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Literature summary for 2.7.12.1 extracted from

  • Koo, K.A.; Kim, N.D.; Chon, Y.S.; Jung, M.S.; Lee, B.J.; Kim, J.H.; Song, W.J.
    QSAR analysis of pyrazolidine-3,5-diones derivatives as Dyrk1A inhibitors (2009), Bioorg. Med. Chem. Lett., 19, 2324-2328.
    View publication on PubMed
Search for more literature for 2.7.12.1

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Mus musculus Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(4Z)-1-(3,4-dichlorophenyl)-4-(4-hydroxy-3-methoxybenzylidene)pyrazolidine-3,5-dione 82.6% inhibition at 0.01 mM Homo sapiens
(4Z)-1-(3,4-dichlorophenyl)-4-(4-hydroxy-3-nitrobenzylidene)pyrazolidine-3,5-dione 76% inhibition at 0.01 mM Homo sapiens
(4Z)-1-(3,4-dichlorophenyl)-4-(4-hydroxybenzylidene)pyrazolidine-3,5-dione 73% inhibition at 0.01 mM Homo sapiens
(4Z)-1-(4-fluorophenyl)-4-(4-hydroxy-3-methoxybenzylidene)pyrazolidine-3,5-dione 44% inhibition at 0.01 mM Homo sapiens
(4Z)-4-(4-hydroxy-3-methoxybenzylidene)-1-(4-methoxyphenyl)pyrazolidine-3,5-dione 55% inhibition at 0.01 mM Homo sapiens
4-[(4Z)-4-(4-hydroxy-3-methoxybenzylidene)-3,5-dioxopyrazolidin-1-yl]benzonitrile 78% inhibition at 0.01 mM Homo sapiens
harmine
-
 Homo sapiens
HCD160 82.6% inhibition at 0.01 mM Homo sapiens
roscovitine 63% inhibition at 0.01 mM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

Synonyms Comment Organism
dual specificity tyrosine phosphorylation regulated kinase 1A
-
 Homo sapiens
Dyrk1A kinase
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0006
-
 for autophosphorylation Homo sapiens (4Z)-1-(3,4-dichlorophenyl)-4-(4-hydroxy-3-nitrobenzylidene)pyrazolidine-3,5-dione
0.0006
-
 for autophosphorylation Homo sapiens 4-[(4Z)-4-(4-hydroxy-3-methoxybenzylidene)-3,5-dioxopyrazolidin-1-yl]benzonitrile
0.001
-
-
 Homo sapiens harmine
0.0012
-
 for autophosphorylation Homo sapiens (4Z)-4-(4-hydroxy-3-methoxybenzylidene)-1-(4-methoxyphenyl)pyrazolidine-3,5-dione
0.0025
-
 for autophosphorylation Homo sapiens (4Z)-1-(3,4-dichlorophenyl)-4-(4-hydroxy-3-methoxybenzylidene)pyrazolidine-3,5-dione
0.0025
-
 for autophosphorylation Homo sapiens (4Z)-1-(3,4-dichlorophenyl)-4-(4-hydroxybenzylidene)pyrazolidine-3,5-dione
0.0025
-
 for autophosphorylation Homo sapiens (4Z)-1-(4-fluorophenyl)-4-(4-hydroxy-3-methoxybenzylidene)pyrazolidine-3,5-dione