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Literature summary extracted from

  • Coombs, T.; Tanega, C.; Shen, M.; Wang, J.; Auld, D.; Gerritz, S.; Schoenen, F.; Thomas, C.; Aube, J.
    Small-molecule pyrimidine inhibitors of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases: Development of chemical probe ML315 (2013), Bioorg. Med. Chem. Lett., 23, 3654-3661.
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.12.1 (1Z)-1-(3-ethyl-5-methoxy-1,3-benzothiazol-2(3H)-ylidene)propan-2-one
-
Homo sapiens
2.7.12.1 2-(1,3-benzodioxol-5-yl)-N-(3,4-dichlorobenzyl)pyrimidin-4-amine
-
Homo sapiens
2.7.12.1 2-(1,3-benzodioxol-5-yl)-N-(4-chlorobenzyl)pyrimidin-4-amine
-
Homo sapiens
2.7.12.1 2-(1,3-benzodioxol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-4-amine
-
Homo sapiens
2.7.12.1 2-(1H-indazol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-4-amine
-
Homo sapiens
2.7.12.1 2-(1H-indazol-6-yl)-N-(pyridin-3-ylmethyl)pyrimidin-4-amine
-
Homo sapiens
2.7.12.1 3-[4-(2-phenylethyl)quinazolin-6-yl]benzonitrile
-
Homo sapiens
2.7.12.1 3-[4-[2-(4-methoxyphenyl)ethyl]quinazolin-6-yl]benzonitrile
-
Homo sapiens
2.7.12.1 3-[4-[2-(4-methylphenyl)ethyl]quinazolin-6-yl]benzonitrile
-
Homo sapiens
2.7.12.1 4-(1,3-benzodioxol-5-yl)-N-(3,4-dibromobenzyl)pyrimidin-2-amine
-
Homo sapiens
2.7.12.1 4-(1,3-benzodioxol-5-yl)-N-(3,4-dichlorobenzyl)pyrimidin-2-amine
-
Homo sapiens
2.7.12.1 4-(1,3-benzodioxol-5-yl)-N-(3,5-dibromobenzyl)pyrimidin-2-amine
-
Homo sapiens
2.7.12.1 4-(1,3-benzodioxol-5-yl)-N-(3,5-dichlorobenzyl)pyrimidin-2-amine
-
Homo sapiens
2.7.12.1 4-(1,3-benzodioxol-5-yl)-N-(4-chlorobenzyl)pyrimidin-2-amine
-
Homo sapiens
2.7.12.1 4-(1,3-benzodioxol-5-yl)-N-(4-chlorophenyl)pyrimidin-2-amine
-
Homo sapiens
2.7.12.1 4-(1,3-benzodioxol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-2-amine
-
Homo sapiens
2.7.12.1 4-(1,3-benzodioxol-5-yl)-N-[2-bromo-4-(trifluoromethyl)phenyl]pyrimidin-2-amine
-
Homo sapiens
2.7.12.1 4-(1,3-benzodioxol-5-yl)-N-[4-(trifluoromethyl)phenyl]pyrimidin-2-amine
-
Homo sapiens
2.7.12.1 4-(1H-indazol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-2-amine
-
Homo sapiens
2.7.12.1 4-(1H-indazol-6-yl)-N-(pyridin-3-ylmethyl)pyrimidin-2-amine
-
Homo sapiens
2.7.12.1 6-(1,3-benzodioxol-5-yl)-N-(3,4-dichlorobenzyl)pyrimidin-4-amine
-
Homo sapiens
2.7.12.1 6-(1,3-benzodioxol-5-yl)-N-(3,5-dichlorobenzyl)pyrimidin-4-amine
-
Homo sapiens
2.7.12.1 6-(1,3-benzodioxol-5-yl)-N-(3,5-dichlorobenzyl)quinazolin-4-amine
-
Homo sapiens
2.7.12.1 6-(1,3-benzodioxol-5-yl)-N-(4-chlorobenzyl)pyrimidin-4-amine
-
Homo sapiens
2.7.12.1 6-(1,3-benzodioxol-5-yl)-N-(4-methoxybenzyl)quinazolin-4-amine
-
Homo sapiens
2.7.12.1 6-(1,3-benzodioxol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-4-amine
-
Homo sapiens
2.7.12.1 6-(1,3-benzodioxol-5-yl)-N-benzylquinazolin-4-amine
-
Homo sapiens
2.7.12.1 6-(3-methoxyphenyl)-N-(4-methylbenzyl)quinazolin-4-amine
-
Homo sapiens
2.7.12.1 6-(3-methoxyphenyl)quinazoline
-
Homo sapiens
2.7.12.1 harmine a plant-derived beta-carboline alkaloid, ATP-competitive; a plant-derived beta-carboline alkaloid, ATP-competitive Homo sapiens
2.7.12.1 leucettamine B marine alkaloid, strong inhibitor Homo sapiens
2.7.12.1 leucettine L-41
-
Homo sapiens
2.7.12.1 ML315
-
Homo sapiens
2.7.12.1 additional information analysis of highly selective substituted pyrimidine inhibitors of the Dyrk kinase Dyrk1A, structure-activity relationships, overview. No inhibition by 6-(1,3-benzodioxol-5-yl)-N-(3,4-dichlorobenzyl)quinazolin-4-amine6-(1,3-benzodioxol-5-yl)-N-(3,4-dichlorobenzyl)quinazolin-4-amine, 6-(1,3-benzodioxol-5-yl)-N-(4-methylbenzyl)quinazolin-4-amine, 6-(1,3-benzodioxol-5-yl)-N-(4-chlorobenzyl)quinazolin-4-amine, 6-(1,3-benzodioxol-5-yl)quinazoline, 3-(quinazolin-6-yl)benzonitrile, N-(3,4-dichlorobenzyl)-6-(3-methoxyphenyl)quinazolin-4-amine, N-benzyl-6-(3,5-dimethyl-1,2-oxazol-4-yl)quinazolin-4-amine, N-(3,4-dichlorobenzyl)-6-(3,5-dimethyl-1,2-oxazol-4-yl)quinazolin-4-amine, 6-(3,5-dimethyl-1,2-oxazol-4-yl)-N-(4-methylbenzyl)quinazolin-4-amine, N-(4-chlorobenzyl)-6-(3,5-dimethyl-1,2-oxazol-4-yl)quinazolin-4-amine, 6-(3,5-dimethyl-1,2-oxazol-4-yl)-N-(4-methoxybenzyl)quinazolin-4-amine, 6-(3,5-dimethyl-1,2-oxazol-4-yl)quinazoline, N-benzyl-6-[4-(dimethylamino)phenyl]quinazolin-4-amine, N-(3,4-dichlorobenzyl)-6-[4-(dimethylamino)phenyl]quinazolin-4-amine, 6-[4-(dimethylamino)phenyl]-N-(4-methylbenzyl)quinazolin-4-amine, N-(4-chlorobenzyl)-6-[4-(dimethylamino)phenyl]quinazolin-4-amine, 6-[4-(dimethylamino)phenyl]-N-(4-methoxybenzyl)quinazolin-4-amine, N,N-dimethyl-4-(quinazolin-6-yl)aniline, N-(4-methylbenzyl)-6-(pyridin-3-yl)quinazolin-4-amine, and N-benzyl-6-(4-methoxyphenyl)quinazolin-4-amine, N-(3,4-dichlorobenzyl)-6-(4-methoxyphenyl)quinazolin-4-amine, 6-(4-methoxyphenyl)-N-(4-methylbenzyl)quinazolin-4-amine, N-(4-chlorobenzyl)-6-(4-methoxyphenyl)quinazolin-4-amine, N-(4-methoxybenzyl)-6-(4-methoxyphenyl)quinazolin-4-amine, and 6-(4-methoxyphenyl)quinazoline; analysis of highly selective substituted pyrimidine inhibitors of the Dyrk kinase Dyrk1B, structure-activity relationships, overview. No inhibition by N-(3,4-dichlorobenzyl)-4-(3,4-dimethoxyphenyl)pyrimidin-2-amine Homo sapiens
2.7.12.1 N,4-bis(1,3-benzodioxol-5-yl)pyrimidin-2-amine
-
Homo sapiens
2.7.12.1 N-(3,4-dichlorobenzyl)-2-(1H-indazol-5-yl)pyrimidin-4-amine
-
Homo sapiens
2.7.12.1 N-(3,4-dichlorobenzyl)-4-(1H-indazol-5-yl)pyrimidin-2-amine
-
Homo sapiens
2.7.12.1 N-(3,4-dichlorobenzyl)-4-(1H-indazol-6-yl)pyrimidin-2-amine
-
Homo sapiens
2.7.12.1 N-(3,4-dichlorobenzyl)-4-(2,3-dihydro-1,4-benzodioxin-6-yl)pyrimidin-2-amine
-
Homo sapiens
2.7.12.1 N-(3,4-dichlorobenzyl)-4-(3,4-dimethoxyphenyl)pyrimidin-2-amine
-
Homo sapiens
2.7.12.1 N-(3,4-dichlorobenzyl)-4-(3-methoxyphenyl)pyrimidin-2-amine
-
Homo sapiens
2.7.12.1 N-(3,4-dichlorobenzyl)-4-(4-methoxyphenyl)pyrimidin-2-amine
-
Homo sapiens
2.7.12.1 N-(3,4-dichlorobenzyl)-6-(pyridin-3-yl)quinazolin-4-amine
-
Homo sapiens
2.7.12.1 N-(4-chlorobenzyl)-4-(3-methoxyphenyl)pyrimidin-2-amine
-
Homo sapiens
2.7.12.1 N-(4-chlorobenzyl)-4-(4-methoxyphenyl)pyrimidin-2-amine
-
Homo sapiens
2.7.12.1 N-(4-chlorobenzyl)-6-(3-methoxyphenyl)quinazolin-4-amine
-
Homo sapiens
2.7.12.1 N-(4-chlorobenzyl)-6-(pyridin-3-yl)quinazolin-4-amine
-
Homo sapiens
2.7.12.1 N-(4-methoxybenzyl)-6-(3-methoxyphenyl)quinazolin-4-amine
-
Homo sapiens
2.7.12.1 N-(4-methoxybenzyl)-6-(pyridin-3-yl)quinazolin-4-amine
-
Homo sapiens
2.7.12.1 TG003
-
Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
2.7.12.1 Homo sapiens Q13627
-
-
2.7.12.1 Homo sapiens Q9Y463
-
-

Synonyms

EC Number Synonyms Comment Organism
2.7.12.1 dual specificity tyrosine phosphorylation-regulated kinase
-
Homo sapiens
2.7.12.1 Dyrk kinase
-
Homo sapiens
2.7.12.1 DYRK1A
-
Homo sapiens
2.7.12.1 DYRK1B
-
Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.12.1 0.000012
-
pH and temperature not specified in the publication Homo sapiens TG003
2.7.12.1 0.000033 0.00008 pH and temperature not specified in the publication Homo sapiens harmine
2.7.12.1 0.00004
-
pH and temperature not specified in the publication Homo sapiens leucettine L-41
2.7.12.1 0.00013
-
pH and temperature not specified in the publication Homo sapiens TG003
2.7.12.1 0.000166
-
pH and temperature not specified in the publication Homo sapiens harmine
2.7.12.1 0.004
-
pH and temperature not specified in the publication Homo sapiens 4-(1,3-benzodioxol-5-yl)-N-(3,5-dichlorobenzyl)pyrimidin-2-amine
2.7.12.1 0.007
-
pH and temperature not specified in the publication Homo sapiens 4-(1,3-benzodioxol-5-yl)-N-(3,5-dichlorobenzyl)pyrimidin-2-amine
2.7.12.1 0.009
-
pH and temperature not specified in the publication Homo sapiens 4-(1,3-benzodioxol-5-yl)-N-(3,5-dibromobenzyl)pyrimidin-2-amine
2.7.12.1 0.01
-
pH and temperature not specified in the publication Homo sapiens 4-(1,3-benzodioxol-5-yl)-N-[4-(trifluoromethyl)phenyl]pyrimidin-2-amine
2.7.12.1 0.012
-
pH and temperature not specified in the publication Homo sapiens 4-(1,3-benzodioxol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-2-amine
2.7.12.1 0.0129
-
pH and temperature not specified in the publication Homo sapiens N-(3,4-dichlorobenzyl)-4-(1H-indazol-5-yl)pyrimidin-2-amine
2.7.12.1 0.013
-
pH and temperature not specified in the publication Homo sapiens N-(3,4-dichlorobenzyl)-4-(2,3-dihydro-1,4-benzodioxin-6-yl)pyrimidin-2-amine
2.7.12.1 0.014
-
pH and temperature not specified in the publication Homo sapiens 4-(1,3-benzodioxol-5-yl)-N-(3,4-dichlorobenzyl)pyrimidin-2-amine
2.7.12.1 0.016
-
pH and temperature not specified in the publication Homo sapiens 4-(1,3-benzodioxol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-2-amine
2.7.12.1 0.0164
-
pH and temperature not specified in the publication Homo sapiens 3-[4-[2-(4-methoxyphenyl)ethyl]quinazolin-6-yl]benzonitrile
2.7.12.1 0.0169
-
pH and temperature not specified in the publication Homo sapiens N-(3,4-dichlorobenzyl)-4-(1H-indazol-6-yl)pyrimidin-2-amine
2.7.12.1 0.018
-
pH and temperature not specified in the publication Homo sapiens 4-(1,3-benzodioxol-5-yl)-N-(3,4-dibromobenzyl)pyrimidin-2-amine
2.7.12.1 0.018
-
pH and temperature not specified in the publication Homo sapiens 4-(1,3-benzodioxol-5-yl)-N-(3,5-dibromobenzyl)pyrimidin-2-amine
2.7.12.1 0.018
-
pH and temperature not specified in the publication Homo sapiens 4-(1,3-benzodioxol-5-yl)-N-[4-(trifluoromethyl)phenyl]pyrimidin-2-amine
2.7.12.1 0.0207
-
pH and temperature not specified in the publication Homo sapiens N-(4-chlorobenzyl)-6-(3-methoxyphenyl)quinazolin-4-amine
2.7.12.1 0.025
-
pH and temperature not specified in the publication Homo sapiens N,4-bis(1,3-benzodioxol-5-yl)pyrimidin-2-amine
2.7.12.1 0.026
-
pH and temperature not specified in the publication Homo sapiens 6-(1,3-benzodioxol-5-yl)-N-benzylquinazolin-4-amine
2.7.12.1 0.026
-
pH and temperature not specified in the publication Homo sapiens 6-(3-methoxyphenyl)quinazoline
2.7.12.1 0.026
-
pH and temperature not specified in the publication Homo sapiens N-(4-methoxybenzyl)-6-(3-methoxyphenyl)quinazolin-4-amine
2.7.12.1 0.0292
-
pH and temperature not specified in the publication Homo sapiens N-(4-chlorobenzyl)-6-(pyridin-3-yl)quinazolin-4-amine
2.7.12.1 0.0328
-
pH and temperature not specified in the publication Homo sapiens N-(4-methoxybenzyl)-6-(pyridin-3-yl)quinazolin-4-amine
2.7.12.1 0.038
-
pH and temperature not specified in the publication Homo sapiens 4-(1,3-benzodioxol-5-yl)-N-(3,4-dichlorobenzyl)pyrimidin-2-amine
2.7.12.1 0.0412
-
pH and temperature not specified in the publication Homo sapiens 3-[4-[2-(4-methylphenyl)ethyl]quinazolin-6-yl]benzonitrile
2.7.12.1 0.0412
-
pH and temperature not specified in the publication Homo sapiens N-(3,4-dichlorobenzyl)-6-(pyridin-3-yl)quinazolin-4-amine
2.7.12.1 0.042
-
pH and temperature not specified in the publication Homo sapiens N,4-bis(1,3-benzodioxol-5-yl)pyrimidin-2-amine
2.7.12.1 0.0463
-
pH and temperature not specified in the publication Homo sapiens 6-(1,3-benzodioxol-5-yl)-N-(4-methoxybenzyl)quinazolin-4-amine
2.7.12.1 0.055
-
pH and temperature not specified in the publication Homo sapiens N-(3,4-dichlorobenzyl)-4-(2,3-dihydro-1,4-benzodioxin-6-yl)pyrimidin-2-amine
2.7.12.1 0.061
-
pH and temperature not specified in the publication Homo sapiens 4-(1H-indazol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-2-amine
2.7.12.1 0.0654
-
pH and temperature not specified in the publication Homo sapiens 6-(3-methoxyphenyl)-N-(4-methylbenzyl)quinazolin-4-amine
2.7.12.1 0.093
-
pH and temperature not specified in the publication Homo sapiens 4-(1H-indazol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-2-amine
2.7.12.1 0.107
-
pH and temperature not specified in the publication Homo sapiens 4-(1,3-benzodioxol-5-yl)-N-[2-bromo-4-(trifluoromethyl)phenyl]pyrimidin-2-amine
2.7.12.1 0.112
-
pH and temperature not specified in the publication Homo sapiens 4-(1,3-benzodioxol-5-yl)-N-(3,4-dibromobenzyl)pyrimidin-2-amine
2.7.12.1 0.125
-
pH and temperature not specified in the publication Homo sapiens N-(3,4-dichlorobenzyl)-4-(1H-indazol-5-yl)pyrimidin-2-amine
2.7.12.1 0.137
-
pH and temperature not specified in the publication Homo sapiens 4-(1,3-benzodioxol-5-yl)-N-[2-bromo-4-(trifluoromethyl)phenyl]pyrimidin-2-amine
2.7.12.1 0.179
-
pH and temperature not specified in the publication Homo sapiens 2-(1H-indazol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-4-amine
2.7.12.1 0.203
-
pH and temperature not specified in the publication Homo sapiens N-(3,4-dichlorobenzyl)-4-(4-methoxyphenyl)pyrimidin-2-amine
2.7.12.1 0.273
-
pH and temperature not specified in the publication Homo sapiens 4-(1,3-benzodioxol-5-yl)-N-(4-chlorophenyl)pyrimidin-2-amine
2.7.12.1 0.282
-
pH and temperature not specified in the publication Homo sapiens 6-(1,3-benzodioxol-5-yl)-N-(3,5-dichlorobenzyl)quinazolin-4-amine
2.7.12.1 0.349
-
pH and temperature not specified in the publication Homo sapiens 2-(1H-indazol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-4-amine
2.7.12.1 0.411
-
pH and temperature not specified in the publication Homo sapiens N-(3,4-dichlorobenzyl)-4-(4-methoxyphenyl)pyrimidin-2-amine
2.7.12.1 0.514
-
pH and temperature not specified in the publication Homo sapiens N-(3,4-dichlorobenzyl)-2-(1H-indazol-5-yl)pyrimidin-4-amine
2.7.12.1 0.558
-
pH and temperature not specified in the publication Homo sapiens N-(4-chlorobenzyl)-4-(4-methoxyphenyl)pyrimidin-2-amine
2.7.12.1 0.599
-
pH and temperature not specified in the publication Homo sapiens N-(3,4-dichlorobenzyl)-4-(1H-indazol-6-yl)pyrimidin-2-amine
2.7.12.1 0.829
-
pH and temperature not specified in the publication Homo sapiens 2-(1H-indazol-6-yl)-N-(pyridin-3-ylmethyl)pyrimidin-4-amine
2.7.12.1 0.871
-
pH and temperature not specified in the publication Homo sapiens N-(4-chlorobenzyl)-4-(4-methoxyphenyl)pyrimidin-2-amine
2.7.12.1 0.884
-
pH and temperature not specified in the publication Homo sapiens 4-(1,3-benzodioxol-5-yl)-N-(4-chlorophenyl)pyrimidin-2-amine
2.7.12.1 1.156
-
pH and temperature not specified in the publication Homo sapiens 6-(1,3-benzodioxol-5-yl)-N-(3,5-dichlorobenzyl)quinazolin-4-amine
2.7.12.1 1.434
-
pH and temperature not specified in the publication Homo sapiens 2-(1H-indazol-6-yl)-N-(pyridin-3-ylmethyl)pyrimidin-4-amine
2.7.12.1 2.352
-
pH and temperature not specified in the publication Homo sapiens N-(3,4-dichlorobenzyl)-2-(1H-indazol-5-yl)pyrimidin-4-amine
2.7.12.1 3.454
-
pH and temperature not specified in the publication Homo sapiens 2-(1,3-benzodioxol-5-yl)-N-(3,4-dichlorobenzyl)pyrimidin-4-amine
2.7.12.1 4.579
-
pH and temperature not specified in the publication Homo sapiens 2-(1,3-benzodioxol-5-yl)-N-(4-chlorobenzyl)pyrimidin-4-amine
2.7.12.1 4.654
-
pH and temperature not specified in the publication Homo sapiens N-(3,4-dichlorobenzyl)-4-(3-methoxyphenyl)pyrimidin-2-amine
2.7.12.1 6.361
-
pH and temperature not specified in the publication Homo sapiens N-(4-chlorobenzyl)-4-(3-methoxyphenyl)pyrimidin-2-amine
2.7.12.1 6.782
-
pH and temperature not specified in the publication Homo sapiens N-(4-chlorobenzyl)-4-(3-methoxyphenyl)pyrimidin-2-amine
2.7.12.1 8.862
-
pH and temperature not specified in the publication Homo sapiens 2-(1,3-benzodioxol-5-yl)-N-(4-chlorobenzyl)pyrimidin-4-amine
2.7.12.1 10
-
above, pH and temperature not specified in the publication Homo sapiens 2-(1,3-benzodioxol-5-yl)-N-(3,4-dichlorobenzyl)pyrimidin-4-amine
2.7.12.1 10
-
above, pH and temperature not specified in the publication Homo sapiens 2-(1,3-benzodioxol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-4-amine
2.7.12.1 10
-
above, pH and temperature not specified in the publication Homo sapiens N-(3,4-dichlorobenzyl)-4-(3-methoxyphenyl)pyrimidin-2-amine
2.7.12.1 10
-
above, pH and temperature not specified in the publication Homo sapiens N-(3,4-dichlorobenzyl)-4-(3,4-dimethoxyphenyl)pyrimidin-2-amine