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Literature summary for 2.7.12.1 extracted from

  • Leal, F.D.; da Silva Lima, C.H.; de Alencastro, R.B.; Castro, H.C.; Rodrigues, C.R.; Albuquerque, M.G.
    Hologram QSAR models of a series of 6-arylquinazolin-4-amine inhibitors of a new Alzheimers disease target: dual specificity tyrosine-phosphorylation-regulated kinase-1A enzyme (2015), Int. J. Mol. Sci., 16, 5235-5253.
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
drug development the enzyme is a target in drug development for treatment of Alzheimer's disease Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(5-[4-[ethyl(thiophen-2-ylmethyl)amino]quinazolin-6-yl]furan-2-yl)methanol
-
Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-(1,3-thiazol-2-ylmethyl)quinazolin-4-amine
-
Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-(1H-imidazol-2-ylmethyl)-N-methylquinazolin-4-amine
-
Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-(1H-imidazol-2-ylmethyl)quinazolin-4-amine
-
Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-(2,2-dimethylpropyl)quinazolin-4-amine
-
Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-(cyclopentylmethyl)quinazolin-4-amine
-
Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-(furan-2-ylmethyl)-N-methylquinazolin-4-amine
-
Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-(furan-2-ylmethyl)quinazolin-4-amine
-
Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-(furan-3-ylmethyl)quinazolin-4-amine
-
Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-(tetrahydro-2H-pyran-2-ylmethyl)quinazolin-4-amine
-
Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-(tetrahydrofuran-2-ylmethyl)quinazolin-4-amine
-
Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-(tetrahydrofuran-3-ylmethyl)quinazolin-4-amine
-
Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-(thiophen-2-ylmethyl)quinazolin-4-amine
-
Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-ethyl-N-(thiophen-2-ylmethyl)quinazolin-4-amine
-
Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-methyl-N-(1,3-thiazol-2-ylmethyl)quinazolin-4-amine
-
Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-methyl-N-(thiophen-2-ylmethyl)quinazolin-4-amine
-
Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-methyl-N-[(3-methylthiophen-2-yl)methyl]quinazolin-4-amine
-
Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-methyl-N-[(4-methyl-1,3-thiazol-2-yl)methyl]quinazolin-4-amine
-
Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-methyl-N-[(5-methyl-1,3,4-oxadiazol-2-yl)methyl]quinazolin-4-amine
-
Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-[(2-methylfuran-3-yl)methyl]quinazolin-4-amine
-
Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-[(3-methylthiophen-2-yl)methyl]quinazolin-4-amine
-
Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-[(4-methyl-1,3-thiazol-2-yl)methyl]quinazolin-4-amine
-
Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-[(5-methylfuran-2-yl)methyl]quinazolin-4-amine
-
Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-[(5-methylthiophen-2-yl)methyl]quinazolin-4-amine
-
Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-[2-(1H-imidazol-4-yl)ethyl]quinazolin-4-amine
-
Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-[2-(furan-2-yl)ethyl]quinazolin-4-amine
-
Homo sapiens
6-(1-methyl-1H-indol-5-yl)-N-(thiophen-2-ylmethyl)quinazolin-4-amine
-
Homo sapiens
6-(2,3-dihydro-1,4-benzodioxin-6-yl)-N-(thiophen-2-ylmethyl)quinazolin-4-amine
-
Homo sapiens
6-(2-chlorophenyl)-N-(thiophen-2-ylmethyl)quinazolin-4-amine
-
Homo sapiens
6-(2-methylfuran-3-yl)-N-[(5-methylfuran-2-yl)methyl]quinazolin-4-amine
-
Homo sapiens
6-(3-methoxyphenyl)-N-(thiophen-2-ylmethyl)quinazolin-4-amine
-
Homo sapiens
6-(4-fluoro-1,3-benzodioxol-5-yl)-N-(thiophen-2-ylmethyl)quinazolin-4-amine
-
Homo sapiens
6-(4-methoxyphenyl)-N-(thiophen-2-ylmethyl)quinazolin-4-amine
-
Homo sapiens
6-(furan-2-yl)-N-(thiophen-2-ylmethyl)quinazolin-4-amine
-
Homo sapiens
6-(furan-3-yl)-N-(thiophen-2-ylmethyl)quinazolin-4-amine
-
Homo sapiens
6-(furan-3-yl)-N-methyl-N-[(3-methylthiophen-2-yl)methyl]quinazolin-4-amine
-
Homo sapiens
6-(furan-3-yl)-N-[(2-methyl-1,3-thiazol-4-yl)methyl]quinazolin-4-amine
-
Homo sapiens
ethyl 5-(4-[[(2-methyl-1,3-thiazol-4-yl)methyl]amino]quinazolin-6-yl)furan-2-carboxylate
-
Homo sapiens
ethyl 5-(4-[[(3-methylthiophen-2-yl)methyl]amino]quinazolin-6-yl)furan-2-carboxylate
-
Homo sapiens
ethyl 5-(4-[[(5-methylfuran-2-yl)methyl]amino]quinazolin-6-yl)furan-2-carboxylate
-
Homo sapiens
ethyl 5-(4-[[2-(1H-imidazol-4-yl)ethyl]amino]quinazolin-6-yl)furan-2-carboxylate
-
Homo sapiens
ethyl 5-[4-[(1H-imidazol-2-ylmethyl)amino]quinazolin-6-yl]furan-2-carboxylate
-
Homo sapiens
ethyl 5-[4-[ethyl(thiophen-2-ylmethyl)amino]quinazolin-6-yl]furan-2-carboxylate
-
Homo sapiens
additional information synthesis and evaluation of a series of 6-arylquinazolin-4-amine inhibitors as potential enzyme inhibitors, hologram quantitative structure-activity relationship (QSAR) studies, molecular modeling, overview Homo sapiens
N-(2,2-dimethylpropyl)-6-[5-[(ethylamino)methyl]furan-2-yl]quinazolin-4-amine
-
Homo sapiens
[5-(4-[methyl[(3-methylthiophen-2-yl)methyl]amino]quinazolin-6-yl)furan-2-yl]methanol
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q13627
-
-

Source Tissue

Source Tissue Comment Organism Textmining
brain
-
Homo sapiens
-
cerebellum
-
Homo sapiens
-
hippocampus
-
Homo sapiens
-
additional information DYRK1A protein expression is widespread throughout the human body, but is particularly abundant in the cerebellum, olfactory bulb, and hippocampus. The enzyme is up-regulated in the early stages of embryonic development, followed by gradual decrease in the later levels Homo sapiens
-
olfactory bulb
-
Homo sapiens
-

Synonyms

Synonyms Comment Organism
dual specificity tyrosine-phosphorylation-regulated kinase-1A
-
Homo sapiens
DYRK1A
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
additional information
-
pIC50 values of 6-arylquinazolin-4-amine inhibitors, overview Homo sapiens additional information

General Information

General Information Comment Organism
malfunction increased expression of this enzyme leads to hyper-phosphorylation of Tau protein and amyloid precursor protein, which results in high levels of beta-amyloid peptide (leading to beta-amyloidosis) and aggregation of Tau protein, and subsequent formation of neurofibrillary tangles Homo sapiens