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Literature summary for 2.7.11.26 extracted from

  • Ye, Q.; Li, M.; Zhou, Y.B.; Cao, J.Y.; Xu, L.; Li, Y.J.; Han, L.; Gao, J.R.; Hu, Y.Z.; Li, J.
    Design, synthesis, and evaluation of 3-aryl-4-pyrrolyl-maleimides as glycogen synthase kinase-3beta inhibitors (2013), Arch. Pharm., 346, 349-358.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
recombinant expression of GST-tagged enzyme in Escherichia coli strain BL21-CodonPlus(DE3) Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
3-(1-(2-morpholinoethyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
Homo sapiens
3-(1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
Homo sapiens
3-(1-(3-(piperidin-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
Homo sapiens
3-(1-(3-hydroxypropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
Homo sapiens
3-(1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-1,2,4-triazol-1-yl)-1H-pyrrole-2,5-dione
-
Homo sapiens
3-(1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
Homo sapiens
3-(1-(4-morpholinobutyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
Homo sapiens
3-(1-methyl-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
Homo sapiens
3-(1H-imidazol-1-yl)-4-(1-(3-morpholinopropyl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
Homo sapiens
3-(1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
Homo sapiens
3-(5-methoxy-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
Homo sapiens
3-(6-bromo-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
Homo sapiens
3-(6-chloro-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
Homo sapiens
3-(6-fluoro-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1Hpyrrol-3-yl)-1H-pyrrole-2,5-dione
-
Homo sapiens
3-(imidazo[1,2-a]pyridin-3-yl)-4-[2-(morpholine-4-carbonyl)-1,2,3,4-tetrahydro[1,4]diazepino[6,7,1-hi]indol-7-yl]-1H-pyrrole-2,5-dione an imidazo[1,2-a]pyridinylindolylmaleimide Homo sapiens
3-(naphthalen-1-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
Homo sapiens
3-phenyl-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
Homo sapiens
GF 109203X a benzofuranylindolylmaleimide Homo sapiens
additional information design, synthesis, and evaluation of 3-aryl-4-pyrrolyl-maleimides as glycogen synthase kinase-3beta inhibitors. Compounds 3-(1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione, 3-(1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione, 3-(6-fluoro-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1Hpyrrol-3-yl)-1H-pyrrole-2,5-dione, 3-(1-(3-hydroxypropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione, and 3-(1-methyl-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione significantly reduce amyloidbeta-induced Tau hyperphosphorylation, showing the inhibition of GSK-3beta at the cellular level. Structure-activity relationships, in silico molecular modeling study, overview Homo sapiens
Ro 31-8220 a benzofuranylindolylmaleimide Homo sapiens
staurosporine a benzofuranylindolylmaleimide Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ required Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + [tau-protein] Homo sapiens
-
ADP + O-phospho-[tau-protein]
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens P49841
-
-

Purification (Commentary)

Purification (Comment) Organism
recombinant GST-tagged enzyme from Escherichia coli strain BL21-CodonPlus(DE3) by glutathione affinity chromatography and tag cleavage by thrombin Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
neuroblastoma cell
-
Homo sapiens
-
SH-SY5Y cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + [tau-protein]
-
Homo sapiens ADP + O-phospho-[tau-protein]
-
?

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
0.000028
-
pH and temperature not specified in the publication Homo sapiens staurosporine
0.0001
-
pH and temperature not specified in the publication Homo sapiens 3-(1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
0.00015
-
pH and temperature not specified in the publication Homo sapiens 3-(1-(3-hydroxypropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
0.00016
-
pH and temperature not specified in the publication Homo sapiens 3-(6-fluoro-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1Hpyrrol-3-yl)-1H-pyrrole-2,5-dione
0.00021
-
pH and temperature not specified in the publication Homo sapiens 3-(1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
0.00026
-
pH and temperature not specified in the publication Homo sapiens 3-(1-methyl-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
0.00036
-
pH and temperature not specified in the publication Homo sapiens 3-(6-chloro-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
0.00053
-
pH and temperature not specified in the publication Homo sapiens 3-(1-(4-morpholinobutyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
0.00057
-
pH and temperature not specified in the publication Homo sapiens 3-(5-methoxy-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
0.00101
-
pH and temperature not specified in the publication Homo sapiens 3-(6-bromo-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
0.00129
-
pH and temperature not specified in the publication Homo sapiens 3-(1-(3-(piperidin-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
0.00192
-
pH and temperature not specified in the publication Homo sapiens 3-(1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
0.00204
-
pH and temperature not specified in the publication Homo sapiens 3-(1H-imidazol-1-yl)-4-(1-(3-morpholinopropyl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione
0.00424
-
pH and temperature not specified in the publication Homo sapiens 3-phenyl-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
0.00645
-
pH and temperature not specified in the publication Homo sapiens 3-(1-(2-morpholinoethyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
0.0116
-
pH and temperature not specified in the publication Homo sapiens 3-(1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-1,2,4-triazol-1-yl)-1H-pyrrole-2,5-dione
0.01186
-
pH and temperature not specified in the publication Homo sapiens 3-(naphthalen-1-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione