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Literature summary for 2.7.11.26 extracted from

  • Saitoh, M.; Kunitomo, J.; Kimura, E.; Hayase, Y.; Kobayashi, H.; Uchiyama, N.; Kawamoto, T.; Tanaka, T.; Mol, C.D.; Dougan, D.R.; Textor, G.S.; Snell, G.P.; Itoh, F.
    Design, synthesis and structure-activity relationships of 1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta (2009), Bioorg. Med. Chem., 17, 2017-2029.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
using a baculovirus expression system Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-(4-methoxyphenyl)-6-(5-[[3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1H-benzimidazole
-
Homo sapiens
1-(4-methoxyphenyl)-6-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1H-benzimidazole
-
Homo sapiens
1-methyl-6-(5-[[3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1H-benzimidazole
-
Homo sapiens
2-(1,3-benzodioxol-5-yl)-5-[(3-fluoro-4-methoxybenzyl)sulfanyl]-1,3,4-oxadiazole
-
Homo sapiens
2-(1-benzofuran-5-yl)-5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
-
Homo sapiens
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[(3-fluoro-4-methoxybenzyl)sulfanyl]-1,3,4-oxadiazole
-
Homo sapiens
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[(3-fluorobenzyl)sulfanyl]-1,3,4-oxadiazole
-
Homo sapiens
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[(4-methoxybenzyl)sulfanyl]-1,3,4-oxadiazole
-
Homo sapiens
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[2-(3-fluorophenyl)ethyl]-1,3,4-oxadiazole
-
Homo sapiens
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[[(3-fluorophenyl)sulfanyl]methyl]-1,3,4-oxadiazole
-
Homo sapiens
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[[3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
-
Homo sapiens
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
-
Homo sapiens
2-(benzylsulfanyl)-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
-
Homo sapiens
2-[(2-chlorobenzyl)sulfanyl]-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
-
Homo sapiens
2-[(3-chloro-4-methoxybenzyl)sulfanyl]-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
-
Homo sapiens
2-[(3-chlorobenzyl)sulfanyl]-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
-
Homo sapiens
2-[(4-chlorobenzyl)sulfanyl]-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
-
Homo sapiens
2-[3-(4-methoxyphenyl)-1-benzofuran-5-yl]-5-[[3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
-
Homo sapiens
2-[3-(4-methoxyphenyl)-1-benzofuran-5-yl]-5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
-
Homo sapiens
3-([[5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazol-2-yl]sulfanyl]methyl)benzo-nitrile
-
Homo sapiens
3-[([5-[1-(4-methoxyphenyl)-1H-benzimidazol-6-yl]-1,3,4-oxadiazol-2-yl]sulfanyl)methyl]benzonitrile
-
Homo sapiens
3-[([5-[3-(4-methoxyphenyl)-1-benzofuran-5-yl]-1,3,4-oxadiazol-2-yl]sulfanyl)methyl]benzonitrile
-
Homo sapiens
5-(2,3-dihydro-1-benzofuran-5-yl)-N-(3-fluorobenzyl)-1,3,4-oxadiazol-2-amine
-
Homo sapiens
5-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1H-indazole
-
Homo sapiens
5-([ [5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazol-2-yl]sulfanyl]methyl)-2-methoxybenzonitrile
-
Homo sapiens
6-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1,3-benzothiazole
-
Homo sapiens
6-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)imidazo[1,2-a]pyridine
-
Homo sapiens
6-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)quinoline
-
Homo sapiens
methyl 3-([[5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazol-2-yl]sulfanyl]methyl)benzoate
-
Homo sapiens
additional information not inhibited by 2-(2,3-dihydro-1-benzofuran-5-yl)-5-[(3-fluorobenzyl)oxy]-1,3,4-oxadiazole Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P49841
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + protein tau
-
Homo sapiens ADP + protein tau phosphate
-
?

Synonyms

Synonyms Comment Organism
glycogen synthase kinase-3beta
-
Homo sapiens
GSK-3beta
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000023
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin Homo sapiens 3-[([5-[1-(4-methoxyphenyl)-1H-benzimidazol-6-yl]-1,3,4-oxadiazol-2-yl]sulfanyl)methyl]benzonitrile
0.0000025
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin Homo sapiens 1-(4-methoxyphenyl)-6-(5-[[3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1H-benzimidazole
0.0000031
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin Homo sapiens 6-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1,3-benzothiazole
0.0000035
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin Homo sapiens 3-[([5-[3-(4-methoxyphenyl)-1-benzofuran-5-yl]-1,3,4-oxadiazol-2-yl]sulfanyl)methyl]benzonitrile
0.0000049
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin Homo sapiens 2-(1-benzofuran-5-yl)-5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
0.0000057
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin Homo sapiens 2-(2,3-dihydro-1-benzofuran-5-yl)-5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
0.0000065
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin Homo sapiens 6-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)imidazo[1,2-a]pyridine
0.0000086
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin Homo sapiens 1-(4-methoxyphenyl)-6-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1H-benzimidazole
0.0000094
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin Homo sapiens 1-methyl-6-(5-[[3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1H-benzimidazole
0.000013
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin Homo sapiens 2-[(3-chloro-4-methoxybenzyl)sulfanyl]-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
0.000016
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin Homo sapiens 5-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1H-indazole
0.000018
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin Homo sapiens 6-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)quinoline
0.000025
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin Homo sapiens 2-[3-(4-methoxyphenyl)-1-benzofuran-5-yl]-5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
0.000028
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin Homo sapiens 5-([ [5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazol-2-yl]sulfanyl]methyl)-2-methoxybenzonitrile
0.000044
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin Homo sapiens 2-(2,3-dihydro-1-benzofuran-5-yl)-5-[(3-fluoro-4-methoxybenzyl)sulfanyl]-1,3,4-oxadiazole
0.000054
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin Homo sapiens 2-(2,3-dihydro-1-benzofuran-5-yl)-5-[(3-fluorobenzyl)sulfanyl]-1,3,4-oxadiazole
0.000065
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin Homo sapiens 2-(1,3-benzodioxol-5-yl)-5-[(3-fluoro-4-methoxybenzyl)sulfanyl]-1,3,4-oxadiazole
0.000068
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin Homo sapiens 2-(2,3-dihydro-1-benzofuran-5-yl)-5-[[3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
0.000084
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin Homo sapiens 2-[3-(4-methoxyphenyl)-1-benzofuran-5-yl]-5-[[3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
0.000091
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin Homo sapiens 3-([[5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazol-2-yl]sulfanyl]methyl)benzo-nitrile
0.000094
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin Homo sapiens 2-[(2-chlorobenzyl)sulfanyl]-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
0.0002
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin Homo sapiens 2-[(3-chlorobenzyl)sulfanyl]-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
0.00021
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin Homo sapiens 2-(benzylsulfanyl)-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
0.00022
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin Homo sapiens 2-(2,3-dihydro-1-benzofuran-5-yl)-5-[(4-methoxybenzyl)sulfanyl]-1,3,4-oxadiazole
0.00028
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin Homo sapiens 2-[(4-chlorobenzyl)sulfanyl]-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
0.00033
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin Homo sapiens 5-(2,3-dihydro-1-benzofuran-5-yl)-N-(3-fluorobenzyl)-1,3,4-oxadiazol-2-amine
0.00034
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin Homo sapiens 2-(2,3-dihydro-1-benzofuran-5-yl)-5-[2-(3-fluorophenyl)ethyl]-1,3,4-oxadiazole
0.00063
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin Homo sapiens methyl 3-([[5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazol-2-yl]sulfanyl]methyl)benzoate
0.00068
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin Homo sapiens 2-(2,3-dihydro-1-benzofuran-5-yl)-5-[[(3-fluorophenyl)sulfanyl]methyl]-1,3,4-oxadiazole