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Literature summary extracted from

  • Dinges, J.; Harris, C.M.; Wallace, G.A.; Argiriadi, M.A.; Queeney, K.L.; Perron, D.C.; Dominguez, E.; Kebede, T.; Desino, K.E.; Patel, H.; Vasudevan, A.
    Hit-to-lead evaluation of a novel class of sphingosine 1-phosphate lyase inhibitors (2016), Bioorg. Med. Chem. Lett., 26, 2297-2302 .
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
4.1.2.27 2-acetyl-4-(1R,2S,3R,4-tetrahydroxybutyl)-1H-imidazole
-
 Homo sapiens
4.1.2.27 4'-deoxypyridoxine
-
 Homo sapiens
4.1.2.27 5-cyclopropyl-N-[2-[(4-ethoxy-2,5-dimethylbenzyl)amino]-1-(4-fluorophenyl)ethyl]-1,2-oxazole-3-carboxamide
-
 Homo sapiens
4.1.2.27 5-cyclopropyl-N-[2-[(4-methoxy-2,5-dimethylbenzyl)amino]-1-phenylethyl]-1,2-oxazole-3-carboxamide
-
 Homo sapiens
4.1.2.27 5-methoxy-N-[2-[(4-methoxy-2,5-dimethylbenzyl)amino]-1-phenylethyl]-1,2-oxazole-3-carboxamide
-
 Homo sapiens
4.1.2.27 benzylphthalazine
-
 Homo sapiens
4.1.2.27 N-(2-[[2,5-dimethyl-4-(2,2,2-trifluoroethoxy)benzyl]amino]-1-phenylethyl)-5-methyl-1,2-oxazole-3-carboxamide
-
 Homo sapiens
4.1.2.27 N-(2-[[2,5-dimethyl-4-(pyridin-4-ylmethoxy)benzyl]amino]-1-phenylethyl)-5-methyl-1,2-oxazole-3-carboxamide
-
 Homo sapiens
4.1.2.27 N-(2-[[4-methoxy-2-methyl-5-(trifluoromethyl)benzyl]amino]-1-phenylethyl)-5-methyl-1,2-oxazole-3-carboxamide
-
 Homo sapiens
4.1.2.27 N-[1-(4-fluorophenyl)-2-[(4-methoxy-2,5-dimethylbenzyl)amino]ethyl]-5-methyl-1,2-oxazole-3-carboxamide
-
 Homo sapiens
4.1.2.27 N-[1-[3-(4-amino-4-oxobutyl)phenyl]-2-[(4-methoxy-2,5-dimethylbenzyl)amino]ethyl]-5-methyl-1,2-oxazole-3-carboxamide
-
 Homo sapiens
4.1.2.27 N-[1-[4-(3-hydroxyprop-1-yn-1-yl)phenyl]-2-[(4-methoxy-2,5-dimethylbenzyl)amino]ethyl]-5-methyl-1,2-oxazole-3-carboxamide
-
 Homo sapiens
4.1.2.27 N-[1-[4-(4-amino-4-oxobutyl)phenyl]-2-[(4-methoxy-2,5-dimethylbenzyl)amino]ethyl]-5-methyl-1,2-oxazole-3-carboxamide
-
 Homo sapiens
4.1.2.27 N-[2-[(4-butoxy-2,5-dimethylbenzyl)amino]-1-phenylethyl]-5-methyl-1,2-oxazole-3-carboxamide
-
 Homo sapiens
4.1.2.27 N-[2-[(4-ethoxy-2,5-dimethylbenzyl)amino]-1-phenylethyl]-5-methyl-1,2-oxazole-3-carboxamide
-
 Homo sapiens
4.1.2.27 N-[2-[(4-methoxy-2,5-dimethylbenzyl)amino]-1-(2-methoxyphenyl)ethyl]-5-methyl-1,2-oxazole-3-carboxamide
-
 Homo sapiens
4.1.2.27 N-[2-[(4-methoxy-2,5-dimethylbenzyl)amino]-1-(3-methoxyphenyl)ethyl]-5-methyl-1,2-oxazole-3-carboxamide
-
 Homo sapiens
4.1.2.27 N-[2-[(4-methoxy-2,5-dimethylbenzyl)amino]-1-(4-methoxyphenyl)ethyl]-5-methyl-1,2-oxazole-3-carboxamide
-
 Homo sapiens
4.1.2.27 N-[2-[(4-methoxy-2,5-dimethylbenzyl)amino]-1-phenylethyl]-1,2-oxazole-3-carboxamide
-
 Homo sapiens
4.1.2.27 N-[2-[(4-methoxy-2,5-dimethylbenzyl)amino]-1-phenylethyl]-3-methyl-1,2-oxazole-5-carboxamide
-
 Homo sapiens
4.1.2.27 N-[2-[(4-methoxy-2,5-dimethylbenzyl)amino]-1-phenylethyl]-5-methyl-1,2-oxazole-3-carboxamide
-
 Homo sapiens
4.1.2.27 N-[2-[(4-methoxy-2,5-dimethylbenzyl)amino]-1-[4-(pyridin-4-yl)phenyl]ethyl]-5-methyl-1,2-oxazole-3-carboxamide
-
 Homo sapiens
4.1.2.27 N-[2-[(4-methoxybenzyl)amino]-1-phenylethyl]-5-methyl-1,2-oxazole-3-carboxamide
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
4.1.2.27 sphinganine 1-phosphate Homo sapiens
-
 phosphoethanolamine + palmitaldehyde
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
4.1.2.27 Homo sapiens
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4.1.2.27 sphinganine 1-phosphate
-
 Homo sapiens phosphoethanolamine + palmitaldehyde
-
 ?

Synonyms

EC Number Synonyms Comment Organism
4.1.2.27 S1P lyase
-
 Homo sapiens
4.1.2.27 sphingosine 1-phosphate lyase
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
4.1.2.27 pyridoxal 5'-phosphate
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
4.1.2.27 0.00012
-
 pH and temperature not specified in the publication Homo sapiens N-[2-[(4-butoxy-2,5-dimethylbenzyl)amino]-1-phenylethyl]-5-methyl-1,2-oxazole-3-carboxamide
4.1.2.27 0.00015
-
 pH and temperature not specified in the publication Homo sapiens N-[1-[4-(3-hydroxyprop-1-yn-1-yl)phenyl]-2-[(4-methoxy-2,5-dimethylbenzyl)amino]ethyl]-5-methyl-1,2-oxazole-3-carboxamide
4.1.2.27 0.00015
-
 pH and temperature not specified in the publication Homo sapiens N-[1-[4-(4-amino-4-oxobutyl)phenyl]-2-[(4-methoxy-2,5-dimethylbenzyl)amino]ethyl]-5-methyl-1,2-oxazole-3-carboxamide
4.1.2.27 0.00026
-
 pH and temperature not specified in the publication Homo sapiens N-[2-[(4-ethoxy-2,5-dimethylbenzyl)amino]-1-phenylethyl]-5-methyl-1,2-oxazole-3-carboxamide
4.1.2.27 0.00059
-
 pH and temperature not specified in the publication Homo sapiens N-(2-[[2,5-dimethyl-4-(2,2,2-trifluoroethoxy)benzyl]amino]-1-phenylethyl)-5-methyl-1,2-oxazole-3-carboxamide
4.1.2.27 0.00072
-
 pH and temperature not specified in the publication Homo sapiens N-[1-(4-fluorophenyl)-2-[(4-methoxy-2,5-dimethylbenzyl)amino]ethyl]-5-methyl-1,2-oxazole-3-carboxamide
4.1.2.27 0.00073
-
 pH and temperature not specified in the publication Homo sapiens 5-cyclopropyl-N-[2-[(4-methoxy-2,5-dimethylbenzyl)amino]-1-phenylethyl]-1,2-oxazole-3-carboxamide
4.1.2.27 0.00085
-
 pH and temperature not specified in the publication Homo sapiens N-[2-[(4-methoxy-2,5-dimethylbenzyl)amino]-1-[4-(pyridin-4-yl)phenyl]ethyl]-5-methyl-1,2-oxazole-3-carboxamide
4.1.2.27 0.001
-
 pH and temperature not specified in the publication Homo sapiens N-(2-[[2,5-dimethyl-4-(pyridin-4-ylmethoxy)benzyl]amino]-1-phenylethyl)-5-methyl-1,2-oxazole-3-carboxamide
4.1.2.27 0.001
-
 pH and temperature not specified in the publication Homo sapiens N-[2-[(4-methoxy-2,5-dimethylbenzyl)amino]-1-phenylethyl]-5-methyl-1,2-oxazole-3-carboxamide
4.1.2.27 0.0012
-
 pH and temperature not specified in the publication Homo sapiens N-(2-[[4-methoxy-2-methyl-5-(trifluoromethyl)benzyl]amino]-1-phenylethyl)-5-methyl-1,2-oxazole-3-carboxamide
4.1.2.27 0.0038
-
 pH and temperature not specified in the publication Homo sapiens N-[2-[(4-methoxy-2,5-dimethylbenzyl)amino]-1-phenylethyl]-3-methyl-1,2-oxazole-5-carboxamide
4.1.2.27 0.0046
-
 pH and temperature not specified in the publication Homo sapiens 5-cyclopropyl-N-[2-[(4-ethoxy-2,5-dimethylbenzyl)amino]-1-(4-fluorophenyl)ethyl]-1,2-oxazole-3-carboxamide
4.1.2.27 0.005
-
 pH and temperature not specified in the publication Homo sapiens N-[2-[(4-methoxy-2,5-dimethylbenzyl)amino]-1-(4-methoxyphenyl)ethyl]-5-methyl-1,2-oxazole-3-carboxamide
4.1.2.27 0.0064
-
 pH and temperature not specified in the publication Homo sapiens N-[2-[(4-methoxy-2,5-dimethylbenzyl)amino]-1-phenylethyl]-1,2-oxazole-3-carboxamide
4.1.2.27 0.0073
-
 pH and temperature not specified in the publication Homo sapiens N-[2-[(4-methoxy-2,5-dimethylbenzyl)amino]-1-(3-methoxyphenyl)ethyl]-5-methyl-1,2-oxazole-3-carboxamide
4.1.2.27 0.0092
-
 pH and temperature not specified in the publication Homo sapiens 5-methoxy-N-[2-[(4-methoxy-2,5-dimethylbenzyl)amino]-1-phenylethyl]-1,2-oxazole-3-carboxamide
4.1.2.27 0.0096
-
 pH and temperature not specified in the publication Homo sapiens N-[1-[3-(4-amino-4-oxobutyl)phenyl]-2-[(4-methoxy-2,5-dimethylbenzyl)amino]ethyl]-5-methyl-1,2-oxazole-3-carboxamide
4.1.2.27 0.05
-
 IC50 above 0.05 mM, pH and temperature not specified in the publication Homo sapiens N-[2-[(4-methoxy-2,5-dimethylbenzyl)amino]-1-(2-methoxyphenyl)ethyl]-5-methyl-1,2-oxazole-3-carboxamide
4.1.2.27 0.05
-
 IC50 above 0.05 mM, pH and temperature not specified in the publication Homo sapiens N-[2-[(4-methoxybenzyl)amino]-1-phenylethyl]-5-methyl-1,2-oxazole-3-carboxamide