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Literature summary 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

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.12.1 expressed in Mus musculus Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.12.1 (4Z)-1-(3,4-dichlorophenyl)-4-(4-hydroxy-3-methoxybenzylidene)pyrazolidine-3,5-dione 82.6% inhibition at 0.01 mM Homo sapiens
2.7.12.1 (4Z)-1-(3,4-dichlorophenyl)-4-(4-hydroxy-3-nitrobenzylidene)pyrazolidine-3,5-dione 76% inhibition at 0.01 mM Homo sapiens
2.7.12.1 (4Z)-1-(3,4-dichlorophenyl)-4-(4-hydroxybenzylidene)pyrazolidine-3,5-dione 73% inhibition at 0.01 mM Homo sapiens
2.7.12.1 (4Z)-1-(4-fluorophenyl)-4-(4-hydroxy-3-methoxybenzylidene)pyrazolidine-3,5-dione 44% inhibition at 0.01 mM Homo sapiens
2.7.12.1 (4Z)-4-(4-hydroxy-3-methoxybenzylidene)-1-(4-methoxyphenyl)pyrazolidine-3,5-dione 55% inhibition at 0.01 mM Homo sapiens
2.7.12.1 4-[(4Z)-4-(4-hydroxy-3-methoxybenzylidene)-3,5-dioxopyrazolidin-1-yl]benzonitrile 78% inhibition at 0.01 mM Homo sapiens
2.7.12.1 harmine
-
 Homo sapiens
2.7.12.1 HCD160 82.6% inhibition at 0.01 mM Homo sapiens
2.7.12.1 roscovitine 63% inhibition at 0.01 mM Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
2.7.12.1 Homo sapiens
-
-
-

Synonyms

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

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.12.1 0.0006
-
 for autophosphorylation Homo sapiens (4Z)-1-(3,4-dichlorophenyl)-4-(4-hydroxy-3-nitrobenzylidene)pyrazolidine-3,5-dione
2.7.12.1 0.0006
-
 for autophosphorylation Homo sapiens 4-[(4Z)-4-(4-hydroxy-3-methoxybenzylidene)-3,5-dioxopyrazolidin-1-yl]benzonitrile
2.7.12.1 0.001
-
-
 Homo sapiens harmine
2.7.12.1 0.0012
-
 for autophosphorylation Homo sapiens (4Z)-4-(4-hydroxy-3-methoxybenzylidene)-1-(4-methoxyphenyl)pyrazolidine-3,5-dione
2.7.12.1 0.0025
-
 for autophosphorylation Homo sapiens (4Z)-1-(3,4-dichlorophenyl)-4-(4-hydroxy-3-methoxybenzylidene)pyrazolidine-3,5-dione
2.7.12.1 0.0025
-
 for autophosphorylation Homo sapiens (4Z)-1-(3,4-dichlorophenyl)-4-(4-hydroxybenzylidene)pyrazolidine-3,5-dione
2.7.12.1 0.0025
-
 for autophosphorylation Homo sapiens (4Z)-1-(4-fluorophenyl)-4-(4-hydroxy-3-methoxybenzylidene)pyrazolidine-3,5-dione