Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 2.7.1.91 extracted from

  • Vettorazzi, M.; Insuasty, D.; Lima, S.; Gutierrez, L.; Nogueras, M.; Marchal, A.; Abonia, R.; Andujar, S.; Spiegel, S.; Cobo, J.; Enriz, R.
    Design of new quinolin-2-one-pyrimidine hybrids as sphingosine kinases inhibitors (2020), Bioorg. Chem., 94, 103414 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.7.1.91

Inhibitors

Inhibitors Comment Organism Structure
(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
(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
-
 Homo sapiens
(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
3-(((4-((4-(4-chlorophenyl)pyrimidin-2-yl)amino)phenyl)amino)methyl)-6,7-dimethoxyquinolin-2(1H)-one
-
 Homo sapiens
3-((4-(4-chlorophenyl)pyrimidin-2-yl)-1-yl)oxymethyl)quinolin-2(1H)-one
-
 Homo sapiens
4-((4-(4-chlorophenyl)pyrimidin-2-yl)amino)phenol
-
 Homo sapiens
6,7-dihydroxy-3-(((4-((4-(naphthalene-2-yl)pyrimidin-2-yl)amino)phenyl)amino)methyl)quinolin-2(1H)-one
-
 Homo sapiens
6,7-dimethoxy-3-(((4-((4-(naphthalen-2-yl)pyrimidin-2-yl)amino)phenyl)amino)methyl)quinolin-2(1H)-one
-
 Homo sapiens
6-methoxy-3-(((4-((4-(naphthalen-2-yl)pyrimidin-2-yl)amino)phenyl)amino)methyl)quinolin-2(1H)-one
-
 Homo sapiens
PF-543 potent inhibitor of isoform SphK1 Homo sapiens
SKI-II
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + sphingosine Homo sapiens
-
 ADP + sphingosine 1-phosphate
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9NRA0
-
-
Homo sapiens Q9NYA1
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + NBD-sphingosine
-
 Homo sapiens ADP + NBD-sphingosine 1-phosphate
-
 ?
ATP + sphingosine
-
 Homo sapiens ADP + sphingosine 1-phosphate
-
 ?

Synonyms

Synonyms Comment Organism
sphingosine kinase 1
-
 Homo sapiens
sphingosine kinase 2
-
 Homo sapiens
SPHK1 isoform Homo sapiens
SPHK2 isoform Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000016
-
 at pH 7.4 and 37°C Homo sapiens PF-543
0.0005
-
 at pH 7.4 and 37°C Homo sapiens SKI-II
0.0031
-
 isoform SphK1, at pH 7.4 and 37°C Homo sapiens (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
0.0071
-
 isoform SphK2, at pH 7.4 and 37°C Homo sapiens (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
0.0079
-
 isoform SphK1, at pH 7.4 and 37°C Homo sapiens 6-methoxy-3-(((4-((4-(naphthalen-2-yl)pyrimidin-2-yl)amino)phenyl)amino)methyl)quinolin-2(1H)-one
0.0089
-
 isoform SphK2, at pH 7.4 and 37°C Homo sapiens 6-methoxy-3-(((4-((4-(naphthalen-2-yl)pyrimidin-2-yl)amino)phenyl)amino)methyl)quinolin-2(1H)-one
0.0107
-
 isoform SphK1, at pH 7.4 and 37°C Homo sapiens 3-((4-(4-chlorophenyl)pyrimidin-2-yl)-1-yl)oxymethyl)quinolin-2(1H)-one
0.0139
-
 isoform SphK2, at pH 7.4 and 37°C Homo sapiens 6,7-dimethoxy-3-(((4-((4-(naphthalen-2-yl)pyrimidin-2-yl)amino)phenyl)amino)methyl)quinolin-2(1H)-one
0.0141
-
 isoform SphK1, at pH 7.4 and 37°C Homo sapiens (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
0.0156
-
 isoform SphK2, at pH 7.4 and 37°C Homo sapiens 6,7-dihydroxy-3-(((4-((4-(naphthalene-2-yl)pyrimidin-2-yl)amino)phenyl)amino)methyl)quinolin-2(1H)-one
0.0157
-
 isoform SphK1, at pH 7.4 and 37°C Homo sapiens 6,7-dihydroxy-3-(((4-((4-(naphthalene-2-yl)pyrimidin-2-yl)amino)phenyl)amino)methyl)quinolin-2(1H)-one
0.0182
-
 isoform SphK2, at pH 7.4 and 37°C Homo sapiens 3-((4-(4-chlorophenyl)pyrimidin-2-yl)-1-yl)oxymethyl)quinolin-2(1H)-one
0.0187
-
 isoform SphK1, at pH 7.4 and 37°C Homo sapiens 6,7-dimethoxy-3-(((4-((4-(naphthalen-2-yl)pyrimidin-2-yl)amino)phenyl)amino)methyl)quinolin-2(1H)-one
0.0282
-
 isoform SphK1, at pH 7.4 and 37°C Homo sapiens (E)-3-(3-(4-((4-(4-chlorophenyl)pyrimidin-2-yl)amino)phenyl)-3-oxoprop-1-en-1-yl)-6-methoxyquinolin-2(1H)-one
0.0439
-
 isoform SphK1, at pH 7.4 and 37°C Homo sapiens 4-((4-(4-chlorophenyl)pyrimidin-2-yl)amino)phenol
0.0591
-
 isoform SphK1, at pH 7.4 and 37°C Homo sapiens 3-(((4-((4-(4-chlorophenyl)pyrimidin-2-yl)amino)phenyl)amino)methyl)-6,7-dimethoxyquinolin-2(1H)-one