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2-(dimethylamino)-ethanol + ATP
ADP + 2-(dimethylamino)-ethyl phosphate
2-aminoethanol + ATP
ADP + 2-aminoethyl phosphate
-
-
-
-
?
2-methylaminoethanol + ATP
ADP + 2-methylaminoethyl phosphate
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
ATP + choline
ADP + phosphocholine
ATP + dimethylethanolamine
ADP + phosphodimethylethanolamine
-
-
-
-
?
ATP + ethanolamine
ADP + ethanolamine phosphate
ATP + ethanolamine
ADP + O-phosphoethanolamine
ATP + ethanolamine
ADP + phosphoethanolamine
-
-
-
-
?
beta-methylcholine + ATP
ADP + beta-methylcholine phosphate
-
-
-
-
?
choline + ATP
O-phosphocholine + ADP
choline + ATP
phosphocholine + ADP
choline + ATP
phosphorylcholine + ADP
-
-
-
?
CTP + choline
CDP + choline phosphate
-
12% of the activity with ATP
-
-
?
diethanolamine + ATP
ADP + O-phospho-diethanolamine
-
-
-
-
?
ethanolamine + ATP
ADP + ethanolamine phosphate
ethanolamine + ATP
O-phosphoethanolamine + ADP
-
first step in the biosynthesis of the glycerophospholipid glycerophosphoethanolamine
-
-
?
ethanolamine + ATP
phosphoethanolamine + ADP
-
-
-
?
GTP + choline
GDP + choline phosphate
N,N,N-triethylethanolamine + ATP
ADP + N,N,N-triethylethanolamine phosphate
-
weak
-
-
?
N,N-diethyl-N-methylethanolamine + ATP
ADP + N,N-diethyl-N-methylethanolamine phosphate
-
weak
-
-
?
N,N-diethylethanolamine + ATP
ADP + N,N-diethylethanolamine phosphate
N,N-diethylethanolamine + ATP
ADP + O-phospho-N-diethylethanolamine
-
-
-
-
?
N,N-diisopropylethanolamine + ATP
ADP + N,N-diisopropylethanolamine phosphate
-
-
-
-
?
N,N-dimethyl-N-propylethanolamine + ATP
ADP + N,N-dimethyl-N-propylethanolamine phosphate
-
-
-
-
?
N,N-dimethylaminopropanol + ATP
ADP + N,N-dimethylaminopropyl phosphate
-
-
-
-
?
N,N-dimethylethanolamine + ATP
ADP + N,N-dimethylethanolamine phosphate
N,N-dimethylethanolamine + ATP
ADP + O-phospho-N,N-dimethylethanolamine
-
-
-
-
?
N,N-dimethylethylcholine + ATP
ADP + N,N-dimethylethylcholine phosphate
-
-
-
-
?
N,N-dimethylisopropylcholine + ATP
ADP + N,N-dimethylisopropylcholine phosphate
-
-
-
-
?
N,N-dimethylpropylcholine + ATP
ADP + N,N-dimethylpropylcholine phosphate
-
-
-
-
?
N-ethylethanolamine + ATP
ADP + O-phospho-N-ethylethanolamine
-
-
-
-
?
N-methylethanolamine + ATP
ADP + N-methylethanolamine phosphate
N-methylethanolamine + ATP
ADP + O-phospho-N-methylethanolamine
-
-
-
-
?
N-monoethylethanolamine + ATP
ADP + N-monoethylethanolamine phosphate
-
-
-
-
?
N-monomethylethanolamine + ATP
ADP + N-monomethylethanolamine phosphate
UTP + choline
UDP + choline phosphate
additional information
?
-
2-(dimethylamino)-ethanol + ATP

ADP + 2-(dimethylamino)-ethyl phosphate
-
-
-
-
?
2-(dimethylamino)-ethanol + ATP
ADP + 2-(dimethylamino)-ethyl phosphate
-
-
-
-
?
ATP + choline

ADP + O-phosphocholine
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
-
initial step of the Kennedy pathway, that yields phosphatidylcholine as final product, increased activity under salt stress and cold conditions
-
-
?
ATP + choline
ADP + O-phosphocholine
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
-
initial step of the CDP-choline pathway, that yields phosphatidylcholine as final product, involved in mitogenic signaling transduction
-
-
?
ATP + choline
ADP + O-phosphocholine
-
-
-
?
ATP + choline
ADP + O-phosphocholine
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
-
-
-
?
ATP + choline
ADP + O-phosphocholine
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
-
-
-
?
ATP + choline
ADP + O-phosphocholine
-
-
-
?
ATP + choline
ADP + O-phosphocholine
-
-
-
?
ATP + choline
ADP + O-phosphocholine
-
-
-
?
ATP + choline
ADP + O-phosphocholine
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
-
-
-
?
ATP + choline
ADP + O-phosphocholine
-
-
-
?
ATP + choline
ADP + O-phosphocholine
-
initial enzyme of the CDP-choline pathway and the CDP-ethanolamine pathway
-
-
?
ATP + choline
ADP + O-phosphocholine
-
choline pathway or CDP-ethanolamine pathway is so-called Kennedy pathway
-
-
?
ATP + choline
ADP + O-phosphocholine
-
initial step of the CDP-choline pathway, that yields phosphatidylcholine as final product, involved in mitogenic signaling transduction, possible role in carcinogenesis
-
-
?
ATP + choline
ADP + O-phosphocholine
initial step of the Kennedy pathway, that yields phosphatidylcholine as final product, involved in mitogenic signaling transduction, the product O-phosphocholine serves as second messenger and is essential for cell growth, enzyme plays a role in tumor generation
-
-
?
ATP + choline
ADP + O-phosphocholine
-
-
-
?
ATP + choline
ADP + O-phosphocholine
the catalytic efficiency (Vmax/Km) using choline as substrate is 2000fold greater than the efficiency using ethanolamine as substrate
-
-
?
ATP + choline
ADP + O-phosphocholine
the catalytic efficiency (Vmax/Km) using choline as substrate is 2000fold greater than the efficiency using ethanolamine as substrate
-
-
?
ATP + choline
ADP + O-phosphocholine
-
-
-
?
ATP + choline
ADP + O-phosphocholine
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
-
-
-
?
ATP + choline
ADP + O-phosphocholine
-
initial step of the CDP-choline pathway, that yields phosphatidylcholine as final product, involved in mitogenic signaling transduction, involved in cell stress response
-
-
?
ATP + choline
ADP + O-phosphocholine
initial step of the Kennedy pathway, that yields phosphatidylcholine as final product, involved in mitogenic signaling transduction
-
-
?
ATP + choline
ADP + O-phosphocholine
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
-
enzyme of the CDP-choline pathway of lecithin biosynthesis
-
-
?
ATP + choline
ADP + O-phosphocholine
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
-
-
-
?
ATP + choline
ADP + O-phosphocholine
-
-
641347, 641348, 641349, 641352, 641359, 641360, 641366, 641368, 641370, 641371, 641372, 663274, 673201 -
-
?
ATP + choline
ADP + O-phosphocholine
-
both isoforms
-
-
?
ATP + choline
ADP + O-phosphocholine
-
initial enzyme of the CDP-choline pathway and the CDP-ethanolamine pathway
-
-
?
ATP + choline
ADP + O-phosphocholine
-
choline pathway or CDP-ethanolamine pathway is so-called Kennedy pathway
-
-
?
ATP + choline
ADP + O-phosphocholine
-
enzyme of the CDP-choline pathway of lecithin biosynthesis
-
?
ATP + choline
ADP + O-phosphocholine
-
initial step of the CDP-choline pathway, that yields phosphatidylcholine as final product, involved in mitogenic signaling transduction and cell stress regulation
-
-
?
ATP + choline
ADP + O-phosphocholine
-
-
-
-
r
ATP + choline
ADP + O-phosphocholine
-
-
-
?
ATP + choline
ADP + O-phosphocholine
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
-
-
-
-
r
ATP + choline
ADP + O-phosphocholine
-
initial enzyme of the CDP-choline pathway and the CDP-ethanolamine pathway
-
-
?
ATP + choline
ADP + O-phosphocholine
-
initial step of the CDP-choline pathway, that yields phosphatidylcholine as final product, involved in mitogenic signaling transduction
-
-
?
ATP + choline
ADP + O-phosphocholine
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
-
-
-
-
?
ATP + choline

ADP + phosphocholine
-
-
-
?
ATP + choline
ADP + phosphocholine
-
-
-
?
ATP + choline
ADP + phosphocholine
-
-
-
?
ATP + choline
ADP + phosphocholine
-
-
-
?
ATP + choline
ADP + phosphocholine
-
-
-
?
ATP + choline
ADP + phosphocholine
-
-
-
-
?
ATP + choline
ADP + phosphocholine
-
-
-
-
?
ATP + choline
ADP + phosphocholine
-
-
-
?
ATP + choline
ADP + phosphocholine
-
-
-
?
ATP + choline
ADP + phosphocholine
-
-
-
?
ATP + choline
ADP + phosphocholine
-
-
-
-
?
ATP + choline
ADP + phosphocholine
-
-
-
?
ATP + choline
ADP + phosphocholine
-
-
-
-
?
ATP + choline
ADP + phosphocholine
-
-
-
?
ATP + choline
ADP + phosphocholine
-
-
-
-
?
ATP + choline
ADP + phosphocholine
-
-
-
?
ATP + choline
ADP + phosphocholine
-
-
-
-
?
ATP + choline
ADP + phosphocholine
-
-
-
?
ATP + choline
ADP + phosphocholine
transfer of the gamma-phosphoryl group of ATP
-
-
?
ATP + choline
ADP + phosphocholine
-
-
-
-
?
ATP + choline
ADP + phosphocholine
-
-
-
-
?
ATP + choline
ADP + phosphocholine
-
-
-
-
?
ATP + choline
ADP + phosphocholine
-
-
-
?
ATP + choline
ADP + phosphocholine
-
-
-
?
ATP + choline
ADP + phosphocholine
-
-
-
-
?
ATP + choline
ADP + phosphocholine
-
-
-
?
ATP + choline
ADP + phosphocholine
-
-
-
?
ATP + choline
ADP + phosphocholine
-
-
-
-
?
ATP + ethanolamine

ADP + ethanolamine phosphate
-
poor substrate compared to choline
-
-
?
ATP + ethanolamine
ADP + ethanolamine phosphate
-
can not phosphorylate ethanolamine efficiently
-
-
?
ATP + ethanolamine
ADP + ethanolamine phosphate
-
-
-
-
?
ATP + ethanolamine
ADP + ethanolamine phosphate
-
not: basic isoform
-
-
?
ATP + ethanolamine
ADP + ethanolamine phosphate
-
poor substrate compared to choline
-
-
?
ATP + ethanolamine

ADP + O-phosphoethanolamine
-
-
-
?
ATP + ethanolamine
ADP + O-phosphoethanolamine
-
-
-
?
choline + ATP

O-phosphocholine + ADP
-
-
-
?
choline + ATP
O-phosphocholine + ADP
-
first step in the biosynthesis of the glycerophospholipid glycerophosphocholine
-
-
?
choline + ATP

phosphocholine + ADP
-
-
-
-
?
choline + ATP
phosphocholine + ADP
-
-
-
?
choline + ATP
phosphocholine + ADP
-
catalyzes the first phosphorylation reaction in the Kennedy pathway (biosynthesis of the major membrane phospholipid phosphatidylcholine)
-
-
?
choline + ATP
phosphocholine + ADP
first enzyme in the CDP-choline (Kennedy) pathway for the biosynthesis of phosphatidylcholine
choline kinase supply phosphocholine for the biosynthesis of phosphatidylcholine that is essential for growth and cell division
-
?
choline + ATP
phosphocholine + ADP
-
choline kinase may have a regulatory role in phosphatidylcholine biosynthesis
-
-
?
choline + ATP
phosphocholine + ADP
-
The induction of CKI1 expression in zinc-depleted cells translated into increased choline kinase activity in vitro and in vivo and in an increase in phosphatidylcholine synthesis via the Kennedy pathway
-
-
?
ethanolamine + ATP

ADP + ethanolamine phosphate
-
-
-
-
?
ethanolamine + ATP
ADP + ethanolamine phosphate
-
-
-
-
?
GTP + choline

GDP + choline phosphate
-
at 50% of the activity with ATP
-
-
?
GTP + choline
GDP + choline phosphate
-
poor substrate
-
-
?
GTP + choline
GDP + choline phosphate
-
at 50% of the activity with ATP
-
-
?
N,N-diethylethanolamine + ATP

ADP + N,N-diethylethanolamine phosphate
-
-
-
-
?
N,N-diethylethanolamine + ATP
ADP + N,N-diethylethanolamine phosphate
-
-
-
-
?
N,N-dimethylethanolamine + ATP

ADP + N,N-dimethylethanolamine phosphate
-
-
-
-
?
N,N-dimethylethanolamine + ATP
ADP + N,N-dimethylethanolamine phosphate
-
not: basic isoform
-
-
?
N,N-dimethylethanolamine + ATP
ADP + N,N-dimethylethanolamine phosphate
-
-
-
-
?
N-methylethanolamine + ATP

ADP + N-methylethanolamine phosphate
-
-
-
-
?
N-methylethanolamine + ATP
ADP + N-methylethanolamine phosphate
-
not: basic isoform
-
-
?
N-monomethylethanolamine + ATP

ADP + N-monomethylethanolamine phosphate
-
-
-
-
?
N-monomethylethanolamine + ATP
ADP + N-monomethylethanolamine phosphate
-
-
-
-
?
UTP + choline

UDP + choline phosphate
-
at 20% of the activity with ATP
-
-
?
UTP + choline
UDP + choline phosphate
-
poor substrate
-
-
?
UTP + choline
UDP + choline phosphate
-
at 20% of the activity with ATP
-
-
?
additional information

?
-
detection via quantitative TLC
-
-
-
additional information
?
-
detection via quantitative TLC
-
-
-
additional information
?
-
detection via quantitative TLC
-
-
-
additional information
?
-
detection via quantitative TLC
-
-
-
additional information
?
-
detection via quantitative TLC
-
-
-
additional information
?
-
detection via quantitative TLC
-
-
-
additional information
?
-
-
specificity overview
-
-
?
additional information
?
-
-
microarray analysis detected changes in the expression of 33 proliferation-related genes with Chk down-regulation
-
-
?
additional information
?
-
usage of a coupled assay method with pyruvate kinase, and lactate dehydrogenase, at pH 7.5 and 37°C
-
-
-
additional information
?
-
-
usage of a coupled assay method with pyruvate kinase, and lactate dehydrogenase, at pH 7.5 and 37°C
-
-
-
additional information
?
-
-
specificity overview
-
-
?
additional information
?
-
-
specificity overview
-
-
?
additional information
?
-
-
specificity overview
-
-
?
additional information
?
-
-
specificity overview
-
-
?
additional information
?
-
-
Further substrate specificity analysis reveals that TbC/EK2 are able to tolerate various modifications at the amino group, with the exception of a quaternary amine for TbEK1 (choline). The enzyme recognizes analogues with substituents on C-2, but substitutions on C-1 and elongations of the carbon chain are not well tolerate. Secondary and tertiary amino modifications are better than choline. A reduction of activity is seen with the elongation of the carbon chain, but it is not abolished even when increased by an ethylene unit. Modifications at the hydroxy group result in no detectable reactivity.
-
-
?
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(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
-
IC50: 0.0482 mM; IC50: above 0.1 mM
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]
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-8-yl)methyl]phenyl]butyl)benzyl]-4-(dimethylamino)pyridinium bromide
-
-
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
3-Trimethylammonio-1-propanol
-
-
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
5,5'-dithiobis(2-nitrobenzoic acid)
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
-
-
-
Cytidine diphosphocholine
-
-
EDTA
about 10% residual activity at 5 mM
H-89
-
no activity on choline kinase at 5 mM ATP, decreasing the ATP concentration to 100 microM has no effect on choline kinase
hexadecyltrimethylammonium bromide
-
60% inhibition at 0.1 mM; HDTAB, structural resemblance to hexadecylphosphocholine, exhibits an antimalarial effect and inhibits choline kinase in a dose-dependent manner. For purified protein: 60% inhibition at 100 microM (in presence of 250 microM choline), 60% inhibition at 50 microM (in presence of 100 microM choline). HDTAB may compete with choline for the choline binding site of choline kinase and may offer competitive inhibition with respect to choline. The concentration of HDTAB required to inhibit Plasmodium falciparum growth by 62% was 10times lower than the concentration required to inhibit purified choline kinase by 60% in vitro
methyl 4'-((4-methyl-1,4-diazepan-1-yl)methyl)-[1,1'-biphenyl]-4-carboxylate
N,N,N-trimethyl-N-(5,5-diphenylpent-4-en-1-yl)ammonium iodide
-
-
N,N,N-trimethyl-N-(6,6-diphenylhex-5-en-1-yl)ammonium iodide
-
-
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-iodomethyl-N,N-dimethyl-N-(4,4-diphenylbut-3-en-1-yl)ammonium iodide
-
-
N-iodomethyl-N,N-dimethyl-N-(5,5-diphenylpen-4-en-1-yl)ammonium iodide
-
-
N-iodomethyl-N,N-dimethyl-N-(6,6-diphenylhex-5-en-1-yl)ammonium iodide
-
-
N-iodomethylcholine iodide
-
-
N-Methyl-N,N-diisopropylethanolamine
-
-
N-Methyl-N-isopropylethanolamine
-
-
N-[2-bromocinnamyl(amino)ethyl]-5-isoquinoline sulfonamide
-
-
NaCl
-
8.7-35 mM: slight activation, 70 mM: inactivation
p-chloromercuribenzoate
-
-
p-hydroxymercuribenzoate
-
-
phosphocholine
-
40% and 66% inhibition at 2.5 mM and 10 mM, respectively
piperazine
-
modest inhibitory activity
purinyl-6-histamine
-
modest inhibitory activity
Quinacrine
-
indirect inhibitor
RSM932A
also called TCD-717
Triethanolammonio-1-choline
-
-
[4-(4-methyl-1,4-diazepan-1-yl)phenyl]methanol
-
(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'-[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
1,1'-[butane-1,4-diylbis[(4,1-phenylene)methylene]]bis[4-(dimethylamino)pyridin-1-ium]
MN58b, mixed inhibition type with both choline and ATP
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
1,1'-[[1,1'-biphenyl]-4,4'-diylbis(methylene)]bis[4-[(4-chlorophenyl)(methyl)amino]quinolin-1-ium]
RSM-932A, mixed inhibition type with choline, non-competitive with ATP
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
-
5,5'-dithiobis(2-nitrobenzoic acid)

-
5,5'-dithiobis(2-nitrobenzoic acid)
-
5,5'-dithiobis(2-nitrobenzoic acid)
-
-
5,5'-dithiobis(2-nitrobenzoic acid)
-
-
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
-
Acetylcholine

-
-
adenosine

competitive with MgATP2-
adenosine
competitive with MgATP2-
ADP

-
-
ADP
-
50% inhibition at 0.32 mM, in a positive cooperative manner
AMP

-
-
ATP

-
at 4.9 mM and 8.0 mM 30% inhibition; optimum concentration: 3.2-4.0 mM
Ca2+

-
-
choline

-
-
Choline analogues

several compounds tested and found to be inhibitory
Choline analogues
several compounds tested and found to be inhibitory
choline kinase inhibitor Mn58b

-
-
-
choline kinase inhibitor Mn58b
-
-
ethanolamine

-
inhibition only at very high concentration, 100-150 mM
ethanolamine
-
no significant effect
ethanolamine
-
poor inhibitor
ethanolamine
-
weak competitive inhibitor
HC-3

-
HC-3
-
poor inhibition of 16% and 18% is observed at 50 microM and 150 microM, respectively, at both 100 and 250 microM choline
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; 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
hemicholinium-3
-
poor inhibition of 16% and 18% at 0.050 mM and 0.15 mM, respectively, not significantly inhibited by hemicholinium-3 up to 0.025 mM
hemicholinium-3
HC-3, HC-3 competes with the Cho substrate by directly displacing it from the active site of hChoK. Hemocholinium-3 blocks cell division, reduces LTA production, distorts the cell wall, and inhibits sChoK activity
hemicholinium-3
HC-3, MIC is 5.4 mM
KF

-
methionine

-
-
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

-
specific inhibitor, IC50: 0.0005-0.072 mM depending on cell type
MN58b
-
specific for choline kinase
MN58b
dysregulates the production of LTA, distorts the cell wall, and affects cell sensitivity to deoxycholate induced autolysis
N-ethylmaleimide

-
N-ethylmaleimide
-
modest inhibitory activity
phosphorylcholine

-
-
RSM-932A

-
RSM-932A
dysregulates the production of LTA, distorts the cell wall, and affects cell sensitivity to deoxycholate induced autolysis
serine

-
not
stearoyl-CoA

-
additional information

not inhibited by 1-[4-(4-[4-[(3-aminophenoxy)methyl]phenyl]butyl)-benzyl]-4-(dimethylamino)pyridinium bromide
-
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
-
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
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
-
the lethality of the homozygous choline kinase alpha knock-out mice embryos indicates the indispensable role of CK-alphain early embryogenesis
-
additional information
-
not: neostigmine
-
additional information
-
not: p-chloromercuribenzoate, N-ethylmaleeimide
-
additional information
-
not: CTP, ethanolamine phosphate
-
additional information
-
-
-
additional information
repurposing of drugs known to inhibit the human isoform of ChoK (hChoK), is a promising strategy for blocking the growth of Streptococcus pneumoniae cells and inhibiting the activity of the Streptococcus pneumoniae isoform of ChoK (sChok), with downstream physiological effects on the cell wall
-
additional information
-
repurposing of drugs known to inhibit the human isoform of ChoK (hChoK), is a promising strategy for blocking the growth of Streptococcus pneumoniae cells and inhibiting the activity of the Streptococcus pneumoniae isoform of ChoK (sChok), with downstream physiological effects on the cell wall
-
additional information
docking of MN58b and RSM-932A onto sChoK, overview. MN58b and RSM-932A fit into the active site of sChoK in a differential manner. In enzymatic assays with Streptoccocus pneumoniae extracts MN58b is still an inhibitor, while RSM-932A becomes an agonist
-
additional information
-
docking of MN58b and RSM-932A onto sChoK, overview. MN58b and RSM-932A fit into the active site of sChoK in a differential manner. In enzymatic assays with Streptoccocus pneumoniae extracts MN58b is still an inhibitor, while RSM-932A becomes an agonist
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
0.94
dimethylethanolamine
-
in 100 mM Tris-HCl (pH 8.5), at 37°C
0.025
N,N-diethylethanolamine
0.4
N,N-Diisopropylethanolamine
0.208
N,N-Dimethylaminopropanol
0.022 - 0.085
N,N-dimethylethanolamine
0.118 - 3.7
N-Monomethylethanolamine
additional information
ethanolamine
0.0206
ATP

-
-
0.4
ATP
isoform ChoKalpha2 mutant F352L, pH and temperature not specified in the publication
0.4
ATP
wild type isoform ChoKalpha2, pH and temperature not specified in the publication
0.4
ATP
wild type isoform ChoKbeta, pH and temperature not specified in the publication
0.486
ATP
in 100 mM Tris-HCl pH 7.5, 100 mM KCl, 10 mM MgCl2, at 25°C
0.55
ATP
isoform ChoKalpha2 mutant F352A, pH and temperature not specified in the publication
0.58
ATP
mutant choline kinase beta S39D/S40D, at pH 7.5 and 30°C
0.65
ATP
isoform ChoKbeta mutant F352A, pH and temperature not specified in the publication
0.65
ATP
phosphorylated choline kinase beta, at pH 7.5 and 30°C
0.7
ATP
-
isozyme CKB-2, pH 10.0, 37°C
0.7
ATP
isoform ChoKbeta mutant F352L, pH and temperature not specified in the publication
0.76
ATP
wild type isoform ChoKalpha1, pH and temperature not specified in the publication
1
ATP
-
C252S mutant enzyme, pH 10, 37°C
1
ATP
-
N308Q mutant enzyme, pH 10, 37°C
1.2
ATP
-
N354A mutant enzyme, pH 10, 37°C
1.3
ATP
-
D255D mutant enzyme, pH 10, 37°C
1.5
ATP
-
N308D mutant enzyme, pH 10, 37°C
1.7
ATP
-
E134A mutant enzyme, pH 10, 37°C
1.7
ATP
-
N87A mutant enzyme, pH 10, 37°C
1.7
ATP
-
wild type enzyme including His-tag, pH 10, 37°C
1.9
ATP
-
H253A mutant enzyme, pH 10, 37°C
1.9
ATP
-
S85T mutant enzyme, pH 10, 37°C
2
ATP
-
N308A mutant enzyme, pH 10, 37°C
2.2
ATP
-
E125D mutant enzyme, pH 10, 37°C
2.2
ATP
-
R149A mutant enzyme, pH 10, 37°C
2.2
ATP
-
W387A mutant enzyme, pH 10, 37°C
2.3
ATP
-
R149K mutant enzyme, pH 10, 37°C
2.4
ATP
-
isozyme CKA-2, pH 10.0, 37°C
2.4
ATP
-
wild type enzyme, pH 10, 37°C
2.5
ATP
-
S86A mutant enzyme, pH 10, 37°C
2.5
ATP
-
in 100 mM Tris/HCl, 6 mM MgCl2, 5 mM ATP, pH 8.8, at 37°C
3.1
ATP
-
N260A mutant enzyme, pH 10, 37°C
3.2
ATP
-
E125A mutant enzyme, pH 10, 37°C
4.2
ATP
-
E125Q mutant enzyme, pH 10, 37°C
4.5
ATP
-
E151A mutant enzyme, pH 10, 37°C
5.4
ATP
-
E303A mutant enzyme, pH 10, 37°C
6.9
ATP
-
E303D mutant enzyme, pH 10, 37°C
7
ATP
-
R111A mutant enzyme, pH 10, 37°C
8.8
ATP
-
E303Q mutant enzyme, pH 10, 37°C
45
ATP
-
E320A mutant enzyme, pH 10, 37°C
0.444
beta-Methylcholine

-
30°C
0.444
beta-Methylcholine
-
30°C, pH 8.0
0.002
choline

-
dimer
0.013
choline
-
liver enzyme
0.013
choline
-
pH 8.5, 37°C
0.014
choline
-
brain enzyme
0.021
choline
isoform ChoKalpha2 mutant F352L, pH and temperature not specified in the publication
0.032
choline
-
isozyme CK-beta
0.033
choline
wild type isoform ChoKbeta, pH and temperature not specified in the publication
0.041
choline
isoform ChoKbeta mutant F352L, pH and temperature not specified in the publication
0.055
choline
-
isozyme CK-alpha1/beta
0.07
choline
in 100 mM Tris-HCl buffer (pH 7.5) containing 100 mM KCl, 10 mM MgCl2, 0.5 mM phosphoenolpyruvate, 0.25 mM NADH, 4 units pyruvate kinase, and 5 units lactate dehydrogenase
0.083
choline
-
isozyme CK-alpha
0.086
choline
wild type isoform ChoKalpha2, pH and temperature not specified in the publication
0.089
choline
at pH 9.0 and 37°C
0.1
choline
-
kidney enzyme
0.102
choline
isoform ChoKbeta mutant F352A, pH and temperature not specified in the publication
0.107
choline
isoform ChoKalpha2 mutant F352A, pH and temperature not specified in the publication
0.13
choline
recombinant enzyme, pH 8.0, 25°C
0.1353
choline
recombinant protein
0.145
choline
-
in 100 mM Tris/HCl, 6 mM MgCl2, 5 mM ATP, pH 8.8, at 37°C
0.15
choline
at pH 8.0 and 37°C
0.157
choline
-
N-terminal truncated enzyme version of CK-beta
0.18
choline
wild type isoform ChoKalpha1, pH and temperature not specified in the publication
0.188
choline
in 100 mM Tris-HCl pH 7.5, 100 mM KCl, 10 mM MgCl2, at 25°C
0.27
choline
-
pH 9.5, 30°C
0.4
choline
-
N260A mutant enzyme, pH 10, 37°C
0.42
choline
phosphorylated choline kinase beta, at pH 7.5 and 30°C
0.46
choline
mutant choline kinase beta S39D/S40D, at pH 7.5 and 30°C
0.7
choline
-
R149A mutant enzyme, pH 10, 37°C
0.7
choline
-
S85T mutant enzyme, pH 10, 37°C
0.77
choline
-
in 100 mM Tris-HCl (pH 8.5), at 37°C
0.8
choline
-
E125D mutant enzyme, pH 10, 37°C
0.8
choline
-
N308Q mutant enzyme, pH 10, 37°C
1
choline
-
C252S mutant enzyme, pH 10, 37°C
1
choline
-
N308D mutant enzyme, pH 10, 37°C
1
choline
-
N354A mutant enzyme, pH 10, 37°C
1
choline
-
wild type enzyme including His-tag, pH 10, 37°C
1.1
choline
-
E125A mutant enzyme, pH 10, 37°C
1.2
choline
-
R149K mutant enzyme, pH 10, 37°C
1.2
choline
-
W387A mutant enzyme, pH 10, 37°C
1.5
choline
-
N308A mutant enzyme, pH 10, 37°C
1.6
choline
-
isozyme CKA-2, pH 10.0, 37°C
1.6
choline
-
E125Q mutant enzyme, pH 10, 37°C
1.6
choline
-
H253A mutant enzyme, pH 10, 37°C
1.6
choline
-
wild type enzyme, pH 10, 37°C
1.7
choline
-
R111A mutant enzyme, pH 10, 37°C
1.8
choline
-
E134A mutant enzyme, pH 10, 37°C
1.8
choline
-
N87A mutant enzyme, pH 10, 37°C
2.2
choline
-
E151A mutant enzyme, pH 10, 37°C
3
choline
-
E320A mutant enzyme, pH 10, 37°C
3.4
choline
-
E303Q mutant enzyme, pH 10, 37°C
3.6
choline
-
E303D mutant enzyme, pH 10, 37°C
5
choline
-
S86A mutant enzyme, pH 10, 37°C
5.4
choline
-
D255D mutant enzyme, pH 10, 37°C
10
choline
-
E303A mutant enzyme, pH 10, 37°C
13
choline
-
isozyme CKB-2, pH 10.0, 37°C
0.787
ethanolamine

-
30°C
0.787
ethanolamine
-
30°C, pH 8.0
1.2
ethanolamine
-
pH 8.5, 37°C
1.2
ethanolamine
-
30°C, pH 8.0
5
ethanolamine
-
in 100 mM Tris/HCl, 6 mM MgCl2, 5 mM ATP, pH 8.8, at 37°C
8.1
ethanolamine
-
pH 9.0
75
ethanolamine
at pH 9.0 and 37°C
0.025
N,N-diethylethanolamine

-
30°C, pH 8.0
0.025
N,N-diethylethanolamine
-
pH 9.6, 37°C
0.4
N,N-Diisopropylethanolamine

-
30°C
0.4
N,N-Diisopropylethanolamine
-
30°C, pH 8.0
0.208
N,N-Dimethylaminopropanol

-
30°C
0.208
N,N-Dimethylaminopropanol
-
30°C, pH 8.0
0.022
N,N-dimethylethanolamine

-
30°C
0.022
N,N-dimethylethanolamine
-
30°C, pH 8.0
0.085
N,N-dimethylethanolamine
-
pH 9.0
0.118
N-Monomethylethanolamine

-
30°C
0.118
N-Monomethylethanolamine
-
30°C, pH 8.0
3.7
N-Monomethylethanolamine
-
-
3.7
N-Monomethylethanolamine
-
cosubstrate ATP
additional information
ethanolamine

above 500 mM
additional information
additional information
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-
-
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-
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-
-
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-
-
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-
-
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-
-
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-
-
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-
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-
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-
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-
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-
-
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-
-
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-
-
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additional information
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-
-
additional information
additional information
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-
-
additional information
additional information
steady-state kinetics
-
additional information
additional information
steady-state kinetics
-
additional information
additional information
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steady-state kinetics
-
additional information
additional information
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Km of MgATP2-: 10 mM, in presence of equimolar amounts of ATP and Mg2+, 1.5 mM, in 2.5-fold higher concentration of Mg2+ than ATP
-
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