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Literature summary for 2.7.1.91 extracted from

  • Xiang, Y.; Asmussen, G.; Booker, M.; Hirth, B.; Kane, J.L.; Liao, J.; Noson, K.D.; Yee, C.
    Discovery of novel sphingosine kinase 1 inhibitors (2009), Bioorg. Med. Chem. Lett., 19, 6119-6121.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(2R,3S)-2-[[(4-octylphenyl)amino]methyl]pyrrolidin-3-ol inhibition of isoform Sk1 Homo sapiens
(2S)-2-amino-N-(4-octylphenyl)-4-hydroxybutanamide inhibition of isoform Sk1 Homo sapiens
(2S,3R)-2-amino-N-(4-octylphenyl)-3-hydroxybutanamide inhibition of isoform Sk1 Homo sapiens
(2S,3S)-3-hydroxy-N-(4-octylbenzyl)pyrrolidine-2-carboxamide inhibition of isoform Sk1 Homo sapiens
(2S,3S)-3-hydroxy-N-(4-octylphenyl)pyrrolidine-2-carboxamide inhibition of isoform Sk1 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation
-
Homo sapiens
-

Substrates and Products (Substrate)

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00005
-
pH 7.5, 22°C Homo sapiens (2S)-2-amino-N-(4-octylphenyl)-4-hydroxybutanamide
0.000062
-
pH 7.5, 22°C Homo sapiens (2S,3S)-3-hydroxy-N-(4-octylphenyl)pyrrolidine-2-carboxamide
0.00043
-
pH 7.5, 22°C Homo sapiens (2S,3S)-3-hydroxy-N-(4-octylbenzyl)pyrrolidine-2-carboxamide
0.00065
-
pH 7.5, 22°C Homo sapiens (2S,3R)-2-amino-N-(4-octylphenyl)-3-hydroxybutanamide
0.00074
-
pH 7.5, 22°C Homo sapiens (2R,3S)-2-[[(4-octylphenyl)amino]methyl]pyrrolidin-3-ol