choline kinase down-regulation in breast cancer cells
Neoplasia
11
477-484
2009
Homo sapiens
brenda
Yalcin, A.; Clem, B.; Makoni, S.; Clem, A.; Nelson, K.; Thornburg, J.; Siow, D.; Lane, A.N.; Brock, S.E.; Goswami, U.; Eaton, J.W.; Telang, S.; Chesney, J.
Selective inhibition of choline kinase simultaneously attenuates MAPK and PI3K/AKT signaling
Oncogene
29
139-149
2009
Homo sapiens
brenda
Gallego-Ortega, D.; Ramirez de Molina, A.; Ramos, M.A.; Valdes-Mora, F.; Barderas, M.G.; Sarmentero-Estrada, J.; Lacal, J.C.
Differential role of human choline kinase alpha and beta enzymes in lipid metabolism: implications in cancer onset and treatment
PLoS ONE
4
e7819
2009
Homo sapiens (P35790), Homo sapiens (Q9Y259), Homo sapiens
brenda
Hudson, C.S.; Knegtel, R.M.; Brown, K.; Charlton, P.A.; Pollard, J.R.
Kinetic and mechanistic characterisation of choline kinase-alpha
Biochim. Biophys. Acta
1834
1107-1116
2013
Homo sapiens (P35790), Homo sapiens
brenda
Rubio-Ruiz, B.; Conejo-Garcia, A.; Rios-Marco, P.; Carrasco-Jimenez, M.P.; Segovia, J.; Marco, C.; Gallo, M.A.; Espinosa, A.; Entrena, A.
Design, synthesis, theoretical calculations and biological evaluation of new non-symmetrical choline kinase inhibitors
Eur. J. Med. Chem.
50
154-162
2012
Homo sapiens (P35790)
brenda
Gruber, J.; See Too, W.C.; Wong, M.T.; Lavie, A.; McSorley, T.; Konrad, M.
Balance of human choline kinase isoforms is critical for cell cycle regulation: implications for the development of choline kinase-targeted cancer therapy
FEBS J.
279
1915-1928
2012
Homo sapiens
brenda
Hong, B.S.; Allali-Hassani, A.; Tempel, W.; Finerty, P.J.; Mackenzie, F.; Dimov, S.; Vedadi, M.; Park, H.W.
Crystal structures of human choline kinase isoforms in complex with hemicholinium-3: single amino acid near the active site influences inhibitor sensitivity
J. Biol. Chem.
285
16330-16340
2010
Homo sapiens (P35790), Homo sapiens (Q9Y259), Homo sapiens
brenda
Bansal, A.; Harris, R.A.; DeGrado, T.R.
Choline phosphorylation and regulation of transcription of choline kinase alpha in hypoxia
J. Lipid Res.
53
149-157
2012
Homo sapiens
brenda
Miyake, T.; Parsons, S.J.
Functional interactions between choline kinase alpha, epidermal growth factor receptor and c-Src in breast cancer cell proliferation
Oncogene
31
1431-1441
2012
Homo sapiens (P35790)
brenda
Li, Z.; Wu, G.; van der Veen, J.N.; Hermansson, M.; Vance, D.E.
Phosphatidylcholine metabolism and choline kinase in human osteoblasts
Biochim. Biophys. Acta
1841
859-867
2014
Homo sapiens (P35790), Homo sapiens
brenda
Schiaffino-Ortega, S.; Lopez-Cara, L.C.; Rios-Marco, P.; Carrasco-Jimenez, M.P.; Gallo, M.A.; Espinosa, A.; Marco, C.; Entrena, A.
New non-symmetrical choline kinase inhibitors
Bioorg. Med. Chem.
21
7146-7154
2013
Homo sapiens (P35790)
brenda
Rubio-Ruiz, B.; Figuerola-Conchas, A.; Ramos-Torrecillas, J.; Capitan-Canadas, F.; Rios-Marco, P.; Carrasco, M.P.; Gallo, M.A.; Espinosa, A.; Marco, C.; Ruiz, C.; Entrena, A.; Hurtado-Guerrero, R.; Conejo-Garcia, A.
Discovery of a new binding site on human choline kinase alpha1: design, synthesis, crystallographic studies, and biological evaluation of asymmetrical bispyridinium derivatives
J. Med. Chem.
57
507-515
2014
Homo sapiens (P35790), Homo sapiens
brenda
Zech, S.G.; Kohlmann, A.; Zhou, T.; Li, F.; Squillace, R.M.; Parillon, L.E.; Greenfield, M.T.; Miller, D.P.; Qi, J.; Thomas, R.M.; Wang, Y.; Xu, Y.; Miret, J.J.; Shakespeare, W.C.; Zhu, X.; Dalgarno, D.C.
Novel small molecule inhibitors of choline kinase identified by fragment-based drug discovery
J. Med. Chem.
59
671-686
2016
Homo sapiens (P35790), Homo sapiens
brenda
Trousil, S.; Carroll, L.; Kalusa, A.; Aberg, O.; Kaliszczak, M.; Aboagye, E.O.
Design of symmetrical and nonsymmetrical N,N-dimethylaminopyridine derivatives as highly potent choline kinase alpha inhibitors
MedChemComm
2013
693-696
2013
Homo sapiens
brenda
Mori, N.; Gadiya, M.; Wildes, F.; Krishnamachary, B.; Glunde, K.; Bhujwalla, Z.M.
Characterization of choline kinase in human endothelial cells
NMR Biomed.
26
1501-1507
2013
Homo sapiens (P35790), Homo sapiens
brenda
Chang, C.C.; Few, L.L.; Konrad, M.; See Too, W.C.
Phosphorylation of human choline kinase beta by protein kinase A: its impact on activity and inhibition
PLoS ONE
11
e0154702
2016
Homo sapiens (Q9Y259), Homo sapiens
brenda
Schiaffino-Ortega, S.; Baglioni, E.; Mariotto, E.; Bortolozzi, R.; Serran-Aguilera, L.; Rios-Marco, P.; Carrasco-Jimenez, M.P.; Gallo, M.A.; Hurtado-Guerrero, R.; Marco, C.; Basso, G.; Viola, G.; Entrena, A.; Lopez-Cara, L.C.
Design, synthesis, crystallization and biological evaluation of new symmetrical biscationic compounds as selective inhibitors of human choline kinase alpha1 (ChoKalpha1)
Sci. Rep.
6
23793
2016
Homo sapiens (P35790), Homo sapiens
brenda
Kall, S.L.; Delikatny, E.J.; Lavie, A.
Identification of a unique inhibitor-binding site on choline kinase alpha
Biochemistry
57
1316-1325
2018
Homo sapiens (P35790)
brenda
Zech, S.; Kohlmann, A.; Zhou, T.; Li, F.; Squillace, R.; Parillon, L.; Greenfield, M.; Miller, D.; Qi, J.; Thomas, R.; Wang, Y.; Xu, Y.; Miret, J.; Shakespeare, W.; Zhu, X.; Dalgarno, D.
Novel small molecule inhibitors of choline kinase identified by fragment-based drug discovery
J. Med. Chem.
59
671-686
2016
Homo sapiens (O54804), Homo sapiens
brenda
Rubio-Ruiz, B.; Rixados-Marco, P.; Carrasco-Jimenez, M.; Espinosa, A.; Hurtado-Guerrero, R.; Marco, C.; Conejo-Garcixada, A.; Entrena, A.
Choline kinase inhibition and docking studies of a series of 6-(benzylthio)-9H-purin-9-yl-pyridinium derivatives
Med. Chem. Res.
26
2809-2815
2017
Homo sapiens (O54804)
-
brenda
Kall, S.L.; Whitlatch, K.; Smithgall, T.E.; Lavie, A.
Molecular basis for the interaction between human choline kinase alpha and the SH3 domain of the c-Src tyrosine kinase
Sci. Rep.
9
17121
2019
Homo sapiens (P35790), Homo sapiens
brenda