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Literature summary for 2.7.12.1 extracted from

  • Pan, Y.; Wang, Y.; Bryant, S.H.
    Pharmacophore and 3D-QSAR characterization of 6-arylquinazolin-4-amines as Cdc2-like kinase 4 (Clk4) and dual specificity tyrosine-phosphorylation-regulated kinase 1A (Dyrk1A) inhibitors (2013), J. Chem. Inf. Model., 53, 938-947.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.7.12.1

Inhibitors

Inhibitors Comment Organism Structure
(5-{4-[(5-methylfuran-2-yl)amino]quinazolin-6-yl}furan-2-yl)methanol
-
 Homo sapiens
(5-{4-[methyl(3-methylthiophen-2-yl)amino]quinazolin-6-yl}furan-2-yl)methanol
-
 Homo sapiens
5-[4-(thiophen-2-ylamino)quinazolin-6-yl]furan-2-carboxylic acid
-
 Homo sapiens
5-{4-[(5-methylfuran-2-yl)amino]quinazolin-6-yl}furan-2-carboxylic acid
-
 Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-(1,3-thiazol-2-yl)quinazolin-4-amine
-
 Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-(1H-imidazol-2-yl)-N-methylquinazolin-4-amine
-
 Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-(1H-imidazol-2-yl)quinazolin-4-amine
-
 Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-(1H-imidazol-4-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-(2-methyl-1,3-thiazol-4-yl)quinazolin-4-amine
-
 Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-(2-methylfuran-3-yl)quinazolin-4-amine
-
 Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-(3-methylthiophen-2-yl)quinazolin-4-amine
-
 Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-(5-methylfuran-2-yl)quinazolin-4-amine
-
 Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-(5-methylthiophen-2-yl)quinazolin-4-amine
-
 Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-(furan-2-yl)-N-methylquinazolin-4-amine
-
 Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-(furan-2-yl)quinazolin-4-amine
-
 Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-(furan-3-yl)quinazolin-4-amine
-
 Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-(tetrahydro-2H-pyran-3-yl)quinazolin-4-amine
-
 Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-(tetrahydrofuran-2-yl)quinazolin-4-amine
-
 Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-(tetrahydrofuran-3-yl)quinazolin-4-amine
-
 Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-(thiophen-2-yl)quinazolin-4-amine
-
 Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-cyclopentylquinazolin-4-amine
-
 Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-ethyl-N-(thiophen-2-yl)quinazolin-4-amine
-
 Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-methyl-N-(1,3-thiazol-2-yl)quinazolin-4-amine
-
 Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-methyl-N-(2-methyl-1,3-thiazol-4-yl)quinazolin-4-amine
-
 Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-methyl-N-(3-methylthiophen-2-yl)quinazolin-4-amine
-
 Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-methyl-N-(4-methyl-1,3-thiazol-2-yl)quinazolin-4-amine
-
 Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-methyl-N-(5-methyl-1,3,4-oxadiazol-2-yl)quinazolin-4-amine
-
 Homo sapiens
6-(1,3-benzodioxol-5-yl)-N-methyl-N-(thiophen-2-yl)quinazolin-4-amine
-
 Homo sapiens
6-(1-methyl-1H-indazol-6-yl)-N-(thiophen-2-yl)quinazolin-4-amine
-
 Homo sapiens
6-(1-methyl-1H-indol-5-yl)-N-(thiophen-2-yl)quinazolin-4-amine
-
 Homo sapiens
6-(2-chlorophenyl)-N-(thiophen-2-yl)quinazolin-4-amine
-
 Homo sapiens
6-(2-methylfuran-3-yl)-N-(5-methylfuran-2-yl)quinazolin-4-amine
-
 Homo sapiens
6-(3,4-dimethoxyphenyl)-N-(thiophen-2-yl)quinazolin-4-amine
-
 Homo sapiens
6-(3-chlorophenyl)-N-(thiophen-2-yl)quinazolin-4-amine
-
 Homo sapiens
6-(3-methoxyphenyl)-N-(thiophen-2-yl)quinazolin-4-amine
-
 Homo sapiens
6-(3-methylphenyl)-N-(thiophen-2-yl)quinazolin-4-amine
-
 Homo sapiens
6-(4-fluoro-1,3-benzodioxol-5-yl)-N-(thiophen-2-yl)quinazolin-4-amine
-
 Homo sapiens
6-(4-methoxyphenyl)-N-(thiophen-2-yl)quinazolin-4-amine
-
 Homo sapiens
6-(furan-2-yl)-N-(thiophen-2-yl)quinazolin-4-amine
-
 Homo sapiens
6-(furan-3-yl)-N-(2-methyl-1,3-thiazol-4-yl)quinazolin-4-amine
-
 Homo sapiens
6-(furan-3-yl)-N-(thiophen-2-yl)quinazolin-4-amine
-
 Homo sapiens
6-(furan-3-yl)-N-methyl-N-(3-methylthiophen-2-yl)quinazolin-4-amine
-
 Homo sapiens
6-(pyridin-3-yl)-N-(thiophen-2-yl)quinazolin-4-amine
-
 Homo sapiens
7-(1,3-benzodioxol-5-yl)-N-(thiophen-2-yl)quinazolin-4-amine
-
 Homo sapiens
ethyl 5-[4-(1H-imidazol-2-ylamino)quinazolin-6-yl]furan-2-carboxylate
-
 Homo sapiens
ethyl 5-[4-(thiophen-2-ylamino)quinazolin-6-yl]furan-2-carboxylate
-
 Homo sapiens
ethyl 5-{4-[(1H-imidazol-4-ylmethyl)amino]quinazolin-6-yl}furan-2-carboxylate
-
 Homo sapiens
ethyl 5-{4-[(2-methyl-1,3-thiazol-4-yl)amino]quinazolin-6-yl}furan-2-carboxylate
-
 Homo sapiens
ethyl 5-{4-[(5-methylfuran-2-yl)amino]quinazolin-6-yl}furan-2-carboxylate
-
 Homo sapiens
ethyl 5-{4-[methyl(3-methylthiophen-2-yl)amino]quinazolin-6-yl}furan-2-carboxylate
-
 Homo sapiens
additional information synthesis and evaluation of a series of 6-arylquinazolin-4-amine inhibitors as enzyme inhibitors, three-dimensional quantitative structure-activity relationship (3D-QSAR) studies, binding mode from docking studies, molecular homology modeling, overview. A hydrogen bond between ligand and the counterpart Lys 188 in Dyrk1A is present in part of the crystal structures of Dyrk1A (PDB IDs 3ANQ and 3ANR). By contrast, the involvement of the residue at the same position as Leu242 in the hydrogen bond interaction is available in all identified Dyrk1A structures (PDB IDs: 3ANQ, 3ANR, 2WO6, and 2VX3) Homo sapiens
N-(thiophen-2-yl)-6-(3,4,5-trimethoxyphenyl)quinazolin-4-amine
-
 Homo sapiens
N-tert-butyl-6-{5-[(ethylamino)methyl]furan-2-yl}quinazolin-4-amine
-
 Homo sapiens
{5-[4-(thiophen-2-ylamino)quinazolin-6-yl]furan-2-yl}methanol
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q13627
-
-

Synonyms

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