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2.7.1.91: sphingosine kinase

This is an abbreviated version!
For detailed information about sphingosine kinase, go to the full flat file.

Word Map on EC 2.7.1.91

Reaction

ATP
+
a sphingoid base
=
ADP
+
a sphingoid base 1-phosphate

Synonyms

dihydrosphingosine kinase, kinase, dihydrosphingosine (phosphorylating), kinase, sphingosine (phosphorylating), More, SGK, SK, SK-1, SK-2, SK1, SK2, sphinganine kinase, sphingoid base kinase, sphingosine kinase, sphingosine kinase 1, sphingosine kinase 2, sphingosine kinase type 1, sphingosine kinase type 2, sphingosine kinase-1, sphingosine kinase-2, SPHK, SPHK-1, SPHK1, SPHK1a, SPHK1b, SPHK2, SPK

ECTree

     2 Transferases
         2.7 Transferring phosphorus-containing groups
             2.7.1 Phosphotransferases with an alcohol group as acceptor
                2.7.1.91 sphingosine kinase

IC50 Value

IC50 Value on EC 2.7.1.91 - sphingosine kinase

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IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00074
(2R,3S)-2-[[(4-octylphenyl)amino]methyl]pyrrolidin-3-ol
Homo sapiens
-
pH 7.5, 22°C
0.00002
(2R,4S)-2-(hydroxymethyl)-1-[2-[4-([4-[4-(trifluoromethyl)phenyl]-1,3-thiazol-2-yl]amino)phenyl]ethyl]piperidin-4-ol
Homo sapiens
isoform SphK2, pH and temperature not specified in the publication
-
0.00028
(2S)-2-([3-[4-([4-[3-(trifluoromethyl)phenyl]-1,3-thiazol-2-yl]amino)phenyl]-1,2,4-oxadiazol-5-yl]methyl)pyrrolidine-1-carboximidamide
Homo sapiens
isoform SphK2, at pH 8.0 and 25°C
-
0.00005
(2S)-2-amino-N-(4-octylphenyl)-4-hydroxybutanamide
Homo sapiens
-
pH 7.5, 22°C
0.00065
(2S,3R)-2-amino-N-(4-octylphenyl)-3-hydroxybutanamide
Homo sapiens
-
pH 7.5, 22°C
0.00043
(2S,3S)-3-hydroxy-N-(4-octylbenzyl)pyrrolidine-2-carboxamide
Homo sapiens
-
pH 7.5, 22°C
0.000062
(2S,3S)-3-hydroxy-N-(4-octylphenyl)pyrrolidine-2-carboxamide
Homo sapiens
-
pH 7.5, 22°C
0.0282
(E)-3-(3-(4-((4-(4-chlorophenyl)pyrimidin-2-yl)amino)phenyl)-3-oxoprop-1-en-1-yl)-6-methoxyquinolin-2(1H)-one
Homo sapiens
isoform SphK1, at pH 7.4 and 37°C
-
0.0071 - 0.0141
(E)-6,7-dimethoxy-3-(3-(4-((4-(naphthalen-2-yl)pyrimidin-2-yl)amino)phenyl)-3-oxoprop-1-en-1-yl)quinolin-2(1H)-one
-
0.0031
(E)-6-methoxy-3-(3-(4-((4-(naphthalen-2-yl)pyrimidin-2-yl)amino)phenyl)-3-oxoprop-1-en-1-yl)quinolin-2(1H)-one
Homo sapiens
isoform SphK1, at pH 7.4 and 37°C
-
0.0165
(R)-FTY720-OMe
Homo sapiens
isoform SphK2, at pH 8.0 and 25°C
0.000234
(S)-2-((3-(4-((4-(1-methyl-1H-pyrazol-4-yl)-1H-1,2,3-triazol-1-yl)methyl)phenyl)-1,2,4-oxadiazol-5-yl)methyl)pyrrolidine-1-carboximidamide
Homo sapiens
isoform SphK2, at pH 8.0 and 25°C
-
0.000359
(S)-2-((3-(4-((4-(4-(trifluoromethyl)phenyl)-1H-1,2,3-triazol-1-yl)methyl)phenyl)-1,2,4-oxadiazol-5-yl)pyrrolidine-1-carboximidamide
Homo sapiens
isoform SphK2, at pH 8.0 and 25°C
-
0.000391
(S)-2-((3-(4-((4-(4-fluorophenyl)-1H-1,2,3-triazol-1-yl)methyl)phenyl)-1,2,4-oxadiazol-5-yl)-pyrrolidine-1-carboximidamide
Homo sapiens
isoform SphK2, at pH 8.0 and 25°C
-
0.000266
(S)-2-((3-(4-((4-(4-methoxyphenyl)-1H-1,2,3-triazol-1-yl)methyl)phenyl)-1,2,4-oxadiazol-5-yl)-pyrrolidine-1-carboximidamide
Homo sapiens
isoform SphK2, at pH 8.0 and 25°C
-
0.00064
(S)-2-((3-(4-((4-(4-methoxyphenyl)-1H-1,2,3-triazol-1-yl)methyl)phenyl)-1,2,4-oxadiazol-5-yl)methyl)pyrrolidine-1-carboximidamide
Homo sapiens
isoform SphK2, at pH 8.0 and 25°C
-
0.000452
(S)-2-((3-(4-((4-(pyridin-2-yl)-1H-1,2,3-triazol-1-yl)methyl)phenyl)-1,2,4-oxadiazol-5-yl)methyl)pyrrolidine-1-carboximidamide
Homo sapiens
isoform SphK2, at pH 8.0 and 25°C
-
0.000687
(S)-2-((3-(4-((4-(thiophen-2-yl)-1H-1,2,3-triazol-1-yl)methyl)phenyl)-1,2,4-oxadiazol-5-yl)-pyrrolidine-1-carboximidamide
Homo sapiens
isoform SphK2, at pH 8.0 and 25°C
-
0.000254
(S)-2-((3-(4-((4-butyl-1H-1,2,3-triazol-1-yl)methyl)phenyl)-1,2,4-oxadiazol-5-yl)pyrrolidine-1-carboximidamide
Homo sapiens
isoform SphK2, at pH 8.0 and 25°C
-
0.000248
(S)-2-((3-(4-((4-cyclopropyl-1H-1,2,3-triazol-1-yl)methyl)phenyl)-1,2,4-oxadiazol-5-yl)pyrrolidine-1-carboximidamide
Homo sapiens
isoform SphK2, at pH 8.0 and 25°C
-
0.000396
(S)-2-((3-(4-((4-phenyl-1H-1,2,3-triazol-1-yl)methyl)phenyl)-1,2,4-oxadiazol-5yl)methyl)pyrrolidine-1-carboximidamide
Homo sapiens
isoform SphK2, at pH 8.0 and 25°C
-
0.000909
(S)-2-(3-(4-((4-(pyridin-2-yl)-1H-1,2,3-triazol-1-yl)methyl)phenyl)-1,2,4-oxadiazol-5-yl)pyrrolidine-1-carboximidamide
Homo sapiens
isoform SphK2, at pH 8.0 and 25°C
-
0.000269
1-(3-(4-((4-(1-methyl-1H-pyrazol-5-yl)-1H-1,2,3-triazol-1-yl)methyl)phenyl)-1,2,4-oxadiazol-5-yl)cyclopropanecarboximidamide
Homo sapiens
isoform SphK2, at pH 8.0 and 25°C
-
0.000717
1-(3-(4-((4-cyclopropyl-1H-1,2,3-triazol-1-yl)methyl)phenyl)-1,2,4-oxadiazol-5-yl)cyclopropanecarboximidamide
Homo sapiens
isoform SphK2, at pH 8.0 and 25°C
-
0.000261
1-(3-(4-((4-phenyl-1H-1,2,3-triazol-1-yl)methyl)phenyl)-1,2,4-oxadiazol-5-yl)cyclopropanecarboximidamide
Homo sapiens
isoform SphK2, at pH 8.0 and 25°C
-
0.0005
2-(p-hydroxyanilino)-4-(p-chlorophenyl)thiazole
Homo sapiens
-
0.0591
3-(((4-((4-(4-chlorophenyl)pyrimidin-2-yl)amino)phenyl)amino)methyl)-6,7-dimethoxyquinolin-2(1H)-one
Homo sapiens
isoform SphK1, at pH 7.4 and 37°C
-
0.0107 - 0.0182
3-((4-(4-chlorophenyl)pyrimidin-2-yl)-1-yl)oxymethyl)quinolin-2(1H)-one
-
0.0439
4-((4-(4-chlorophenyl)pyrimidin-2-yl)amino)phenol
Homo sapiens
isoform SphK1, at pH 7.4 and 37°C
-
0.0156 - 0.0157
6,7-dihydroxy-3-(((4-((4-(naphthalene-2-yl)pyrimidin-2-yl)amino)phenyl)amino)methyl)quinolin-2(1H)-one
-
0.0139 - 0.0187
6,7-dimethoxy-3-(((4-((4-(naphthalen-2-yl)pyrimidin-2-yl)amino)phenyl)amino)methyl)quinolin-2(1H)-one
-
0.0079 - 0.0089
6-methoxy-3-(((4-((4-(naphthalen-2-yl)pyrimidin-2-yl)amino)phenyl)amino)methyl)quinolin-2(1H)-one
-
0.0098
ABC294640
Homo sapiens
isoform SphK2, at pH 8.0 and 25°C
0.00002 - 0.00016
Amgen 23
-
0.002 - 100
CB5468139
-
0.0024
dimethylsphingosine
Rattus norvegicus
at 37°C, in the presence of 0.25% Triton X-100
0.0024
DL-threo-dihydrosphingosine
Rattus norvegicus
at 37°C, in the presence of 0.25% Triton X-100
0.0064
K145
Homo sapiens
isoform SphK2, at pH 8.0 and 25°C
-
200
KCl
Mus musculus
IC50 200 mM
0.0069 - 0.027
MP-A08
-
200
NaCl
Mus musculus
IC50 200 mM
0.0000036 - 0.000016
PF-543
0.0002
Ro-31-8220
Rattus norvegicus
at 37°C, in the presence of 0.25% Triton X-100
0.0025
S-12183a
Homo sapiens
-
0.0016
S-12183b
Homo sapiens
-
0.022
SG-12
Homo sapiens
isoform SphK2, at pH 8.0 and 25°C
-
0.0005
SKI-II
Homo sapiens
at pH 7.4 and 37°C
0.000048 - 0.01
SLP7111228
-
0.00055
U-73122
Rattus norvegicus
at 37°C, in the presence of 0.25% Triton X-100
0.0021
Y-27632
Rattus norvegicus
at 37°C, in the presence of 0.25% Triton X-100
0.0000017
[(2R)-1-([4-[(3-cyclohexylphenoxy)methyl]phenyl]methyl)pyrrolidin-2-yl]methanol
-