Table 5 Optimization of the fused derivative 26

From: Development of Nurr1 agonists from amodiaquine by scaffold hopping and fragment growing

ID

R3 = 

EC50(Nurr1) (max. activation)a

27

4 ± 1 µM (2.1 ± 0.1-fold)

26

1.6 ± 0.5 µM (1.8 ± 0.1-fold)

31

1.1 ± 0.3 µM (1.8 ± 0.1-fold)

32

0.13 ± 0.02 µM (2.0 ± 0.2-fold)

33

0.8 ± 0.2 µM (2.0 ± 0.1-fold)

34

0.16 ± 0.06 µM (1.7 ± 0.1-fold)

35

0.30 ± 0.02 µM (1.8 ± 0.1-fold)

36

0.090 ± 0.005 µM (2.1 ± 0.1-fold)

  1. aNurr1 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.
Back to article page