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Literature summary extracted from

  • Eccles, W.; Blevitt, J.M.; Booker, J.N.; Chrovian, C.C.; Crawford, S.; de Leon, A.R.; Deng, X.; Fourie, A.M.; Grice, C.A.; Herman, K.; Karlsson, L.; Kearney, A.M.; Lee-Dutra, A.; Liang, J.; Luna, R.; Pippel, D.; Rao, N.; Riley, J.P.; Santillan, A.; Savall, B.; Tanis, V.M.; Xue, X.; Young, A.L.
    Identification of benzofuran central cores for the inhibition of leukotriene A4 hydrolase (2013), Bioorg. Med. Chem. Lett., 23, 811-815.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.3.2.6 1-(1-[2-[4-(1,3-benzothiazol-2-yloxy)phenoxy]ethyl]piperidin-4-yl)pyrrolidin-2-one
-
 Homo sapiens
3.3.2.6 1-(1-[2-[4-(1,3-benzothiazol-2-yloxy)phenoxy]ethyl]piperidin-4-yl)pyrrolidin-2-one
-
 Mus musculus
3.3.2.6 1-(1-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)pyrrolidin-2-one
-
 Homo sapiens
3.3.2.6 1-(1-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)pyrrolidin-2-one
-
 Mus musculus
3.3.2.6 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
3.3.2.6 1-(1-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)pyrrolidin-2-one
-
 Mus musculus
3.3.2.6 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
3.3.2.6 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
-
 Mus musculus
3.3.2.6 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
3.3.2.6 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
-
 Mus musculus
3.3.2.6 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
3.3.2.6 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
-
 Mus musculus
3.3.2.6 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
3.3.2.6 1-(5-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
-
 Mus musculus
3.3.2.6 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
3.3.2.6 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
-
 Mus musculus
3.3.2.6 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
3.3.2.6 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
-
 Mus musculus
3.3.2.6 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
3.3.2.6 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
-
 Mus musculus
3.3.2.6 1-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]piperidine-4-carboxylic acid
-
 Homo sapiens
3.3.2.6 1-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]piperidine-4-carboxylic acid
-
 Mus musculus
3.3.2.6 1-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]piperidine-4-carboxylic acid
-
 Homo sapiens
3.3.2.6 1-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]piperidine-4-carboxylic acid
-
 Mus musculus
3.3.2.6 2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-5-yl]oxy]-1,3-benzothiazole
-
 Homo sapiens
3.3.2.6 2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-5-yl]oxy]-1,3-benzothiazole
-
 Mus musculus
3.3.2.6 2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-5-yl]oxy][1,3]thiazolo[4,5-b]pyridine
-
 Homo sapiens
3.3.2.6 2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-5-yl]oxy][1,3]thiazolo[4,5-b]pyridine
-
 Mus musculus
3.3.2.6 2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy]-1,3-benzothiazole
-
 Homo sapiens
3.3.2.6 2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy]-1,3-benzothiazole
-
 Mus musculus
3.3.2.6 2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy][1,3]thiazolo[4,5-b]pyridine
-
 Homo sapiens
3.3.2.6 2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy][1,3]thiazolo[4,5-b]pyridine
-
 Mus musculus
3.3.2.6 2-[[3-(morpholin-4-ylmethyl)-1-benzofuran-6-yl]oxy]-1,3-benzothiazole
-
 Homo sapiens
3.3.2.6 2-[[3-(morpholin-4-ylmethyl)-1-benzofuran-6-yl]oxy]-1,3-benzothiazole
-
 Mus musculus
3.3.2.6 2-[[3-(morpholin-4-ylmethyl)-1-benzofuran-6-yl]oxy][1,3]thiazolo[4,5-b]pyridine
-
 Homo sapiens
3.3.2.6 2-[[3-(morpholin-4-ylmethyl)-1-benzofuran-6-yl]oxy][1,3]thiazolo[4,5-b]pyridine
-
 Mus musculus
3.3.2.6 2-[[3-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy]-1,3-benzothiazole
-
 Homo sapiens
3.3.2.6 2-[[3-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy]-1,3-benzothiazole
-
 Mus musculus
3.3.2.6 2-[[3-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy][1,3]thiazolo[4,5-b]pyridine
-
 Homo sapiens
3.3.2.6 2-[[3-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy][1,3]thiazolo[4,5-b]pyridine
-
 Mus musculus
3.3.2.6 N-(1-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)acetamide
-
 Homo sapiens
3.3.2.6 N-(1-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)acetamide
-
 Mus musculus
3.3.2.6 N-(1-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)acetamide
-
 Homo sapiens
3.3.2.6 N-(1-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)acetamide
-
 Mus musculus
3.3.2.6 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
3.3.2.6 N-[(3-endo)-8-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]-8-azabicyclo[3.2.1]oct-3-yl]acetamide
-
 Mus musculus
3.3.2.6 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
3.3.2.6 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
-
 Mus musculus

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
3.3.2.6 cytosol
-
 Mus musculus 5829
-
3.3.2.6 cytosol
-
 Homo sapiens 5829
-

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
3.3.2.6 Zn2+ contains zinc Mus musculus
3.3.2.6 Zn2+ contains zinc Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.3.2.6 leukotriene A4 + H2O Mus musculus
-
 leukotriene B4
-
 ?
3.3.2.6 leukotriene A4 + H2O Homo sapiens
-
 leukotriene B4
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
3.3.2.6 Homo sapiens
-
-
-
3.3.2.6 Mus musculus
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.3.2.6 blood
-
 Mus musculus
-
3.3.2.6 blood
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.3.2.6 leukotriene A4 + H2O
-
 Mus musculus leukotriene B4
-
 ?
3.3.2.6 leukotriene A4 + H2O
-
 Homo sapiens leukotriene B4
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.3.2.6 leukotriene A4 hydrolase
-
 Mus musculus
3.3.2.6 leukotriene A4 hydrolase
-
 Homo sapiens
3.3.2.6 LTA4H
-
 Mus musculus
3.3.2.6 LTA4H
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.3.2.6 0.0000016
-
 pH and temperature not specified in the publication Homo sapiens 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
3.3.2.6 0.000003
-
 pH and temperature not specified in the publication Homo sapiens 1-(1-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)pyrrolidin-2-one
3.3.2.6 0.0000037
-
 pH and temperature not specified in the publication Homo sapiens N-(1-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)acetamide
3.3.2.6 0.0000046
-
 pH and temperature not specified in the publication Homo sapiens 2-[[3-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy][1,3]thiazolo[4,5-b]pyridine
3.3.2.6 0.000007
-
 pH and temperature not specified in the publication Homo sapiens 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
3.3.2.6 0.0000073
-
 pH and temperature not specified in the publication Homo sapiens N-[(3-endo)-8-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]-8-azabicyclo[3.2.1]oct-3-yl]acetamide
3.3.2.6 0.0000073
-
 pH and temperature not specified in the publication Homo sapiens 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
3.3.2.6 0.0000083
-
 pH and temperature not specified in the publication Homo sapiens 1-[[6-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)-1-benzofuran-3-yl]methyl]piperidine-4-carboxylic acid
3.3.2.6 0.000014
-
 pH and temperature not specified in the publication Homo sapiens 1-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]piperidine-4-carboxylic acid
3.3.2.6 0.000025
-
 pH and temperature not specified in the publication Homo sapiens 2-[[3-(morpholin-4-ylmethyl)-1-benzofuran-6-yl]oxy][1,3]thiazolo[4,5-b]pyridine
3.3.2.6 0.000026
-
 pH and temperature not specified in the publication Homo sapiens N-(1-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)acetamide
3.3.2.6 0.000034
-
 pH and temperature not specified in the publication Homo sapiens 1-(5-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl)ethanone
3.3.2.6 0.000051
-
 pH and temperature not specified in the publication Homo sapiens 2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy][1,3]thiazolo[4,5-b]pyridine
3.3.2.6 0.000058
-
 pH and temperature not specified in the publication Homo sapiens 1-(1-[[6-(1,3-benzothiazol-2-yloxy)-1-benzofuran-3-yl]methyl]piperidin-4-yl)pyrrolidin-2-one
3.3.2.6 0.000062
-
 pH and temperature not specified in the publication Homo sapiens 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
3.3.2.6 0.000066
-
 pH and temperature not specified in the publication Homo sapiens 2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-5-yl]oxy][1,3]thiazolo[4,5-b]pyridine
3.3.2.6 0.000067
-
 pH and temperature not specified in the publication Homo sapiens 2-[[3-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy]-1,3-benzothiazole
3.3.2.6 0.00014
-
 pH and temperature not specified in the publication Homo sapiens 2-[[3-(morpholin-4-ylmethyl)-1-benzofuran-6-yl]oxy]-1,3-benzothiazole
3.3.2.6 0.0003
-
 pH and temperature not specified in the publication Homo sapiens 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
3.3.2.6 0.00033
-
 pH and temperature not specified in the publication Homo sapiens 2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-5-yl]oxy]-1,3-benzothiazole
3.3.2.6 0.00034
-
 pH and temperature not specified in the publication Homo sapiens 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
3.3.2.6 0.00034
-
 pH and temperature not specified in the publication Homo sapiens 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
3.3.2.6 0.00034
-
 pH and temperature not specified in the publication Homo sapiens 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
3.3.2.6 0.00043
-
 pH and temperature not specified in the publication Homo sapiens 2-[[2-(piperidin-1-ylmethyl)-1-benzofuran-6-yl]oxy]-1,3-benzothiazole
3.3.2.6 0.00213
-
 pH and temperature not specified in the publication Homo sapiens 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
3.3.2.6 0.00237
-
 pH and temperature not specified in the publication Homo sapiens 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