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(7E,9E,11Z,14Z)-(5S,6S)-5,6-epoxyicosa-7,9,11,14-tetraenoate + H2O
(6Z,8E,10E,14Z)-(5S,12R)-5,12-dihydroxyicosa-6,8,10,14-tetraenoate
Ala-4-nitroanilide + H2O
Ala + 4-nitroaniline
-
-
-
-
?
Arg-Ala-Arg + H2O
?
-
-
-
?
Arg-Ser-Arg + H2O
?
-
-
-
?
L-Ala-4-nitroanilide + H2O
L-Ala + 4-nitroaniline
L-Ala-p-nitroanilide + H2O
L-Ala + p-nitroaniline
-
-
-
?
L-alanine 2-naphthylamide + H2O
L-alanine + 2-naphthylamine
-
-
-
-
?
L-alanine-4-nitroanilide + H2O
L-alanine + 4-nitroaniline
L-alanine-7-amido-4-methylcoumarin + H2O
L-alanine + 7-amino-4-methylcoumarin
-
-
-
-
?
L-Arg-L-Ala-L-Arg + H2O
?
-
bi-functional enzyme that also exhibits aminopeptidase activity with a preference over arginyl tripeptides
-
-
?
L-Arg-p-nitroanilide + H2O
L-Arg + p-nitroaniline
-
-
-
?
L-arginine + H2O
?
-
the best proteinogenic amino acid recognized by the enzyme is L-arginine
-
-
?
L-arginine 2-naphthylamide + H2O
L-arginine + 2-naphthylamine
-
-
-
-
?
L-arginine-4-nitroanilide + H2O
L-arginine + 4-nitroaniline
-
-
-
-
?
L-arginine-7-amido-4-methylcoumarin + H2O
L-arginine + 7-amino-4-methylcoumarin
-
-
-
-
?
L-arginine-7-amido-4-methylcoumarine + H2O
L-arginine + 4-methylcoumarin-7-amine
an artificial substrate
-
-
?
L-glutamate-7-amido-4-methylcoumarin + H2O
L-glutamate + 7-amino-4-methylcoumarin
-
-
-
-
?
L-histidine-7-amido-4-methylcoumarin + H2O
L-histidine + 7-amino-4-methylcoumarin
-
-
-
-
?
L-isoleucine 2-naphthylamide + H2O
L-isoleucine + 2-naphthylamine
-
-
-
-
?
L-leucine 2-naphthylamide + H2O
L-leucine + 2-naphthylamine
-
-
-
-
?
L-leucine-4-nitroanilide + H2O
L-leucine + 4-nitroaniline
L-leucine-7-amido-4-methylcoumarin + H2O
L-leucine + 7-amino-4-methylcoumarin
-
-
-
-
?
L-lysine-7-amido-4-methylcoumarin + H2O
L-lysine + 7-amino-4-methylcoumarin
-
-
-
-
?
L-methionine 2-naphthylamide + H2O
L-methionine + 2-naphthylamine
-
-
-
-
?
L-methionine-7-amido-4-methylcoumarin + H2O
L-methionine + 7-amino-4-methylcoumarin
-
-
-
-
?
L-phenylalanine-7-amido-4-methylcoumarin + H2O
L-phenylalanine + 7-amino-4-methylcoumarin
-
-
-
-
?
L-Pro-Gly-L-Pro + H2O
?
-
-
-
?
L-proline-7-amido-4-methylcoumarin + H2O
L-proline + 7-amino-4-methylcoumarin
-
-
-
-
?
L-serine-7-amido-4-methylcoumarin + H2O
L-serine + 7-amino-4-methylcoumarin
-
-
-
-
?
L-tyrosine-7-amido-4-methylcoumarin + H2O
L-tyrosine + 7-amino-4-methylcoumarin
-
-
-
-
?
L-Val-4-nitroanilide + H2O
L-Val + 4-nitroaniline
-
-
-
?
L-valine 2-naphthylamide + H2O
L-valine + 2-naphthylamine
-
-
-
-
?
leukotriene A4 + H2O
(5S,6S)-dihydroxy-7,9-trans-11,14-cis-eicosatetraenoic acid
-
-
i.e. DHETE
?
leukotriene A4 + H2O
(5S,6S)-dihydroxy-7,9-trans-11,14-cis-eicosatetraenoic acid + leukotriene B4 + (5S,12R)-dihydroxy-6,10-trans-8,14,cis-eicosatetraenoic acid
-
-
when large amounts of enzyme are incubated with leukotriene A4: 72% (5S,6S)-dihydroxy-7,9-trans-11,14-cis-eicosatetraenoic acid, 18% leukotriene B4 and 10% (5S,12R)-dihydroxy-6,10-trans-8,14,cis-eicosatetraenoic acid
?
leukotriene A4 + H2O
leukotriene B4
leukotriene A4 + H2O
leukotriene B4 + (5S,12R)-dihydroxy-6,10-trans-8,14,cis-eicosatetraenoic acid
-
-
90% leukotriene B4 and 10% (5S,12R)-dihydroxy-6,10-trans-8,14,cis-eicosatetraenoic acid
?
leukotriene A4 + H2O
leukotriene B4 + 5(S),12R-dihydroxy-6,10-trans-8,14-ciseicosatetraenoic acid
-
product ratio 9:1
-
?
lysine-4-nitroanilide + H2O
lysine + 4-nitroaniline
-
-
-
-
?
proline-4-nitroanilide + H2O
proline + 4-nitroaniline
-
-
-
-
?
proline-glycine-proline + H2O
?
PGP
-
-
?
additional information
?
-
(7E,9E,11Z,14Z)-(5S,6S)-5,6-epoxyicosa-7,9,11,14-tetraenoate + H2O
(6Z,8E,10E,14Z)-(5S,12R)-5,12-dihydroxyicosa-6,8,10,14-tetraenoate
-
-
-
-
?
(7E,9E,11Z,14Z)-(5S,6S)-5,6-epoxyicosa-7,9,11,14-tetraenoate + H2O
(6Z,8E,10E,14Z)-(5S,12R)-5,12-dihydroxyicosa-6,8,10,14-tetraenoate
-
-
-
-
?
(7E,9E,11Z,14Z)-(5S,6S)-5,6-epoxyicosa-7,9,11,14-tetraenoate + H2O
(6Z,8E,10E,14Z)-(5S,12R)-5,12-dihydroxyicosa-6,8,10,14-tetraenoate
-
-
-
?
(7E,9E,11Z,14Z)-(5S,6S)-5,6-epoxyicosa-7,9,11,14-tetraenoate + H2O
(6Z,8E,10E,14Z)-(5S,12R)-5,12-dihydroxyicosa-6,8,10,14-tetraenoate
-
substrate for the epoxide hydrolase reaction, in addition LTA4H shows a peptidase activity
-
-
?
(7E,9E,11Z,14Z)-(5S,6S)-5,6-epoxyicosa-7,9,11,14-tetraenoate + H2O
(6Z,8E,10E,14Z)-(5S,12R)-5,12-dihydroxyicosa-6,8,10,14-tetraenoate
-
-
-
-
?
(7E,9E,11Z,14Z)-(5S,6S)-5,6-epoxyicosa-7,9,11,14-tetraenoate + H2O
(6Z,8E,10E,14Z)-(5S,12R)-5,12-dihydroxyicosa-6,8,10,14-tetraenoate
-
substrate for epoxide hydrolase activity
-
-
?
L-Ala-4-nitroanilide + H2O
L-Ala + 4-nitroaniline
-
-
-
?
L-Ala-4-nitroanilide + H2O
L-Ala + 4-nitroaniline
-
aminopeptidase activity
-
-
?
L-alanine-4-nitroanilide + H2O
L-alanine + 4-nitroaniline
-
-
-
?
L-alanine-4-nitroanilide + H2O
L-alanine + 4-nitroaniline
-
-
-
-
?
L-alanine-4-nitroanilide + H2O
L-alanine + 4-nitroaniline
-
-
-
?
L-leucine-4-nitroanilide + H2O
L-leucine + 4-nitroaniline
-
-
-
-
?
L-leucine-4-nitroanilide + H2O
L-leucine + 4-nitroaniline
-
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
i.e. LTB4, a potent inflammatory mediator originating from membrane-derived arachidonic acid
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
i.e. 5(S)-trans-5,6-oxido-7,9-trans-11,14-cis-eicosatetraenoic acid
-
?
leukotriene A4 + H2O
leukotriene B4
-
model for the binding of leukotriene A4 to the active site
mutants of Tyr378 are able to generate, not only leukotriene B4, but also (5S,12R)-dihydroxy-6,10-trans-8,14-cis-eicosatetraenoic acid, in a yield of about 20-30%
?
leukotriene A4 + H2O
leukotriene B4
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
leukotriene A4 hydrolase catalyzes the final step in the synthesis of leukotriene B4, a potent chemoattractant and proinflammatory eicosanoid. LTB4 functions as a macrophage chemoattractant in the zebrafish, injection into the hindbrain ventricle of wild-type arvae induces rapid recruitment of macrophages
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
696628, 696629, 696636, 696688, 697856, 698172, 699434, 707687, 707704, 708038, 708077, 708181, 708250, 731112, 731116, 731439, 731445, 731746, 731871, 732701 -
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
i.e. LTB4, a powerful proinflammatory agent
-
?
leukotriene A4 + H2O
leukotriene B4
-
model for the binding of leukotriene A4 to the active site
mutants of Tyr378 are able to generate, not only leukotriene B4, but also (5S,12R)-dihydroxy-6,10-trans-8,14-cis-eicosatetraenoic acid, in a yield of about 20-30%
?
leukotriene A4 + H2O
leukotriene B4
-
one of the physiologically important processes in the arachidonic acid biosynthetic pathway, leukotriene B4 is a proinflammatory mediator which stimulates adhesion of circulating neutrophils to vascular endothelium and directs their migration towards sites of inflammation
-
?
leukotriene A4 + H2O
leukotriene B4
-
central enzyme in leukotriene B4 formation, it is likely to be involved in transcellular leukotriene formation
-
?
leukotriene A4 + H2O
leukotriene B4
-
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
-
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
-
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
-
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
-
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
-
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
-
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
-
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
-
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
-
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
-
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
-
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
-
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
-
biosynthesis of leukotriene B4
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
-
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
-
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
-
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
-
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
-
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
-
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
-
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
-
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
-
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
-
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
-
leukotriene A4 hydrolase catalyzes the final step in the synthesis of leukotriene B4, a potent chemoattractant and proinflammatory eicosanoid
-
-
?
leukotriene A4 + H2O
leukotriene B4
LTA4
LTB4
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
LTB4 is an endogenous itch mediator in the skin and is involved in the pruritus response in allergic reactions
-
?
leukotriene A4 + H2O
leukotriene B4
-
model for the binding of leukotriene A4 to the active site
mutants of Tyr378 are able to generate, not only leukotriene B4, but also (5S,12R)-dihydroxy-6,10-trans-8,14-cis-eicosatetraenoic acid, in a yield of about 20-30%
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
-
-
?
leukotriene A4 + H2O
leukotriene B4
-
highly specific
-
?
leukotriene A4 + H2O
leukotriene B4
-
model for the binding of leukotriene A4 to the active site
mutants of Tyr378 are able to generate, not only leukotriene B4, but also (5S,12R)-dihydroxy-6,10-trans-8,14-cis-eicosatetraenoic acid, in a yield of about 20-30%
?
leukotriene A4 + H2O
leukotriene B4
-
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
-
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
-
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
-
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
-
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
-
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
biosynthesis of leukotriene B4
-
?
leukotriene A4 + H2O
leukotriene B4
-
model for the binding of leukotriene A4 to the active site
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-
?
leukotriene A4 + H2O
leukotriene B4
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-
-
?
leukotriene A4 + H2O
leukotriene B4
-
model for the binding of leukotriene A4 to the active site
-
?
leukotriene A5 + H2O
?
-
i.e. 5(S)-trans-5,6-oxido-7,9-trans-11,14,17-cis-eicosatetraenoic acid
-
-
?
leukotriene A5 + H2O
?
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i.e. 5(S)-trans-5,6-oxido-7,9-trans-11,14,17-cis-eicosatetraenoic acid
-
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?
additional information
?
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additional information
?
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additional information
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LTA4H is a zinc metalloprotease
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-
?
additional information
?
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?
additional information
?
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the aminopeptidase activity accepts a variety of substrates and certain arginyl di- and tri-peptides as well as p-nitroanilide derivates of Ala and Arg
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?
additional information
?
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additional information
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additional information
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additional information
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additional information
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additional information
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additional information
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additional information
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additional information
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additional information
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additional information
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additional information
?
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additional information
?
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neutrophil LTA4 hydrolase also converts LTA5 to LTB5, less efficiently than LTA4 to LTB4
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?
additional information
?
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either glutamic or glutamine moiety at amino acid 297 is required for full LTA4 hydrolase activity, free carboxylic acid of glutamic acid is essential for aminopeptidase
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?
additional information
?
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not: glycine-4-nitroanilide, glutamyl-4-nitroanilide, valine-4-nitroanilide
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?
additional information
?
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the aminopeptidase activity accepts a variety of substrates and certain arginyl di- and tri-peptides as well as p-nitroanilide derivates of Ala and Arg
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?
additional information
?
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possible proteolytic function of the enzyme may be limited to the extracellular space
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-
?
additional information
?
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LTA4H is a zinc metalloprotease
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-
?
additional information
?
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no activity with L-Asn, L-Asp, L-Glu, Gly, L-Ile, L-Thr, L-Trp, L-Val, as well as D-amino acids
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-
?
additional information
?
-
proline-glycine-proline (PGP) is a substrate for the enzyme's aminopeptidase (AP) activity
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-
?
additional information
?
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substrates docking and molecular dynamics simulations, interaction analysis. The binding cavity of LTA4H is formed by H299, H295, E318, and Zn2+. Residues R563 and K565 in the C-terminal domain of LTA4H are key residues involved in carboxylate recognition from endogenous substrates of the enzyme
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-
?
additional information
?
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the aminopeptidase binding site shares a similar structure to LTA4H at its ligand binding sites
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?
additional information
?
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the aminopeptidase binding site shares a similar structure to LTA4H at its ligand binding sites
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?
additional information
?
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?
additional information
?
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?
additional information
?
-
-
the aminopeptidase activity accepts a variety of substrates and certain arginyl di- and tri-peptides as well as p-nitroanilide derivates of Ala and Arg
-
-
?
additional information
?
-
the aminopeptidase binding site shares a similar structure to LTA4H at its ligand binding sites
-
-
?
additional information
?
-
-
the aminopeptidase binding site shares a similar structure to LTA4H at its ligand binding sites
-
-
?
additional information
?
-
-
the aminopeptidase activity accepts a variety of substrates and certain arginyl di- and tri-peptides as well as p-nitroanilide derivates of Ala and Arg
-
-
?
additional information
?
-
-
LTA4H is a zinc metalloprotease
-
-
?
additional information
?
-
proline-glycine-proline (PGP) is a substrate for the enzyme's aminopeptidase (AP) activity
-
-
?
additional information
?
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?
additional information
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additional information
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additional information
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additional information
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additional information
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(1-[2-[4-(benzooxazol-2-yloxy)phenoxy]ethyl]piperidin-4-yl)methanol
-
-
(1-[2-[4-(benzothiazol-2-yloxy)phenoxy]ethyl]piperidin-4-yl)-carbamic acid tert-butyl ester
-
-
(1-[2-[4-(benzothiazol-2-yloxy)phenoxy]ethyl]piperidin-4-yl)-methanol
-
-
(2R)-2-([4-[4-(thiophen-2-yl)benzyl]phenoxy]methyl)piperidine
-
-
(2R)-2-([4-[4-(thiophen-3-yl)benzyl]phenoxy]methyl)piperidine
-
-
(2R)-2-([4-[4-(thiophen-3-yl)phenoxy]phenoxy]methyl)piperidine
-
-
(2R)-2-[(4-phenoxyphenoxy)methyl]piperidine
-
-
(2R)-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]-3-[(4-nitrobenzyl)sulfanyl]propanoic acid
-
-
(2R)-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]-3-[(4-phenoxybenzyl)sulfanyl]propanoic acid
-
-
(2R)-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]-3-[(4-propylbenzyl)sulfanyl]propanoic acid
-
-
(2R)-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]-3-[[4-(trifluoromethoxy)benzyl]sulfanyl]propanoic acid
-
-
(2R)-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]-3-[[4-(trifluoromethyl)benzyl]sulfanyl]propanoic acid
-
-
(2R)-2-[[4-(4-chlorobenzyl)phenoxy]methyl]piperidine
-
-
(2R)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]-1-(1,2,4-oxadiazol-2(3H)-ylmethyl)piperidine
-
-
(2R)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]piperidine
-
-
(2R)-2-[[4-(4-fluorophenoxy)phenoxy]methyl]piperidine
-
-
(2R)-2-[[4-(biphenyl-4-yloxy)phenoxy]methyl]piperidine
-
-
(2R)-3-(benzylsulfanyl)-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
-
-
(2R)-3-[(4-bromobenzyl)sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
-
-
(2R)-3-[(4-chlorobenzyl)sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
-
-
(2R)-3-[(4-cyanobenzyl)sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
-
-
(2R)-3-[(4-ethoxybenzyl)sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
-
-
(2R)-3-[(4-ethylbenzyl)sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
-
-
(2R)-3-[(4-fluorobenzyl)sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
-
-
(2R)-3-[(4-iodobenzyl)sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
-
-
(2R)-3-[(4-methoxybenzyl)sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
-
-
(2R)-3-[(4-methylbenzyl)sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
-
-
(2R)-3-[(biphenyl-4-ylmethyl)sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
-
-
(2R)-3-[[3-(dimethylamino)benzyl]sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
-
-
(2R)-3-[[4-(1-methylethyl)benzyl]sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
-
-
(2R)-3-[[4-(dimethylamino)benzyl]sulfanyl]-2-[(3-sulfanylbutanoyl)amino]propanoic acid
-
-
(2R)-3-[[4-(dimethylamino)benzyl]sulfanyl]-2-[(3-sulfanylpropanoyl)amino]propanoic acid
-
-
(2R)-3-[[4-(dimethylamino)benzyl]sulfanyl]-2-[(4-sulfanylbutanoyl)amino]propanoic acid
-
-
(2R)-3-[[4-(dimethylamino)benzyl]sulfanyl]-2-[(sulfanylacetyl)amino]propanoic acid
-
-
(2R)-3-[[4-(dimethylamino)benzyl]sulfanyl]-2-[[(2R)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
-
-
(2R)-3-[[4-(dimethylamino)benzyl]sulfanyl]-2-[[(2R)-2-sulfanylpropanoyl]amino]propanoic acid
-
-
(2R)-3-[[4-(dimethylamino)benzyl]sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
-
SA6541
(2R)-3-[[4-(dimethylamino)benzyl]sulfanyl]-2-[[(2S)-2-sulfanylpropanoyl]amino]propanoic acid
-
-
(2R)-3-[[4-(methoxysulfinyl)benzyl]sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
-
-
(2R)-3-[[4-(methylsulfanyl)benzyl]sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
-
-
(2S)-1-[(2R)-2-methyl-3-sulfanylpropanoyl]pyrrolidine-2-carboxylic acid
-
5% inhibition at 1 mM
(2S)-1-[(2R)-2-sulfanylpropanoyl]pyrrolidine-2-carboxylic acid
-
-
(2S)-2-([4-[4-(trifluoromethyl)phenoxy]phenoxy]methyl)piperidine
-
-
(2S)-2-amino-3-[4-(benzyloxy)phenyl]propane-1-thiol
-
it are about 50 derivates and related structures synthesized and assayed their inhibition of enzyme catalyzes hxdrolysis of L-alanine-4-nitroanilide
(2S)-2-amino-5-oxo-5-[(4-phenoxyphenyl)amino]-1-pentanesulfonic acid
-
(2S)-2-amino-N-[4-(phenylmethoxy)phenyl]-3-[4-(1H-imidazole)]propanamide dihydrochloride
-
(2S)-2-amino-N-[4-(phenylmethoxy)phenyl]-propanamide hydrochloride
-
(2S)-2-amino-N-[4-(phenylmethoxy)phenyl]benzenepropanamide hydrochloride
-
(2S)-2-[(4-benzylphenoxy)methyl]piperidine
-
-
(2S)-2-[(4-phenoxyphenoxy)methyl]piperidine
-
-
(2S)-2-[[4-(4-chlorobenzyl)phenoxy]methyl]piperidine
-
-
(2S)-2-[[4-(biphenyl-4-yloxy)phenoxy]methyl]piperidine
-
-
(2S)-3-[[4-(dimethylamino)benzyl]sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
-
-
(2S)-4-[[4-(dimethylamino)benzyl]sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]butanoic acid
-
-
(2S)-N-[4-(phenylmethoxy)phenyl]-2-pyrrolidinecarboxamide hydrochloride
-
(2S,3S)-2-amino-3-methyl-N-[4-(phenylmethoxy)-phenyl]pentanamide
-
(2S,4R)-3-(2-methyl-3-sulfanylpropanoyl)-2-naphthalen-1-yl-1,3-thiazolidine-4-carboxylic acid
-
58% inhibition at 1 mM
(2S,4S)-1-[(2S)-2-methyl-3-sulfanylpropanoyl]-4-[(2-phenylethyl)sulfanyl]pyrrolidine-2-carboxylic acid
-
-
(2S,4S)-1-[(2S)-2-methyl-3-sulfanylpropanoyl]-4-[(3-phenylpropyl)sulfanyl]pyrrolidine-2-carboxylic acid
-
-
(2S,4S)-1-[(2S)-2-methyl-3-sulfanylpropanoyl]-4-[(naphthalen-1-ylmethyl)sulfanyl]pyrrolidine-2-carboxylic acid
-
-
(2S,4S)-1-[(2S)-2-methyl-3-sulfanylpropanoyl]-4-[(naphthalen-2-ylmethyl)sulfanyl]pyrrolidine-2-carboxylic acid
-
-
(2S,4S)-4-(benzylsulfanyl)-1-[(2S)-2-methyl-3-sulfanylpropanoyl]pyrrolidine-2-carboxylic acid
-
-
(2S,4S)-4-[(2-methylbenzyl)sulfanyl]-1-[(2S)-2-methyl-3-sulfanylpropanoyl]pyrrolidine-2-carboxylic acid
-
-
(2S,4S)-4-[(3-methylbenzyl)sulfanyl]-1-[(2S)-2-methyl-3-sulfanylpropanoyl]pyrrolidine-2-carboxylic acid
-
-
(2S,4S)-4-[[4-(methylsulfanyl)benzyl]sulfanyl]-1-[(2S)-2-methyl-3-sulfanylpropanoyl]pyrrolidine-2-carboxylic acid
-
-
(4-fluorophenyl)(pyridin-4-yl)methanone
-
(4R)-2-furan-2-yl-3-[(2S)-2-methyl-3-sulfanylpropanoyl]-1,3-thiazolidine-4-carboxylic acid
-
36% inhibition at 1 mM
(4R)-3-[(2R)-2-methyl-3-sulfanylpropanoyl]-1,3-thiazolidine-4-carboxylic acid
-
18% inhibition at 1 mM
(4R)-3-[(2S)-2-methyl-3-sulfanylpropanoyl]-1,3-thiazolidine-4-carboxylic acid
-
58% inhibition at 1 mM
(4R)-3-[(2S)-2-methyl-3-sulfanylpropanoyl]-2-pyridin-4-yl-1,3-thiazolidine-4-carboxylic acid
-
25% inhibition at 1 mM
(4R)-3-[(2S)-2-methyl-3-sulfanylpropanoyl]-2-thiophen-2-yl-1,3-thiazolidine-4-carboxylic acid
-
14% inhibition at 1 mM
(4R)-4-[[4-(1-methylethyl)benzyl]sulfanyl]-1-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-proline
-
-
(4R)-N-mercaptoacylthiazolidine-4-carboxylic acid
-
-
-
(4S)-4,5-diamino-N-(4-phenoxyphenyl)pentanamide
-
(4S)-4-([2-[4-(1-methylethyl)phenyl]ethyl]sulfanyl)-1-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-proline
-
-
(4S)-4-([3-[4-(1-methylethyl)phenyl]propyl]sulfanyl)-1-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-proline
-
-
(4S)-4-amino-4-(2-(1,3,4-triazolyl))-N-(4-phenoxyphenyl)butanamide trifluoroacetate
-
(4S)-4-amino-5-(1-phthalimido)-N-(4-phenoxyphenyl)pentanamide trifluoroacetate
-
(4S)-4-amino-5-(1H-pyrrol-1-yl)-N-(4-phenoxyphenyl)pentanamide bistrifluoroacetate
-
(4S)-4-amino-5-(2-thio-5-amino-1,3,4-thiadiazol-2-yl)-N-(4-phenoxyphenyl)pentanamide bistrifluoroacetate
-
(4S)-4-amino-5-hydroxy-N-(4-phenoxyphenyl)pentanamide
(4S)-4-amino-5-methoxy-N-(4-phenoxyphenyl)-pentanamide
-
(4S)-4-[(4-cyclohexylbenzyl)sulfanyl]-1-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-proline
-
-
(4S)-4-[(4-tert-butylbenzyl)sulfanyl]-1-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-proline
-
-
(4S)-4-[[4-(1-methylethyl)benzyl]sulfanyl]-1-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-proline
-
-
(R)-2-(4-benzylphenoxymethyl)pyrrolidine
-
(R)-2-[4-(4-chlorophenoxy)phenoxymethyl]pyrrolidine
-
(R)-2-[4-(4-thiophene-3-ylbenzoyl)phenoxymethyl]pyrrolidine
-
(R)-5-(1,2-dithiolan-3-yl) pentanoic acid
i.e. alpha-lipoic acid, inhibits both activities of the enzyme at concentrations lower than 0.010 mM. The carboxylate group of alpha lipoic acid situates at 3 A from important residues R563 and K565 in the catalytic pocket of the protein, suggesting that alpha lipoic acid participates in electrostatic interactions with these residues
(S)-2-((2S,3R)-3-amino-2-hydroxy-4-phenylbutanamido)-4-methylpentanoic acid
(S)-2-((S)-2-(2-(((R)-1-amino-2-phenylethyl)(hydroxy)phosphoryl)acetamido)-3-phenylpropanamido)-3-phenylpropanoic acid
RB3041, tight slow-binding LTA4H inhibitor
(S)-2-((S)-2-(2-(((R)-1-aminoethyl)(hydroxy)phosphoryl)acetamido)-3-(biphenyl-4-yl)propanamido)propanoic acid
RB3040, tight slow-binding LTA4H inhibitor
1'-[2-[4-(benzothiazol-2-yloxy)phenoxy]ethyl][1,4']bipiperidinyl-2-one
-
-
1,2-dihydroxybisabola-3,10-diene
-
1-(1-[2-[4-(1,3-benzothiazol-2-yloxy)phenoxy]ethyl]piperidin-4-yl)pyrrolidin-2-one
1-(1-[2-[4-(benzothiazol-2-yloxy)phenoxy]ethyl]piperidin-4-yl)pyrrolidin-2-one
-
-
1-(1-[2-[4-(benzothiazol-2-yloxy)phenyl]ethyl]piperidin-4-yl)pyrrolidin-2-one
-
-
1-(1-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenoxy]ethyl]piperidin-4-yl)pyrrolidin-2-one
-
-
1-(1-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenyl]ethyl]piperidin-4-yl)pyrrolidin-2-one
-
-
1-(1-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)pyrrolidin-2-one
1-(1-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)pyrrolidin-2-one
1-(2,2'-bithiophen-5-yl)methanamine
-
1-(2-(4-(2-(trifluoromethyl)phenoxy)phenoxy)ethyl)pyrrolidine
-
dual target inhibitor against cyclooxygenase COX-2 and leukotriene A4 hydrolyase in the enzyme assays and the human whole blood assay with IC50 values in the micromolar to submicromolar range. Inhibitor shows good selectivity for COX-2 over COX-1
1-(2-(4-(2-nitrophenoxy)phenoxy)ethyl)pyrrolidine
-
dual target inhibitor against cyclooxygenase COX-2 and leukotriene A4 hydrolyase in the enzyme assays and the human whole blood assay with IC50 values in the micromolar to submicromolar range. Inhibitor shows good selectivity for COX-2 over COX-1
1-(2-(4-(4-chlorophenoxy)phenoxy)ethyl)pyrrolidine
-
-
1-(2-(4-(4-fluorophenoxy)phenoxy)ethyl)pyrrolidine
-
-
1-(2-(4-(4-nitrophenoxy)phenoxy)ethyl)pyrrolidine
-
-
1-(2-(4-phenoxyphenoxy)ethyl)pyrrolidine
-
i.e. nimesulide
1-(3,4-dihydro-2H-1,5-benzodioxepin-7-yl)-2-[[4-(furan-2-yl)-5-hydroxy-4H-1,2,4-triazol-3-yl]sulfanyl]ethanone
-
compound identified by pharmacophore modeling, binds both human leukotriene hydrolase hLTA4H and the human leukotriene C4 synthase hLTC4S with good binding characteristics
1-(5-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenoxy]ethyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
-
-
1-(5-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenyl]ethyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
-
-
1-(5-[[5-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
1-(5-[[5-([1,3]thiazolo[4,5-c]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
1-(5-[[5-([1,3]thiazolo[5,4-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
1-(5-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
1-(5-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
1-(5-[[6-([1,3]thiazolo[4,5-c]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
1-(5-[[6-([1,3]thiazolo[5,4-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
1-([4-[(1,3-benzothiazol-2-yl)oxy]phenyl]methyl)piperidine-4-carboxylic acid
i.e. JNJ-26993135
1-benzyl-3-[(4-benzylphenoxy)methyl]piperazine
-
-
1-chloro-2,4-dinitrobenzene
-
weak
1-[1-[4-(benzothiazol-2-yloxy)benzyl]piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)benzyl]piperidin-4-yl]pyrrolidin-2-one
-
-
1-[2-(1H-indol-5-yloxy)ethyl]piperidine-4-carboxylic acid
-
1-[2-[4-(benzooxazol-2-yloxy)phenoxy]ethyl]-4-phenylpiperidin-4-ol
-
-
1-[2-[4-(benzooxazol-2-yloxy)phenoxy]ethyl]piperidin-4-ol
-
-
1-[2-[4-(benzothiazol-2-yloxy)phenoxy]ethyl]-4-phenylpiperidin-4-ol
-
-
1-[2-[4-(benzothiazol-2-yloxy)phenoxy]ethyl]piperidin-4-ol
-
-
1-[2-[4-(benzothiazol-2-yloxy)phenoxy]ethyl]piperidin-4-ylamine
-
-
1-[2-[4-(benzothiazol-2-yloxy)phenoxy]ethyl]piperidine-4-carboxylic acid amide
-
-
1-[2-[4-(benzothiazol-2-yloxy)phenyl]ethyl]piperidin-4-ol
-
-
1-[2-[4-(benzothiazol-2-yloxy)phenyl]ethyl]piperidine-4-carboxylic acid amide
-
-
1-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenoxy]ethyl]piperidine-4-carboxamide
-
-
1-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenyl]ethyl]piperidine-4-carboxamide
-
-
1-[4-(1,3-benzothiazol-2-yloxy)benzyl]piperidine-4-carboxamide
-
-
1-[4-(1,3-benzothiazol-2-yloxy)benzyl]piperidine-4-carboxylic acid
1-[4-(benzothiazol-2-yloxy)benzyl]piperidin-4-ol
-
-
1-[4-(benzothiazol-2-yloxy)benzyl]piperidine-4-carboxylic acid
-
-
1-[4-(benzothiazol-2-yloxy)benzyl]piperidine-4-carboxylic acid amide
-
-
1-[4-(thiophen-2-yl)phenyl]methanamine
-
1-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)benzyl]piperidine-4-carboxamide
-
-
1-[4-([1,3]thiazolo[5,4-b]pyridin-2-yloxy)benzyl]piperidine-4-carboxamide
-
-
1-[5-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenoxy]ethyl]hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl]ethanone
-
-
1-[5-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenyl]ethyl]hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl]ethanone
-
-
1-[5-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)benzyl]-2,5-diazabicyclo[2.2.1]hept-2-yl]ethanone
-
-
1-[5-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)benzyl]hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl]ethanone
-
-
1-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]piperidine-4-carboxylic acid
1-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]piperidine-4-carboxylic acid
2,3-Butanedione
-
preincubation with bestatin partially protects enzyme from inactivation
2,4-dimethyl-N-[[2-(thiophen-2-yl)-1,3-thiazol-4-yl]methyl]-1,3-thiazole-5-sulfonamide
-
compound identified by pharmacophore modeling, binds both human leukotriene hydrolase hLTA4H and the human leukotriene C4 synthase hLTC4S with good binding characteristics
2-(4-piperidin-1-ylmethylphenoxy)benzothiazole
-
-
2-(5-(2-(4-phenoxyphenoxy)ethoxy)-1H-indol-3-yl)ethanaminium chloride
-
-
2-(5-(3-phenoxybenzyloxy)-1H-indol-3-yl)ethanaminium chloride
-
-
2-(5-(4-phenylbenzyloxy)-1H-indol-3-yl)ethanaminium chloride
-
-
2-amino-N-[4-(phenylmethoxy)phenyl]-acetamide
-
2-bromo-4-[(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)methyl]benzoic acid
-
-
2-fluoro-4-[(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)methyl]benzoic acid
-
-
2-oxo-3-amino carboxylic esters
-
2-[(4-benzylphenoxy)methyl]piperazine
-
-
2-[(4-benzylphenoxy)methyl]piperidine
-
-
2-[(4-phenoxyphenoxy)methyl]piperidine
-
-
2-[4-(2-azepan-1-ylethoxy)phenoxy]-1H-benzoimidazole
-
-
2-[4-(2-azepan-1-ylethoxy)phenoxy]benzooxazole
-
-
2-[4-(2-azepan-1-ylethoxy)phenoxy]benzothiazole
-
-
2-[4-(2-morpholin-4-ylethoxy)phenoxy]-1-(2-trimethylsilanylethoxymethyl)-1H-benzoimidazole
-
-
2-[4-(2-morpholin-4-ylethoxy)phenoxy]-1H-benzoimidazole
-
-
2-[4-(2-morpholin-4-ylethoxy)phenoxy]benzooxazole
-
-
2-[4-(2-morpholin-4-ylethoxy)phenoxy]benzothiazole
-
-
2-[4-(2-piperidin-1-ylethoxy)phenoxy]-1H-benzoimidazole
-
-
2-[4-(2-piperidin-1-ylethoxy)phenoxy]benzooxazole
-
-
2-[4-(2-piperidin-1-ylethoxy)phenoxy]benzothiazole
-
-
2-[4-(2-piperidin-1-ylethyl)phenoxy]benzothiazole
-
-
2-[4-(2-pyrrolidin-1-ylethoxy)phenoxy]-1H-benzoimidazole
-
-
2-[4-(2-pyrrolidin-1-ylethoxy)phenoxy]benzooxazole
-
-
2-[4-(2-pyrrolidin-1-ylethoxy)phenoxy]benzothiazole
-
-
2-[4-(piperidin-1-ylmethyl)phenoxy][1,3]thiazolo[4,5-b]pyridine
-
-
2-[4-(piperidin-1-ylmethyl)phenoxy][1,3]thiazolo[4,5-c]pyridine
-
-
2-[4-(piperidin-1-ylmethyl)phenoxy][1,3]thiazolo[5,4-c]pyridine
-
-
2-[4-[2-(piperidin-1-yl)ethoxy]phenoxy][1,3]thiazolo[4,5-b]pyridine
-
-
2-[4-[2-(piperidin-1-yl)ethyl]phenoxy][1,3]thiazolo[4,5-b]pyridine
-
-
2-[4-[4-[2-[1-pyrrolidinyl]ethoxy]phenoxy]phenyl]-oxazole
-
-
2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-5-yl]oxy]-1,3-benzothiazole
2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-5-yl]oxy][1,3]thiazolo[4,5-b]pyridine
2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy]-1,3-benzothiazole
2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy][1,3]thiazolo[4,5-b]pyridine
2-[[3-(morpholin-4-ylmethyl)-1-benzofuran-6-yl]oxy]-1,3-benzothiazole
2-[[3-(morpholin-4-ylmethyl)-1-benzofuran-6-yl]oxy][1,3]thiazolo[4,5-b]pyridine
2-[[3-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy]-1,3-benzothiazole
2-[[3-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy][1,3]thiazolo[4,5-b]pyridine
2-[[4-methyl-5-([[2-oxo-2-(phenylamino)ethyl]sulfanyl]methyl)-4H-1,2,4-triazol-3-yl]sulfanyl]-N-phenylacetamide
-
compound identified by pharmacophore modeling, binds both human leukotriene hydrolase hLTA4H and the human leukotriene C4 synthase hLTC4S with good binding characteristics
2S-2,6-diamino-N-[4-(phenylmethoxy)phenyl]hexanamide dihydrochloride
-
3-(1-[2-[4-(benzothiazol-2-yloxy)phenoxy]ethyl]piperidin-4-yl)oxazolidin-2-one
-
-
3-(1-[2-[4-(benzothiazol-2-yloxy)phenyl]ethyl]piperidin-4-yl)oxazolidin-2-one
-
-
3-(2-(5-(4-phenylbenzyloxy)-1H-indol-3-yl)ethylamino)propanoic acid
-
-
3-(4-fluorophenyl)-5-[2-methyl-5-(pyrrolidin-1-ylsulfonyl)furan-3-yl]-1,2,4-oxadiazole
-
compound identified by pharmacophore modeling, binds both human leukotriene hydrolase hLTA4H and the human leukotriene C4 synthase hLTC4S with good binding characteristics
3-(benzyloxy)pyridin-2-amine
-
3-amino-3,4-dihydro-1H-naphthalen-2-one O-(2-phenylethyl)oxime
-
-
3-amino-3,4-dihydro-1H-naphthalen-2-one O-(3-phenylpropyl)oxime
-
-
3-amino-3,4-dihydro-1H-naphthalen-2-one O-(4-phenylbutyl)oxime
-
-
3-amino-3,4-dihydro-1H-naphthalen-2-one O-(5-phenylpentyl)oxime
-
-
3-fluoro-4-[(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)methyl]benzoic acid
-
-
3-[(2R)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]piperidin-1-yl]propanoic acid
-
-
3-[1-[4-(benzothiazol-2-yloxy)benzyl]piperidin-4-yl]oxazolidin-2-one
-
-
3-[methyl[3-[4-(phenylmethyl)phenoxy]propyl]amino]-propanoic acid
3-[[4-(1-methylethyl)benzyl]sulfanyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-valine
-
-
4',5-O-dimethyl-[6]-gingerol
-
4'-O-allyl-[6]-gingerol
-
4'-O-methyl shogoal
a potent enzyme inhibitor, non-cytotoxic to normal cells
4'-O-methyl-[6]-gingerol
-
4-((R)-2-(4-(4-chlorophenoxy)phenoxymethyl)pyrrolidin-1-yl)-l-butyric acid
-
4-((S)-2-[4-(4-chlorophenoxy)phenoxymethyl]pyrrolidin-1-yl)-butyric acid
-
4-(2-amino-1,3-thiazol-4-yl)phenol
-
4-(4-benzylphenyl)-1,3-thiazol-2-amine
i.e. ARM1
4-(4-benzylphenyl)-thiazol-2-amine
4BSA
4-(4-benzylphenyl)thiazol-2-amine
-
4-(dimethylamino)-N-[7-(hydroxyamino)-7-oxoheptyl]benzamide
4-([(1R,5S)-3-[(4-benzylphenyl)amino]-8-azabicyclo[3.2.1]oct-8-yl]methyl)benzoic acid
-
-
4-([(1R,5S)-3-[(4-phenoxyphenyl)amino]-8-azabicyclo[3.2.1]oct-8-yl]methyl)benzoic acid
-
-
4-([(2R)-2-[(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)methyl]pyrrolidin-1-yl]methyl)benzoic acid
-
-
4-([2-[(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)methyl]pyrrolidin-1-yl]methyl)benzoic acid
-
-
4-([4-[([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)methyl]piperidin-1-yl]methyl)benzoic acid
-
-
4-([methyl[2-(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)ethyl]amino]methyl)benzoic acid
-
-
4-([methyl[2-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)ethyl]amino]methyl)benzoic acid
-
-
4-([methyl[3-([2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)propyl]amino]methyl)benzoic acid
-
-
4-([methyl[3-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)propyl]amino]methyl)benzoic acid
-
-
4-([methyl[4-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)cyclohexyl]amino]methyl)benzoic acid
-
-
4-([[2,2-dimethyl-3-(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)propyl](methyl)amino]methyl)benzoic acid
-
-
4-([[3-(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)propyl]amino]methyl)benzoic acid
-
-
4-([[3-([2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)propyl]amino]methyl)benzoic acid
-
-
4-([[4-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)cyclohexyl]amino]methyl)benzoic acid
-
-
4-amino-N-[4-(benzyloxy)-phenyl]butanamide
4BS
4-amino-N-[4-(phenylmethoxy)phenyl]butanamide hydrochloride
-
4-dimethylamino-N-[4-(phenylmethoxy)phenyl]-butanamide trifluoroacetate
-
4-methylamino-N-[4-(phenylmethoxy)phenyl]butanamide trifluoroacetate
-
4-[(2R)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]piperidin-1-yl]butanoic acid
-
-
4-[(2R)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]pyrrolidin-1-yl]butanoic acid
4-[(2S)-2-([4-(4-chlorophenoxy)phenoxy]methyl)-1-pyrrolidinyl]butanoic acid
i.e. DG-051
4-[(2S)-2-([4-[4-(thiophen-3-yl)benzyl]phenoxy]methyl)piperidin-1-yl]butanoic acid
-
-
4-[(2S)-2-[[4-(4-chloro-2-hydroxyphenoxy)phenoxy]methyl]pyrrolidin-1-yl]butanoic acid
4-[(2S)-2-[[4-(4-chloro-3-hydroxyphenoxy)phenoxy]methyl]pyrrolidin-1-yl]butanoic acid
4-[(2S)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]-1-oxidopyrrolidin-1-yl]butanoic acid
4-[(2S)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]piperidin-1-yl]butanoic acid
-
-
4-[(4-[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]-1,4-diazepan-1-yl)methyl]benzoic acid
-
-
4-[(4-[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]piperazin-1-yl)methyl]benzoic acid
-
-
4-[(5-[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)methyl]benzoic acid
-
-
4-[(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)methyl]-3-nitrobenzoic acid
-
-
4-[(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)methyl]benzoic acid
-
-
4-[(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)methyl]cyclohexanecarboxylic acid
-
-
4-[(methyl[[(2R)-1-[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]piperidin-2-yl]methyl]amino)methyl]benzoic acid
-
-
4-[(methyl[[(2R)-1-[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]pyrrolidin-2-yl]methyl]amino)methyl]benzoic acid
-
-
4-[(methyl[[(2S)-1-[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]piperidin-2-yl]methyl]amino)methyl]benzoic acid
-
-
4-[(methyl[[(2S)-1-[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]pyrrolidin-2-yl]methyl]amino)methyl]benzoic acid
-
-
4-[2-(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)ethyl]benzoic acid
-
-
4-[2-[(1R,5S)-3-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)-8-azabicyclo[3.2.1]oct-8-yl]ethyl]benzoic acid
-
-
4-[2-[3-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)piperidin-1-yl]ethyl]benzoic acid
-
-
4-[2-[4-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)piperidin-1-yl]ethyl]benzoic acid
-
-
4-[[(1R,5S)-3-([4-[3-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
-
JNJ-26993135
4-[[(1R,5S)-3-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
-
-
4-[[(1R,5S)-3-([4-[4-(1,3-thiazol-2-yl)phenoxy]phenyl]amino)-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
-
-
4-[[(1R,5S)-3-([4-[4-(1H-pyrrol-1-yl)phenoxy]phenyl]amino)-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
-
-
4-[[(1R,5S)-3-([4-[4-(trifluoromethyl)phenoxy]phenyl]amino)-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
-
-
4-[[(1R,5S)-3-[[4-(1,3-benzothiazol-2-yloxy)phenyl]amino]-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
-
-
4-[[(1R,5S)-3-[[4-(2-chlorophenoxy)phenyl]amino]-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
-
-
4-[[(1R,5S)-3-[[4-(2-fluorophenoxy)phenyl]amino]-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
-
-
4-[[(1R,5S)-3-[[4-(4-chlorophenoxy)phenyl]amino]-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
-
-
4-[[(1R,5S)-3-[[4-(4-fluorophenoxy)phenyl]amino]-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
-
-
4-[[(1R,5S)-3-[[4-(4-methoxyphenoxy)phenyl]amino]-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
-
-
4-[[(1R,5S)-3-[[4-(benzyloxy)phenyl]amino]-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
-
-
4-[[(1R,5S)-3-[[4-(biphenyl-4-yloxy)phenyl]amino]-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
-
-
4-[[(1R,5S)-3-[[4-(pyridin-4-ylmethyl)phenyl]amino]-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
-
-
4-[[(3-[[2-([4-[(2R)-2-hydroxy-2-phenylethoxy]phenyl]amino)-2-oxoethyl](methyl)amino]propyl)(methyl)amino]methyl]benzoic acid
-
-
4-[[(3R)-3-(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)pyrrolidin-1-yl]methyl]benzoic acid
-
-
4-[[(3S)-3-(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)pyrrolidin-1-yl]methyl]benzoic acid
-
-
4-[[3-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)piperidin-1-yl]methyl]benzoic acid
-
-
4-[[3-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)pyrrolidin-1-yl]methyl]benzoic acid
-
-
4-[[4-(1-[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]hydrazino)piperidin-1-yl]methyl]benzoic acid
-
-
4-[[4-(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)azepan-1-yl]methyl]benzoic acid
-
-
4-[[4-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)azepan-1-yl]methyl]benzoic acid
-
-
4-[[4-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)piperidin-1-yl]methyl]benzoic acid
-
-
4-[[methyl(1-[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]azepan-4-yl)amino]methyl]benzoic acid
-
-
4-[[methyl(1-[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]piperidin-4-yl)amino]methyl]benzoic acid
-
-
4-[[methyl(3-[methyl[2-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)-2-oxoethyl]amino]propyl)amino]methyl]benzoic acid
-
-
4-[[[3-[(2-[[4-(2-fluorophenoxy)phenyl]amino]-2-oxoethyl)(methyl)amino]propyl](methyl)amino]methyl]benzoic acid
-
-
4-[[[3-[(2-[[4-(4-chlorophenoxy)phenyl]amino]-2-oxoethyl)(methyl)amino]propyl](methyl)amino]methyl]benzoic acid
-
-
4-[[[3-[(2-[[4-(4-fluorophenoxy)phenyl]amino]-2-oxoethyl)(methyl)amino]propyl](methyl)amino]methyl]benzoic acid
-
-
4-[[[3-[[2-[(4-benzylphenyl)amino]-2-oxoethyl](methyl)amino]propyl](methyl)amino]methyl]benzoic acid
-
-
5-(2-pyrrolidin-1-ylethoxy)-1H-indole
-
5-O-methyl-[6]-gingerol
-
5-oxo-5-[[4-(phenylmethoxy)phenyl]amino]pentanoic acid
-
5-[(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)methyl]furan-2-carboxylic acid
-
-
6-chloro-2-[4-(piperidin-1-ylmethyl)phenoxy][1,3]thiazolo[4,5-b]pyridine
-
-
6-fluoro-2-[4-(piperidin-1-ylmethyl)phenoxy][1,3]thiazolo[4,5-b]pyridine
-
-
7,11-trans-9-cis-Leukotriene A4
-
-
7-methyl-2-[4-(piperidin-1-ylmethyl)phenoxy][1,3]thiazolo[4,5-b]pyridine
-
-
7-trans-9,11-cis-Leukotriene A4
-
-
8-Hydroxy-quinoline-5-sulfonic acid
-
-
acetic acid (1-[2-[4-(benzothiazol-2-yloxy)phenyl]ethyl]piperidin-4-ylcarbamoyl)methyl ester
-
-
acetic acid [1-[4-(benzothiazol-2-yloxy)benzyl]piperidin-4-ylcarbamoyl]methyl ester
-
-
Acetic anhydride
-
complete loss of peptidase activity and epoxide hydrolase activity
acrolein
acrolein in cigarette smoke in part inhibits LTA4H peptidase activity
benzyl[4-((R)-1-pyrrolidin-2-ylmethoxy)phenyl]amine
-
bis-(I-5'->II-5')-[6]-gingerol
-
citraconic anhydride
-
complete loss of peptidase activity and epoxide hydrolase activity
diamide/glutathione combination
-
complete loss of peptidase activity and epoxide hydrolase activity
-
JMC08-4
-
i.e. 1,2-amino-3-[5-(benzyloxy)-1H-indol-3-yl] propanoic acid
JNJ 26993135
-
a selective LTA4H inhibitor, leads to reduction of TH2 cytokines and mucin levels, and blocks mast cell production of LTB4 and suppresses airway hyperresponsiveness
JNJ-26993135
shows selective inhibition of LTB4 biosynthesis in a murine model, suggesting a potent compound targeting LTA4H
leukotriene A4 ethyl ester
-
comparison of inactivation of wild-type and mutant enzymes
leukotriene A4 methyl ester
methyl 3-(2-(5-(3-phenoxybenzyloxy)-1H-indol-3-yl)ethylamino)propanoate
-
-
methyl 3-(2-(5-(4-phenylbenzyloxy)-1H-indol-3-yl)ethylamino)propanoate
-
-
methyl 5-(1,2-dithiolan-3-yl) pentanoate
i.e. alpha-lipoic acid methyl ester or LAME
methyl methanethiosulfonate
-
inhibition of epoxide hydrolase activity, stimulation of peptidase activity
methyl shogoal
a [6]-gingerol derivative
methyl-methane thiosulfonate
-
inhibits aminopeptidase activity and NaCl stimulates this inactivation, beta-mercaptoethanol reactivates this inactivation, bestatin protects inactivation, little effect on epoxid hydrolase activity
methyl-N-[3-[4-(phenylmethyl)-phenoxy]propyl]-beta-alanine
-
-
N-(1-[2-[4-(benzothiazol-2-yloxy)phenyl]ethyl]piperidin-4-yl)acetamide
-
-
N-(1-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)acetamide
N-(1-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)acetamide
N-(2-[[6-(4-fluorophenyl)pyridazin-3-yl]amino]ethyl)-1,2-dimethyl-1H-imidazole-4-sulfonamide
-
compound identified by pharmacophore modeling, binds both human leukotriene hydrolase hLTA4H and the human leukotriene C4 synthase hLTC4S with good binding characteristics
N-(6-(2-aminophenylamino)-6-oxyhexyl)-4-methylbenzamide
N-(8-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenoxy]ethyl]-8-azabicyclo[3.2.1]oct-3-yl)acetamide
-
-
N-(8-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenyl]ethyl]-8-azabicyclo[3.2.1]oct-3-yl)acetamide
-
-
N-Acetylimidazole
-
75 min, loss of 92% peptidase activity and 78% of epoxide hydrolase activity, both activities are restored by hydroxylamine and bestatin protects
N-mercaptoacyl-L-proline
-
-
-
N-methyl-1-[2-(thiophen-2-yl)phenyl]methanamine
-
N-[(3-endo)-8-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]-8-azabicyclo[3.2.1]oct-3-yl]acetamide
N-[(3-endo)-8-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-8-azabicyclo[3.2.1]oct-3-yl]acetamide
N-[1-[4-(1,3-benzothiazol-2-yloxy)benzyl]piperidin-4-yl]-2-hydroxyacetamide
N-[1-[4-(benzothiazol-2-yloxy)benzyl]piperidin-4-yl]-2-hydroxyacetamide
-
-
N-[1-[4-(benzothiazol-2-yloxy)benzyl]piperidin-4-yl]acetamide
-
-
N-[2-[(furan-2-ylmethyl)sulfanyl]ethyl]-2-[[1-(4-hydroxyphenyl)-1H-tetrazol-5-yl]sulfanyl]acetamide
-
compound identified by pharmacophore modeling, binds both human leukotriene hydrolase hLTA4H and the human leukotriene C4 synthase hLTC4S with good binding characteristics
N-[3(R)-[(hydroxyamino)carbonyl]-2-benzyl-1-oxopropyl]-L-alanine
i.e. kelatorphan, potent inhibitor of Zn-metalloenzymes
N-[3-(4-benzylphenoxy)propyl]-N-methyl-beta-alanine
N-[3-[3-(acetylamino)phenoxy]propyl]-3-[3-(pyridin-2-yl)-1,2,4-oxadiazol-5-yl]propanamide
-
compound identified by pharmacophore modeling, binds both human leukotriene hydrolase hLTA4H and the human leukotriene C4 synthase hLTC4S with good binding characteristics
N-[4-(3-chlorophenyl)-2,5-dioxopiperazin-1-yl]-2-[[4-methyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl]sulfanyl]acetamide
-
compound identified by pharmacophore modeling, binds both human leukotriene hydrolase hLTA4H and the human leukotriene C4 synthase hLTC4S with good binding characteristics
N-[8-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)benzyl]-8-azabicyclo[3.2.1]oct-3-yl]acetamide
-
-
N1-(2-aminoethyl)-N5-(4-phenoxyphenyl)-L-glutamamide hydrochloride
-
N1-(2-carboxyethyl)-N5-(4-phenoxyphenyl)-L-glutamamide trifluoroacetate
-
N1-(2-hydroxyethyl)-N5-(4-phenoxyphenyl)-L-glutamamide trifluoroacetate
-
N1-(3-carboxypropyl)-N5-(4-phenoxyphenyl)-L-glutamamide trifluoroacetate
-
N1-(4-carboxybutyl)-N5-(4-phenoxyphenyl)-L-glutamamide bistrifluoroacetate
-
N1-hydroxy-N5-[4-(phenylmethoxy)phenyl]-L-glutamamide trifluoroacetate
-
N1-[4-(phenylmethoxy)phenyl]-D-aspartamine
-
N1-[4-(phenylmethoxy)phenyl]-D-glutamine trifluoroacetate
-
N1-[4-(phenylmethoxy)phenyl]-L-aspartamine trifluoroacetate
-
N1-[4-(phenylmethoxy)phenyl]-L-glutamamide hydrochloride
-
N1-[4-(phenylmethoxy)phenyl]-L-glutamine trifluoroacetate
-
N2-methyl-N-(4-phenoxyphenyl)-N2-[4-(1H-tetrazol-5-yl)benzyl]glycinamide
-
-
N2-methyl-N2-[3-[methyl(4-oxobutyl)amino]propyl]-N-(4-phenoxyphenyl)glycinamide
-
-
N2-methyl-N2-[4-[methyl(4-oxobutyl)amino]butyl]-N-(4-phenoxyphenyl)glycinamide
-
-
N2-[3-(dimethylamino)propyl]-N2-methyl-N-(4-phenoxyphenyl)glycinamide
-
-
N2-[3-[benzyl(methyl)amino]propyl]-N2-methyl-N-(4-phenoxyphenyl)glycinamide
-
-
N2-[4-[(aminooxy)sulfinyl]benzyl]-N2-methyl-N-(4-phenoxyphenyl)glycinamide
-
-
N4-[4-(phenylmethoxy)phenyl]-L-aspartamine trifluoroacetate
-
N5-(4-phenoxyphenyl)-L-glutamine
-
N5-phenyl-L-glutamamide dihydrochloride
-
N5-[(4-phenoxy)-3-pyridyl]-L-glutamamide tristrifluoroacetate
-
N5-[3-(phenylmethoxy)phenyl]-L-glutamine methyl ester
-
N5-[4-(1H-pyrrol-1-yl)phenyl]-L-glutamamide hydrochloride
-
N5-[4-(2-hydroxy-3-phenylpropoxy)phenyl]-L-glutamine trifluoroacetate
-
N5-[4-(2-methylphenoxy)phenyl]-L-glutamamide hydrochloride
-
N5-[4-(2-oxo-3-phenylpropoxy)phenyl]-L-glutamine trifluoroacetate
-
N5-[4-(2-phenylethoxy)phenyl]-L-glutamine
-
N5-[4-(3-methylphenoxy)phenyl]-L-glutamamide hydrochloride
-
N5-[4-(3-phenylpropoxy)phenyl]-L-glutamine
-
N5-[4-(4-(3-furyl)phenoxy)phenyl]-L-glutamamide trifluoroacetate
-
N5-[4-(4-methylphenoxy)phenyl]-L-glutamamide hydrochloride
-
N5-[4-(cyclohexyloxy)phenyl]-L-glutamamide
-
N5-[4-(N-methyl-N-phenylamino)phenyl]-L-glutamine methyl ester trifluoroacetate
-
N5-[4-(N-phenylamino)phenyl]-L-glutamine bistrifluoroacetate
-
N5-[4-(phenylmethoxy)phenyl]-D-glutamine hydrochloride
-
N5-[4-(phenylmethoxy)phenyl]-L-glutamamide trifluoroacetate
-
N5-[4-(phenylmethoxy)phenyl]-L-glutamine 1,1-dimethylethyl ester
-
N5-[4-(phenylmethoxy)phenyl]-L-glutamine hemitrifluoroacetate
-
N5-[4-(phenylmethoxy)phenyl]-L-glutamine methyl ester hydrochloride
-
N5-[4-benzylphenyl]-L-glutamamide trifluoroacetate
-
N5-[4-methoxyphenyl]-L-glutamine methyl ester trifluoroacetate
-
N5-[4-[4-(1H-pyrrol-1-yl)phenoxy]phenyl]-L-glutamine hemitrifluoroacetate
-
N6-[4-(4-methylphenoxy)phenyl]-L-homoglutamine trifluoroacetate
-
omega-[(omega-arylalkyl)aryl]alkanoid acids
-
-
-
p-hydroxymercuribenzoate
-
bestatin protects inactivation
Phenylglyoxal
-
preincubation with captopril protects enzyme from inactivation
pyridin-4-yl[4-(2-pyrrolidin-1-ylethoxy)phenyl]methanol
-
S-(4-cyclohexylbenzyl)-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
-
-
S-(4-tert-butylbenzyl)-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
-
-
S-[(4-cyclohexylphenyl)(phenyl)methyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
-
-
S-[1-(4-cyclohexylphenyl)-1-methylethyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
-
-
S-[1-methyl-1-[4-(1-methylethyl)phenyl]ethyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
-
-
S-[1-[4-(1-methylethyl)phenyl]butyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
-
-
S-[1-[4-(1-methylethyl)phenyl]ethyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
-
-
S-[1-[4-(1-methylethyl)phenyl]pentyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
-
-
S-[1-[4-(1-methylethyl)phenyl]propyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
-
-
S-[2-methyl-1-[4-(1-methylethyl)phenyl]propyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
-
-
S-[4-(diethylamino)benzyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
-
-
S-[4-(dimethylamino)benzyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
-
i.e. SA6541, a specific inhibiter of LTA4 hydrolase, that attenuates 5-lipoxygenase metabolite-induced scratching behavior, but does not affect the increase in vascular permeability caused by 5-hydroperoxyeicosatetraenoic acid, 5-HPETE, overview
S-[[4-(1-methylethyl)phenyl](phenyl)methyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
-
-
suberanilohydroxamic acid
-
sulindac sulfide
reduces LTA4H activity in HT29 CRC cells, thus lowering LTB4 levels and decreasing HT29 cell viability
Tetranitromethane
-
preincubation with bestatin prevents the inactivation
Trinitrobenzenesulfonate
-
complete loss of peptidase activity and epoxide hydrolase activity
[(2R)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]piperidin-1-yl]acetic acid
-
-
(4S)-4-amino-5-hydroxy-N-(4-phenoxyphenyl)pentanamide
-
(4S)-4-amino-5-hydroxy-N-(4-phenoxyphenyl)pentanamide
-
-
(S)-2-((2S,3R)-3-amino-2-hydroxy-4-phenylbutanamido)-4-methylpentanoic acid
-
(S)-2-((2S,3R)-3-amino-2-hydroxy-4-phenylbutanamido)-4-methylpentanoic acid
-
1-(1-[2-[4-(1,3-benzothiazol-2-yloxy)phenoxy]ethyl]piperidin-4-yl)pyrrolidin-2-one
-
-
1-(1-[2-[4-(1,3-benzothiazol-2-yloxy)phenoxy]ethyl]piperidin-4-yl)pyrrolidin-2-one
-
-
1-(1-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)pyrrolidin-2-one
-
-
1-(1-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)pyrrolidin-2-one
-
-
1-(1-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)pyrrolidin-2-one
-
-
1-(1-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)pyrrolidin-2-one
-
-
1-(5-[[5-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
-
-
1-(5-[[5-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
-
-
1-(5-[[5-([1,3]thiazolo[4,5-c]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
-
-
1-(5-[[5-([1,3]thiazolo[4,5-c]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
-
-
1-(5-[[5-([1,3]thiazolo[5,4-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
-
-
1-(5-[[5-([1,3]thiazolo[5,4-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
-
-
1-(5-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
-
-
1-(5-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
-
-
1-(5-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
-
-
1-(5-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
-
-
1-(5-[[6-([1,3]thiazolo[4,5-c]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
-
-
1-(5-[[6-([1,3]thiazolo[4,5-c]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
-
-
1-(5-[[6-([1,3]thiazolo[5,4-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
-
-
1-(5-[[6-([1,3]thiazolo[5,4-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
-
-
1-[4-(1,3-benzothiazol-2-yloxy)benzyl]piperidine-4-carboxylic acid
-
JNJ-27265732
1-[4-(1,3-benzothiazol-2-yloxy)benzyl]piperidine-4-carboxylic acid
-
-
1-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]piperidine-4-carboxylic acid
-
-
1-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]piperidine-4-carboxylic acid
-
-
1-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]piperidine-4-carboxylic acid
-
-
1-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]piperidine-4-carboxylic acid
-
-
2-oxo-3-amino carboxylic esters
-
-
-
2-oxo-3-amino carboxylic esters
-
contain a transition state mimic of the enzyme-catalyzed amide cleavage as a core and additional complementary components which resemble the hydrophobic nature of the conjugated polyene system of the natural substrate LTA4
-
2-oxo-3-amino carboxylic esters
-
-
-
2-oxo-3-amino carboxylic esters
-
comparison of inhibition of mutant and wild-type enzymes
-
2-oxo-3-amino carboxylic esters
-
-
-
2-oxo-3-amino carboxylic esters
-
-
-
2-oxo-3-amino carboxylic esters
-
-
-
2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-5-yl]oxy]-1,3-benzothiazole
-
-
2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-5-yl]oxy]-1,3-benzothiazole
-
-
2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-5-yl]oxy][1,3]thiazolo[4,5-b]pyridine
-
-
2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-5-yl]oxy][1,3]thiazolo[4,5-b]pyridine
-
-
2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy]-1,3-benzothiazole
-
-
2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy]-1,3-benzothiazole
-
-
2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy][1,3]thiazolo[4,5-b]pyridine
-
-
2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy][1,3]thiazolo[4,5-b]pyridine
-
-
2-[[3-(morpholin-4-ylmethyl)-1-benzofuran-6-yl]oxy]-1,3-benzothiazole
-
-
2-[[3-(morpholin-4-ylmethyl)-1-benzofuran-6-yl]oxy]-1,3-benzothiazole
-
-
2-[[3-(morpholin-4-ylmethyl)-1-benzofuran-6-yl]oxy][1,3]thiazolo[4,5-b]pyridine
-
-
2-[[3-(morpholin-4-ylmethyl)-1-benzofuran-6-yl]oxy][1,3]thiazolo[4,5-b]pyridine
-
-
2-[[3-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy]-1,3-benzothiazole
-
-
2-[[3-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy]-1,3-benzothiazole
-
-
2-[[3-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy][1,3]thiazolo[4,5-b]pyridine
-
-
2-[[3-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy][1,3]thiazolo[4,5-b]pyridine
-
-
3-[methyl[3-[4-(phenylmethyl)phenoxy]propyl]amino]-propanoic acid
-
3-[methyl[3-[4-(phenylmethyl)phenoxy]propyl]amino]-propanoic acid
-
4'-O-prenyl-[6]-gingerol
-
4'-O-prenyl-[6]-gingerol
-
-
4-(dimethylamino)-N-[7-(hydroxyamino)-7-oxoheptyl]benzamide
enzyme binding structure, overview
4-(dimethylamino)-N-[7-(hydroxyamino)-7-oxoheptyl]benzamide
markedly diminishes early neutrophilic inflammation in mouse models of ALI and IPF under a clinical safety dose, enzyme binding structure, overview
4-[(2R)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]pyrrolidin-1-yl]butanoic acid
-
i.e. DG-051, a phase II clinical candidate
4-[(2R)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]pyrrolidin-1-yl]butanoic acid
-
i.e. DG-051, a phase II clinical candidate
4-[(2R)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]pyrrolidin-1-yl]butanoic acid
-
-
4-[(2R)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]pyrrolidin-1-yl]butanoic acid
i.e. DG-051
4-[(2R)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]pyrrolidin-1-yl]butanoic acid
i.e. DG051
4-[(2R)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]pyrrolidin-1-yl]butanoic acid
-
i.e. DG-051, a phase II clinical candidate
4-[(2S)-2-[[4-(4-chloro-2-hydroxyphenoxy)phenoxy]methyl]pyrrolidin-1-yl]butanoic acid
-
i.e. DG-051 M1-A, a derivative derived from DG-051
4-[(2S)-2-[[4-(4-chloro-2-hydroxyphenoxy)phenoxy]methyl]pyrrolidin-1-yl]butanoic acid
-
i.e. DG-051 M1-A, a derivative derived from DG-051
4-[(2S)-2-[[4-(4-chloro-2-hydroxyphenoxy)phenoxy]methyl]pyrrolidin-1-yl]butanoic acid
-
i.e. DG-051 M1-A, a derivative derived from DG-051
4-[(2S)-2-[[4-(4-chloro-3-hydroxyphenoxy)phenoxy]methyl]pyrrolidin-1-yl]butanoic acid
-
i.e. DG-051 M1-B, a derivative derived from DG-051
4-[(2S)-2-[[4-(4-chloro-3-hydroxyphenoxy)phenoxy]methyl]pyrrolidin-1-yl]butanoic acid
-
i.e. DG-051 M1-B, a derivative derived from DG-051
4-[(2S)-2-[[4-(4-chloro-3-hydroxyphenoxy)phenoxy]methyl]pyrrolidin-1-yl]butanoic acid
-
i.e. DG-051 M1-B, a derivative derived from DG-051
4-[(2S)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]-1-oxidopyrrolidin-1-yl]butanoic acid
-
i.e. DG-051 M2, an N-oxide derivative derived from DG-051
4-[(2S)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]-1-oxidopyrrolidin-1-yl]butanoic acid
-
i.e. DG-051 M2, an N-oxide derivative derived from DG-051
4-[(2S)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]-1-oxidopyrrolidin-1-yl]butanoic acid
-
i.e. DG-051 M2, an N-oxide derivative derived from DG-051
abexinostat
-
aminohydroxamic acid
-
-
belinostat
-
bestatin
-
-
bestatin
-
immediate and reversible effect on isolated enzyme
bestatin
isolated from Streptomyces olivoreticuli, a general AP inhibitor, inhibits LTB4 biosynthesis. Treatment with bestatin inhibits cell proliferation of lung carcinoma A549 cells by significantly reducing LTA4H activity
bestatin
significantly inhibits LTB4 production, samples from13 CRC patients show a significant decrease in LTB4, the LTA4H signaling pathway, and Ki-67 in the bestatin-treated group compared with the untreated group
bestatin
-
comparison of inhibition of mutant and wild-type enzymes, mechanism
bestatin
significantly inhibit LTB4 production, bestatin effectively inhibits LTB4 synthesis and tumorigenesis in the ApcMin/+ and CRC patient-derived xenograft mouse model
bestatin
bestatin inhibits leukotriene B4 biosynthesis in the esophageal tissues
bestatin
isolated from Streptomyces olivoreticuli, a general AP inhibitor, inhibits LTB4 biosynthesis. Following a short-term intraperitoneal treatment with 10 mg/kg bestatin, LTB4 biosynthesis in the esophagoduodenal junction is significantly suppressed in rats treated with EGDA compared to that in the untreated group, in an esophagogastroduodenal anastomosis (EGDA) surgical model. Bestatin inhibits LTA4H/LTB4 activation and reduces tumorigenesis in EGDA rats
bestatin
-
aminopeptidase activity, leukotriene A4 competes partially
captopril
-
-
captopril
-
59% inhibition at 1 mM
Co2+
-
-
Co2+
-
reversible by addition of EDTA
CUDC-101
-
DG-051
-
-
DG-051
-
a LTA4H inhibitor, used for therapeutic modulation of the leukotriene synthesis pathway in case of myocardial infarction
diacetyl-[6]-gingerol
-
diacetyl-[6]-gingerol
-
-
entinostat
-
givinostat
-
hydroxamic acid
-
hydroxamic acid
-
comparison of inhibition of mutant and wild-type enzymes
hydroxamic acid
-
aminopeptidase activity
JNJ-26481585
-
Kelatorphan
-
-
leukotriene A4
-
-
leukotriene A4
-
suicide inactivation
leukotriene A4
-
suicide inactivation via an apparently mechanism-based irreversible binding of leukotriene A4 to the protein in a 1:1 stoichiometry, comparison of inactivation of wild-type and mutant enzymes, Tyr378 is a residue, which is involved in the binding of leukotriene A4
leukotriene A4
-
comparison of inactivation of wild-type and mutant enzymes; suicide inactivation
leukotriene A4
-
leukotriene A4 binds covalently to Tyr378 and blocks epoxide hydrolase and aminopeptidase activities
leukotriene A4
-
pre-treatment of enzyme by methyl-methane thiosulfonate does not protect against suicide inactivation by leukotriene A4
leukotriene A4
-
inhibits epoxid hydrolase activity and stimulates peptidase activity
leukotriene A4 methyl ester
-
-
leukotriene A4 methyl ester
-
comparison of inactivation of wild-type and mutant enzymes
leukotriene A4 methyl ester
-
-
leukotriene A4 methyl ester
-
no influence
Leukotriene A5
-
-
mocetinostat
-
N-(1-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)acetamide
-
-
N-(1-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)acetamide
-
-
N-(1-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)acetamide
-
-
N-(1-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)acetamide
-
-
N-(6-(2-aminophenylamino)-6-oxyhexyl)-4-methylbenzamide
-
N-(6-(2-aminophenylamino)-6-oxyhexyl)-4-methylbenzamide
-
N-ethylmaleimide
-
-
N-[(3-endo)-8-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]-8-azabicyclo[3.2.1]oct-3-yl]acetamide
-
-
N-[(3-endo)-8-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]-8-azabicyclo[3.2.1]oct-3-yl]acetamide
-
-
N-[(3-endo)-8-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-8-azabicyclo[3.2.1]oct-3-yl]acetamide
-
-
N-[(3-endo)-8-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-8-azabicyclo[3.2.1]oct-3-yl]acetamide
-
-
N-[1-[4-(1,3-benzothiazol-2-yloxy)benzyl]piperidin-4-yl]-2-hydroxyacetamide
-
SC-57461A
N-[1-[4-(1,3-benzothiazol-2-yloxy)benzyl]piperidin-4-yl]-2-hydroxyacetamide
-
-
N-[3-(4-benzylphenoxy)propyl]-N-methyl-beta-alanine
-
SA-6541
N-[3-(4-benzylphenoxy)propyl]-N-methyl-beta-alanine
i.e. SC-57461A
panobinostat
-
PCMB
-
-
pracinostat
-
resminostat
-
resveratrol
-
resveratrol
binds directly to LTA4H and inhibits its activity. The antiproliferative effect of resveratrol is decreased in LTA4H mRNA knockdown cells, LTA4H is a direct target of resveratrol
rocilinostat
-
SA6541
-
-
SA6541
inhibits LTA4H activation
SC-57461A
-
-
SC-57461A
i.e. N-[3-(4-benzylphenoxy)propyl]-N-methyl-beta-L-alanine
scriptaid
-
suberanilohydroxamic acid
enzyme binding structure, overview
-
suberanilohydroxamic acid
markedly diminishes early neutrophilic inflammation in mouse models of ALI and IPF under a clinical safety dose, enzyme binding structure, overview
-
thioamine
-
-
thioamine
-
comparison of inhibition of mutant and wild-type enzymes
thioamine
-
aminopeptidase activity, leukotriene A4 restores
trichostatin A
-
tubacin
-
Valproate
-
Zn2+
-
-
Zn2+
-
reversible by addition of EDTA
[10]-gingerol
-
[6]-gingerol
from ginger, [6]-gingerol suppresses anchorage-independent cancer cell growth by inhibiting LTA4H activity in HCT116 colorectal cancer cells, overview. [6]-Gingerol specifically binds with LTA4H in vitro and ex vivo
[6]-gingerol
-
from ginger, [6]-gingerol suppresses anchorage-independent cancer cell growth by inhibiting LTA4H activity in mice, overview. [6]-Gingerol specifically binds with LTA4H in vitro and ex vivo
additional information
-
not: EDTA, dipicolinic acid
-
additional information
-
not diethyl dicarbonate
-
additional information
-
some enzyme inhibitors also affect the cytotoxicity of the anthrax lethal factor on macrophage cell lines
-
additional information
-
leukotriene A4 inhibitors based on piperidine and piperazine scaffolds, overview
-
additional information
structure-based drug discovery, inhibitor binding and molecular docking, overview
-
additional information
inhibitor structure-function analysis, overview
-
additional information
-
inhibitor structure-function analysis, overview
-
additional information
-
combined molecular docking and pharmacophore filtering assay for identification of chemical compounds that can simultaneously inhibit the human leukotriene hydrolase hLTA4H and the human leukotriene C4 synthase hLTC4S enzymes
-
additional information
-
not inhibited by NI101, 2-(5-(benzyloxy)-1H-indol-3-yl)ethanaminium chloride, 2-(5-(naphthalen-2-ylmethoxy)-1H-indol-3-yl)ethanaminiumchloride, 2-(5-(naphthalen-1-ylmethoxy)-1H-indol-3-yl)ethanaminium chloride, 2-(5-(3-phenoxybenzyloxy)-1H-indol-3-yl)ethanaminium chloride, 2-(5-(2-(4-(4-nitrophenoxy)phenoxy)ethoxy)-1H-indol-3-yl)ethanaminium chloride, 2-(5-(2-(4-(2-nitrophenoxy)phenoxy)ethoxy)-1H-indol-3-yl) ethanaminium chloride, 3-(2-(5-(3-phenoxybenzyloxy)-1H-indol-3-yl)ethylamino)propanoic acid, and 3-(2-(5-(2-(4-phenoxyphenoxy)ethoxy)-1H-indol-3-yl) ethylamino)propanoic acid
-
additional information
tosedostat, or CHR-2797 shows inhibition of the aminopeptidase activity. [6]-Gingerol and derivatives show chemopreventive effects and selective cytotoxicity toward HCT-116 cells but not toward healthy cells
-
additional information
thermodynamic properties of structurally distinct leukotriene A4 hydrolase inhibitors. An in silico method for the determination of stabilized water molecules in the binding site of the apo structure of LTA4H is used to interpret the measured thermodynamic data and provided insights for design of novel LTA4H inhibitors. Fluorescence-based assay system with recombinant His6-tagged enzyme is used for determination of the inhibition kinetics
-
additional information
synthesis, docking, cytotoxicity, and LTA4H inhibitory activity of gingerol derivatives as potential colorectal cancer therapy. NMR spectroscopic structure analysis, enzyme-inhibitor interactions, molecular modeling and docking study, overview. IC50 for cytotoxicity with HCT-116, TIG-1, and HF-1 cells
-
additional information
-
synthesis, docking, cytotoxicity, and LTA4H inhibitory activity of gingerol derivatives as potential colorectal cancer therapy. NMR spectroscopic structure analysis, enzyme-inhibitor interactions, molecular modeling and docking study, overview. IC50 for cytotoxicity with HCT-116, TIG-1, and HF-1 cells
-
additional information
5-lipoxygenase inhibitor zileuton, or the 5-lipoxygenase activating protein inhibitor MK-886, are unable to inhibit the activity of the enzyme. Inhibitor docking and molecular dynamics simulations, interaction analysis
-
additional information
drug repurposing of histone deacetylase (HDAC) inhibitors that alleviate neutrophilic inflammation in acute lung injury and idiopathic pulmonary fibrosis via inhibiting leukotriene A4 hydrolase and blocking LTB4 biosynthesis, overview. Analysis of potential inhibitors of LTA4H across a panel of 18 HDAC inhibitors, using enzymatic assay, thermofluor assay, and X-ray crystallographic investigation. Detailed mechanisms of down-regulation of proinflammatory cytokines by SAHA or M344 are determined in vivo. Cotreatment of N-(6-(2-aminophenylamino)-6-oxyhexyl)-4-methylbenzamide and (S)-2-((2S,3R)-3-amino-2-hydroxy-4-phenylbutanamido)-4-methylpentanoic acid synergistically represses the migration of neutrophil and LTB4-induced neutrophil migration is not affected by these treatments. Molecular modelling of HDAC inhibitors against LTA4H hydrolase and aminopeptidase
-
additional information
-
drug repurposing of histone deacetylase (HDAC) inhibitors that alleviate neutrophilic inflammation in acute lung injury and idiopathic pulmonary fibrosis via inhibiting leukotriene A4 hydrolase and blocking LTB4 biosynthesis, overview. Analysis of potential inhibitors of LTA4H across a panel of 18 HDAC inhibitors, using enzymatic assay, thermofluor assay, and X-ray crystallographic investigation. Detailed mechanisms of down-regulation of proinflammatory cytokines by SAHA or M344 are determined in vivo. Cotreatment of N-(6-(2-aminophenylamino)-6-oxyhexyl)-4-methylbenzamide and (S)-2-((2S,3R)-3-amino-2-hydroxy-4-phenylbutanamido)-4-methylpentanoic acid synergistically represses the migration of neutrophil and LTB4-induced neutrophil migration is not affected by these treatments. Molecular modelling of HDAC inhibitors against LTA4H hydrolase and aminopeptidase
-
additional information
-
cigarette smoke exposure acidifies the airspaces and induced localization of the LTA4H protein into the nuclei of the epithelial cells. This results in accumulation of proline-glycine-proline in the airspaces by suppressing the LTA4H aminopeptidase activity
-
additional information
treatment with bestatin does not inhibit cell proliferation of NIH/3T3 normal mouse embryo fibroblast cells
-
additional information
drug repurposing of histone deacetylase (HDAC) inhibitors that alleviate neutrophilic inflammation in acute lung injury and idiopathic pulmonary fibrosis via inhibiting leukotriene A4 hydrolase and blocking LTB4 biosynthesis, overview. Analysis of potential inhibitors of LTA4H across a panel of 18 HDAC inhibitors, using enzymatic assay, thermofluor assay, and X-ray crystallographic investigation. Detailed mechanisms of down-regulation of proinflammatory cytokines by SAHA or M344 are determined in vivo. Cotreatment of N-(6-(2-aminophenylamino)-6-oxyhexyl)-4-methylbenzamide and (S)-2-((2S,3R)-3-amino-2-hydroxy-4-phenylbutanamido)-4-methylpentanoic acid synergistically represses the migration of neutrophil and LTB4-induced neutrophil migration is not affected by these treatments. Molecular modeling of HDAC inhibitors against LTA4H hydrolase and aminopeptidase
-
additional information
-
drug repurposing of histone deacetylase (HDAC) inhibitors that alleviate neutrophilic inflammation in acute lung injury and idiopathic pulmonary fibrosis via inhibiting leukotriene A4 hydrolase and blocking LTB4 biosynthesis, overview. Analysis of potential inhibitors of LTA4H across a panel of 18 HDAC inhibitors, using enzymatic assay, thermofluor assay, and X-ray crystallographic investigation. Detailed mechanisms of down-regulation of proinflammatory cytokines by SAHA or M344 are determined in vivo. Cotreatment of N-(6-(2-aminophenylamino)-6-oxyhexyl)-4-methylbenzamide and (S)-2-((2S,3R)-3-amino-2-hydroxy-4-phenylbutanamido)-4-methylpentanoic acid synergistically represses the migration of neutrophil and LTB4-induced neutrophil migration is not affected by these treatments. Molecular modeling of HDAC inhibitors against LTA4H hydrolase and aminopeptidase
-
additional information
-
not: PMSF, GEMSA, iodoacetamide
-
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0.000014
(1-[2-[4-(benzooxazol-2-yloxy)phenoxy]ethyl]piperidin-4-yl)methanol
Homo sapiens
-
-
0.000013
(1-[2-[4-(benzothiazol-2-yloxy)phenoxy]ethyl]piperidin-4-yl)-methanol
Homo sapiens
-
-
0.000056
(2R)-2-([4-[4-(thiophen-2-yl)benzyl]phenoxy]methyl)piperidine
Homo sapiens
-
-
0.00006
(2R)-2-([4-[4-(thiophen-3-yl)benzyl]phenoxy]methyl)piperidine
Homo sapiens
-
-
0.000093
(2R)-2-([4-[4-(thiophen-3-yl)phenoxy]phenoxy]methyl)piperidine
Homo sapiens
-
-
0.000044
(2R)-2-[(4-phenoxyphenoxy)methyl]piperidine
Homo sapiens
-
-
0.0049
(2R)-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]-3-[(4-nitrobenzyl)sulfanyl]propanoic acid
Homo sapiens
-
-
0.0017
(2R)-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]-3-[(4-phenoxybenzyl)sulfanyl]propanoic acid
Homo sapiens
-
-
0.000072
(2R)-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]-3-[(4-propylbenzyl)sulfanyl]propanoic acid
Homo sapiens
-
-
0.0004
(2R)-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]-3-[[4-(trifluoromethoxy)benzyl]sulfanyl]propanoic acid
Homo sapiens
-
-
0.00014
(2R)-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]-3-[[4-(trifluoromethyl)benzyl]sulfanyl]propanoic acid
Homo sapiens
-
-
0.000438
(2R)-2-[[4-(4-chlorobenzyl)phenoxy]methyl]piperidine
Homo sapiens
-
-
0.0000069
(2R)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]-1-(1,2,4-oxadiazol-2(3H)-ylmethyl)piperidine
Homo sapiens
-
-
0.00011
(2R)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]piperidine
Homo sapiens
-
-
0.000174
(2R)-2-[[4-(4-fluorophenoxy)phenoxy]methyl]piperidine
Homo sapiens
-
-
0.000114
(2R)-2-[[4-(biphenyl-4-yloxy)phenoxy]methyl]piperidine
Homo sapiens
-
-
0.01
(2R)-3-(benzylsulfanyl)-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
Homo sapiens
-
IC50 above 0.01 mM
0.00061
(2R)-3-[(4-bromobenzyl)sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
Homo sapiens
-
-
0.0017
(2R)-3-[(4-chlorobenzyl)sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
Homo sapiens
-
-
0.00053
(2R)-3-[(4-cyanobenzyl)sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
Homo sapiens
-
-
0.00064
(2R)-3-[(4-ethoxybenzyl)sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
Homo sapiens
-
-
0.00028
(2R)-3-[(4-ethylbenzyl)sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
Homo sapiens
-
-
0.01
(2R)-3-[(4-fluorobenzyl)sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
Homo sapiens
-
IC50 above 0.01 mM
0.000015
(2R)-3-[(4-iodobenzyl)sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
Homo sapiens
-
-
0.0024
(2R)-3-[(4-methoxybenzyl)sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
Homo sapiens
-
-
0.0072
(2R)-3-[(4-methylbenzyl)sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
Homo sapiens
-
-
0.0006
(2R)-3-[(biphenyl-4-ylmethyl)sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
Homo sapiens
-
-
0.01
(2R)-3-[[3-(dimethylamino)benzyl]sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
Homo sapiens
-
IC50 above 0.01 mM
0.0002
(2R)-3-[[4-(1-methylethyl)benzyl]sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
Homo sapiens
-
-
0.0074
(2R)-3-[[4-(dimethylamino)benzyl]sulfanyl]-2-[(3-sulfanylbutanoyl)amino]propanoic acid
Homo sapiens
-
-
0.01
(2R)-3-[[4-(dimethylamino)benzyl]sulfanyl]-2-[(3-sulfanylpropanoyl)amino]propanoic acid
Homo sapiens
-
IC50 above 0.01 mM
0.01
(2R)-3-[[4-(dimethylamino)benzyl]sulfanyl]-2-[(4-sulfanylbutanoyl)amino]propanoic acid
Homo sapiens
-
IC50 above 0.01 mM
0.00047
(2R)-3-[[4-(dimethylamino)benzyl]sulfanyl]-2-[(sulfanylacetyl)amino]propanoic acid
Homo sapiens
-
-
0.0015
(2R)-3-[[4-(dimethylamino)benzyl]sulfanyl]-2-[[(2R)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
Homo sapiens
-
-
0.01
(2R)-3-[[4-(dimethylamino)benzyl]sulfanyl]-2-[[(2R)-2-sulfanylpropanoyl]amino]propanoic acid
Homo sapiens
-
IC50 above 0.01 mM
0.00027
(2R)-3-[[4-(dimethylamino)benzyl]sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
Homo sapiens
-
-
0.01
(2R)-3-[[4-(dimethylamino)benzyl]sulfanyl]-2-[[(2S)-2-sulfanylpropanoyl]amino]propanoic acid
Homo sapiens
-
IC50 above 0.01 mM
0.00016
(2R)-3-[[4-(methoxysulfinyl)benzyl]sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
Homo sapiens
-
-
0.000046
(2R)-3-[[4-(methylsulfanyl)benzyl]sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
Homo sapiens
-
-
0.0058
(2S)-2,6-diamino-N-[4-(phenylmethoxy)phenyl]hexanamide dihydrochloride
Homo sapiens
-
0.000093
(2S)-2-([4-[4-(trifluoromethyl)phenoxy]phenoxy]methyl)piperidine
Homo sapiens
-
-
0.00013
(2S)-2-amino-5-oxo-5-[(4-phenoxyphenyl)amino]-1-pentanesulfonic acid
Homo sapiens
-
0.01
(2S)-2-amino-N-[4-(phenylmethoxy)phenyl]-3-[4-(1H-imidazole)]propanamide dihydrochloride
Homo sapiens
-
0.00015
(2S)-2-amino-N-[4-(phenylmethoxy)phenyl]-propanamide hydrochloride
Homo sapiens
-
0.002
(2S)-2-amino-N-[4-(phenylmethoxy)phenyl]benzenepropanamide hydrochloride
Homo sapiens
IC50 above 0.002 mM
0.000094
(2S)-2-[(4-benzylphenoxy)methyl]piperidine
Homo sapiens
-
-
0.000048
(2S)-2-[(4-phenoxyphenoxy)methyl]piperidine
Homo sapiens
-
-
0.000315
(2S)-2-[[4-(4-chlorobenzyl)phenoxy]methyl]piperidine
Homo sapiens
-
-
0.000096
(2S)-2-[[4-(biphenyl-4-yloxy)phenoxy]methyl]piperidine
Homo sapiens
-
-
0.01
(2S)-3-[[4-(dimethylamino)benzyl]sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]propanoic acid
Homo sapiens
-
IC50 above 0.01 mM
0.01
(2S)-4-[[4-(dimethylamino)benzyl]sulfanyl]-2-[[(2S)-2-methyl-3-sulfanylpropanoyl]amino]butanoic acid
Homo sapiens
-
IC50 above 0.01 mM
0.002
(2S)-N-[4-(phenylmethoxy)phenyl]-2-pyrrolidinecarboxamide hydrochloride
Homo sapiens
IC50 above 0.002 mM
0.002
(2S,3S)-2-amino-3-methyl-N-[4-(phenylmethoxy)-phenyl]pentanamide
Homo sapiens
IC50 above 0.002 mM
0.0051
(2S,4S)-1-[(2S)-2-methyl-3-sulfanylpropanoyl]-4-[(2-phenylethyl)sulfanyl]pyrrolidine-2-carboxylic acid
Homo sapiens
-
-
0.0011
(2S,4S)-1-[(2S)-2-methyl-3-sulfanylpropanoyl]-4-[(3-phenylpropyl)sulfanyl]pyrrolidine-2-carboxylic acid
Homo sapiens
-
-
0.0092
(2S,4S)-1-[(2S)-2-methyl-3-sulfanylpropanoyl]-4-[(naphthalen-1-ylmethyl)sulfanyl]pyrrolidine-2-carboxylic acid
Homo sapiens
-
-
0.0011
(2S,4S)-1-[(2S)-2-methyl-3-sulfanylpropanoyl]-4-[(naphthalen-2-ylmethyl)sulfanyl]pyrrolidine-2-carboxylic acid
Homo sapiens
-
-
0.0036
(2S,4S)-4-(benzylsulfanyl)-1-[(2S)-2-methyl-3-sulfanylpropanoyl]pyrrolidine-2-carboxylic acid
Homo sapiens
-
-
0.00084
(2S,4S)-4-[(2-methylbenzyl)sulfanyl]-1-[(2S)-2-methyl-3-sulfanylpropanoyl]pyrrolidine-2-carboxylic acid
Homo sapiens
-
-
0.01
(2S,4S)-4-[(3-methylbenzyl)sulfanyl]-1-[(2S)-2-methyl-3-sulfanylpropanoyl]pyrrolidine-2-carboxylic acid
Homo sapiens
-
IC50 above 0.01 mM
0.00012
(2S,4S)-4-[[4-(methylsulfanyl)benzyl]sulfanyl]-1-[(2S)-2-methyl-3-sulfanylpropanoyl]pyrrolidine-2-carboxylic acid
Homo sapiens
-
-
0.00029
(4R)-4-[[4-(1-methylethyl)benzyl]sulfanyl]-1-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-proline
Homo sapiens
-
-
0.000021
(4S)-4,5-diamino-N-(4-phenoxyphenyl)pentanamide
Homo sapiens
-
0.00079
(4S)-4-([2-[4-(1-methylethyl)phenyl]ethyl]sulfanyl)-1-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-proline
Homo sapiens
-
-
0.0027
(4S)-4-([3-[4-(1-methylethyl)phenyl]propyl]sulfanyl)-1-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-proline
Homo sapiens
-
-
0.00074
(4S)-4-amino-4-(2-(1,3,4-triazolyl))-N-(4-phenoxyphenyl)butanamide trifluoroacetate
Homo sapiens
-
0.000085
(4S)-4-amino-5-(1-phthalimido)-N-(4-phenoxyphenyl)pentanamide trifluoroacetate
Homo sapiens
-
0.00039
(4S)-4-amino-5-(1H-pyrrol-1-yl)-N-(4-phenoxyphenyl)pentanamide bistrifluoroacetate
Homo sapiens
-
0.00035
(4S)-4-amino-5-(2-thio-5-amino-1,3,4-thiadiazol-2-yl)-N-(4-phenoxyphenyl)pentanamide bistrifluoroacetate
Homo sapiens
-
0.000014
(4S)-4-amino-5-hydroxy-N-(4-phenoxyphenyl)pentanamide
Homo sapiens
-
0.0056
(4S)-4-amino-5-methoxy-N-(4-phenoxyphenyl)-pentanamide
Homo sapiens
-
0.000034
(4S)-4-[(4-cyclohexylbenzyl)sulfanyl]-1-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-proline
Homo sapiens
-
-
0.000031
(4S)-4-[(4-tert-butylbenzyl)sulfanyl]-1-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-proline
Homo sapiens
-
-
0.000052
(4S)-4-[[4-(1-methylethyl)benzyl]sulfanyl]-1-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-proline
Homo sapiens
-
-
0.000087
(R)-2-(4-benzylphenoxymethyl)pyrrolidine
Homo sapiens
-
0.00003
(R)-2-[4-(4-chlorophenoxy)phenoxymethyl]pyrrolidine
Homo sapiens
-
0.00023
(R)-5-(1,2-dithiolan-3-yl) pentanoic acid
Homo sapiens
pH 7.4, 37°C
0.00007
1'-[2-[4-(benzothiazol-2-yloxy)phenoxy]ethyl][1,4']bipiperidinyl-2-one
Homo sapiens
-
-
0.000016
1-(1-[2-[4-(benzothiazol-2-yloxy)phenoxy]ethyl]piperidin-4-yl)pyrrolidin-2-one
Homo sapiens
-
-
0.000013
1-(1-[2-[4-(benzothiazol-2-yloxy)phenyl]ethyl]piperidin-4-yl)pyrrolidin-2-one
Homo sapiens
-
-
0.000006
1-(1-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenoxy]ethyl]piperidin-4-yl)pyrrolidin-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.000014
1-(1-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenyl]ethyl]piperidin-4-yl)pyrrolidin-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.000058
1-(1-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)pyrrolidin-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.000003
1-(1-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)pyrrolidin-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.00022
1-(2-(4-(2-(trifluoromethyl)phenoxy)phenoxy)ethyl)pyrrolidine
Homo sapiens
-
pH 7.4, 37°C
0.00068
1-(2-(4-(2-nitrophenoxy)phenoxy)ethyl)pyrrolidine
Homo sapiens
-
pH 7.4, 37°C
0.00004
1-(2-(4-(4-chlorophenoxy)phenoxy)ethyl)pyrrolidine
Homo sapiens
-
pH 7.4, 37°C
0.00008
1-(2-(4-(4-fluorophenoxy)phenoxy)ethyl)pyrrolidine
Homo sapiens
-
pH 7.4, 37°C
0.00037
1-(2-(4-(4-nitrophenoxy)phenoxy)ethyl)pyrrolidine
Homo sapiens
-
pH 7.4, 37°C
0.00003
1-(2-(4-phenoxyphenoxy)ethyl)pyrrolidine
Homo sapiens
-
pH 7.4, 37°C
0.000007
1-(5-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenoxy]ethyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
Homo sapiens
-
pH and temperature not specified in the publication
0.000014
1-(5-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenyl]ethyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
Homo sapiens
-
pH and temperature not specified in the publication
0.000007
1-(5-[[5-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
Homo sapiens
-
pH and temperature not specified in the publication
0.00034
1-(5-[[5-([1,3]thiazolo[4,5-c]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
Homo sapiens
-
pH and temperature not specified in the publication
0.00034
1-(5-[[5-([1,3]thiazolo[5,4-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
Homo sapiens
-
pH and temperature not specified in the publication
0.000034
1-(5-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
Homo sapiens
-
pH and temperature not specified in the publication
0.0000073 - 0.000062
1-(5-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
0.00034 - 0.00237
1-(5-[[6-([1,3]thiazolo[4,5-c]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
0.0003 - 0.00213
1-(5-[[6-([1,3]thiazolo[5,4-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
0.000011
1-([4-[(1,3-benzothiazol-2-yl)oxy]phenyl]methyl)piperidine-4-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication
0.00066
1-benzyl-3-[(4-benzylphenoxy)methyl]piperazine
Homo sapiens
-
-
0.000012
1-[1-[4-(benzothiazol-2-yloxy)benzyl]piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.000049
1-[1-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)benzyl]piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.000006
1-[2-[4-(benzooxazol-2-yloxy)phenoxy]ethyl]-4-phenylpiperidin-4-ol
Homo sapiens
-
-
0.000009
1-[2-[4-(benzooxazol-2-yloxy)phenoxy]ethyl]piperidin-4-ol
Homo sapiens
-
-
0.000066
1-[2-[4-(benzothiazol-2-yloxy)phenoxy]ethyl]-4-phenylpiperidin-4-ol
Homo sapiens
-
-
0.000031
1-[2-[4-(benzothiazol-2-yloxy)phenoxy]ethyl]piperidin-4-ol
Homo sapiens
-
-
0.000013
1-[2-[4-(benzothiazol-2-yloxy)phenoxy]ethyl]piperidine-4-carboxylic acid amide
Homo sapiens
-
-
0.000008
1-[2-[4-(benzothiazol-2-yloxy)phenyl]ethyl]piperidin-4-ol
Homo sapiens
-
-
0.000028
1-[2-[4-(benzothiazol-2-yloxy)phenyl]ethyl]piperidine-4-carboxylic acid amide
Homo sapiens
-
-
0.000016
1-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenoxy]ethyl]piperidine-4-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000011
1-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenyl]ethyl]piperidine-4-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000017
1-[4-(1,3-benzothiazol-2-yloxy)benzyl]piperidine-4-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000011
1-[4-(1,3-benzothiazol-2-yloxy)benzyl]piperidine-4-carboxylic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.000034
1-[4-(benzothiazol-2-yloxy)benzyl]piperidin-4-ol
Homo sapiens
-
-
0.000011
1-[4-(benzothiazol-2-yloxy)benzyl]piperidine-4-carboxylic acid
Homo sapiens
-
-
0.000017
1-[4-(benzothiazol-2-yloxy)benzyl]piperidine-4-carboxylic acid amide
Homo sapiens
-
-
0.000006
1-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)benzyl]piperidine-4-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000733
1-[4-([1,3]thiazolo[5,4-b]pyridin-2-yloxy)benzyl]piperidine-4-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000007
1-[5-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenoxy]ethyl]hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl]ethanone
Homo sapiens
-
pH and temperature not specified in the publication
0.000006
1-[5-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenyl]ethyl]hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl]ethanone
Homo sapiens
-
pH and temperature not specified in the publication
0.000053
1-[5-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)benzyl]-2,5-diazabicyclo[2.2.1]hept-2-yl]ethanone
Homo sapiens
-
pH and temperature not specified in the publication
0.00003
1-[5-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)benzyl]hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl]ethanone
Homo sapiens
-
pH and temperature not specified in the publication
0.000014
1-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]piperidine-4-carboxylic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0000083
1-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]piperidine-4-carboxylic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.000059
2-(4-piperidin-1-ylmethylphenoxy)benzothiazole
Homo sapiens
-
-
0.015
2-(5-(2-(4-phenoxyphenoxy)ethoxy)-1H-indol-3-yl)ethanaminium chloride
Homo sapiens
-
in 10 mM sodium phosphate, pH 7.4, at 37°C
0.018
2-(5-(4-phenylbenzyloxy)-1H-indol-3-yl)ethanaminium chloride
Homo sapiens
-
in 10 mM sodium phosphate, pH 7.4, at 37°C
0.00028
2-amino-N-[4-(phenylmethoxy)phenyl]-acetamide
Homo sapiens
-
0.00001
2-bromo-4-[(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)methyl]benzoic acid
Homo sapiens
-
-
0.000006
2-fluoro-4-[(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)methyl]benzoic acid
Homo sapiens
-
-
0.000342
2-[(4-benzylphenoxy)methyl]piperazine
Homo sapiens
-
-
0.000134
2-[(4-benzylphenoxy)methyl]piperidine
Homo sapiens
-
-
0.00007
2-[(4-phenoxyphenoxy)methyl]piperidine
Homo sapiens
-
-
0.00014
2-[4-(2-azepan-1-ylethoxy)phenoxy]-1H-benzoimidazole
Homo sapiens
-
-
0.000004
2-[4-(2-azepan-1-ylethoxy)phenoxy]benzooxazole
Homo sapiens
-
-
0.000066
2-[4-(2-azepan-1-ylethoxy)phenoxy]benzothiazole
Homo sapiens
-
-
0.003
2-[4-(2-morpholin-4-ylethoxy)phenoxy]-1H-benzoimidazole
Homo sapiens
-
-
0.000058
2-[4-(2-morpholin-4-ylethoxy)phenoxy]benzooxazole
Homo sapiens
-
-
0.00035
2-[4-(2-morpholin-4-ylethoxy)phenoxy]benzothiazole
Homo sapiens
-
-
0.00011
2-[4-(2-piperidin-1-ylethoxy)phenoxy]-1H-benzoimidazole
Homo sapiens
-
-
0.000011
2-[4-(2-piperidin-1-ylethoxy)phenoxy]benzooxazole
Homo sapiens
-
-
0.000054
2-[4-(2-piperidin-1-ylethoxy)phenoxy]benzothiazole
Homo sapiens
-
-
0.000017
2-[4-(2-piperidin-1-ylethyl)phenoxy]benzothiazole
Homo sapiens
-
-
0.000084
2-[4-(2-pyrrolidin-1-ylethoxy)phenoxy]-1H-benzoimidazole
Homo sapiens
-
-
0.000007
2-[4-(2-pyrrolidin-1-ylethoxy)phenoxy]benzooxazole
Homo sapiens
-
-
0.000014
2-[4-(2-pyrrolidin-1-ylethoxy)phenoxy]benzothiazole
Homo sapiens
-
-
0.000003
2-[4-(piperidin-1-ylmethyl)phenoxy][1,3]thiazolo[4,5-b]pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.0018
2-[4-(piperidin-1-ylmethyl)phenoxy][1,3]thiazolo[4,5-c]pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.000614
2-[4-(piperidin-1-ylmethyl)phenoxy][1,3]thiazolo[5,4-c]pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.000008
2-[4-[2-(piperidin-1-yl)ethoxy]phenoxy][1,3]thiazolo[4,5-b]pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.000003
2-[4-[2-(piperidin-1-yl)ethyl]phenoxy][1,3]thiazolo[4,5-b]pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.00033
2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-5-yl]oxy]-1,3-benzothiazole
Homo sapiens
-
pH and temperature not specified in the publication
0.000066
2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-5-yl]oxy][1,3]thiazolo[4,5-b]pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.00043
2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy]-1,3-benzothiazole
Homo sapiens
-
pH and temperature not specified in the publication
0.000051
2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy][1,3]thiazolo[4,5-b]pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.00014
2-[[3-(morpholin-4-ylmethyl)-1-benzofuran-6-yl]oxy]-1,3-benzothiazole
Homo sapiens
-
pH and temperature not specified in the publication
0.000025
2-[[3-(morpholin-4-ylmethyl)-1-benzofuran-6-yl]oxy][1,3]thiazolo[4,5-b]pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.000067
2-[[3-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy]-1,3-benzothiazole
Homo sapiens
-
pH and temperature not specified in the publication
0.0000046
2-[[3-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy][1,3]thiazolo[4,5-b]pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.000011
3-(1-[2-[4-(benzothiazol-2-yloxy)phenoxy]ethyl]piperidin-4-yl)oxazolidin-2-one
Homo sapiens
-
-
0.000029
3-(1-[2-[4-(benzothiazol-2-yloxy)phenyl]ethyl]piperidin-4-yl)oxazolidin-2-one
Homo sapiens
-
-
0.0038
3-(2-(5-(4-phenylbenzyloxy)-1H-indol-3-yl)ethylamino)propanoic acid
Homo sapiens
-
in 10 mM sodium phosphate, pH 7.4, at 37°C
0.5
3-amino-3,4-dihydro-1H-naphthalen-2-one O-(2-phenylethyl)oxime
Homo sapiens
-
-
0.000007
3-fluoro-4-[(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)methyl]benzoic acid
Homo sapiens
-
-
0.000212
3-[(2R)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]piperidin-1-yl]propanoic acid
Homo sapiens
-
-
0.00001
3-[1-[4-(benzothiazol-2-yloxy)benzyl]piperidin-4-yl]oxazolidin-2-one
Homo sapiens
-
-
0.01
3-[[4-(1-methylethyl)benzyl]sulfanyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-valine
Homo sapiens
-
IC50 above 0.01 mM
0.02687
4'-O-acetyl shogoal
Homo sapiens
pH 7.4, 22°C
0.01127
4'-O-methyl shogoal
Homo sapiens
pH 7.4, 22°C
0.00725
4'-O-prenyl-[6]-gingerol
Homo sapiens
pH 7.4, 22°C
0.000047
4-((S)-2-[4-(4-chlorophenoxy)phenoxymethyl]pyrrolidin-1-yl)-butyric acid
Homo sapiens
-
0.0005
4-(4-benzylphenyl)-1,3-thiazol-2-amine
Homo sapiens
pH and temperature not specified in the publication
0.03054
4-(4-benzylphenyl)-thiazol-2-amine
Homo sapiens
pH 7.4, 22°C
0.0005
4-(4-benzylphenyl)thiazol-2-amine
Homo sapiens
at pH 7.8 and 37°C
0.00068
4-(dimethylamino)-N-[7-(hydroxyamino)-7-oxoheptyl]benzamide
0.000003
4-([(1R,5S)-3-[(4-benzylphenyl)amino]-8-azabicyclo[3.2.1]oct-8-yl]methyl)benzoic acid
Homo sapiens
-
-
0.000014
4-([(1R,5S)-3-[(4-phenoxyphenyl)amino]-8-azabicyclo[3.2.1]oct-8-yl]methyl)benzoic acid
Homo sapiens
-
-
0.000007 - 0.0001
4-([2-[(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)methyl]pyrrolidin-1-yl]methyl)benzoic acid
0.000005
4-([4-[([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)methyl]piperidin-1-yl]methyl)benzoic acid
Homo sapiens
-
-
0.000015
4-([methyl[2-(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)ethyl]amino]methyl)benzoic acid
Homo sapiens
-
-
0.00013
4-([methyl[2-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)ethyl]amino]methyl)benzoic acid
Homo sapiens
-
-
0.00033
4-([methyl[3-([2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)propyl]amino]methyl)benzoic acid
Homo sapiens
-
-
0.000003
4-([methyl[3-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)propyl]amino]methyl)benzoic acid
Homo sapiens
-
-
0.000009
4-([methyl[4-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)cyclohexyl]amino]methyl)benzoic acid
Homo sapiens
-
-
0.000007
4-([[2,2-dimethyl-3-(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)propyl](methyl)amino]methyl)benzoic acid
Homo sapiens
-
-
0.000019
4-([[3-(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)propyl]amino]methyl)benzoic acid
Homo sapiens
-
-
0.00037
4-([[3-([2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)propyl]amino]methyl)benzoic acid
Homo sapiens
-
-
0.000011
4-([[4-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)cyclohexyl]amino]methyl)benzoic acid
Homo sapiens
-
-
0.000061
4-amino-N-[4-(phenylmethoxy)phenyl]butanamide hydrochloride
Homo sapiens
-
0.0094
4-dimethylamino-N-[4-(phenylmethoxy)phenyl]-butanamide trifluoroacetate
Homo sapiens
-
0.011
4-methylamino-N-[4-(phenylmethoxy)phenyl]butanamide trifluoroacetate
Homo sapiens
-
0.000106
4-[(2R)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]piperidin-1-yl]butanoic acid
Homo sapiens
-
-
0.000047
4-[(2R)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]pyrrolidin-1-yl]butanoic acid
Homo sapiens
pH and temperature not specified in the publication
0.000049
4-[(2S)-2-([4-[4-(thiophen-3-yl)benzyl]phenoxy]methyl)piperidin-1-yl]butanoic acid
Homo sapiens
-
-
0.000053
4-[(2S)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]piperidin-1-yl]butanoic acid
Homo sapiens
-
-
0.00007
4-[(4-[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]-1,4-diazepan-1-yl)methyl]benzoic acid
Homo sapiens
-
-
0.001
4-[(4-[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]piperazin-1-yl)methyl]benzoic acid
Homo sapiens
-
-
0.000044
4-[(5-[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)methyl]benzoic acid
Homo sapiens
-
-
0.000015
4-[(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)methyl]-3-nitrobenzoic acid
Homo sapiens
-
-
0.000006
4-[(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)methyl]benzoic acid
Homo sapiens
-
-
0.000025
4-[(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)methyl]cyclohexanecarboxylic acid
Homo sapiens
-
-
0.000016
4-[(methyl[[(2R)-1-[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]piperidin-2-yl]methyl]amino)methyl]benzoic acid
Homo sapiens
-
-
0.000026
4-[(methyl[[(2R)-1-[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]pyrrolidin-2-yl]methyl]amino)methyl]benzoic acid
Homo sapiens
-
-
0.000017
4-[(methyl[[(2S)-1-[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]piperidin-2-yl]methyl]amino)methyl]benzoic acid
Homo sapiens
-
-
0.000017
4-[(methyl[[(2S)-1-[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]pyrrolidin-2-yl]methyl]amino)methyl]benzoic acid
Homo sapiens
-
-
0.000003
4-[2-(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)ethyl]benzoic acid
Homo sapiens
-
-
0.000001
4-[2-[(1R,5S)-3-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)-8-azabicyclo[3.2.1]oct-8-yl]ethyl]benzoic acid
Homo sapiens
-
-
0.000002
4-[2-[3-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)piperidin-1-yl]ethyl]benzoic acid
Homo sapiens
-
-
0.000003
4-[2-[4-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)piperidin-1-yl]ethyl]benzoic acid
Homo sapiens
-
-
0.000005
4-[[(1R,5S)-3-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
Homo sapiens
-
-
0.000008
4-[[(1R,5S)-3-([4-[4-(1,3-thiazol-2-yl)phenoxy]phenyl]amino)-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
Homo sapiens
-
-
0.000004
4-[[(1R,5S)-3-([4-[4-(1H-pyrrol-1-yl)phenoxy]phenyl]amino)-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
Homo sapiens
-
-
0.000013
4-[[(1R,5S)-3-([4-[4-(trifluoromethyl)phenoxy]phenyl]amino)-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
Homo sapiens
-
-
0.000009
4-[[(1R,5S)-3-[[4-(1,3-benzothiazol-2-yloxy)phenyl]amino]-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
Homo sapiens
-
-
0.00032
4-[[(1R,5S)-3-[[4-(2-chlorophenoxy)phenyl]amino]-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
Homo sapiens
-
-
0.000006
4-[[(1R,5S)-3-[[4-(2-fluorophenoxy)phenyl]amino]-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
Homo sapiens
-
-
0.000006
4-[[(1R,5S)-3-[[4-(4-chlorophenoxy)phenyl]amino]-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
Homo sapiens
-
-
0.00004
4-[[(1R,5S)-3-[[4-(4-fluorophenoxy)phenyl]amino]-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
Homo sapiens
-
-
0.000023
4-[[(1R,5S)-3-[[4-(4-methoxyphenoxy)phenyl]amino]-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
Homo sapiens
-
-
0.000047
4-[[(1R,5S)-3-[[4-(benzyloxy)phenyl]amino]-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
Homo sapiens
-
-
0.000005
4-[[(1R,5S)-3-[[4-(biphenyl-4-yloxy)phenyl]amino]-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
Homo sapiens
-
-
0.000075
4-[[(1R,5S)-3-[[4-(pyridin-4-ylmethyl)phenyl]amino]-8-azabicyclo[3.2.1]oct-8-yl]methyl]benzoic acid
Homo sapiens
-
-
0.000019
4-[[(3-[[2-([4-[(2R)-2-hydroxy-2-phenylethoxy]phenyl]amino)-2-oxoethyl](methyl)amino]propyl)(methyl)amino]methyl]benzoic acid
Homo sapiens
-
-
0.00012
4-[[(3R)-3-(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)pyrrolidin-1-yl]methyl]benzoic acid
Homo sapiens
-
-
0.000057
4-[[(3S)-3-(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)pyrrolidin-1-yl]methyl]benzoic acid
Homo sapiens
-
-
0.00006
4-[[3-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)piperidin-1-yl]methyl]benzoic acid
Homo sapiens
-
-
0.000007
4-[[3-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)pyrrolidin-1-yl]methyl]benzoic acid
Homo sapiens
-
-
0.00006
4-[[4-(1-[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]hydrazino)piperidin-1-yl]methyl]benzoic acid
Homo sapiens
-
-
0.00016
4-[[4-(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)azepan-1-yl]methyl]benzoic acid
Homo sapiens
-
-
0.000015
4-[[4-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)azepan-1-yl]methyl]benzoic acid
Homo sapiens
-
-
0.00003
4-[[4-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)piperidin-1-yl]methyl]benzoic acid
Homo sapiens
-
-
0.00014
4-[[methyl(1-[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]azepan-4-yl)amino]methyl]benzoic acid
Homo sapiens
-
-
0.00049
4-[[methyl(1-[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]piperidin-4-yl)amino]methyl]benzoic acid
Homo sapiens
-
-
0.000005
4-[[methyl(3-[methyl[2-([4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl]amino)-2-oxoethyl]amino]propyl)amino]methyl]benzoic acid
Homo sapiens
-
-
0.000016
4-[[[3-[(2-[[4-(2-fluorophenoxy)phenyl]amino]-2-oxoethyl)(methyl)amino]propyl](methyl)amino]methyl]benzoic acid
Homo sapiens
-
-
0.000017
4-[[[3-[(2-[[4-(4-chlorophenoxy)phenyl]amino]-2-oxoethyl)(methyl)amino]propyl](methyl)amino]methyl]benzoic acid
Homo sapiens
-
-
0.000006
4-[[[3-[(2-[[4-(4-fluorophenoxy)phenyl]amino]-2-oxoethyl)(methyl)amino]propyl](methyl)amino]methyl]benzoic acid
Homo sapiens
-
-
0.000003
4-[[[3-[[2-[(4-benzylphenyl)amino]-2-oxoethyl](methyl)amino]propyl](methyl)amino]methyl]benzoic acid
Homo sapiens
-
-
0.018
5-oxo-5-[[4-(phenylmethoxy)phenyl]amino]pentanoic acid
Homo sapiens
IC50 above 0.018 mM
0.000028
5-[(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)methyl]furan-2-carboxylic acid
Homo sapiens
-
-
0.00004
6-chloro-2-[4-(piperidin-1-ylmethyl)phenoxy][1,3]thiazolo[4,5-b]pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.000029
6-fluoro-2-[4-(piperidin-1-ylmethyl)phenoxy][1,3]thiazolo[4,5-b]pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.000033
7-methyl-2-[4-(piperidin-1-ylmethyl)phenoxy][1,3]thiazolo[4,5-b]pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.00005
acetic acid (1-[2-[4-(benzothiazol-2-yloxy)phenyl]ethyl]piperidin-4-ylcarbamoyl)methyl ester
Homo sapiens
-
-
0.000021
acetic acid [1-[4-(benzothiazol-2-yloxy)benzyl]piperidin-4-ylcarbamoyl]methyl ester
Homo sapiens
-
-
0.0004
ARM1
Homo sapiens
pH and temperature not specified in the publication
0.0003 - 0.04254
bestatin
0.03095
diacetyl-[6]-gingerol
Homo sapiens
pH 7.4, 22°C
0.231
JMC08-4
Homo sapiens
-
in 10 mM sodium phosphate, pH 7.4, at 37°C
0.0158
methyl 3-(2-(5-(3-phenoxybenzyloxy)-1H-indol-3-yl)ethylamino)propanoate
Homo sapiens
-
in 10 mM sodium phosphate, pH 7.4, at 37°C
0.0024 - 0.0076
methyl 3-(2-(5-(4-phenylbenzyloxy)-1H-indol-3-yl)ethylamino)propanoate
0.000035
N-(1-[2-[4-(benzothiazol-2-yloxy)phenyl]ethyl]piperidin-4-yl)acetamide
Homo sapiens
-
-
0.000026
N-(1-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)acetamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000037
N-(1-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)acetamide
Homo sapiens
-
pH and temperature not specified in the publication
0.01
N-(6-(2-aminophenylamino)-6-oxyhexyl)-4-methylbenzamide
0.000004
N-(8-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenoxy]ethyl]-8-azabicyclo[3.2.1]oct-3-yl)acetamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000003
N-(8-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenyl]ethyl]-8-azabicyclo[3.2.1]oct-3-yl)acetamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000073
N-[(3-endo)-8-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]-8-azabicyclo[3.2.1]oct-3-yl]acetamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000016
N-[(3-endo)-8-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-8-azabicyclo[3.2.1]oct-3-yl]acetamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000013
N-[1-[4-(1,3-benzothiazol-2-yloxy)benzyl]piperidin-4-yl]-2-hydroxyacetamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000008
N-[1-[4-(benzothiazol-2-yloxy)benzyl]piperidin-4-yl]-2-hydroxyacetamide
Homo sapiens
-
-
0.000012
N-[1-[4-(benzothiazol-2-yloxy)benzyl]piperidin-4-yl]acetamide
Homo sapiens
-
-
0.00017
N-[3(R)-[(hydroxyamino)carbonyl]-2-benzyl-1-oxopropyl]-L-alanine
Homo sapiens
pH 8.0, temperature not specified in the publication
0.000025
N-[3-(4-benzylphenoxy)propyl]-N-methyl-beta-alanine
Homo sapiens
pH and temperature not specified in the publication
0.000083
N-[8-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)benzyl]-8-azabicyclo[3.2.1]oct-3-yl]acetamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000022
N1-(2-aminoethyl)-N5-(4-phenoxyphenyl)-L-glutamamide hydrochloride
Homo sapiens
-
0.000022
N1-(2-carboxyethyl)-N5-(4-phenoxyphenyl)-L-glutamamide trifluoroacetate
Homo sapiens
-
0.00002
N1-(2-hydroxyethyl)-N5-(4-phenoxyphenyl)-L-glutamamide trifluoroacetate
Homo sapiens
-
0.000017
N1-(3-carboxypropyl)-N5-(4-phenoxyphenyl)-L-glutamamide trifluoroacetate
Homo sapiens
-
0.000019
N1-(4-carboxybutyl)-N5-(4-phenoxyphenyl)-L-glutamamide bistrifluoroacetate
Homo sapiens
-
0.000025
N1-hydroxy-N5-[4-(phenylmethoxy)phenyl]-L-glutamamide trifluoroacetate
Homo sapiens
-
0.0093
N1-[4-(phenylmethoxy)phenyl]-D-aspartamine
Homo sapiens
-
0.0072
N1-[4-(phenylmethoxy)phenyl]-D-glutamine trifluoroacetate
Homo sapiens
-
0.0054
N1-[4-(phenylmethoxy)phenyl]-L-aspartamine trifluoroacetate
Homo sapiens
-
0.002
N1-[4-(phenylmethoxy)phenyl]-L-glutamamide hydrochloride
Homo sapiens
IC50 above 0.002 mM
0.00068
N1-[4-(phenylmethoxy)phenyl]-L-glutamine trifluoroacetate
Homo sapiens
-
0.000004
N2-methyl-N-(4-phenoxyphenyl)-N2-[4-(1H-tetrazol-5-yl)benzyl]glycinamide
Homo sapiens
-
-
0.00011
N2-methyl-N2-[3-[methyl(4-oxobutyl)amino]propyl]-N-(4-phenoxyphenyl)glycinamide
Homo sapiens
-
-
0.000018
N2-methyl-N2-[4-[methyl(4-oxobutyl)amino]butyl]-N-(4-phenoxyphenyl)glycinamide
Homo sapiens
-
-
0.00016
N2-[3-(dimethylamino)propyl]-N2-methyl-N-(4-phenoxyphenyl)glycinamide
Homo sapiens
-
-
0.00009
N2-[3-[benzyl(methyl)amino]propyl]-N2-methyl-N-(4-phenoxyphenyl)glycinamide
Homo sapiens
-
-
0.000033
N2-[4-[(aminooxy)sulfinyl]benzyl]-N2-methyl-N-(4-phenoxyphenyl)glycinamide
Homo sapiens
-
-
0.0011
N4-[4-(phenylmethoxy)phenyl]-L-aspartamine trifluoroacetate
Homo sapiens
-
0.000019
N5-(4-phenoxyphenyl)-L-glutamine
Homo sapiens
-
0.018
N5-phenyl-L-glutamamide dihydrochloride
Homo sapiens
IC50 above 0.018 mM
0.0026
N5-[(4-phenoxy)-3-pyridyl]-L-glutamamide tristrifluoroacetate
Homo sapiens
-
0.00073
N5-[3-(phenylmethoxy)phenyl]-L-glutamine methyl ester
Homo sapiens
-
0.0097
N5-[4-(1H-pyrrol-1-yl)phenyl]-L-glutamamide hydrochloride
Homo sapiens
-
0.000017
N5-[4-(2-hydroxy-3-phenylpropoxy)phenyl]-L-glutamine trifluoroacetate
Homo sapiens
-
0.0028
N5-[4-(2-methylphenoxy)phenyl]-L-glutamamide hydrochloride
Homo sapiens
-
0.000018
N5-[4-(2-oxo-3-phenylpropoxy)phenyl]-L-glutamine trifluoroacetate
Homo sapiens
-
0.000046
N5-[4-(2-phenylethoxy)phenyl]-L-glutamine
Homo sapiens
-
0.00015
N5-[4-(3-methylphenoxy)phenyl]-L-glutamamide hydrochloride
Homo sapiens
-
0.000031
N5-[4-(3-phenylpropoxy)phenyl]-L-glutamine
Homo sapiens
-
0.000029
N5-[4-(4-(3-furyl)phenoxy)phenyl]-L-glutamamide trifluoroacetate
Homo sapiens
-
0.000013
N5-[4-(4-methylphenoxy)phenyl]-L-glutamamide hydrochloride
Homo sapiens
-
0.018
N5-[4-(cyclohexyloxy)phenyl]-L-glutamamide
Homo sapiens
IC50 above 0.018 mM
0.008
N5-[4-(N-methyl-N-phenylamino)phenyl]-L-glutamine methyl ester trifluoroacetate
Homo sapiens
-
0.00021
N5-[4-(N-phenylamino)phenyl]-L-glutamine bistrifluoroacetate
Homo sapiens
-
0.0016
N5-[4-(phenylmethoxy)phenyl]-D-glutamine hydrochloride
Homo sapiens
-
0.000023
N5-[4-(phenylmethoxy)phenyl]-L-glutamamide trifluoroacetate
Homo sapiens
-
0.00006
N5-[4-(phenylmethoxy)phenyl]-L-glutamine 1,1-dimethylethyl ester
Homo sapiens
-
0.00002
N5-[4-(phenylmethoxy)phenyl]-L-glutamine hemitrifluoroacetate
Homo sapiens
-
0.000039
N5-[4-(phenylmethoxy)phenyl]-L-glutamine methyl ester hydrochloride
Homo sapiens
-
0.000021
N5-[4-benzylphenyl]-L-glutamamide trifluoroacetate
Homo sapiens
-
0.018
N5-[4-methoxyphenyl]-L-glutamine methyl ester trifluoroacetate
Homo sapiens
IC50 above 0.018 mM
0.000022
N5-[4-[4-(1H-pyrrol-1-yl)phenoxy]phenyl]-L-glutamine hemitrifluoroacetate
Homo sapiens
-
0.000006
N6-[4-(4-methylphenoxy)phenyl]-L-homoglutamine trifluoroacetate
Homo sapiens
-
0.00006
RB202
Homo sapiens
pH and temperature not specified in the publication
0.000079
S-(4-cyclohexylbenzyl)-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
Homo sapiens
-
-
0.000024
S-(4-tert-butylbenzyl)-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
Homo sapiens
-
-
0.00021
S-[(4-cyclohexylphenyl)(phenyl)methyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
Homo sapiens
-
-
0.000055
S-[1-(4-cyclohexylphenyl)-1-methylethyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
Homo sapiens
-
-
0.000079
S-[1-methyl-1-[4-(1-methylethyl)phenyl]ethyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
Homo sapiens
-
-
0.00018
S-[1-[4-(1-methylethyl)phenyl]butyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
Homo sapiens
-
-
0.000055
S-[1-[4-(1-methylethyl)phenyl]ethyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
Homo sapiens
-
-
0.00051
S-[1-[4-(1-methylethyl)phenyl]pentyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
Homo sapiens
-
-
0.000067
S-[1-[4-(1-methylethyl)phenyl]propyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
Homo sapiens
-
-
0.00052
S-[2-methyl-1-[4-(1-methylethyl)phenyl]propyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
Homo sapiens
-
-
0.0009
S-[4-(diethylamino)benzyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
Homo sapiens
-
-
0.000091
S-[[4-(1-methylethyl)phenyl](phenyl)methyl]-N-[(2S)-2-methyl-3-sulfanylpropanoyl]-L-cysteine
Homo sapiens
-
-
0.000006
SC57461A
Homo sapiens
pH and temperature not specified in the publication
0.00765
suberanilohydroxamic acid
-
0.00088
[(2R)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]piperidin-1-yl]acetic acid
Homo sapiens
-
-
0.05829
[6]-gingerol
Homo sapiens
pH 7.4, 22°C
0.01287
[6]-shogaol
Homo sapiens
pH 7.4, 22°C
0.0000073
1-(5-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
Homo sapiens
-
pH and temperature not specified in the publication
0.000062
1-(5-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
Homo sapiens
-
pH and temperature not specified in the publication
0.00034
1-(5-[[6-([1,3]thiazolo[4,5-c]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
Homo sapiens
-
pH and temperature not specified in the publication
0.00237
1-(5-[[6-([1,3]thiazolo[4,5-c]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
Homo sapiens
-
pH and temperature not specified in the publication
0.0003
1-(5-[[6-([1,3]thiazolo[5,4-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
Homo sapiens
-
pH and temperature not specified in the publication
0.00213
1-(5-[[6-([1,3]thiazolo[5,4-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
Homo sapiens
-
pH and temperature not specified in the publication
0.00068
4-(dimethylamino)-N-[7-(hydroxyamino)-7-oxoheptyl]benzamide
Homo sapiens
pH and temperature not specified in the publication
0.00068
4-(dimethylamino)-N-[7-(hydroxyamino)-7-oxoheptyl]benzamide
Mus musculus
pH and temperature not specified in the publication
0.000007
4-([2-[(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)methyl]pyrrolidin-1-yl]methyl)benzoic acid
Homo sapiens
-
-
0.0001
4-([2-[(methyl[2-oxo-2-[(4-phenoxyphenyl)amino]ethyl]amino)methyl]pyrrolidin-1-yl]methyl)benzoic acid
Homo sapiens
-
-
0.01
abexinostat
Homo sapiens
above, pH and temperature not specified in the publication
0.01
abexinostat
Mus musculus
above, pH and temperature not specified in the publication
0.01
belinostat
Homo sapiens
above, pH and temperature not specified in the publication
0.01
belinostat
Mus musculus
above, pH and temperature not specified in the publication
0.0003
bestatin
Homo sapiens
pH and temperature not specified in the publication
0.0005
bestatin
Homo sapiens
-
-
0.0042
bestatin
Homo sapiens
-
in 10 mM sodium phosphate, pH 7.4, at 37°C
0.04254
bestatin
Homo sapiens
pH 7.4, 22°C
0.0036
captopril
Homo sapiens
pH and temperature not specified in the publication
0.63
captopril
Homo sapiens
-
-
0.01
CUDC-101
Homo sapiens
above, pH and temperature not specified in the publication
0.01
CUDC-101
Mus musculus
above, pH and temperature not specified in the publication
0.01
entinostat
Homo sapiens
above, pH and temperature not specified in the publication
0.01
entinostat
Mus musculus
above, pH and temperature not specified in the publication
0.01
givinostat
Homo sapiens
above, pH and temperature not specified in the publication
0.01
givinostat
Mus musculus
above, pH and temperature not specified in the publication
0.01
JNJ-26481585
Homo sapiens
above, pH and temperature not specified in the publication
0.01
JNJ-26481585
Mus musculus
above, pH and temperature not specified in the publication
0.0024
methyl 3-(2-(5-(4-phenylbenzyloxy)-1H-indol-3-yl)ethylamino)propanoate
Homo sapiens
-
in 10 mM sodium phosphate, pH 7.4, at 37°C
0.0076
methyl 3-(2-(5-(4-phenylbenzyloxy)-1H-indol-3-yl)ethylamino)propanoate
Homo sapiens
-
in 10 mM sodium phosphate, pH 7.4, at 37°C
0.01
mocetinostat
Homo sapiens
above, pH and temperature not specified in the publication
0.01
mocetinostat
Mus musculus
above, pH and temperature not specified in the publication
0.01
N-(6-(2-aminophenylamino)-6-oxyhexyl)-4-methylbenzamide
Homo sapiens
above, pH and temperature not specified in the publication
0.01
N-(6-(2-aminophenylamino)-6-oxyhexyl)-4-methylbenzamide
Mus musculus
above, pH and temperature not specified in the publication
0.01
panobinostat
Homo sapiens
above, pH and temperature not specified in the publication
0.01
panobinostat
Mus musculus
above, pH and temperature not specified in the publication
0.01
pracinostat
Homo sapiens
above, pH and temperature not specified in the publication
0.01
pracinostat
Mus musculus
above, pH and temperature not specified in the publication
0.01
resminostat
Homo sapiens
above, pH and temperature not specified in the publication
0.01
resminostat
Mus musculus
above, pH and temperature not specified in the publication
0.01
rocilinostat
Homo sapiens
above, pH and temperature not specified in the publication
0.01
rocilinostat
Mus musculus
above, pH and temperature not specified in the publication
0.01
scriptaid
Homo sapiens
above, pH and temperature not specified in the publication
0.01
scriptaid
Mus musculus
above, pH and temperature not specified in the publication
0.00765
suberanilohydroxamic acid
Homo sapiens
pH and temperature not specified in the publication
-
0.00765
suberanilohydroxamic acid
Mus musculus
pH and temperature not specified in the publication
-
0.01
trichostatin A
Homo sapiens
above, pH and temperature not specified in the publication
0.01
trichostatin A
Mus musculus
above, pH and temperature not specified in the publication
0.01
tubacin
Homo sapiens
above, pH and temperature not specified in the publication
0.01
tubacin
Mus musculus
above, pH and temperature not specified in the publication
0.01
Valproate
Homo sapiens
above, pH and temperature not specified in the publication
0.01
Valproate
Mus musculus
above, pH and temperature not specified in the publication
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malfunction
-
enzyme inhibition blocks lung inflammation, antigen uptake by lung dendritic cells and subsequent trafficking of dendritic cells to draining lymph nodes and the lung are decreased upon enzyme inhibition
malfunction
increase of leukotriene synthesis in spinal microglia produced via p38 MAPK plays a role in the generation of neuropathic pain
malfunction
-
LTA4H polymorphisms are involved in pathogenesis of asthma
malfunction
-
the enzyme is linked to inflammation diseases, especially asthma and also rheumatoid arthritis, significant role for LTB4 production in the pathogenesis of asthma, overview. LTB4 and BLT1 may be involved in the steroid resistance experienced by some patients with asthma
malfunction
-
the enzyme is linked to inflammation diseases, especially asthma and rheumatoid arthritis , mouse model, overview
malfunction
-
cigarette smoke exposure promotes the development of cigarette smoke-induced emphysema by suppressing the enzymatic activities of the LTA4H aminopeptidase in lung tissues
malfunction
leukotriene A4 hydrolase (LTA4H) regulates the balance between the anti-inflammatory lipoxins and pro-inflammatory leukotriene B4, with direct implications in tuberculosis-driven inflammation. In humans, a single nucleotide polymorphism in the LTA4H promoter which regulates its transcriptional activity (rs17525495) is identified and described to impact clinical severity of tuberculosis presentation and response to corticosteroid therapy. A higher incidence of severe tuberculosis-associated immune reconstitution inflammatorysyndrome among patients with mutant LTA4H genotypes is observed compared to the wild type, despite similar incidence of tuberculosis-associated immune reconstitution inflammatory syndrome and similar immune restoration in both groups. Steroids are effective in alleviating IRIS in all the genotypes
malfunction
imbalances in leukotriene B4 synthesis are related to several pathologic conditions
malfunction
inhibition of the LTB4 conversion ameliorates inflammation and leads to accumulation of pro-resolving Lipoxin A4 (LXA4) while inhibition of PGP degradation potentiates neutrophilic inflammation
malfunction
knocking out LTA4H significantly reduces skin cancer development in the 7,12-dimethylbenz(a)anthracene (DMBA)-initiated/12-O-tetradecanoylphorbol-13-acetate (TPA)-promoted two-stage skin cancer mouse model. LTA4H depletion dramatically decreases anchorage-dependent and -independent skin cancer cell growth by inducing cell cycle arrest at the G0/G1 phase. Depletion of LTA4H enhances p27 protein stability, which is associated with decreased phosphorylation of CDK2 at Thr160 and inhibition of the CDK2/cyclin E complex, resulting in down-regulated p27 ubiquitination. Cell phenotypes, overview
malfunction
LTB4 levels are persistently elevated in bronchoalveolar lavage fluid (BALF) of lipopolysaccharide (LPS)-induced ALI, and the leukotriene levels in pulmonary edema fluid are significantly higher in ALI patients compared to control patients with hydrostatic pulmonary edema. In addition, LTB4 level is increased in lung homogenates, and BALF of patients with IPF and the level of LTB4 correlate with the extent of fibrosis in histological sections
malfunction
silencing of LTA4H translation by shRNA in HCT116 human colorectal carcinoma cells suppresses cell growth, stimulation of the aminopeptidase (AP) activity of LTA4H enhanced colony formation in HCT116 cells, indicating that LTA4H activity is associated with the malignant potential of CRC cells
malfunction
-
enzyme inhibition blocks lung inflammation, antigen uptake by lung dendritic cells and subsequent trafficking of dendritic cells to draining lymph nodes and the lung are decreased upon enzyme inhibition
-
malfunction
-
the enzyme is linked to inflammation diseases, especially asthma and rheumatoid arthritis , mouse model, overview
-
metabolism
-
leukotriene A4 hydrolase catalyzes the final step in the synthesis of leukotriene B4, LTB4, a potent chemoattractant and proinflammatory eicosanoid
metabolism
-
leukotriene A4 hydrolase catalyzes the final step in the synthesis of leukotriene B4, LTB4, a potent chemoattractant and proinflammatory eicosanoid
metabolism
-
leukotriene A4 hydrolase is a key enzyme in the leukotriene pathway, which hydrolyzes leukotriene A4 to leukotriene B4, a proinflammatory mediator
metabolism
-
LTA4H catalyzes the last step in the synthesis of the pro-inflammatory molecule leukotriene B4
metabolism
-
LTA4H catalyzes the last step in the synthesis of the pro-inflammatory molecule leukotriene B4
metabolism
-
LTA4H catalyzes the last step in the synthesis of the pro-inflammatory molecule leukotriene B4
metabolism
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LTA4H in reactive oxygen species detoxification pathways and eicosanoid biosynthetic pathways, overview
metabolism
LTA4H is a key enzyme in the leukotriene pathway, which catalyzes the final and rate-determining step in the synthesis of LTB4
metabolism
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no difference in LTA4 hydrolase expression in patients with naturally occurring allergic rhinitis compared to controls, suggesting that LTB4 is less important chronically or that LTA4 hydrolase is not the rate-limiting step in its synthesis
metabolism
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the enzyme is involved in the leukotriene metabolism. In the leukotriene biosynthesis, cells expressing 5-lipoxygenase form LTA4 and transfer it to cells expressing LTA4 hydrolase or LTC4 synthase to produce LTB4 or LTC4
metabolism
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the enzyme takes part in the pathway for the conversion of arachidonic acid to eicosanoids, overview
metabolism
leukotriene A4 hydrolase participates in the metabolism of lipid mediators and peptides
metabolism
the enzyme catalyzes the final rate-limiting step in the biosynthesis of leukotriene B4
metabolism
the enzyme is involved in the LTA4H/LTB4 biosynthesis pathway, overview. 5-Lipoxygenase catalyzes the conversion of to (5S)-hydroperoxy-6-trans-8,11,14-cis-eicosatetraenoic (5-HpETE) to LTA4 in the presence of 5-lipoxygenase-activating protein (FLAP). LTA4 is unstable and hydrolyzes to LTB4 by LTA4H. LTB4 then activates the G protein-coupled receptors BLT1 and BLT2. Biosynthesis of LTB4 typically occurs in a cell that expresses both 5-LOX and LTA4H. LTA4H is expressed in cells and tissues without 5-LOX activity, indicating that they cannot produce the substrate for LTA4H, such as in erythrocytes and endothelial cells. LTB4 biosynthesis pathway and cancer development, overview
physiological function
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leukotriene A4 hydrolase is involved in recruitment of both CD4+ and CD8+ T cells to inflammation sites, as well as trafficking of dendritic cells to draining lymph nodes
physiological function
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leukotrienes are involved in antiinflammation via eicosanoids, lipid mediators derived from arachidonic acid including the proinflammatory leukotrienes as well as the anti-inflammatory lipoxins, complex interplay between proinflammatory leukotrienes and antiinflammatory lipoxins. The enzyme is important in the balance between proinflammatory and anti-inflammatory responses in tuberculosis
physiological function
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the enzyme is involved in the leukotriene metabolism, leukotrienes are lipid mediators of inflammation formed by enzymatic oxidation of arachidonic acid
physiological function
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the correlations between leukotriene B4 and the enzyme have significance on resistance and development of arthritis
physiological function
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the enzyme plays a key role in innate immune responses
physiological function
leukotriene A4 hydrolase (LTA4H) regulates the balance between the anti-inflammatory lipoxins and pro-inflammatory leukotriene B4, with direct implications in tuberculosis-driven inflammation. In humans, a single nucleotide polymorphism in the LTA4H promoter which regulates its transcriptional activity (rs17525495) is identified and described to impact clinical severity of tuberculosis presentation and response to corticosteroid therapy. A higher incidence of severe tuberculosis-associated immune reconstitution inflammatorysyndrome among patients with mutant LTA4H genotypes is observed compared to the wild type, despite similar incidence of tuberculosis-associated immune reconstitution inflammatory syndrome and similar immune restoration in both groups. Steroids are effective in alleviating IRIS in all the genotypes
physiological function
ELR1 CXC chemokines (e.g. interleukin-8) bind to CXCR1 and CXCR2 receptors expressed on neutrophils, and attract them to sites of inflammation. Ensuing degradation of collagen by neutrophil-derived proteases generates many tripeptide proline-glycine-proline (PGP) peptides that mimic key sequences found in ELR1 CXC chemokines, and act as a potent neutrophil chemoattractant. Extracellular leukotriene (LT) A4 hydrolase (LTA4H) degrades PGP and resolves neutrophilic inflammation, whereas intracellular epoxide hydrolase function (EC 3.3.2.10) of the same enzyme converts LTA4 to LTB4. LTB4 is a proinflammatory lipid mediator capable of recruiting and activating an array of cells, including neutrophils. The intracellular activity of LTA4H within leukocytes can generate the lipid mediator LTB4 that can also promote neutrophil recruitment by binding to LTB4 receptor (BLT1).Thus, LTA4H exhibits opposing pro- and anti-inflammatory roles that govern neutrophil recruitment. Cigarette smoke disrupts leukotriene (LT) A4 hydrolase (LTA4H)-mediated resolution of pulmonary neutrophilic inflammation. In response to infection or injury, resident cells within the lung will release chemoattractants that will promote neutrophil recruitment from the vasculature and into the tissue. Epithelial cells and alveolar macrophages, for example, may release IL-8 that will bind to CXCR1/2 on the surface of the neutrophil and promote recruitment. Cigarette smoke chemically acetylates PGP, enhancing its chemotactic activity and protecting it from degradation by LTA4H. Second, biochemical and preliminary murine studies suggest that cigarette smoke can selectively abrogate the peptidase activity of LTA4H, with minimal effect on the hydrolase activity. Thus, cigarette smoke pushes LTA4H toward a uniquely proinflammatory phenotype, whereby LTB4 and PGP together induce increased pulmonary neutrophilic inflammation. Acrolein in cigarette smoke in part inhibits LTA4H peptidase activity. Acrolein, derived from cigarette smoke or physiologically during inflammation (lipid peroxidation, metabolism of threonine or spermine), can inhibit LTA4H-mediated degradation of PGP, allowing the peptide to accumulate and maintain neutrophilic inflammation. LTA4H enzyme inhibitors may fail to distinguish between the opposing activities of the enzyme, and could inadvertently lead to persistent neutrophilia
physiological function
enzyme leukotriene A4 hydrolase (LTA4H) is a bifunctional enzyme with epoxide hydrolase (EH) and aminopeptidase (AP) activities
physiological function
enzyme leukotriene A4 hydrolase (LTA4H) is characterized as a bifunctional enzyme with epoxide hydrolase (EH) and aminopeptidase (AP) activities. LTA4H plays a critical role in modulating inflammation by producing LTB4 via its EH activity. LTA4H also has putative roles in cancer development
physiological function
enzyme leukotriene A4 hydrolase (LTA4H) is characterized as a bifunctional enzyme with epoxide hydrolase (EH) and aminopeptidase (AP) activities. LTA4H plays a critical role in modulating inflammation by producing LTB4 via its EH activity. LTA4H also has putative roles in cancer development. An increased level of leukotriene B4 (LTB4), which is biosynthesized by leukotriene A4 hydrolase (LTA4H), is implicated in several types of cancer, including colon and prostate cancer. LTB4 is formed from an unstable intermediate, leukotriene A4 (LTA4). The aminopeptidase activity substrate proline-glycine-proline (PGP) generated from collagen acts as a proinflammatory factor by neutrophilic chemotaxis. Enzyme LTA4H precisely controls EH activity toward LTB4 and AP activity toward PGP
physiological function
enzyme leukotriene A4 hydrolase (LTA4H) is characterized as a bifunctional enzyme with epoxide hydrolase (EH) and aminopeptidase (AP) activities. LTA4H plays a critical role in modulating inflammation by producing LTB4 via its epoxide hydrolase activity. LTA4H also has putative roles in cancer development. Enzyme LTA4H precisely controls EH activity toward LTB4 and AP activity toward PGP
physiological function
in the eicosanoid metabolic processes, leukotriene A4 hydrolase (LTA4H) is an epoxide hydrolase that catalyzes conversion of the unstable allelic epoxide leukotriene A4 (LTA4) to leukotriene B4 (LTB4), which is known to have classical biological functions including chemotaxis, endothelial adherence, and activation of leukocytes. It exerts its actions through a transmembrane protein receptor, LTB4 receptor type 1 (BLT1). The leukotriene A4 hydrolase (LTA4H) pathway plays a role in colorectal cancer (CRC). High expression of LTA4H and leukotriene B4 receptor type 1 (BLT1) are also associated with CRC survival probability
physiological function
in the eicosanoid metabolic processes, leukotriene A4 hydrolase (LTA4H) is an epoxide hydrolase that catalyzes conversion of the unstable allelic epoxide leukotriene A4 (LTA4) to leukotriene B4 (LTB4), which is known to have classical biological functions including chemotaxis, endothelial adherence, and activation of leukocytes. It exerts its actions through a transmembrane protein receptor, LTB4 receptor type 1 (BLT1). The leukotriene A4 hydrolase (LTA4H) pathway plays a role in colorectal cancer (CRC). High expression of LTA4H and leukotriene B4 receptor type 1 (BLT1) are also associated with CRC survival probability. High expression of LTA4H and BLT1 negatively correlate with CRC patient survival probability
physiological function
leukotriene A4 hydrolase (LTA4H) is a bifunctional enzyme that exhibits LTA4H and aminopeptidase activities, it is a key enzyme in the biosynthesis of leukotriene B4 (LTB4). LTA4H is well-known to regulate chemotactic activity of human neutrophils. LTB4 is secreted by neutrophils at inflammation sites in response to formyl peptides, playing an important role in neutrophil activation and migration to formyl peptides
physiological function
leukotriene A4 hydrolase (LTA4H) is a bifunctional zinc metalloenzyme overexpressed in several human cancers. LTA4H regulates cell cycle and skin carcinogenesis. LTA4H is a key modulator of cell cycle through its negative effect on p27 expression. LTA4H mediates the G0/G1 cell cycle phase through p27 proteasome degradation and is is implicated in cell growth, cell cycle distribution. LTA4H mediates p27 stability through LTB4/BLT1 pathway. LTA4H and BLT1 influence the formation of the CDK2/cyclin E complex and the phosphorylation of CDK2 at Thr160
physiological function
leukotriene A4 hydrolase (LTA4H) is a key enzyme in the biosynthesis of leukotriene B4 (LTB4)
physiological function
leukotriene A4 hydrolase is a soluble enzyme with epoxide hydrolase and aminopeptidase activities catalysing the conversion of leukotriene A4 to leukotriene B4 and the hydrolysis of the peptide proline-glycine-proline. Bifunctional LTA4H shows two catalytic activities, aminopeptidase activity hydrolysing the tripeptide proline-glycine-proline (PGP), and epoxide hydrolase activity on leukotriene A4 (LTA4) generating leukotriene B4 (LTB4), a potent inducer of macrophage, T-lymphocyte and neutrophil chemotaxis
physiological function
the human leukotriene A4 hydrolase (LTA4H) is a 69 kDa protein involved in the arachidonic acid cascade. LTA4H converts leukotriene A4 (LTA4) into leukotriene B4 (LTB4).1 LTB4 triggers the adhesion and aggregation of leukocytes in the endothelium2 and acts as an attractant for different leukocytes (monocytes, neutrophils, macrophages, and dendritic cells). The overproduction of LTB4 has been associated with different pathological conditions and diseases. The leukotriene A4 hydrolase (LTA4H) is a bifunctional enzyme, containing a peptidase and a hydrolase activity both activities having opposing functions regulating inflammatory response. The hydrolase activity is responsible for the conversion of leukotriene A4 to pro-inflammatory leukotriene B4
physiological function
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leukotriene A4 hydrolase is involved in recruitment of both CD4+ and CD8+ T cells to inflammation sites, as well as trafficking of dendritic cells to draining lymph nodes
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physiological function
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in the eicosanoid metabolic processes, leukotriene A4 hydrolase (LTA4H) is an epoxide hydrolase that catalyzes conversion of the unstable allelic epoxide leukotriene A4 (LTA4) to leukotriene B4 (LTB4), which is known to have classical biological functions including chemotaxis, endothelial adherence, and activation of leukocytes. It exerts its actions through a transmembrane protein receptor, LTB4 receptor type 1 (BLT1). The leukotriene A4 hydrolase (LTA4H) pathway plays a role in colorectal cancer (CRC). High expression of LTA4H and leukotriene B4 receptor type 1 (BLT1) are also associated with CRC survival probability
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additional information
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HIV-1 transforms the monocyte plasma membrane proteome including also cytosolic LTA4H, the process is linked to cell viability, overview
additional information
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protection from both tuberculosis and multibacillary leprosy is associated with heterozygosity for LTA4H polymorphisms
additional information
binding pocket of the apo LTA4H protein (PDB entry 5FWQ) with bound Zn2+, overview
additional information
enzyme residues E271, D375, Arg563, and Lys555 are involved in enzyme-substrate interactions
additional information
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enzyme residues E271, D375, Arg563, and Lys555 are involved in enzyme-substrate interactions
additional information
eosinophils express LTA4 hydrolase and release LTB4. In addition to neutrophils, epithelial cells, and certain phagocytes, eosinophils are classified as contributors to the generation of the inflammatory mediator LTB4. Leukotriene B4 (LTB4) is a potent neutrophil chemoattractant, and this mediator might be an alternative to the Th17 axis as a potential mechanism leading to airway neutrophils. The enzyme might play a role in asthma
additional information
LTA4H folds into three domains and creates a deep cleft harboring the catalytic Zn2+ site, forming the active site with an L-shaped hydrophobic pocket deep into the protein
additional information
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LTA4H folds into three domains and creates a deep cleft harboring the catalytic Zn2+ site, forming the active site with an L-shaped hydrophobic pocket deep into the protein
additional information
LTA4H folds into three domains and creates a deep cleft harboring the catalytic Zn2+ site, forming the active site with an L-shaped hydrophobic pocket deep into the protein
additional information
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LTA4H folds into three domains and creates a deep cleft harboring the catalytic Zn2+ site, forming the active site with an L-shaped hydrophobic pocket deep into the protein
additional information
the enzyme has two catalytic pockets, a hydrophobic domain that recognizes the lipophilic hydrocarbon chain of LTA4 and a hydrophilic domain that recognizes the N-terminal region of PGP. Both domains converge in a common catalytic zone where the carboxylate group of each substrate interacts with alkaline amino acids in the protein. Thus, different catalytic pockets for separate activities share a carboxylate group recognition zone
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