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Literature summary extracted from

  • Grimm, E.L.; Brideau, C.; Chauret, N.; Chan, C.C.; Delorme, D.; Ducharme, Y.; Ethier, D.; Falgueyret, J.P.; Friesen, R.W.; Guay, J.; Hamel, P.; Riendeau, D.; Soucy-Breau, C.; Tagari, P.; Girard, Y.
    Substituted coumarins as potent 5-lipoxygenase inhibitors (2006), Bioorg. Med. Chem. Lett., 16, 2528-2531.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.13.11.34 4-(4-chlorophenyl)-7-([3-fluoro-5-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]sulfanyl)-2H-chromen-2-one IC50: 180 nM Homo sapiens
1.13.11.34 4-(4-fluorophenyl)-7-([3-fluoro-5-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenoxy]methyl)-2H-chromen-2-one IC50: 55 nM Homo sapiens
1.13.11.34 4-(4-fluorophenyl)-7-([3-fluoro-5-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]sulfanyl)-2H-chromen-2-one IC50: 27 nM Homo sapiens
1.13.11.34 7-([3-fluoro-5-[(1R)-1-hydroxy-1-pyridin-2-ylpropyl]phenoxy]methyl)-4-furan-3-yl-2H-chromen-2-one IC50: 175 nM Homo sapiens
1.13.11.34 7-([3-fluoro-5-[(1R,3R,5S)-3-hydroxy-6,8-dioxabicyclo[3.2.1]oct-3-yl]phenoxy]methyl)-4-(4-fluorophenyl)-2H-chromen-2-one
-
 Homo sapiens
1.13.11.34 7-([3-fluoro-5-[(1R,3R,5S)-3-hydroxy-6,8-dioxabicyclo[3.2.1]oct-3-yl]phenoxy]methyl)-4-furan-3-yl-2H-chromen-2-one IC50: 200 nM Homo sapiens
1.13.11.34 7-([3-fluoro-5-[(1R,3R,5S)-3-hydroxy-6,8-dioxabicyclo[3.2.1]oct-3-yl]phenoxy]methyl)-4-phenyl-2H-chromen-2-one IC50: 300 nM Homo sapiens
1.13.11.34 7-([3-fluoro-5-[(1S)-1-hydroxy-1-(1,3-thiazol-2-yl)propyl]phenoxy]methyl)-4-(4-fluorophenyl)-2H-chromen-2-one IC50: 175 nM Homo sapiens
1.13.11.34 7-([3-fluoro-5-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]sulfanyl)-4-furan-3-yl-2H-chromen-2-one IC50: 9 nM Homo sapiens
1.13.11.34 7-([3-fluoro-5-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]sulfanyl)-4-phenyl-2H-chromen-2-one IC50: 26 nM Homo sapiens
1.13.11.34 7-[[3-(1-ethyl-1-hydroxypropyl)-5-fluorophenoxy]methyl]-4-furan-3-yl-2H-chromen-2-one IC50: 15 nM Homo sapiens
1.13.11.34 L-739,010
-
 Homo sapiens
1.13.11.34 L-746,530 IC50: 27 nM Homo sapiens

Organism

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

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.13.11.34 arachidonate + O2
-
 Homo sapiens (6E,8Z,11Z,14Z)-(5S)-hydroperoxyicosa-6,8,11,14-tetraenoate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.13.11.34 H5-LO
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.13.11.34 0.000009
-
 IC50: 9 nM Homo sapiens 7-([3-fluoro-5-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]sulfanyl)-4-furan-3-yl-2H-chromen-2-one
1.13.11.34 0.000015
-
 IC50: 15 nM Homo sapiens 7-[[3-(1-ethyl-1-hydroxypropyl)-5-fluorophenoxy]methyl]-4-furan-3-yl-2H-chromen-2-one
1.13.11.34 0.000026
-
 IC50: 26 nM Homo sapiens 7-([3-fluoro-5-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]sulfanyl)-4-phenyl-2H-chromen-2-one
1.13.11.34 0.000027
-
 IC50: 27 nM Homo sapiens L-746,530
1.13.11.34 0.000027
-
 IC50: 27 nM Homo sapiens 4-(4-fluorophenyl)-7-([3-fluoro-5-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]sulfanyl)-2H-chromen-2-one
1.13.11.34 0.000055
-
 IC50: 55 nM Homo sapiens 4-(4-fluorophenyl)-7-([3-fluoro-5-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenoxy]methyl)-2H-chromen-2-one
1.13.11.34 0.000175
-
 IC50: 175 nM Homo sapiens 7-([3-fluoro-5-[(1S)-1-hydroxy-1-(1,3-thiazol-2-yl)propyl]phenoxy]methyl)-4-(4-fluorophenyl)-2H-chromen-2-one
1.13.11.34 0.000175
-
 IC50: 175 nM Homo sapiens 7-([3-fluoro-5-[(1R)-1-hydroxy-1-pyridin-2-ylpropyl]phenoxy]methyl)-4-furan-3-yl-2H-chromen-2-one
1.13.11.34 0.00018
-
 IC50: 180 nM Homo sapiens 4-(4-chlorophenyl)-7-([3-fluoro-5-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]sulfanyl)-2H-chromen-2-one
1.13.11.34 0.0002
-
 IC50: 200 nM Homo sapiens 7-([3-fluoro-5-[(1R,3R,5S)-3-hydroxy-6,8-dioxabicyclo[3.2.1]oct-3-yl]phenoxy]methyl)-4-furan-3-yl-2H-chromen-2-one
1.13.11.34 0.0003
-
 IC50: 300 nM Homo sapiens 7-([3-fluoro-5-[(1R,3R,5S)-3-hydroxy-6,8-dioxabicyclo[3.2.1]oct-3-yl]phenoxy]methyl)-4-phenyl-2H-chromen-2-one