Application | Comment | Organism |
---|---|---|
drug development | the enzyme is a target in drug development for treatment of Alzheimer's disease | Homo sapiens |
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 | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | Q13627 | - |
- |
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 | Comment | Organism |
---|---|---|
dual specificity tyrosine-phosphorylation-regulated kinase-1A | - |
Homo sapiens |
DYRK1A | - |
Homo sapiens |
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 | 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 |