Table 4. Modification of the amide linker.
| ID | EC50(Nurr1) (max. activation) a |
|
|---|---|---|
| 37 |
|
0.06±0.02 μM (1.9±0.1-fold) |
| 48 |
|
inactive (10 μM) |
| 49 |
|
1.2±0.2 μM (1.5±0.1-fold) |
| 50 |
|
inactive (10 μM) |
| 51 |
|
0.21±0.07 μM (1.6±0.1-fold) |
Nurr1 modulation was determined in a Gal4-Nurr1 hybrid reporter gene assay. Max. activation refers to the maximum effect vs. 0.1% DMSO control. Data are the mean±SD; n≥3.