EC Number   |
Inhibitors |
Structure |
|---|
   2.7.11.25 | (E)-N-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)-phenyl)-3-(2-(4-methoxy-1H-pyrrolo[2,3-b]pyridin-5-yl)vinyl)-4-methylbenzamide |
88,5% inhibition of TAK1 at 500 nM |
   |
| 2.7.11.25 | 14-3-3 |
the binding site is on the CR2 domain of the enzyme |
|
| 2.7.11.25 | 2-amino-1-{4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}-2-[4-methyl-3-(1H-pyrrolo[2,3-b]pyridin-4-yloxy)phenyl]ethanone |
- |
|
| 2.7.11.25 | 3-((1H-pyrrolo[2,3-b]pyridin-4-yl)oxy)-N-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-4-methylbenzamide |
a type II inhibitor, 97.1% inhibition of TAK1 at 500 nM |
|
| 2.7.11.25 | 3-[(6,7-dimethoxyquinazolin-4-yl)oxy]-N-{4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}-4-methylbenzamide |
83.7% inhibition of TAK1 at 0.001 mM |
|
| 2.7.11.25 | 4-methyl-3-{[6-(methylamino)pyrimidin-4-yl]oxy}-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]benzamide |
selectivity analysis with diverse enzymes, overview. 29.3% Inhibition of TAK1 at 0.001 mM |
|
| 2.7.11.25 | 4-methyl-3-{[6-(methylamino)pyrimidin-4-yl]oxy}-N-[3-(4-methylpiperazin-1-yl)-5-(trifluoromethyl)phenyl]benzamide |
selectivity analysis with diverse enzymes, overview. 7.0% Inhibition of TAK1 at 0.001 mM |
|
| 2.7.11.25 | 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-(1H-pyrrolo[2,3-b]pyridin-4-yloxy)benzamide |
- |
|
| 2.7.11.25 | 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[2-(1H-pyrrolo[2,3-b]pyridin-4-yl)ethyl]benzamide |
- |
|
| 2.7.11.25 | 4-methyl-N-[3-(4-methylpiperazin-1-yl)-5-(trifluoromethyl)phenyl]-3-(7H-pyrrolo[2,3-d]pyrimidin-4-yloxy)benzamide |
29.3% inhibition of TAK1 at 0.001 mM |
|
