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Literature summary for 2.7.12.1 extracted from
- 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.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| (1Z)-1-(3-ethyl-5-methoxy-1,3-benzothiazol-2(3H)-ylidene)propan-2-one | - |
Homo sapiens |  |
| 2-(1,3-benzodioxol-5-yl)-N-(3,4-dichlorobenzyl)pyrimidin-4-amine | - |
Homo sapiens | |
| 2-(1,3-benzodioxol-5-yl)-N-(4-chlorobenzyl)pyrimidin-4-amine | - |
Homo sapiens | |
| 2-(1,3-benzodioxol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-4-amine | - |
Homo sapiens | |
| 2-(1H-indazol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-4-amine | - |
Homo sapiens | |
| 2-(1H-indazol-6-yl)-N-(pyridin-3-ylmethyl)pyrimidin-4-amine | - |
Homo sapiens | |
| 3-[4-(2-phenylethyl)quinazolin-6-yl]benzonitrile | - |
Homo sapiens | |
| 3-[4-[2-(4-methoxyphenyl)ethyl]quinazolin-6-yl]benzonitrile | - |
Homo sapiens | |
| 3-[4-[2-(4-methylphenyl)ethyl]quinazolin-6-yl]benzonitrile | - |
Homo sapiens | |
| 4-(1,3-benzodioxol-5-yl)-N-(3,4-dibromobenzyl)pyrimidin-2-amine | - |
Homo sapiens | |
| 4-(1,3-benzodioxol-5-yl)-N-(3,4-dichlorobenzyl)pyrimidin-2-amine | - |
Homo sapiens | |
| 4-(1,3-benzodioxol-5-yl)-N-(3,5-dibromobenzyl)pyrimidin-2-amine | - |
Homo sapiens | |
| 4-(1,3-benzodioxol-5-yl)-N-(3,5-dichlorobenzyl)pyrimidin-2-amine | - |
Homo sapiens | |
| 4-(1,3-benzodioxol-5-yl)-N-(4-chlorobenzyl)pyrimidin-2-amine | - |
Homo sapiens | |
| 4-(1,3-benzodioxol-5-yl)-N-(4-chlorophenyl)pyrimidin-2-amine | - |
Homo sapiens | |
| 4-(1,3-benzodioxol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-2-amine | - |
Homo sapiens | |
| 4-(1,3-benzodioxol-5-yl)-N-[2-bromo-4-(trifluoromethyl)phenyl]pyrimidin-2-amine | - |
Homo sapiens | |
| 4-(1,3-benzodioxol-5-yl)-N-[4-(trifluoromethyl)phenyl]pyrimidin-2-amine | - |
Homo sapiens | |
| 4-(1H-indazol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-2-amine | - |
Homo sapiens | |
| 4-(1H-indazol-6-yl)-N-(pyridin-3-ylmethyl)pyrimidin-2-amine | - |
Homo sapiens | |
| 6-(1,3-benzodioxol-5-yl)-N-(3,4-dichlorobenzyl)pyrimidin-4-amine | - |
Homo sapiens | |
| 6-(1,3-benzodioxol-5-yl)-N-(3,5-dichlorobenzyl)pyrimidin-4-amine | - |
Homo sapiens | |
| 6-(1,3-benzodioxol-5-yl)-N-(3,5-dichlorobenzyl)quinazolin-4-amine | - |
Homo sapiens | |
| 6-(1,3-benzodioxol-5-yl)-N-(4-chlorobenzyl)pyrimidin-4-amine | - |
Homo sapiens | |
| 6-(1,3-benzodioxol-5-yl)-N-(4-methoxybenzyl)quinazolin-4-amine | - |
Homo sapiens | |
| 6-(1,3-benzodioxol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-4-amine | - |
Homo sapiens | |
| 6-(1,3-benzodioxol-5-yl)-N-benzylquinazolin-4-amine | - |
Homo sapiens | |
| 6-(3-methoxyphenyl)-N-(4-methylbenzyl)quinazolin-4-amine | - |
Homo sapiens | |
| 6-(3-methoxyphenyl)quinazoline | - |
Homo sapiens | |
| harmine | a plant-derived beta-carboline alkaloid, ATP-competitive; a plant-derived beta-carboline alkaloid, ATP-competitive | Homo sapiens | |
| leucettamine B | marine alkaloid, strong inhibitor | Homo sapiens | |
| leucettine L-41 | - |
Homo sapiens | |
| ML315 | - |
Homo sapiens | |
| 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 | |
| N,4-bis(1,3-benzodioxol-5-yl)pyrimidin-2-amine | - |
Homo sapiens | |
| N-(3,4-dichlorobenzyl)-2-(1H-indazol-5-yl)pyrimidin-4-amine | - |
Homo sapiens | |
| N-(3,4-dichlorobenzyl)-4-(1H-indazol-5-yl)pyrimidin-2-amine | - |
Homo sapiens | |
| N-(3,4-dichlorobenzyl)-4-(1H-indazol-6-yl)pyrimidin-2-amine | - |
Homo sapiens | |
| N-(3,4-dichlorobenzyl)-4-(2,3-dihydro-1,4-benzodioxin-6-yl)pyrimidin-2-amine | - |
Homo sapiens | |
| N-(3,4-dichlorobenzyl)-4-(3,4-dimethoxyphenyl)pyrimidin-2-amine | - |
Homo sapiens | |
| N-(3,4-dichlorobenzyl)-4-(3-methoxyphenyl)pyrimidin-2-amine | - |
Homo sapiens | |
| N-(3,4-dichlorobenzyl)-4-(4-methoxyphenyl)pyrimidin-2-amine | - |
Homo sapiens | |
| N-(3,4-dichlorobenzyl)-6-(pyridin-3-yl)quinazolin-4-amine | - |
Homo sapiens | |
| N-(4-chlorobenzyl)-4-(3-methoxyphenyl)pyrimidin-2-amine | - |
Homo sapiens | |
| N-(4-chlorobenzyl)-4-(4-methoxyphenyl)pyrimidin-2-amine | - |
Homo sapiens | |
| N-(4-chlorobenzyl)-6-(3-methoxyphenyl)quinazolin-4-amine | - |
Homo sapiens | |
| N-(4-chlorobenzyl)-6-(pyridin-3-yl)quinazolin-4-amine | - |
Homo sapiens | |
| N-(4-methoxybenzyl)-6-(3-methoxyphenyl)quinazolin-4-amine | - |
Homo sapiens | |
| N-(4-methoxybenzyl)-6-(pyridin-3-yl)quinazolin-4-amine | - |
Homo sapiens | |
| TG003 | - |
Homo sapiens | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | Q13627 | - |
- |
| Homo sapiens | Q9Y463 | - |
- |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| dual specificity tyrosine phosphorylation-regulated kinase | - |
Homo sapiens |
| Dyrk kinase | - |
Homo sapiens |
| DYRK1A | - |
Homo sapiens |
| DYRK1B | - |
Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.000012 | - |
pH and temperature not specified in the publication | Homo sapiens | TG003 | |
| 0.000033 | 0.00008 | pH and temperature not specified in the publication | Homo sapiens | harmine | |
| 0.00004 | - |
pH and temperature not specified in the publication | Homo sapiens | leucettine L-41 | |
| 0.00013 | - |
pH and temperature not specified in the publication | Homo sapiens | TG003 | |
| 0.000166 | - |
pH and temperature not specified in the publication | Homo sapiens | harmine | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 0.0129 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(3,4-dichlorobenzyl)-4-(1H-indazol-5-yl)pyrimidin-2-amine | |
| 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 | |
| 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 | |
| 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 | |
| 0.0164 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-[4-[2-(4-methoxyphenyl)ethyl]quinazolin-6-yl]benzonitrile | |
| 0.0169 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(3,4-dichlorobenzyl)-4-(1H-indazol-6-yl)pyrimidin-2-amine | |
| 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 | |
| 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 | |
| 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 | |
| 0.0207 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(4-chlorobenzyl)-6-(3-methoxyphenyl)quinazolin-4-amine | |
| 0.025 | - |
pH and temperature not specified in the publication | Homo sapiens | N,4-bis(1,3-benzodioxol-5-yl)pyrimidin-2-amine | |
| 0.026 | - |
pH and temperature not specified in the publication | Homo sapiens | 6-(1,3-benzodioxol-5-yl)-N-benzylquinazolin-4-amine | |
| 0.026 | - |
pH and temperature not specified in the publication | Homo sapiens | 6-(3-methoxyphenyl)quinazoline | |
| 0.026 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(4-methoxybenzyl)-6-(3-methoxyphenyl)quinazolin-4-amine | |
| 0.0292 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(4-chlorobenzyl)-6-(pyridin-3-yl)quinazolin-4-amine | |
| 0.0328 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(4-methoxybenzyl)-6-(pyridin-3-yl)quinazolin-4-amine | |
| 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 | |
| 0.0412 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-[4-[2-(4-methylphenyl)ethyl]quinazolin-6-yl]benzonitrile | |
| 0.0412 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(3,4-dichlorobenzyl)-6-(pyridin-3-yl)quinazolin-4-amine | |
| 0.042 | - |
pH and temperature not specified in the publication | Homo sapiens | N,4-bis(1,3-benzodioxol-5-yl)pyrimidin-2-amine | |
| 0.0463 | - |
pH and temperature not specified in the publication | Homo sapiens | 6-(1,3-benzodioxol-5-yl)-N-(4-methoxybenzyl)quinazolin-4-amine | |
| 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 | |
| 0.061 | - |
pH and temperature not specified in the publication | Homo sapiens | 4-(1H-indazol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-2-amine | |
| 0.0654 | - |
pH and temperature not specified in the publication | Homo sapiens | 6-(3-methoxyphenyl)-N-(4-methylbenzyl)quinazolin-4-amine | |
| 0.093 | - |
pH and temperature not specified in the publication | Homo sapiens | 4-(1H-indazol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-2-amine | |
| 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 | |
| 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 | |
| 0.125 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(3,4-dichlorobenzyl)-4-(1H-indazol-5-yl)pyrimidin-2-amine | |
| 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 | |
| 0.179 | - |
pH and temperature not specified in the publication | Homo sapiens | 2-(1H-indazol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-4-amine | |
| 0.203 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(3,4-dichlorobenzyl)-4-(4-methoxyphenyl)pyrimidin-2-amine | |
| 0.273 | - |
pH and temperature not specified in the publication | Homo sapiens | 4-(1,3-benzodioxol-5-yl)-N-(4-chlorophenyl)pyrimidin-2-amine | |
| 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 | |
| 0.349 | - |
pH and temperature not specified in the publication | Homo sapiens | 2-(1H-indazol-5-yl)-N-(pyridin-3-ylmethyl)pyrimidin-4-amine | |
| 0.411 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(3,4-dichlorobenzyl)-4-(4-methoxyphenyl)pyrimidin-2-amine | |
| 0.514 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(3,4-dichlorobenzyl)-2-(1H-indazol-5-yl)pyrimidin-4-amine | |
| 0.558 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(4-chlorobenzyl)-4-(4-methoxyphenyl)pyrimidin-2-amine | |
| 0.599 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(3,4-dichlorobenzyl)-4-(1H-indazol-6-yl)pyrimidin-2-amine | |
| 0.829 | - |
pH and temperature not specified in the publication | Homo sapiens | 2-(1H-indazol-6-yl)-N-(pyridin-3-ylmethyl)pyrimidin-4-amine | |
| 0.871 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(4-chlorobenzyl)-4-(4-methoxyphenyl)pyrimidin-2-amine | |
| 0.884 | - |
pH and temperature not specified in the publication | Homo sapiens | 4-(1,3-benzodioxol-5-yl)-N-(4-chlorophenyl)pyrimidin-2-amine | |
| 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 | |
| 1.434 | - |
pH and temperature not specified in the publication | Homo sapiens | 2-(1H-indazol-6-yl)-N-(pyridin-3-ylmethyl)pyrimidin-4-amine | |
| 2.352 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(3,4-dichlorobenzyl)-2-(1H-indazol-5-yl)pyrimidin-4-amine | |
| 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 | |
| 4.579 | - |
pH and temperature not specified in the publication | Homo sapiens | 2-(1,3-benzodioxol-5-yl)-N-(4-chlorobenzyl)pyrimidin-4-amine | |
| 4.654 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(3,4-dichlorobenzyl)-4-(3-methoxyphenyl)pyrimidin-2-amine | |
| 6.361 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(4-chlorobenzyl)-4-(3-methoxyphenyl)pyrimidin-2-amine | |
| 6.782 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(4-chlorobenzyl)-4-(3-methoxyphenyl)pyrimidin-2-amine | |
| 8.862 | - |
pH and temperature not specified in the publication | Homo sapiens | 2-(1,3-benzodioxol-5-yl)-N-(4-chlorobenzyl)pyrimidin-4-amine | |
| 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 | |
| 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 | |
| 10 | - |
above, pH and temperature not specified in the publication | Homo sapiens | N-(3,4-dichlorobenzyl)-4-(3-methoxyphenyl)pyrimidin-2-amine | |
| 10 | - |
above, pH and temperature not specified in the publication | Homo sapiens | N-(3,4-dichlorobenzyl)-4-(3,4-dimethoxyphenyl)pyrimidin-2-amine | |
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