Table 4 Fusion of 8 with N-substituents

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

ID

R2 = 

EC50(Nurr1) (max. activation)a

8

7 ± 1 µM (2.0 ± 0.1-fold)

26

1.6 ± 0.5 µM (1.8 ± 0.1-fold)

27

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4 ± 1 µM (2.1 ± 0.1-fold)

28

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3.2 ± 0.4 µM (2.1 ± 0.1-fold)

29

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inactive (10 µMb)

30

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inactive (10 µMb)

  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. bHighest non-toxic concentration.