General Information of the Protein
Protein ID
PT02129
Protein Name
Leukotriene A-4 hydrolase
Secondarily
Protein Name
Leukotriene A(4) hydrolase
Tripeptide aminopeptidase LTA4H
Gene Name
LTA4H
Secondarily
Gene Name
LTA4
Sequence
MPEIVDTCSLASPASVCRTKHLHLRCSVDFTRRTLTGTAALTVQSQEDNLRSLVLDTKDLTIEKVVINGQEVKYALGERQSYKGSPMEISLPIALSKNQEIVIEISFETSPKSSALQWLTPEQTSGKEHPYLFSQCQAIHCRAILPCQDTPSVKLTYTAEVSVPKELVALMSAIRDGETPDPEDPSRKIYKFIQKVPIPCYLIALVVGALESRQIGPRTLVWSEKEQVEKSAYEFSETESMLKIAEDLGGPYVWGQYDLLVLPPSFPYGGMENPCLTFVTPTLLAGDKSLSNVIAHEISHSWTGNLVTNKTWDHFWLNEGHTVYLERHICGRLFGEKFRHFNALGGWGELQNSVKTFGETHPFTKLVVDLTDIDPDVAYSSVPYEKGFALLFYLEQLLGGPEIFLGFLKAYVEKFSYKSITTDDWKDFLYSYFKDKVDVLNQVDWNAWLYSPGLPPIKPNYDMTLTNACIALSQRWITAKEDDLNSFNATDLKDLSSHQLNEFLAQTLQRAPLPLGHIKRMQEVYNFNAINNSEIRFRWLRLCIQSKWEDAIPLALKMATEQGRMKFTRPLFKDLAAFDKSHDQAVRTYQEHKASMHPVTAMLVGKDLKVD
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Protease
>
Metallo protease
>
Metallo protease MAE clan
>
Metallo protease M1 family
Function
Bifunctional zinc metalloenzyme that comprises both epoxide hydrolase (EH) and aminopeptidase activities. Acts as an epoxide hydrolase to catalyze the conversion of LTA4 to the pro-inflammatory mediator leukotriene B4 (LTB4) (PubMed:11917124, PubMed:12207002, PubMed:15078870, PubMed:18804029, PubMed:1897988, PubMed:1975494, PubMed:2244921). Has also aminopeptidase activity, with high affinity for N-terminal arginines of various synthetic tripeptides (PubMed:20813919, PubMed:18804029). In addition to its pro-inflammatory EH activity, may also counteract inflammation by its aminopeptidase activity, which inactivates by cleavage another neutrophil attractant, the tripeptide Pro-Gly-Pro (PGP), a bioactive fragment of collagen generated by the action of matrix metalloproteinase-9 (MMP9) and prolylendopeptidase (PREPL) (PubMed:20813919, PubMed:24591641). Involved also in the biosynthesis of resolvin E1 and 18S-resolvin E1 from eicosapentaenoic acid, two lipid mediators that show potent anti-inflammatory and pro-resolving actions (PubMed:21206090).
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Uniprot ID
Primary ID:
P09960

Secondarily ID:
B4DNQ9
F8VV40
Q6IAT6
Q9UCT7
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Ensembl ID
ENSG00000111144
HGNC ID
HGNC:6710
Subcellular Location
Cytoplasm
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0461979
 Compound Info 
N-[8-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenyl]ethyl]-8-azabicyclo[3.2.1]octan-3-yl]acetamide
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C23H26N4O2S
  1
1
IC50 = 0.3 nM
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CP0493620
 Compound Info 
N-[8-[[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenyl]methyl]-8-azabicyclo[3.2.1]octan-3-yl]acetamide
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C22H24N4O2S
  1
1
IC50 = 1 nM
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CP0127823
 Compound Info 
N-[(1S,5R)-8-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-8-azabicyclo[3.2.1]octan-3-yl]acetamide
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C24H24N4O3S
  1
1
IC50 = 1.6 nM
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CP0428259
 Compound Info 
2-[4-(2-piperidin-1-ylethyl)phenoxy]-[1,3]thiazolo[4,5-b]pyridine
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C19H21N3OS
  1
1
IC50 = 3 nM
 Bioactivity Info 
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CP0538410
 Compound Info 
2-[4-(piperidin-1-ylmethyl)phenoxy]-[1,3]thiazolo[4,5-b]pyridine
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C18H19N3OS
  1
1
IC50 = 3 nM
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CP0540912
 Compound Info 
1-[2-[[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenyl]methyl]-1,3,3a,4,6,6a-hexahydropyrrolo[3,4-c]pyrrol-5-yl]ethanone
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C21H22N4O2S
  1
1
IC50 = 3 nM
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CP0285661
 Compound Info 
1-[1-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl]pyrrolidin-2-one
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C24H24N4O3S
  1
1
IC50 = 3 nM
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CP0285665
 Compound Info 
N-[1-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl]acetamide
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C22H22N4O3S
  1
1
IC50 = 3.7 nM
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CP0538409
 Compound Info 
N-[8-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenoxy]ethyl]-8-azabicyclo[3.2.1]octan-3-yl]acetamide
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C23H26N4O3S
  1
1
IC50 = 4 nM
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CP0229548
 Compound Info 
2-[[3-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy]-[1,3]thiazolo[4,5-b]pyridine
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C20H19N3O2S
  1
1
IC50 = 4.6 nM
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CP0461978
 Compound Info 
1-[5-[[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenyl]methyl]-2,5-diazabicyclo[2.2.1]heptan-2-yl]ethanone
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C20H20N4O2S
  1
1
IC50 = 5 nM
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CP0461980
 Compound Info 
1-[2-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenyl]ethyl]-1,3,3a,4,6,6a-hexahydropyrrolo[3,4-c]pyrrol-5-yl]ethanone
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C22H24N4O2S
  1
1
IC50 = 6 nM
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CP0488516
 Compound Info 
1-[[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenyl]methyl]piperidine-4-carboxamide
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C19H20N4O2S
  1
1
IC50 = 6 nM
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CP0495589
 Compound Info 
1-[1-[[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenyl]methyl]piperidin-4-yl]pyrrolidin-2-one
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C22H24N4O2S
  1
1
IC50 = 6 nM
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CP0499756
 Compound Info 
1-[1-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenoxy]ethyl]piperidin-4-yl]pyrrolidin-2-one
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C23H26N4O3S
  1
1
IC50 = 6 nM
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CP0461982
 Compound Info 
1-[2-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenoxy]ethyl]-1,3,3a,4,6,6a-hexahydropyrrolo[3,4-c]pyrrol-5-yl]ethanone
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C22H24N4O3S
  1
1
IC50 = 7 nM
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CP0507762
 Compound Info 
1-[5-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenoxy]ethyl]-2,5-diazabicyclo[2.2.1]heptan-2-yl]ethanone
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C21H22N4O3S
  1
1
IC50 = 7 nM
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CP0323958
 Compound Info 
1-[5-[[5-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-2-yl]methyl]-2,5-diazabicyclo[2.2.1]heptan-2-yl]ethanone
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C22H20N4O3S
  1
1
IC50 = 7 nM
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CP0127970
 Compound Info 
1-[(1S,4S)-5-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]heptan-2-yl]ethanone
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C22H20N4O3S
  1
1
IC50 = 7.3 nM
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CP0264046
 Compound Info 
1-[5-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]heptan-2-yl]ethanone
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C22H20N4O3S
  1
1
IC50 = 7.3 nM
 Bioactivity Info 
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CP0318764
 Compound Info 
N-[(1S,5R)-8-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]-8-azabicyclo[3.2.1]octan-3-yl]acetamide
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C25H25N3O3S
  1
1
IC50 = 7.3 nM
 Bioactivity Info 
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CP0428261
 Compound Info 
2-[4-(2-piperidin-1-ylethoxy)phenoxy]-[1,3]thiazolo[4,5-b]pyridine
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C19H21N3O2S
  1
1
IC50 = 8 nM
 Bioactivity Info 
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CP0285666
 Compound Info 
1-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]piperidine-4-carboxylic acid
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C21H19N3O4S
  1
1
IC50 = 8.3 nM
 Bioactivity Info 
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CP0127969
 Compound Info 
1-(1-{2-[4-(1,3-benzothiazol-2-yloxy)phenoxy]ethyl}piperidin-4-yl)pyrrolidin-2-one
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C24H27N3O3S
  1
1
IC50 = 9.7 nM
 Bioactivity Info 
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CP0499395
 Compound Info 
1-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenyl]ethyl]piperidine-4-carboxamide
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C20H22N4O2S
  1
1
IC50 = 11 nM
 Bioactivity Info 
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CP0428258
 Compound Info 
1-[5-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenyl]ethyl]-2,5-diazabicyclo[2.2.1]heptan-2-yl]ethanone
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C21H22N4O2S
  1
1
IC50 = 14 nM
 Bioactivity Info 
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CP0461981
 Compound Info 
1-[1-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenyl]ethyl]piperidin-4-yl]pyrrolidin-2-one
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C23H26N4O2S
  1
1
IC50 = 14 nM
 Bioactivity Info 
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CP0120906
 Compound Info 
1-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]piperidine-4-carboxylic acid
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C22H20N2O4S
  1
1
IC50 = 14 nM
 Bioactivity Info 
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CP0461983
 Compound Info 
1-[2-[4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)phenoxy]ethyl]piperidine-4-carboxamide
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C20H22N4O3S
  1
1
IC50 = 16 nM
 Bioactivity Info 
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CP0120907
 Compound Info 
4-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]morpholine
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C19H17N3O3S
  1
1
IC50 = 25 nM
 Bioactivity Info 
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CP0301676
 Compound Info 
N-[1-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl]acetamide
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C23H23N3O3S
  1
1
IC50 = 26 nM
 Bioactivity Info 
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CP0507764
 Compound Info 
6-fluoro-2-[4-(piperidin-1-ylmethyl)phenoxy]-[1,3]thiazolo[4,5-b]pyridine
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C18H18FN3OS
  1
1
IC50 = 29 nM
 Bioactivity Info 
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CP0461984
 Compound Info 
7-methyl-2-[4-(piperidin-1-ylmethyl)phenoxy]-[1,3]thiazolo[4,5-b]pyridine
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C19H21N3OS
  1
1
IC50 = 33 nM
 Bioactivity Info 
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CP0285663
 Compound Info 
1-[(1S,4S)-5-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]heptan-2-yl]ethanone
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C23H21N3O3S
  1
1
IC50 = 34 nM
 Bioactivity Info 
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CP0507766
 Compound Info 
6-chloro-2-[4-(piperidin-1-ylmethyl)phenoxy]-[1,3]thiazolo[4,5-b]pyridine
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C18H18ClN3OS
  1
1
IC50 = 40 nM
 Bioactivity Info 
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CP0193311
 Compound Info 
2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy]-[1,3]thiazolo[4,5-b]pyridine
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C20H19N3O2S
  1
1
IC50 = 51 nM
 Bioactivity Info 
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CP0229547
 Compound Info 
1-[1-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl]pyrrolidin-2-one
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C25H25N3O3S
  1
1
IC50 = 58 nM
 Bioactivity Info 
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CP0239711
 Compound Info 
1-[5-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-2-yl]methyl]-2,5-diazabicyclo[2.2.1]heptan-2-yl]ethanone
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C22H20N4O3S
  1
1
IC50 = 62 nM
 Bioactivity Info 
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CP0323959
 Compound Info 
2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-5-yl]oxy]-[1,3]thiazolo[4,5-b]pyridine
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C20H19N3O2S
  1
1
IC50 = 66 nM
 Bioactivity Info 
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CP0159583
 Compound Info 
2-[[3-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy]-1,3-benzothiazole
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C21H20N2O2S
  1
1
IC50 = 67 nM
 Bioactivity Info 
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CP0188288
 Compound Info 
4-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]morpholine
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C20H18N2O3S
  1
1
IC50 = 140 nM
 Bioactivity Info 
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CP0239709
 Compound Info 
1-[5-[[6-([1,3]thiazolo[5,4-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]heptan-2-yl]ethanone
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C22H20N4O3S
  1
1
IC50 = 300 nM
 Bioactivity Info 
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CP0155883
 Compound Info 
2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-5-yl]oxy]-1,3-benzothiazole
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C21H20N2O2S
  1
1
IC50 = 330 nM
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CP0264047
 Compound Info 
1-[5-[[5-([1,3]thiazolo[5,4-b]pyridin-2-yloxy)-1-benzofuran-2-yl]methyl]-2,5-diazabicyclo[2.2.1]heptan-2-yl]ethanone
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C22H20N4O3S
  1
1
IC50 = 340 nM
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CP0264048
 Compound Info 
1-[5-[[5-([1,3]thiazolo[4,5-c]pyridin-2-yloxy)-1-benzofuran-2-yl]methyl]-2,5-diazabicyclo[2.2.1]heptan-2-yl]ethanone
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C22H20N4O3S
  1
1
IC50 = 340 nM
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CP0285662
 Compound Info 
1-[5-[[6-([1,3]thiazolo[4,5-c]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]heptan-2-yl]ethanone
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C22H20N4O3S
  1
1
IC50 = 340 nM
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CP0301677
 Compound Info 
2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy]-1,3-benzothiazole
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C21H20N2O2S
  1
1
IC50 = 430 nM
 Bioactivity Info 
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CP0428262
 Compound Info 
2-[4-(piperidin-1-ylmethyl)phenoxy]-[1,3]thiazolo[5,4-c]pyridine
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C18H19N3OS
  1
1
IC50 = 614 nM
 Bioactivity Info 
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CP0499396
 Compound Info 
1-[[4-([1,3]thiazolo[5,4-b]pyridin-2-yloxy)phenyl]methyl]piperidine-4-carboxamide
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C19H20N4O2S
  1
1
IC50 = 733 nM
 Bioactivity Info 
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CP0440954
 Compound Info 
2-[4-(piperidin-1-ylmethyl)phenoxy]-[1,3]thiazolo[4,5-c]pyridine
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C18H19N3OS
  1
1
IC50 = 1800 nM
 Bioactivity Info 
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CP0120905
 Compound Info 
1-[5-[[6-([1,3]thiazolo[5,4-b]pyridin-2-yloxy)-1-benzofuran-2-yl]methyl]-2,5-diazabicyclo[2.2.1]heptan-2-yl]ethanone
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C22H20N4O3S
  1
1
IC50 = 2130 nM
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CP0127821
 Compound Info 
1-[5-[[6-([1,3]thiazolo[4,5-c]pyridin-2-yloxy)-1-benzofuran-2-yl]methyl]-2,5-diazabicyclo[2.2.1]heptan-2-yl]ethanone
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C22H20N4O3S
  1
1
IC50 = 2370 nM
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0127969
 Compound Info 
1-(1-{2-[4-(1,3-benzothiazol-2-yloxy)phenoxy]ethyl}piperidin-4-yl)pyrrolidin-2-one
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C24H27N3O3S
  2
1 IC50 = 16 nM
2 IC50 = 365 nM
CP0285661
 Compound Info 
1-[1-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl]pyrrolidin-2-one
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C24H24N4O3S
  1
1 IC50 = 61 nM
Clinical Information about the Protein
Target 1 ( Leukotriene A-4 hydrolase (LTA4H) )
Target Type Successful Target
Disease 4 Target-related Diseases  4
1 Acute myeloid leukaemia [ICD-11: 2A60]
2 Ulcerative colitis [ICD-11: DD71]
3 Chronic blistering skin disorder [ICD-11: ME63.3]
4 Inflammation [ICD-11: 1A00-CA43.1]
Approved Drug(s) 1 Approved Drug  1
1 Bestatin
 Drug Info 
Approved
Acute myeloid leukaemia
Clinical Trial Drug(s) 2 Clinical Trial Drugs  2
1 LYS006
 Drug Info 
Phase 2
Ulcerative colitis
2 Acebilustat
 Drug Info 
Phase 1
Chronic blistering skin disorder
Investigative Drug(s) 1 Investigative Drug  1
1 SA-6541
 Drug Info 
Investigative
Inflammation