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. 2022 Feb 21;17(8):e202200026. doi: 10.1002/cmdc.202200026

Table 1.

Nurr1 agonism of the purified compounds 3 j, 4, 4 e, and 5. AQ (1), [29] CQ, [29] 2 [24] and lead fragment 3 [24] for comparison. Fold activation refers to the maximum Nurr1 activation vs. DMSO (0.1 %). Data are the mean±S.E.M., n≥3.

ID

structure

EC50(Nurr1) (fold act.)

AQ

graphic file with name CMDC-17-0-g006.jpg

36±4 μM (3.6±0.1‐fold)

CQ

graphic file with name CMDC-17-0-g001.jpg

47±5 μM (2.0±0.1‐fold)

2

graphic file with name CMDC-17-0-g004.jpg

1.8±0.3 μM (1.47±0.03‐fold)

3

graphic file with name CMDC-17-0-g011.jpg

259±70 μM (2.5±0.4‐fold)

3 j

graphic file with name CMDC-17-0-g016.jpg

8±1 μM (2.5±0.1‐fold)

4

graphic file with name CMDC-17-0-g003.jpg

3.0±0.1 μM (2.0±0.1‐fold)

4 e

graphic file with name CMDC-17-0-g015.jpg

6±2 μM (1.40±0.05‐fold)

5

graphic file with name CMDC-17-0-g005.jpg

47±13 μM (2.0±0.2‐fold)