Table 3 Extension of the imidazo[1,2-a]pyridine 8
From: Development of Nurr1 agonists from amodiaquine by scaffold hopping and fragment growing
ID |
| EC50(Nurr1) (max. activation)a |
|---|---|---|
8 |
| 7 ± 1 µM (2.0 ± 0.1-fold) |
14 |
| < 1.2-fold act. |
15 |
| 4 ± 2 µM (1.4 ± 0.1-fold) |
16 |
| < 1.2-fold act. |
17 |
| 15 ± 3 µM (1.7 ± 0.2-fold) |
18 |
| 9 ± 3 µM (1.7 ± 0.1-fold) |
19 |
| inactive (100 µM) |
20 |
| 12 ± 2 µM (2.0 ± 0.2-fold) |
21 |
| < 1.2-fold act. |
22 |
| < 1.2-fold act. |
23 |
| < 1.2-fold act. |
24 |
| 0.4 ± 0.2 µM (1.8 ± 0.1-fold) |
25 |
| 14 ± 2 µM (1.6 ± 0.1-fold) |
R1 = 
