1.13.11.34: arachidonate 5-lipoxygenase
This is an abbreviated version!
For detailed information about arachidonate 5-lipoxygenase, go to the full flat file.
Word Map on EC 1.13.11.34
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1.13.11.34
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cyclooxygenase
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prostaglandin
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leukocyte
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neutrophil
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eicosanoids
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cox-2
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asthma
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indomethacin
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ionophore
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phospholipase
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zileuton
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polymorphonuclear
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thromboxane
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flap
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airway
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peritoneal
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5-hete
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platelet
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eosinophil
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mast
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cysteinyl
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allergic
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edema
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12-lipoxygenase
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histamine
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lta4
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nordihydroguaiaretic
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lipoxygenases
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paf
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ndga
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bronchoconstriction
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5-hydroxyeicosatetraenoic
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asthmatic
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basophil
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platelet-activating
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anaphylaxis
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zymosan
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antigen-induced
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lipoxins
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montelukast
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hetes
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mpges-1
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carrageenan-induced
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a23187-stimulated
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paf-induced
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pro-resolving
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synthesis
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bronchospasm
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medicine
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drug development
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14carachidonic
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pharmacology
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bronchoconstrictors
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ulcerogenic
- 1.13.11.34
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cyclooxygenase
- prostaglandin
- leukocyte
- neutrophil
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eicosanoids
- cox-2
- asthma
- indomethacin
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ionophore
- phospholipase
- zileuton
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polymorphonuclear
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thromboxane
- flap
- airway
- peritoneal
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5-hete
- platelet
-
eosinophil
-
mast
-
cysteinyl
-
allergic
- edema
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12-lipoxygenase
- histamine
- lta4
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nordihydroguaiaretic
- lipoxygenases
- paf
- ndga
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bronchoconstriction
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5-hydroxyeicosatetraenoic
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asthmatic
-
basophil
-
platelet-activating
- anaphylaxis
- zymosan
-
antigen-induced
-
lipoxins
- montelukast
-
hetes
- mpges-1
-
carrageenan-induced
-
a23187-stimulated
-
paf-induced
-
pro-resolving
- synthesis
- bronchospasm
- medicine
- drug development
-
14carachidonic
- pharmacology
-
bronchoconstrictors
-
ulcerogenic
Reaction
Synonyms
5-lipoxygenase, 5-LO, 5-LO1, 5-LOX, 5DELTA-lipoxygenase, 5LO, 5LOX-1, ALOX5, arachidonate 5-LO, arachidonate:oxygen oxidoreductase, arachidonic 5-lipoxygenase, arachidonic acid 5-lipoxygenase, C-5-lipoxygenase, DELTA5-lipoxygenase, H5-LO, leukotriene A4 synthase, leukotriene-A4 synthase, lipoxygenase 15, lipoxygenase 5, lipoxygenase-1, LO-1, LOX-15, LOX-5, LTA synthase, LTA4 synthase, oxygenase, arachidonate, 5-lip-, PMNL 5-lipoxygenase
ECTree
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Inhibitors
Inhibitors on EC 1.13.11.34 - arachidonate 5-lipoxygenase
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(1-[2-[4-(trifluoromethyl)phenyl]ethyl]-1H-1,2,3-triazol-4-yl)methyl (2E)-3-(3,4-dihydroxyphenyl)prop-2-enoate
compound forms pi-pi interactions with residues Phe177, His367 and coordinates iron
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(17S)-hydroperoxy-4,7,10,13,15,19-docosahexaenoyl lysophosphatidylcholine
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(1E)-1-(2,5-dihydroxyphenyl)-5-phenylpent-1-en-3-one
inhibits leukotriene biosynthesis in isolated human neutrophils and in whole blood
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(1E)-1-(3,4-dihydroxyphenyl)-6-phenylhex-1-en-3-one
inhibits leukotriene biosynthesis in isolated human neutrophils and in whole blood
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(1E)-1-(4-hydroxy-3,5-dimethoxyphenyl)-5-phenylpent-1-en-3-one
inhibits leukotriene biosynthesis in isolated human neutrophils and in whole blood, retains 50% of inhibitory activity after up to one hour of incubation
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(2,4-dihydroxyphenyl)[3-(1-[hydroxy[(3,4,5-trihydroxyphenyl)methyl]amino]ethyl)phenyl]methanone
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(2,4-dihydroxyphenyl)[3-(1-[hydroxy[(4-hydroxyphenyl)methyl]amino]ethyl)phenyl]methanone
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(2E)-1-(2-hydroxy-4-methoxyphenyl)-3-(2,4,5-trimethoxyphenyl)prop-2-en-1-one
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(2E)-1-(2-hydroxy-4-methoxyphenyl)-3-(3,4,5-trimethoxyphenyl)prop-2-en-1-one
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(2E)-1-(2-hydroxy-4-methoxyphenyl)-3-[3-methoxy-4-(3-phenoxypropoxy)phenyl]prop-2-en-1-one
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(2E)-1-(2-hydroxy-4-methoxyphenyl)-3-[4-(morpholin-4-ylcarbonyl)phenyl]prop-2-en-1-one
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(2E)-1-(2-hydroxy-4-methoxyphenyl)-3-[4-(piperidin-1-ylcarbonyl)phenyl]prop-2-en-1-one
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(2E)-1-(2-hydroxy-4-methoxyphenyl)-3-[4-(pyrrolidin-1-ylcarbonyl)phenyl]prop-2-en-1-one
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(2E)-1-(2-hydroxy-4-methoxyphenyl)-3-[4-[(4-methylpiperazin-1-yl)carbonyl]phenyl]prop-2-en-1-one
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(2E)-3-[3-(2-ethoxyethoxy)phenyl]-1-(2-hydroxy-4-methoxyphenyl)prop-2-en-1-one
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(2E)-3-[4-(2-ethoxyethoxy)phenyl]-1-(2-hydroxy-4-methoxyphenyl)prop-2-en-1-one
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(2E)-3-[4-(3-ethoxypropoxy)-3-methoxyphenyl]-1-(2-hydroxy-4-methoxyphenyl)prop-2-en-1-one
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(2E)-3-[4-(benzyloxy)-3-bromo-5-methoxyphenyl]-1-(2-hydroxy-4-methoxyphenyl)prop-2-en-1-one
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(2E)-3-[4-(benzyloxy)phenyl]-1-(2-hydroxy-4-methoxyphenyl)prop-2-en-1-one
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(2E)-3-[4-[(1E)-3-[[(2E)-3-(2,3-dihydroxyphenyl)prop-2-enoyl]oxy]prop-1-en-1-yl]phenyl]prop-2-en-1-yl (2E)-3-(3,4-dihydroxyphenyl)prop-2-enoate
caffeic acid phenylethyl ester analogue, IC50 value for inhibition of 5-Lox product synthesis in transfected HEK-293 cells is 0.00061 mM. Compound is a good radical scavenger
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(2E,2'E)-(1,1'-(2,2-bis((4-(((E)-3-(3,4-dihydroxyphenyl)acryloyloxy)methyl)-1H-1,2,3-triazol-1-yl)methyl)propane-1,3-diyl)bis(1H-1,2,3-triazole-4,1-diyl))bis(methylene) bis(3-(3,4-dihydroxyphenyl)acrylate)
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potent inhibition by 92%
(2E,2'E)-(1,1'-(2,2-bis((4-(cinnamoyloxymethyl)-1H-1,2,3-triazol-1-yl)methyl)propane-1,3-diyl)bis(1H-1,2,3-triazole-4,1-diyl))bis(methylene) bis(3-phenylacrylate)
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shows less inhibitory activity than the corresponding clusters bearing the caffeic acid moiety
(2E,2'E)-(1,1'-(2-((4-(((E)-3-(3,4-dihydroxyphenyl)acryloyloxy)methyl)-1H-1,2,3-triazol-1-yl)methyl)-2-(hydroxymethyl)propane-1,3-diyl)bis(1H-1,2,3-triazole-4,1-diyl))bis(methylene) bis(3-(3,4-dihydroxyphenyl)acrylate)
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potent inhibition by 91%
(2E,2'E)-(1,1'-(2-((4-(cinnamoyloxymethyl)-1H-1,2,3-triazol-1-yl)methyl)-2-(hydroxymethyl)propane-1,3-diyl)bis(1H-1,2,3-triazole-4,1-diyl))bis(methylene) bis(3-phenylacrylate)
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shows less inhibitory activity than the corresponding clusters bearing the caffeic acid moiety
(2E,2'E)-2,2'-(4,4'-(2,2-bis(((1-(2-((E)-3-(3,4-dihydroxyphenyl)acryloyloxy)ethyl)-1H-1,2,3-triazol-4-yl)methoxy)methyl)propane-1,3-diyl)bis(oxy)bis(methylene)bis(1H-1,2,3-triazole-4,1-diyl))bis(ethane-2,1-diyl) bis(3-(3,4-dihydroxyphenyl)acrylate)
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(2E,2'E)-2,2'-(4,4'-(2,2-bis(((1-(2-(cinnamoyloxy)ethyl)-1H-1,2,3-triazol-4-yl)methoxy)methyl)propane-1,3-diyl)bis(oxy)bis(methylene)bis(1H-1,2,3-triazole-4,1-diyl))bis(ethane-2,1-diyl) bis(3-phenylacrylate)
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shows less inhibitory activity than the corresponding clusters bearing the caffeic acid moiety
(2E,5E)-5-[(2E)-3-(furan-2-yl)prop-2-en-1-ylidene]-3-phenyl-2-(phenylimino)-1,3-thiazolidin-4-one
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(2E,6E,10E)-13-((R)-6-hydroxy-2,5,7,8-tetramethylchroman-2-yl)-N-(4-methoxybenzyl)-2,6,10-trimethyltrideca-2,6,10-trienamide
significant inhibitory activity in both cell-free and cell-based assays, inhibits leukotriene biosynthesis by human primary polymorphonuclear leukocytes, IC50 value 250 nM
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(2E,6E,10E)-13-((R)-6-hydroxy-2,8-dimethylchroman-2-yl)-N-(4-methoxybenzyl)-2,6,10-trimethyltrideca-2,6,10-trienamide
significant inhibitory activity in both cell-free and cell-based assays, inhibits leukotriene biosynthesis by human primary polymorphonuclear leukocytes, IC50 value 184 nM
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(2E,6E,10E)-13-(6-hydroxy-2,8-dimethylchroman-2-yl)-2,6,10-trimethyl-N-(pyridin-3-ylmethyl)trideca-2,6,10-trienamide
inhibits leukotriene biosynthesis by human primary polymorphonuclear leukocytes, IC50 value 415 nM
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(2E,6E,10E)-N-benzyl-13-((R)-6-hydroxy-2,5,7,8-tetramethylchroman-2-yl)-2,6,10-trimethyltrideca-2,6,10-trienamide
significant inhibitory activity in both cell-free and cell-based assays, inhibits leukotriene biosynthesis by human primary polymorphonuclear leukocytes, IC50 value 173 nM
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(2E,6E,10E)-N-benzyl-13-((R)-6-hydroxy-2,8-dimethylchroman-2-yl)-2,6,10-trimethyltrideca-2,6,10-trienamide
inhibits leukotriene biosynthesis by human primary polymorphonuclear leukocytes, IC50 value 303 nM
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(2Z)-2-[4-(acetylamino)phenyl]-3-[4-(methylsulfonyl)phenyl]prop-2-enoic acid
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(5E)-2-(4-methylphenyl)-5-(3,4,5-trimethoxybenzylidene)-1,3-thiazol-4(5H)-one
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(5E)-5-(2-hydroxy-3-methoxybenzylidene)-2-(4-methylphenyl)-1,3-thiazol-4(5H)-one
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(5E)-5-(3-chloro-4-hydroxy-5-methoxybenzylidene)-2-(4-methylphenyl)-1,3-thiazol-4(5H)-one
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(5E)-5-(3-chloro-4-hydroxy-5-methoxybenzylidene)-2-phenyl-1,3-thiazol-4(5H)-one
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(5E)-5-(3-chloro-5-ethoxy-4-hydroxybenzylidene)-2-(4-methylphenyl)-1,3-thiazol-4(5H)-one
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(5E)-5-(4-hydroxy-3-methoxy-5-nitrobenzylidene)-2-phenyl-1,3-thiazol-4(5H)-one
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(5E)-5-(4-[(methylperoxy)acetyl]benzylidene)-2-(4-methylphenyl)-1,3-thiazol-4(5H)-one
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(5E)-5-(5-chloro-2-hydroxy-3-methoxybenzylidene)-2-phenyl-1,3-thiazol-4(5H)-one
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(5E)-5-[4-(dimethylamino)benzylidene]-2-(piperidin-1-yl)-1,3-thiazol-4(5H)-one
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(5S,6S,7E,9E,11Z,14Z)-5,6-epoxyicosa-7,9,11,14-tetraenoate
product inhibition
(6E,8Z,11Z,14Z)-(5S)-hydroperoxyicosa-6,8,11,14-tetraenoate
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inhibits reaction with arachidonate
(R)-N-((3-(3-fluoro-4-morpholinophenyl)-2-oxooxazolidin-5-yl) methyl)-N-hydroxyheptanamide
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(R)-N-((3-(3-fluoro-4-morpholinophenyl)-2-oxooxazolidin-5-yl) methyl)-N-hydroxyoctanamide
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(R)-N-((3-(3-fluoro-4-morpholinophenyl)-2-oxooxazolidin-5-yl)methyl)-N-hydroxypentanamide
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(R)-N-(2-(diphenylamino)ethyl)-3-(3-(1-hydroxyureido)but-1-yn-1-yl)benzamide
dual 5-LOX/soluble epoxide hydrolase inhibitor
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(R)-N-(3,3-bis(4-fluorophenyl)propyl)-3-(3-(1-hydroxyureido)but-1-yn-1-yl)benzamide
dual 5-LOX/soluble epoxide hydrolase inhibitor
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([3-chloro-5-(2,3-dihydro-1H-inden-4-ylamino)phenyl]sulfanyl)acetic acid
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([4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl]sulfanyl)(naphthalen-1-yl)acetic acid
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1,4a-dimethyl-7-(propan-2-yl)-1-(prop-1-en-2-yl)-1,2,3,4,4a,4b,5,6,10,10a-decahydrophenanthrene (non-preferred name)
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1-(2,4-difluorophenyl)-3-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)urea
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1-(3,4-dichlorobenzyl)-3-(2-morpholin-4-yl-2-oxoethyl)-1H-indole
82% inhibition at 0.005 mM
1-(3,4-dichlorobenzyl)-3-(3-morpholin-4-yl-3-oxopropyl)-1H-indole
38.5% inhibition at 0.005 mM
1-(3-[5-(hydroxyureido)methyl-2-methoxyphenoxy]propyl)-3-[4-(trifluoromethoxy)phenyl]urea
KM55, a multitarget ligand and dual 5-lipoxygenase (5-LO)/soluble epoxide hydrolase (sEH) inhibitor. KM55 potently inhibits both enzymes in vitro and attenuates the formation of leukotrienes in human whole blood. It significantly inhibits the LPS-induced adhesion of leukocytes to endothelial cells by blocking leukocyte activation. Compound synthesis and evaluation, overview. KM55 inhibits the formation of leukotriene B4 and 5-hydroxyeicosatrienoic acid, while the formation of 12-hydroperoxyicosatetraenoate and 15-hydroperoxyicosatetraenoate are unaffected. KM55 blocks leukocyte-endothelial cell interaction by impairing leukocyte activation, whereas endothelial cells are not affected
1-(4-aminosulfonylphenyl)-5-(2-chloropyridin-4-yl)-3-trifluoromethyl-1H-pyrazole
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1-(4-aminosulfonylphenyl)-5-[4-(1-difluoromethyl-1,2-dihydropyrid-2-one)]-3-trifluoromethyl-1H-pyrazole
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1-(4-chlorobenzyl)-2-[2,2-dimethyl-3-(1H-tetrazol-5-yl)propyl]-4-methyl-6-[2-(5-phenylpyridin-2-yl)ethyl]-2,2a,4,5-tetrahydro-1H-thiopyrano[2,3,4-cd]indole
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1-(4-chlorophenoxy)-3-(2-morpholin-4-yl-2-oxoethyl)-1H-indole
22% inhibition at 0.005 mM
1-(4-chlorophenoxy)-3-(3-morpholin-4-yl-3-oxopropyl)-1H-indole
26% inhibition at 0.005 mM
1-(4-chlorophenoxy)-5-methoxy-2-methyl-3-(4-morpholin-4-yl-4-oxobutyl)-1H-indole
70% inhibition at 0.005 mM
1-(4-methanesulfonylphenyl)-5-(2-chloropyridin-4-yl)-3-trifluoromethyl-1H-pyrazole
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1-(4-methanesulfonylphenyl)-5-[4-(1-difluoromethyl-1,2-dihydropyrid-2-one)]-3-trifluoromethyl-1H-pyrazole
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1-(4-methylbenzyl)-3-(2-morpholin-4-yl-2-oxoethyl)-1H-indole
35% inhibition at 0.005 mM
1-(4-methylbenzyl)-3-(3-morpholin-4-yl-3-oxopropyl)-1H-indole
55% inhibition at 0.005 mM
1-(8-tert-butyl-4,4-dimethyl-3,4-dihydro-2H-chromen-6-yl)-4-cyclopropylbutan-1-one
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1-(benzyloxy)hept-2-yn-4-ol
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forms three hydrogen bonds with 5-lipoxygenase
1-(difluoromethyl)-5-[[2-(methylsulfonyl)phenyl]ethynyl]pyridin-2(1H)-one
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1-benzyl-3-(2-morpholin-4-yl-2-oxoethyl)-1H-indole
41% inhibition at 0.005 mM
1-benzyl-3-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)urea
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1-benzyl-3-(3-morpholin-4-yl-3-oxopropyl)-1H-indole
64% inhibition at 0.005 mM
1-benzyl-3-(4-morpholin-4-ylbutyl)-1H-indole
42% inhibition at 0.005 mM
1-benzyl-3-(4-oxo-4-piperazin-1-ylbutyl)-1H-indole
95% inhibition at 0.005 mM
1-benzyl-3-[2-[3-fluoro-5-(4-methoxytetrahydro-2H-pyran-4-yl)phenoxy]ethyl]-1H-indole
32% inhibition at 0.005 mM
1-benzyl-3-[3-[3-fluoro-5-(4-methoxytetrahydro-2H-pyran-4-yl)phenoxy]propyl]-5-methoxy-2-methyl-1H-indole
46.5% inhibition at 0.005 mM
1-benzyl-5-chloro-2-methyl-3-(4-morpholin-4-yl-4-oxobutyl)-1H-indole
80% inhibition at 0.005 mM
1-benzyl-5-methoxy-2-methyl-3-(4-morpholin-4-yl-4-oxobutyl)-1H-indole
54% inhibition at 0.005 mM
1-benzyl-5-methoxy-2-methyl-3-(4-oxo-4-piperazin-1-ylbutyl)-1H-indole
65% inhibition at 0.005 mM
1-O-dodecyl 2,3-O-isopropylidene-5,6-dideoxy-5-N-[4-(2-hydroxy-2-oxoethyl) phenylaminocarbonyl] amino-beta-L-gulofuranoside sodium salt
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competitive inhibitor, IC50: 0.0035 mM with recombinant enzyme, IC50: 0.005 mM with native enzyme
1-[(4methylbenzyl)oxy]hept-2-yn-4-ol
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is more potent than 1-(benzyloxy)hept-2-yn-4-ol to 5-lipoxygenase
1-[3-(methylsulfanyl)phenyl]-3-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)urea
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1-[4-([3-fluoro-5-[4-(methylsulfinyl)tetrahydro-2H-pyran-4-yl]phenoxy]methyl)phenyl]-2-methyl-1H-imidazole
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1-[4-([3-fluoro-5-[4-(methylsulfonyl)tetrahydro-2H-pyran-4-yl]phenoxy]methyl)phenyl]-2-methyl-1H-imidazole
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10-nitro-oleic acid
inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.0015 mM
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2,3,4',5-tetrahydroxystilbene-2-O-D-glucoside
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polymorphonuclear leukocyte
2-(1-difluoromethyl-2-oxo-1,2-dihydropyridin-4-yl)phenylacetic acid
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micromolar 5-LOX inhibitory activity
2-(2,2-dimethyl-6-(4-nitrophenyl)-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl)acetic acid
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2-(2,2-dimethyl-7-phenyl-6-(4-(trifluoromethyl)phenyl)-2,3-dihydro-1H-pyrrolizin-5-yl)acetic acid
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2-(2,4-dihydroxyphenyl)-8,8-dimethyl-3-(3-methylbut-2-en-1-yl)-4H,8H-pyrano[2,3-f]chromen-4-one
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2-(2-methoxyphenyl)-N-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)acetamide
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2-(4-chloro-6-(5-methoxy-2-methylbiphenyl-4-ylamino)pyrimidin-2-ylthio)octanoic acid
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2-(5,8-dimethyl-7-propoxy-1,2,3,4-tetrahydronaphthalen-2-yl)-N-(5-methyl-1,3-thiazol-2-yl)propanamide
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2-(5,8-dimethyl-7-propoxy-1,2,3,4-tetrahydronaphthalen-2-yl)-N-1,3-thiazol-2-ylpropanamide
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2-(5,8-dimethyl-7-propoxy-1,2,3,4-tetrahydronaphthalen-2-yl)-N-pyridin-2-ylpropanamide
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2-(5,8-dimethyl-7-propoxy-1,2,3,4-tetrahydronaphthalen-2-yl)-N-thiophen-3-ylpropanamide
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2-(6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl)-N-(methylsulfonyl)acetamide
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2-(6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl)-N-(phenylsulfonyl)acetamide
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2-(6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl)-N-tosylacetamide
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2-(6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1Hpyrrolizin-5-yl)-N-tosylpropanamide
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2-(6-(4-tert-butylphenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl)acetic acid
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2-(7-methoxy-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl)-N-(thiophen-2-ylmethyl)propanamide
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2-(7-methoxy-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl)-N-1,3-thiazol-2-ylpropanamide
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2-(7-methoxy-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl)-N-pyridin-2-ylpropanamide
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2-([4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl]sulfanyl)octanoic acid
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2-phenylethyl (2E)-3-(4-hydroxy-3,5-dimethoxyphenyl)prop-2-enoate
inhibits leukotriene biosynthesis in isolated human neutrophils and in whole blood
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2-[(4-[[3,5-bis(2,2,2-trifluoroethoxy)phenyl]amino]-6-chloropyrimidin-2-yl)sulfanyl]octanoic acid
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2-[2-(1-difluoromethyl-2-oxo-1,2-dihydropyridin-4-yl)phenyl]propanoic acid
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micromolar 5-LOX inhibitory activity
2-[2-[(2-methyl-1H-benzimidazol-1-yl)methyl]phenoxy]acetamide
a BRP-7 derivative
2-[2-[(2-[1-[4-(2-methylpropyl)phenyl]ethyl]-1H-benzimidazol-1-yl)methyl]phenoxy]acetamide
a BRP-7 derivative
2-[3-(1-difluoromethyl-2-oxo-1,2-dihydropyridin-4-yl)phenyl]propanoic acid
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micromolar 5-LOX inhibitory activity
2-[4'-(iso-propylphenyl)-amino]-5,6-dimethyl-1,4-benzoquinone
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potent inhibitor, IC50: 0.006 mM
2-[4-(1-difluoromethyl-2-oxo-1,2-dihydropyridin-4-yl)phenyl]propanoic acid
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micromolar 5-LOX inhibitory activity
2-[4-([[(2E)-3-phenylprop-2-enoyl]oxy]methyl)-1H-1,2,3-triazol-1-yl]ethyl (2E)-3-(3,4-dihydroxyphenyl)prop-2-enoate
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2-[5,8-dimethyl-7-(2-morpholin-4-ylethoxy)-1,2,3,4-tetrahydronaphthalen-2-yl]-N-1,3-thiazol-2-ylpropanamide
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2-[6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl]acetic acid
-
-
2-[7-[2-(dimethylamino)ethoxy]-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl]-N-1,3-thiazol-2-ylpropanamide
-
-
2-[7-[2-(dimethylamino)ethoxy]-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl]-N-pyridin-2-ylpropanamide
-
-
2-[[5-fluoro-6-(4-fluorophenoxy)-1H-benzimidazol-2-yl]sulfanyl]-2-methylpropanoic acid
-
additionally inhibts soluble epoxide hydrolase. Compound shows potent anti-inflammatory activity and significant inhibition of edema at a dose of 100 mg/kg
-
3,4,5-trimethoxy-N-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)benzamide
-
-
3-(1-acetoxy-10-hydroxydecyl)-2,5-dimethoxycyclohexa-2,5-diene-1,4-dione
-
3-(1-difluoromethyl-2-oxo-1,2-dihydropyridin-4-yl)phenylacetic acid
-
micromolar 5-LOX inhibitory activity
3-(2-(2-[(4-chlorophenyl)sulfanyl]ethoxy)-3-methoxy-5-[5-(3,4,5-trimethoxyphenyl)tetrahydrofuran-2-yl]benzyl)-1-hydroxy-1-methylurea
-
-
3-(2-morpholin-4-yl-2-oxoethyl)-1-phenoxy-1H-indole
21% inhibition at 0.005 mM
3-(2-morpholin-4-yl-2-oxoethyl)-1H-indole
16% inhibition at 0.005 mM
3-(3-(1-hydroxyureido)but-1-yn-1-yl)-N-(2-(trifluoromethyl)-benzyl)benzamide
dual 5-LOX/soluble epoxide hydrolase inhibitor
-
3-(3-(1-hydroxyureido)but-1-yn-1-yl)-N-(3-phenyl-3-(4-(trifluoromethoxy)phenyl)propyl)benzamide
dual 5-LOX/soluble epoxide hydrolase inhibitor
-
3-(3-(1-hydroxyureido)but-1-yn-1-yl)-N-(4-methoxy-2-(trifluoromethyl)benzyl)-benzamide
dual 5-LOX/soluble epoxide hydrolase inhibitor
-
3-(3-(1-hydroxyureido)hex-1-yn-1-yl)-N-(2-(trifluoromethyl)-benzyl)benzamide
dual 5-LOX/soluble epoxide hydrolase inhibitor
-
3-(3-morpholin-4-yl-3-oxopropyl)-1-phenoxy-1H-indole
23% inhibition at 0.005 mM
3-(3-morpholin-4-yl-3-oxopropyl)-1H-indole
33% inhibition at 0.005 mM
3-(4,5-dihydroxy-2-methyl-9,10-dioxo-4a,9,9a,10-tetrahydroanthracen-1-yl)-2-hydroxy-4,6-dimethoxybenzoic acid
-
-
3-(4-morpholin-4-yl-4-oxobutyl)-1H-indole
62% inhibition at 0.005 mM
3-(6-(4-chlorphenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl)propionic acid
-
-
3-(decahydronaphthalen-2-ylmethyl)-2,5-dihydroxycyclohexa-2,5-diene-1,4-dione
-
-
3-acetyl-11-keto-beta-boswellic acid
allosteric inhibitor from frankincense, wedges between the membrane-binding and catalytic domains of 5-LOX, some 30 A from the catalytic iron. Binding promotes a shift in the regiospecificity, i.e. a significant increase in the formation of 12-hydroxyeicosatetraenoic acid with the most prominent effect at 10 microM
3-tridecyl-4,5-dimethoxybenzene-1,2-diol
shows anti-inflammatory effectiveness
3-[2-[3-fluoro-5-(4-methoxytetrahydro-2H-pyran-4-yl)phenoxy]ethyl]-1H-indole
64% inhibition at 0.005 mM
3-[4-(3-[[(2E)-3-(2,3-dihydroxyphenyl)prop-2-enoyl]oxy]prop-1-yn-1-yl)phenyl]prop-2-yn-1-yl (2E)-3-(3,4-dihydroxyphenyl)prop-2-enoate
caffeic acid phenylethyl ester analogue, IC50 value for inhibition of 5-Lox product synthesis in transfected HEK-293 cells is 0.00036 mM. Compound is a good radical scavenger
-
3-[5-[(2E)-3,7-dimethylocta-2,6-dien-1-yl]-2,4-dihydroxyphenyl]-5,7-dihydroxy-2,3-dihydro-4H-chromen-4-one
-
-
3-[[3-fluoro-5-(4-methoxytetrahydro-2H-pyran-4-yl)phenoxy]methyl]-1-[4-(methylsulfonyl)phenyl]-5-phenyl-1H-pyrazole
-
-
4,5-dimethoxy-3-tridecylcyclohexa-3,5-diene-1,2-dione
shows anti-inflammatory effectiveness
4-((3,4-dichlorobenzyl)-1H-indol-3-yl)-1-morpholinobutan-1-one
27% inhibition at 0.005 mM
4-((4-chlorobenzoyl)-1H-indol-3-yl)-1-morpholinobutan-1-one
32% inhibition at 0.005 mM
4-(1-(4-methylbenzyl)-1H-indol-3-yl)-1-morpholinobutan-1-one
34% inhibition at 0.005 mM
4-(1-benzoyl-1H-indol-3-yl)-1-morpholinobutan-1-one
58% inhibition at 0.005 mM
4-(1-benzyl-1H-indol-3-yl)-1-morpholinobutan-1-one
26% inhibition at 0.005 mM
4-(1-difluoromethyl-2-oxo-1,2-dihydropyridin-4-yl)phenylacetic acid
-
micromolar 5-LOX inhibitory activity
4-(3-(1-hydroxyureido)but-1-yn-1-yl)-N-(2-(trifluoromethyl)-benzyl)benzamide
dual 5-LOX/soluble epoxide hydrolase inhibitor, displays cellular activity in human polymorphonuclear leukocytes, oral bioavailability, and target engagement in vivo and demonstrates anti-inflammatory and anti-fibrotic efficiency in a kidney injury model caused by unilateral ureteral obstruction in mice
-
4-(3-fluoro-5-[[4-(2-methyl-1H-imidazol-1-yl)benzyl]oxy]phenyl)-N-methyltetrahydro-2H-pyran-4-carboxamide
-
-
4-(3-fluoro-5-[[4-(2-methyl-1H-imidazol-1-yl)benzyl]oxy]phenyl)tetrahydro-2H-pyran-4-ol
-
-
4-(3-fluoro-5[[4-(2-methyl-1H-imidazol-1-yl)benzyl]oxy]phenyl)tetrahydro-2H-pyran-4-carboxylic acid
-
-
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
4-(4-fluorophenyl)-5-(4-(methylsulfonyl)phenyl)-1,2-selenazole
-
60% inhibition at 0.01 mM
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
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
4-(acetyloxy)-2-[4-(acetyloxy)-6-methylhept-5-en-2-yl]cyclohexyl (2Z)-2-methylbut-2-enoate
-
-
4-(furan-3-yl)-7-[[2-(tetrahydro-2H-pyran-4-yl)pyridin-4-yl]methoxy]naphthalene-2-carbonitrile
-
-
4-(furan-3-yl)-7-[[6-(4-hydroxytetrahydro-2H-pyran-4-yl)pyridin-2-yl]methoxy]naphthalene-2-carbonitrile
-
-
4-(furan-3-yl)-7-[[7-(tetrahydro-2H-pyran-4-yl)-1,2,3,4-tetrahydroquinolin-2-yl]oxy]naphthalene-2-carbonitrile
-
-
4-([[5-fluoro-6-(1H-1,2,4-triazol-1-yl)-1H-benzimidazol-2-yl]sulfanyl]methyl)benzoic acid
-
additionally inhibts soluble epoxide hydrolase. Compound shows potent anti-inflammatory activity and significant inhibition of edema at a dose of 100 mg/kg
-
4-([[5-fluoro-6-(4-fluorophenoxy)-1H-benzimidazol-2-yl]sulfanyl]methyl)benzoic acid
-
additionally inhibts soluble epoxide hydrolase. Compound shows potent anti-inflammatory activity and significant inhibition of edema at a dose of 100 mg/kg
-
4-([[6-(4-chlorophenoxy)-5-fluoro-1H-benzimidazol-2-yl]sulfanyl]methyl)benzoic acid
-
additionally inhibts soluble epoxide hydrolase. Compound shows potent anti-inflammatory activity and significant inhibition of edema at a dose of 100 mg/kg
-
4-chloro-N-([4-[(2E)-3-(2,4-dichlorophenyl)prop-2-enoyl]phenyl]carbamoyl)benzenesulfonamide
-
IC50: 0.00042 mM
4-chloro-N-([4-[(2E)-3-phenylprop-2-enoyl]phenyl]carbamoyl)benzenesulfonamide
-
IC50: 0.00083 mM
4-methoxy-N-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)benzamide
-
-
4-methyl-N-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)-1,2,3-thiadiazole-5-carboxamide
-
-
4-methyl-N-([4-[(2E)-3-(2,3,4-trimethylphenyl)prop-2 enoyl]phenyl]carbamoyl)benzenesulfonamide
-
IC50: 0.00045 mM
4-methyl-N-([4-[(2E)-3-phenylprop-2-enoyl]phenyl]carbamoyl)benzenesulfonamide
-
IC50: 0.00089 mM
4-[(1E)-3-(2-hydroxy-4-methoxyphenyl)-3-oxoprop-1-en-1-yl]-N-(2-hydroxy-5-nitrophenyl)benzamide
-
-
4-[(1E)-3-(2-hydroxy-4-methoxyphenyl)-3-oxoprop-1-en-1-yl]-N-(2-hydroxyphenyl)benzamide
-
-
4-[(1E)-3-(2-hydroxy-4-methoxyphenyl)-3-oxoprop-1-en-1-yl]-N-(2-methoxyphenyl)benzamide
-
-
4-[(1E)-3-(2-hydroxy-4-methoxyphenyl)-3-oxoprop-1-en-1-yl]-N-(2-phenylethyl)benzamide
-
-
4-[(1E)-3-(2-hydroxy-4-methoxyphenyl)-3-oxoprop-1-en-1-yl]-N-(propan-2-yl)benzamide
-
-
4-[(1E)-3-(2-hydroxy-4-methoxyphenyl)-3-oxoprop-1-en-1-yl]-N-methyl-N-phenylbenzamide
-
-
4-[(1E)-3-(2-hydroxy-4-methoxyphenyl)-3-oxoprop-1-en-1-yl]-N-propylbenzamide
-
-
4-[(1E)-3-(3-phenylpropoxy)prop-1-en-1-yl]benzene-1,2-diol
caffeic acid phenylethyl ester analogue, IC50 value for inhibition of 5-Lox product synthesis in transfected HEK-293 cells is 0.00018 mM. Compound is a good radical scavenger
-
4-[(1E)-3-(benzyloxy)prop-1-en-1-yl]benzene-1,2-diol
caffeic acid phenylethyl ester analogue, IC50 value for inhibition of 5-Lox product synthesis in transfected HEK-293 cells is 0.00043 mM. Compound is a good radical scavenger
-
4-[(4-cyclohexyl-5-methyl-1,3-thiazol-2-yl)amino]-2,6-dimethylphenol
lead compound, in vitro pharmacokinetic profile, shows no cytotoxicity, overview
4-[(hydroxy[1-[3'-(morpholin-4-yl)[1,1'-biphenyl]-3-yl]ethyl]amino)methyl]phenol
-
4-[([5-fluoro-6-[4-(1H-imidazol-1-yl)phenoxy]-1H-benzimidazol-2-yl]sulfanyl)methyl]benzoic acid
-
additionally inhibts soluble epoxide hydrolase. Compound shows potent anti-inflammatory activity and significant inhibition of edema at a dose of 100 mg/kg
-
4-[1-(4-chlorobenzyl)-4-methyl-6-[(5-phenylpyridin-2-yl)methoxy]-2,2a,4,5-tetrahydro-1H-thiopyrano[2,3,4-cd]indol-2-yl]-3,3-dimethyl-N-(methylsulfonyl)butanamide
-
-
4-[4-(4-fluoro-phenyl)-thiazol-2-ylamino]-2,6-dimethylphenol
-
KR-33749, the compound exhibits a more than 1000fold selectivity for 5-LO against 12-LO and 15-LO
4-[5-(1H-indol-3-yl)-3-(trifluoromethyl)-4,5-dihydro-1H-pyrazol-1-yl]benzenesulfonamide
-
-
4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide
-
-
4-[5-(6-chloro-1H-indol-3-yl)-3-trifluoromethyl-4,5-dihydropyrazol-1-yl]-benzenesulfonamide
4-[5-(7-chloro-1H-indol-3-yl)-3-trifluoromethyl-4,5-dihydropyrazol-1-yl]-benzenesulfonamide
4-[[4-(2,4-dichlorophenyl)-5-methyl-1,3-thiazol-2-yl]amino]-2,6-dimethylphenol
lead compound, in vitro pharmacokinetic profile, shows no cytotoxicity, overview
4-[[hydroxy(2-methyl-1-[3-[(morpholin-4-yl)oxy]phenyl]propyl)amino]methyl]phenol
-
5-(2-[[3-(trifluoromethyl)phenyl]amino]phenyl)-1,3,4-oxadiazole-2(3H)-thione
-
-
5-(3,5-di-tert-butyl-4-hydroxybenzylidene)thiazolidin-2,4-dione
-
effective inhibitor of 5-LOX in vivo
5-(4-fluorophenyl)-1-[4-(methylsulfonyl)phenyl]-3-(trifluoromethyl)-1H-pyrazole
-
-
5-(7-tert-butyl-3,3-dimethyl-2,3-dihydro-1-benzofuran-5-yl)-5-oxopentanenitrile
-
-
5-amino-2-hydroxy-N-(propan-2-yl)benzamide
-
5-aminosalicylic acid derivative, additionally inhibits cyclooxygenases Cox-1 and Cox-2
-
5-amino-N-cyclohexyl-2-hydroxybenzamide
-
5-aminosalicylic acid derivative, additionally inhibits cyclooxygenases Cox-1 and Cox-2
-
5-amino-N-hexyl-2-hydroxybenzamide
-
5-aminosalicylic acid derivative, additionally inhibits cyclooxygenases Cox-1 and Cox-2
-
5-chloro-1-(4-chlorophenoxy)-2-methyl-3-(4-morpholin-4-yl-4-oxobutyl)-1H-indole
38% inhibition at 0.005 mM
5-chloro-2-methyl-3-(4-morpholin-4-yl-4-oxobutyl)-1H-indole
71% inhibition at 0.005 mM
5-methoxy-2-methyl-1-(4-methylbenzyl)-3-(4-morpholin-4-yl-4-oxobutyl)-1H-indole
26% inhibition at 0.005 mM
5-methoxy-2-methyl-3-(4-morpholin-4-yl-4-oxobutyl)-1H-indole
73% inhibition at 0.005 mM
5-[[(2,5-dihydroxyphenyl)methyl]amino]-2-hydroxy-N-(4-methylphenyl)benzamide
-
5-aminosalicylic acid derivative, additionally inhibits cyclooxygenases Cox-1 and Cox-2
-
5-[[hydroxy(2-methyl-1-[3-[(morpholin-4-yl)oxy]phenyl]propyl)amino]methyl]benzene-1,2,3-triol
-
6-[(4-hydroxy-3,6-dioxocyclohexa-1,4-dien-1-yl)methyl]naphthalene-2-carboxylic acid
-
-
6-[[3-fluoro-5-(4-methoxytetrahydro-2H-pyran-4-yl)phenoxy]methyl]-1-methylquinolin-2(1H)-one
-
-
7-(4-methylphenyl)-6-[4-(methylsulfonyl)phenyl]-2,3-dihydro-1H-pyrrolizine
-
-
7-([3-fluoro-5-[(1R)-1-hydroxy-1-pyridin-2-ylpropyl]phenoxy]methyl)-4-furan-3-yl-2H-chromen-2-one
-
IC50: 175 nM
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
-
-
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
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
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
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
7-([3-fluoro-5-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]sulfanyl)-4-phenyl-2H-chromen-2-one
-
IC50: 26 nM
7-tert-butyl-N-ethyl-N,3,3-trimethyl-2,3-dihydro-1-benzofuran-5-carboxamide
-
-
7-[[3-(1-ethyl-1-hydroxypropyl)-5-fluorophenoxy]methyl]-4-furan-3-yl-2H-chromen-2-one
-
IC50: 15 nM
7-[[3-(4-methoxytetrahydro-2H-pyran-4-yl)benzyl]oxy]-4-phenylnaphtho[2,3-c]furan-1(3H)-one
-
-
7-[[3-fluoro-5-(3-hydroxy-6,8-dioxabicyclo[3.2.1]oct-3-yl)phenoxy]methyl]-4-(furan-3-yl)quinoline-2-carbonitrile
-
-
acetonylacetone bisphenylhydrazone
-
IC50 for reaction with linoleic acid: 0.015 mM, IC50 for reaction with arachidonic acid: 0.0039 mM
benzaldehyde phenylhydrazone
-
IC50 for reaction with linoleic acid: 0.0345 mM, IC50 for reaction with arachidonic acid: 0.0014 mM
BRP-7
benzimidazole derivative BRP-7 inhibits leukotriene biosynthesis in vitro and in vivo by targeting 5-lipoxygenase-activating protein (FLAP). BRP-7 blocks 5-LOX co-localization with FLAP at the nuclear envelope in neutrophils. No complete inhibition up to 0.01 mM
chalcone
inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.006 mM
cholesterol
-
addition to a membrane preperation in vitro reduces 5-lipoxygenase activity by half. Cholesterol sulfate can inhibit 5-lipoxygenase in intact cells
curcumin
inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.0016 mM
delphinidin 3-O-galactoside
-
from Vaccinium myrtillus berries, strong inhibitor, in a concentration-dependent manner
delphinidin 3-O-glucoside
-
from Vaccinium myrtillus berries, strong inhibitor, in a concentration-dependent manner
delta-garcinoic acid
i.e. an omega-oxidized tocotrienol, inhibits leukotriene biosynthesis by human primary polymorphonuclear leukocytes, IC50 value 345 nM
-
delta-tocopherol-13'-carboxychromanol
competitive, compound decreases leukotriene B4 from stimulated neutrophil-like cells without affecting translocation of 5-Lox from cytosol to the nucleus. Compound additionally inhibits cyclooxygenases Cox-1 and Cox-2
-
delta-tocotrienol
competitive, compound decreases leukotriene B4 from stimulated neutrophil-like cells without affecting translocation of 5-Lox from cytosol to the nucleus. Compound additionally inhibits cyclooxygenases Cox-1 and Cox-2
delta-tocotrienol-13'-carboxychromanol
competitive, compound decreases leukotriene B4 from stimulated neutrophil-like cells without affecting translocation of 5-Lox from cytosol to the nucleus. Compound additionally inhibits cyclooxygenases Cox-1 and Cox-2
-
Diamide
in 5-LO/FLAP-transfected HeLa cells, treatment with the thiol-oxidizing agent diamide which promotes glutathionylation at surface Cys residues leads to a decreased leukotriene synthesis by wild-type 5-LO
ethyl 2-((2,4-difluorophenylthio)methyl)-5-hydroxy-1-methyl-1H-indole-3-carboxylate
-
ethyl 2-((2,6-dichlorophenylthio)methyl)-5-hydroxy-1-methyl-1H-indole-3-carboxylate
-
ethyl 2-((2,6-dimethylphenylthio)methyl)-5-hydroxy-1-methyl-1H-indole-3-carboxylate
-
ethyl 2-((3,5-dimethylphenylthio)methyl)-5-hydroxy-1-methyl-1H-indole-3-carboxylate
-
ethyl 2-((3-chlorophenylthio)methyl)-5-hydroxy-1-methyl-1H-indole-3-carboxylate
-
ethyl 2-((4-fluorophenylthio)methyl)-5-hydroxy-1-methyl-1H-indole-3-carboxylate
-
ethyl 2-(3-chlorobenzyl)-5-methoxy-1-methyl-1H-benzo[g]-indole-3-carboxylate
-
-
ethyl 2-(3-chlorobenzyl)-7,8-dimethoxy-5-hydroxy-1H-benzo[g]indole-3-carboxylate
-
-
ethyl 5-hydroxy-1-methyl-2-((2-(trifluoromethyl)phenylthio)methyl)-1H-indole-3-carboxylate
-
ethyl 5-hydroxy-1-methyl-2-((4-(trifluoromethoxy)phenylthio)methyl)-1H-indole-3-carboxylate
-
ethyl 5-hydroxy-1-methyl-2-((4-(trifluoromethyl)phenylthio)methyl)-1H-indole-3-carboxylate
-
ethyl 5-hydroxy-2-((2-methoxyphenylthio)methyl)-1-methyl-1H-indole-3-carboxylate
-
ethyl 5-hydroxy-2-((4-methoxyphenylthio)methyl)-1-methyl-1H-indole-3-carboxylate
-
ethyl [2-[(2-[1-[4-(2-methylpropyl)phenyl]ethyl]-1H-benzimidazol-1-yl)methyl]phenoxy]acetate
a BRP-7 derivative
ferrocenyl carboxylic acid
mixed type inhibitor. The compound shows better antioxidant activity than the antioxidant Trolox
-
L-651,392
-
i.e. 4-bromo-2,7-dimethoxy-3H-phenothiazin-3-one, + 1 mM NADH, IV50: 0.0003-0.0005 mM
L-651,896
-
i.e. 2,3-dihydro-6-[3-(2-hydroxymethyl)-phenyl-2-propenyl]-5-benzofuranol, IC50: 0.0003-0.0004 mM
luteolin
inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.0006 mM
methyl (4-[(5E)-5-(4-methoxybenzylidene)-4-oxo-4,5-dihydro-1,3-thiazol-2-yl]phenoxy)acetate
-
-
mithramycin
-
reduces endogenous 5-lipoxygenase in Mono Mac 6 cell, which blocks GC-boxes in the proximal part of the 5-lipoxygenase gene promoter
MK 886
-
i.e. CAS: 118414-82-7, inhibition of 5-lipoxygenase in prostate cancer cells blocks production of 5-hydroxyeicosatetraenoic acid and induces massive apoptosisin both hormone-responsive and hormone-nonresponsive prostate cancer cells
ML-3000
-
i.e. licofelone, ML-3000 has no effect on 5-LOX product synthesis in whole-blood assay, inhibition of COX pathways does not increase the transformation of arachidonic acid by the 5-LOX pathway
myxochelin A
isolated from extracts of the predatory myxobacterium Pyxidicoccus fallax HKI 727, IC50 values for inhibition of proliferative cells K-562 and HeLa are 0.3052 mM and 0.0039 mM, respectively
myxochelin C
isolated from extracts of the predatory myxobacterium Pyxidicoccus fallax HKI 727, IC50 values for inhibition of proliferative cells K-562 and HeLa are 0.424 mM and 0.0535 mM, respectively
myxochelin D
isolated from extracts of the predatory myxobacterium Pyxidicoccus fallax HKI 727, IC50 values for inhibition of proliferative cells K-562 and HeLa are above 0.5 mM
N-(2,4-dimethylphenyl)-4-[(1E)-3-(2-hydroxy-4-methoxyphenyl)-3-oxoprop-1-en-1-yl]benzamide
-
-
N-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)-1,3-benzodioxole-5-carboxamide
-
-
N-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)cyclopentanecarboxamide
-
-
N-(3-(4-chlorophenyl)-3-phenylpropyl)-3-(3-(1-hydroxyureido)-but-1-yn-1-yl)benzamide
dual 5-LOX/soluble epoxide hydrolase inhibitor
-
N-(furan-2-ylmethyl)-2-(7-methoxy-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl)propanamide
-
-
N-([(5R)-3-[3-fluoro-4-(morpholin-4-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl)-N-hydroxy-2-methylpropanamide
-
-
N-([(5R)-3-[3-fluoro-4-(morpholin-4-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl)-N-hydroxycyclopropanecarboxamide
-
-
N-([4-[(2E)-3-(2,4-dichlorophenyl)prop-2-enoyl]phenyl]carbamoyl)-4-methylbenzenesulfonamide
-
IC50: 0.00045 mM
N-benzyl-4-[(1E)-3-(2-hydroxy-4-methoxyphenyl)-3-oxoprop-1-en-1-yl]benzamide
-
-
N-butyl-5-[[(2,5-dihydroxyphenyl)methyl]amino]-2-hydroxybenzamide
-
5-aminosalicylic acid derivative, additionally inhibits cyclooxygenases Cox-1 and Cox-2
-
N-cyclohexyl-5-[(E)-[(2,5-dihydroxyphenyl)methylidene]amino]-2-hydroxybenzamide
-
5-aminosalicylic acid derivative, additionally inhibits cyclooxygenases Cox-1 and Cox-2
-
N-cyclohexyl-5-[[(2,5-dihydroxyphenyl)methyl]amino]-2-hydroxybenzamide
-
5-aminosalicylic acid derivative, additionally inhibits cyclooxygenases Cox-1 and Cox-2. Compound shows 114% anti-inflammatory activity relative to reference drug indomethacin at 4 h interval
-
N-cyclopentyl-2-[7-(2-methoxyethoxy)-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl]propanamide
-
-
N-dodecyl-4-[(1E)-3-(2-hydroxy-4-methoxyphenyl)-3-oxoprop-1-en-1-yl]benzamide
-
-
N-hexyl-5-[[(2,5-dihydroxyphenyl)methyl]amino]-2-hydroxybenzamide
-
5-aminosalicylic acid derivative, additionally inhibits cyclooxygenases Cox-1 and Cox-2
-
N-methyl-2[4-(2,4,6-trimethylphenyl)phenyl]-propenehydroxamic acid
-
IC50: 0.0005 mM
N-tert-butyl-2-(7-methoxy-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl)propanamide
-
-
naphthalen-1-yl 3,5-dinitrobenzoate
JMC-4, identified from virtual inhibitor screening
NAPQI
compound reacts with catalytically relevant cysteine residues 416 and 418
-
Plumbagin
inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.007 mM
primin
compound reacts with catalytically relevant cysteine residues 416 and 418, inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.0028 mM
-
shikonin
inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.0015 mM
tert-butyl 4-[4-(1-benzyl-1H-indol-3-yl)butanoyl]piperazine-1-carboxylate
38% inhibition at 0.005 mM
tert-butyl 4-[4-(1-benzyl-5-methoxy-2-methyl-1H-indol-3-yl)butanoyl]piperazine-1-carboxylate
51.5% inhibition at 0.005 mM
tert-butyl 4-[4-(1H-indol-3-yl)butanoyl]piperazine-1-carboxylate
84% inhibition at 0.005 mM
tert-butyl 4-[4-(5-methoxy-2-methyl-1H-indol-3-yl)butanoyl]piperazine-1-carboxylate
71% inhibition at 0.005 mM
thymoquinone
compound reacts with catalytically relevant cysteine residues 416 and 418, inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.0015 mM
[1-(2-cyclohexylethyl)-1H-1,2,3-triazol-4-yl]methyl (2E)-3-(3,4-dihydroxyphenyl)prop-2-enoate
compound is equipotent to zileuton. It forms pi-pi interactions with residues His367, Phe421 and coordinates iron
-
[1-(2-[[(2E)-3-(3,4-dihydroxyphenyl)prop-2-enoyl]oxy]ethyl)-1H-1,2,3-triazol-4-yl]methyl (2E)-3-(3,4-dihydroxyphenyl)prop-2-enoate
-
-
[1-(2-[[(2E)-3-phenylprop-2-enoyl]oxy]ethyl)-1H-1,2,3-triazol-4-yl]methyl (2E)-3-(3,4-dihydroxyphenyl)prop-2-enoate
-
-
[1-(2-[[(2E)-3-phenylprop-2-enoyl]oxy]ethyl)-1H-1,2,3-triazol-4-yl]methyl (2E)-3-phenylprop-2-enoate
-
shows less inhibitory activity than the corresponding clusters bearing the caffeic acid moiety
[1-(3-[4-([[(2E)-3-(3,4-dihydroxyphenyl)prop-2-enoyl]oxy]methyl)-1H-1,2,3-triazol-1-yl]-2-[(3-[4-([[(2E)-3-(3,4-dihydroxyphenyl)prop-2-enoyl]oxy]methyl)-1H-1,2,3-triazol-1-yl]-2,2-bis[[4-([[(2E)-3-(3,4-dihydroxyphenyl)prop-2-enoyl]oxy]methyl)-1H-1,2,3-triazol-1-yl]methyl]propoxy)methyl]-2-[[4-([[(2E)-3-(3,4-dihydroxyphenyl)prop-2-enoyl]oxy]methyl)-1H-1,2,3-triazol-1-yl]methyl]propyl)-1H-1,2,3-triazol-4-yl]methyl (2E)-3-(3,4-dihydroxyphenyl)prop-2-enoate
-
incorporation of additional caffeoyl units in hexamer results in less potent inhibition
[1-(3-[4-([[(2E)-3-phenylprop-2-enoyl]oxy]methyl)-1H-1,2,3-triazol-1-yl]-2-[(3-[4-([[(2E)-3-phenylprop-2-enoyl]oxy]methyl)-1H-1,2,3-triazol-1-yl]-2,2-bis[[4-([[(2E)-3-phenylprop-2-enoyl]oxy]methyl)-1H-1,2,3-triazol-1-yl]methyl]propoxy)methyl]-2-[[4-([[(2E)-3-phenylprop-2-enoyl]oxy]methyl)-1H-1,2,3-triazol-1-yl]methyl]propyl)-1H-1,2,3-triazol-4-yl]methyl (2E)-3-phenylprop-2-enoate
-
shows less inhibitory activity than the corresponding clusters bearing the caffeic acid moiety
[2-[(1S,8aR)-2-formyl-5,5,8a-trimethyldecahydronaphthalen-1-yl]ethylidene]propanedial
-
-
[2-[(2-methyl-1H-benzimidazol-1-yl)methyl]phenoxy]acetyl chloride
a BRP-7 derivative
[3-(1-[hydroxy[(3,4,5-trihydroxyphenyl)methyl]amino]ethyl)phenyl](morpholin-4-yl)methanone
-
[3-(1-[hydroxy[(4-hydroxyphenyl)methyl]amino]ethyl)phenyl](morpholin-4-yl)methanone
-
compound reduces the cell viability of renal cancer cells and is more selective toward RCC4 and 786.0 cells deficient for the Von Hippel-Lindau tumor suppressor gene. Compound induces apoptosis in Von Hippel-Lindau-deficient RCC4 cells and may block the autophagic flux in renal cancer cells
-
2-phenylethyl (2E)-3-(2,5-dihydroxyphenyl)prop-2-enoate
inhibits leukotriene biosynthesis in isolated human neutrophils and in whole blood
-
-
0.01 mM inhibits LOX-5 by 41%
4-[5-(1H-indol-3-yl)-3-trifluoromethyl-4,5-dihydropyrazol-1-yl]-benzenesulfonamide
-
0.01 mM inhibits LOX-15 by 31%
-
0.01 mM inhibits LOX-5 by 51%
4-[5-(6-chloro-1H-indol-3-yl)-3-trifluoromethyl-4,5-dihydropyrazol-1-yl]-benzenesulfonamide
-
0.01 mM inhibits LOX-15 by 36%
-
0.01 mM inhibits LOX-5 by 94%
4-[5-(7-chloro-1H-indol-3-yl)-3-trifluoromethyl-4,5-dihydropyrazol-1-yl]-benzenesulfonamide
-
0.01 mM inhibits LOX-15 by 36%
AA-861
compound reacts with catalytically relevant cysteine residues 416 and 418, inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.0082 mM
AA861
-
i.e. 2-(12-hydroxydodeca-5,10-diynyl)-3,5,6-trimethyl-1,4-benzoquinone, IC50: 0.004-0.01 mM
arachidonic acid
-
induces time-dependent enzyme inactivation at concentrations 100fold lower than the Km-value, IC50: 0.00023 mM; substrate inhibition
inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.0014 mM
-
CAS: 66000-40-6; i.e. 3-amino-1-[3-(trifluoromethyl)phenyl]-2-pyrazoline, IC50: 0.013 mM
BWA4C
a direct inhibitor of 5-LO, treatment results not only in a suppression of leukotriene production, but in an almost complete inhibition of enzymatic
BWA4C
inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.00015 mM
IC50 value for inhibition of 5-Lox product synthesis in transfected HEK-293 cells is 0.00099 mM. Compound is a good radical scavenger
caffeic acid phenethyl ester
inhibits leukotriene biosynthesis in isolated human neutrophils and in whole blood
-
induces time-dependent enzyme inactivation at concentrations 100fold lower than the Km-value, IC50: 0.00065 mM; substrate inhibition
embelin
compound reacts with catalytically relevant cysteine residues 416 and 418, inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.0035 mM
ethyl 2-(3-chlorobenzyl)-5-hydroxy-1H-benzo[g]indole-3-carboxylate
-
prevents leukotriene B4 production in pleural exudates of carrageenan-treated rats, associated with reduced severity of pleurisy. Significantly reduces the inflammatory reaction measured as exudate volume (77%), inflammatory cell numbers (40%), and leukotriene B4 levels (49%) in the pleural exudates
glutathione
efficiency of non-redox-type 5-LO inhibitors depends on the presence of glutathione peroxidase activity leading to low hydroperoxide concentration
glutathione
-
efficiency of non-redox-type 5-LO inhibitors depends on the presence of glutathione peroxidase activity leading to low hydroperoxide concentration
glutathione
-
efficiency of non-redox-type 5-LO inhibitors depends on the presence of glutathione peroxidase activity leading to low hydroperoxide concentration
-
i.e. 7-chloro-2-[(4-methoxyphenyl)-methyl]-3-methyl-5-propyl-4-benzofuranol, IC50: 0.0008 mM
MK886
-
specific inhibitor of 5-hydroperoxyeicosatetraenoic acid synthesis by the enzyme
nordihydroguaiaretic acid
redox-type inhibitor, is lodged in the 5-LOX active site, fully exposed by disordering of the helix that caps it in the apo-enzyme
nordihydroguaiaretic acid
-
reduces oxidative damage of erythrocytes in C57BL/6 Trypanosoma cruzi-infected mice but not in C57BL/6 iNOS-/- infected mice
nordihydroguaiaretic acid
-
is more potent inhibitor of 5-lipoxygenase than 1-(benzyloxy)hept-2-yn-4-ol
nordihydroguiaraetic acid
-
IC50 for reaction with linoleic acid: 0.17 mM, IC50 for reaction with arachidonic acid: 0.0365 mM
shogaol
inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.005 mM
U73122
inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.0069 mM
zileuton
-
IC50: 0.0038 mM with recombinant enzyme, IC50: 0.0011 mM with native enzyme
zileuton
IC50 value for inhibition of 5-Lox product synthesis in transfected HEK-293 cells is 0.003 mM. Compound is a good radical scavenger
zileuton
-
reduces exudate formation (77%), cell infiltration (41%), and leukotriene B4 exudate levels (66%)
-
plant extracts with inhibitory activity on arachidonate 5-lipoxygenase, inhibition of the 5-lipoxygenase pathway is considered to be interesting in the treatment of a variety of inflammatory diseases
-
additional information
-
classes of 5-lipoxygenase inhibitors: 1. compounds that inhibit the enzyme via antioxidant mechanism - NGDA, BW755c, AA-861, ICI-207968, and A-53612. High toxicity, unacceptable for clinical development. 2. compounds that interact with the non-heme iron moiety of the enzyme - BW-A4A, and ABT-761 both effective in asthma and zileuton. 3. nonredox competitive inhibitors - ZD-2138 and L-697198
-
additional information
-
plant extracts with inhibitory activity on arachidonate 5-lipoxygenase, inhibition of the 5-lipoxygenase pathway is considered to be interesting in the treatment of a variety of inflammatory diseases.
-
additional information
-
plant extracts with inhibitory activity on arachidonate 5-lipoxygenase, inhibition of the 5-lipoxygenase pathway is considered to be interesting in the treatment of a variety of inflammatory diseases.
-
additional information
-
plant extracts with inhibitory activity on arachidonate 5-lipoxygenase, inhibition of the 5-lipoxygenase pathway is considered to be interesting in the treatment of a variety of inflammatory diseases.
-
additional information
-
classes of 5-lipoxygenase inhibitors: 1. compounds that inhibit the enzyme via antioxidant mechanism - NGDA, BW755c, AA-861, ICI-207968, and A-53612. High toxicity, unacceptable for clinical development. 2. compounds that interact with the non-heme iron moiety of the enzyme - BW-A4A, and ABT-761 both effective in asthma and zileuton. 3. nonredox competitive inhibitors - ZD-2138 and L-697198
-
additional information
-
overview: inhibitors and perspectives for future drug development
-
additional information
-
zinc inhibits leukotriene B4 formation due to a direct or indirect inhibitory effect on 5-lipoxygenase
-
additional information
-
selenium-induced apoptosis in prostate cancer cells may be mediated through inhibition of the activity of arachidonate 5-lipoxygenase. The anti-cancer effects of selenium may be substantially compromised by consumption of high-fat diets rich in arachidonic acid or its precursor fatty acids
-
additional information
-
no inhibition by galanal A, galanal B and 8beta(17)-epoxy-15-hydroxy-12(E)-labden-16-al
-
additional information
-
enzyme activity is inhibited by essential oil from Ballota africana (IC50: 29.99 ppm), methanol extract from Croton sylvaticus (IC50: 25.64 ppm), aqueous extract from Croton sylvaticus (IC50: 60.9 ppm), methanol extract from Melianthus comosus (IC50: 55.05 ppm), aqueous extract from Melianthus comosus (IC50: 13.84 ppm), methanol extract from Pentanisia prunelloides (IC50: 32.7 ppm), and methanol extract from Warburgia salutaris (IC50: 32.11 ppm)
-
additional information
-
isoflavones reduce active state iron to ferrous state and prevent the activation of the resting enzyme, model for the inhibition of lipoxygenase by isoflavones, overview
-
additional information
-
virtual inhibitor screening, structure-function relationship analysis, overview
-
additional information
-
class of dual microsomal PGE2 synthase-1/5-lipoxygenase inhibitors based on the structure of pirinixic acid. Target oriented structural modification of pirinixic acid, particularly R substitution with extended n-alkyl or bulky aryl substituents and concomitant replacement of the 2,3-dimethylaniline by a biphenyl-4-yl-methane-amino residue, results in potent suppression of mPGES-1 and 5-lipoxygenase activity. Is not inhibited by 3-(3-(tert-butylthio)-1-(4-chlorobenzyl)-5-isopropyl-1H-indol-2-yl)-2,2-dimethylpropanoic acid
-
additional information
-
5-lipoxygenase may be inhibited either by the direct interaction with an inhibitor or by the binding of an inhibitor to the 5-lipoxygenase activating protein (FLAP), e.g., the clinically effective MK-0591. Highly potent FLAP inhibitors are 2,2-bisaryl-bicycloheptanes
-
additional information
molecular mechanism of 5-lipoxygenase inhibition by 2-aminothiazoles, overview. ST-1083 and ST-1905, but not the lead compounds, show covalent binding to 5-LO and the potency of ST-1083 and ST-1905, but not of the lead compounds is impaired for 5-LO cysteine mutants. Especially the cysteines 159, 300, 416, and 418, located in the substrate entry channel of 5-LO, are prone to be potential targets for inhibition. The lead compounds show no dependency on thiol level
-
additional information
-
molecular mechanism of 5-lipoxygenase inhibition by 2-aminothiazoles, overview. ST-1083 and ST-1905, but not the lead compounds, show covalent binding to 5-LO and the potency of ST-1083 and ST-1905, but not of the lead compounds is impaired for 5-LO cysteine mutants. Especially the cysteines 159, 300, 416, and 418, located in the substrate entry channel of 5-LO, are prone to be potential targets for inhibition. The lead compounds show no dependency on thiol level
-
additional information
synthesis and evaluation of inhibitors of 5-lipoxygenase catalytic activity based on 2-(3-methylphenyl)propanoic acid and 4-substituted morpholine derivatives, inhibitor molecular docking in the active site of 5-LOX, overview. 2-(3-benzoylphenyl)propanoic acid is an active component of the nonsteroidal antiinflammatory drug ketoprofen
-
additional information
treatement with FLAP inhibitor MK886 does not affect 5-H(p)ETE formation
-
additional information
-
treatement with FLAP inhibitor MK886 does not affect 5-H(p)ETE formation
-
additional information
development of 3,5-dinitrobenzoate-based 5-lipoxygenase inhibitors, structure-activity relationship study, overview
-
additional information
-
development of 3,5-dinitrobenzoate-based 5-lipoxygenase inhibitors, structure-activity relationship study, overview
-
additional information
immobilization of BRP-7 derivatives and pull-down assays, overview
-
additional information
high potency of 4,5-dimethoxy-3-alkyl-1,2-benzoquinones on 5-lipoxygenase inhibition is used for systematic structural optimization through accurate structure-based design of the compounds, improvement of the inhibitory potential in vitro and in vivo, overview. Binding patterns of the quinone- and hydroquinone-based 5-LO inhibitors are analyzed by molecular docking, and determination of the optimal alkyl chain pattern of quinones and corresponding hydroquinones
-
additional information
-
high potency of 4,5-dimethoxy-3-alkyl-1,2-benzoquinones on 5-lipoxygenase inhibition is used for systematic structural optimization through accurate structure-based design of the compounds, improvement of the inhibitory potential in vitro and in vivo, overview. Binding patterns of the quinone- and hydroquinone-based 5-LO inhibitors are analyzed by molecular docking, and determination of the optimal alkyl chain pattern of quinones and corresponding hydroquinones
-
additional information
design, synthesis, and evaluation of 2-phenylthiomethyl-indole derivatives from an ethyl 5-hydroxy-indole-3-carboxylate scaffold as efficient inhibitors of human 5-lipoxygenase, structure-activity relationships, overview. The potency of compounds is closely related to the positioning of the substituents at the phenylthiomethyl ring. The introduction of methyl or chlorine groups in ortho- and ortho/para-position of thiophenol represent the most favorable modifications. Among all tested compounds, ethyl 5-hydroxy-2-(mesitylthiomethyl)-1-methyl-1H-indole-3-carboxylate is the most potent derivative which blocks 5-LO activity in cell-free assays and suppresses 5-LO product synthesis in polymorphonuclear leukocytes. The compounds are not active against 12-LO and 15-LO, EC 1.13.11.31 and EC 1.13.11.33
-
additional information
-
design, synthesis, and evaluation of 2-phenylthiomethyl-indole derivatives from an ethyl 5-hydroxy-indole-3-carboxylate scaffold as efficient inhibitors of human 5-lipoxygenase, structure-activity relationships, overview. The potency of compounds is closely related to the positioning of the substituents at the phenylthiomethyl ring. The introduction of methyl or chlorine groups in ortho- and ortho/para-position of thiophenol represent the most favorable modifications. Among all tested compounds, ethyl 5-hydroxy-2-(mesitylthiomethyl)-1-methyl-1H-indole-3-carboxylate is the most potent derivative which blocks 5-LO activity in cell-free assays and suppresses 5-LO product synthesis in polymorphonuclear leukocytes. The compounds are not active against 12-LO and 15-LO, EC 1.13.11.31 and EC 1.13.11.33
-
additional information
human 5-lipoxygenase (5-LO) is a molecular target of the myxochelins that have antiproliferative effects on K-562 and HeLa cancer cells
-
additional information
-
human 5-lipoxygenase (5-LO) is a molecular target of the myxochelins that have antiproliferative effects on K-562 and HeLa cancer cells
-
additional information
outstanding anti-inflammatory potential of selected Asteraceae species through the potent dual inhibition of cyclooxygenase-1 and 5-lipoxygenase, evaluation of 57 Asteraceae extracts (EtOH:H2O - 7:3 v/v) for in vitro enzyme inhibition activity, e.g. from known anti-inflammatory herbs such as Solidago microglossa, Tithonia diversifolia, Vernonia polyanthes and Viguiera robusta, or food plants or previously uninvestigated species, such a Minasia scapigera, Piptolepis monticola, Prestelia eriopus, Sphagneticola trilobata, Vernonia herbacea, Vernonia platensis, Vernonia rubriramea, and Viguiera trichophylla, chemical profiles, detailed overview
-
additional information
naturally occurring or synthetic anti-inflammatory compounds carrying a Michael acceptor, such as thymoquinone, the paracetamol metabolite NAPQI, the 5-Lox inhibitor AA-861, and bardoxolone methyl (i.e. RTA 402 or CDDO-methyl ester) are direct covalent 5-Lox enzyme inhibitors that target the catalytically relevant cysteines 416 and 418
-
additional information
-
naturally occurring or synthetic anti-inflammatory compounds carrying a Michael acceptor, such as thymoquinone, the paracetamol metabolite NAPQI, the 5-Lox inhibitor AA-861, and bardoxolone methyl (i.e. RTA 402 or CDDO-methyl ester) are direct covalent 5-Lox enzyme inhibitors that target the catalytically relevant cysteines 416 and 418
-
additional information
synthesis of 5-(hydroxamic acid)methyl oxazolidinone derivatives as inhibitors. Increasing alkyl chain length on the hydroxamic acid moiety enhances activity and morpholinyl-containing derivatives are more active than N-acetyl-piperizinyl derivatives. The inhibitory effect of the compounds paralleles their effects in cell-based assays
-
additional information
-
synthesis of 5-(hydroxamic acid)methyl oxazolidinone derivatives as inhibitors. Increasing alkyl chain length on the hydroxamic acid moiety enhances activity and morpholinyl-containing derivatives are more active than N-acetyl-piperizinyl derivatives. The inhibitory effect of the compounds paralleles their effects in cell-based assays
-
additional information
-
plant extracts with inhibitory activity on arachidonate 5-lipoxygenase, inhibition of the 5-lipoxygenase pathway is considered to be interesting in the treatment of a variety of inflammatory diseases.
-
additional information
-
95% ethanol extract of Glycine tomentella inhibits tilapia thrombocyte 5-LOX with IC50 of 0.00043 mg/ml
-
additional information
-
classes of 5-lipoxygenase inhibitors: 1. compounds that inhibit the enzyme via antioxidant mechanism - NGDA, BW755c, AA-861, ICI-207968, and A-53612. High toxicity, unacceptable for clinical development. 2. compounds that interact with the non-heme iron moiety of the enzyme - BW-A4A, and ABT-761 both effective in asthma and zileuton. 3. nonredox competitive inhibitors - ZD-2138 and L-697198
-
additional information
-
plant extracts with inhibitory activity on arachidonate 5-lipoxygenase, inhibition of the 5-lipoxygenase pathway is considered to be interesting in the treatment of a variety of inflammatory diseases.
-
additional information
inhibitor design, synthesis, biological evaluation, and molecular modeling, overview
-
additional information
-
no inhibition by 1-linoleoyl lysophosphatidylcholine and (13S)-hydroperoxy-9,11-octadecadienoyl lysophosphatidylcholine
-
additional information
-
[(hept-2-yn-1-ylsulfanyl)methyl]benzene is no inhibitor, there are no strong interactions to stabilize the compound in the 5-lipoxygenase active site
-
additional information
-
class of 1-(4-methanesulfonylphenyl and 4-aminosulfonylphenyl)-5-[4-(1-difluoromethyl-1,2-dihydropyrid-2-one)]-3-trifluoromethyl-1H-pyrazoles as potent dual 5-LOX and COX-1/COX-2 isozyme inhibitors of inflammation
-
additional information
-
classes of 5-lipoxygenase inhibitors: 1. compounds that inhibit the enzyme via antioxidant mechanism - NGDA, BW755c, AA-861, ICI-207968, and A-53612. High toxicity, unacceptable for clinical development. 2. compounds that interact with the non-heme iron moiety of the enzyme - BW-A4A, and ABT-761 both effective in asthma and zileuton. 3. nonredox competitive inhibitors - ZD-2138 and L-697198
-
additional information
-
plant extracts with inhibitory activity on arachidonate 5-lipoxygenase, inhibition of the 5-lipoxygenase pathway is considered to be interesting in the treatment of a variety of inflammatory diseases.
-