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Literature summary 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

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.1.91 (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
2.7.1.91 (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
2.7.1.91 (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
2.7.1.91 3-(((4-((4-(4-chlorophenyl)pyrimidin-2-yl)amino)phenyl)amino)methyl)-6,7-dimethoxyquinolin-2(1H)-one
-
 Homo sapiens
2.7.1.91 3-((4-(4-chlorophenyl)pyrimidin-2-yl)-1-yl)oxymethyl)quinolin-2(1H)-one
-
 Homo sapiens
2.7.1.91 4-((4-(4-chlorophenyl)pyrimidin-2-yl)amino)phenol
-
 Homo sapiens
2.7.1.91 6,7-dihydroxy-3-(((4-((4-(naphthalene-2-yl)pyrimidin-2-yl)amino)phenyl)amino)methyl)quinolin-2(1H)-one
-
 Homo sapiens
2.7.1.91 6,7-dimethoxy-3-(((4-((4-(naphthalen-2-yl)pyrimidin-2-yl)amino)phenyl)amino)methyl)quinolin-2(1H)-one
-
 Homo sapiens
2.7.1.91 6-methoxy-3-(((4-((4-(naphthalen-2-yl)pyrimidin-2-yl)amino)phenyl)amino)methyl)quinolin-2(1H)-one
-
 Homo sapiens
2.7.1.91 PF-543 potent inhibitor of isoform SphK1 Homo sapiens
2.7.1.91 SKI-II
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

EC Number Organism UniProt Comment Textmining
2.7.1.91 Homo sapiens Q9NRA0
-
-
2.7.1.91 Homo sapiens Q9NYA1
-
-

Substrates and Products (Substrate)

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

Synonyms

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

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.1.91 0.000016
-
 at pH 7.4 and 37°C Homo sapiens PF-543
2.7.1.91 0.0005
-
 at pH 7.4 and 37°C Homo sapiens SKI-II
2.7.1.91 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
2.7.1.91 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
2.7.1.91 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
2.7.1.91 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
2.7.1.91 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
2.7.1.91 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
2.7.1.91 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
2.7.1.91 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
2.7.1.91 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
2.7.1.91 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
2.7.1.91 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
2.7.1.91 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
2.7.1.91 0.0439
-
 isoform SphK1, at pH 7.4 and 37°C Homo sapiens 4-((4-(4-chlorophenyl)pyrimidin-2-yl)amino)phenol
2.7.1.91 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