Table 7 Optimization of 36 for microsomal stability
From: Development of Nurr1 agonists from amodiaquine by scaffold hopping and fragment growing
ID |
| EC50(Nurr1) (max. act.)a | microsomal half-lifeb |
|---|---|---|---|
36 |
| 0.090 ± 0.005 µM (2.1 ± 0.1-fold) | 6.3 ± 0.3 min. |
38 |
| <1.2-fold activation | n.d. |
39 |
| inactive (10 µMc) | n.d. |
40 |
| inactive (10 µMd) | n.d. |
34 |
| 0.16 ± 0.06 µM (1.7 ± 0.1-fold) | 18 ± 2 min. |
41 |
| 0.12 ± 0.03 µM (2.1 ± 0.2-fold) | 42 ± 5 min. |
42 |
| 0.12 ± 0.06 µM (1.5 ± 0.2-fold) | 78 ± 7 min. |
R3 = 
