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. Author manuscript; available in PMC: 2025 Mar 24.
Published in final edited form as: J Med Chem. 2025 Feb 7;68(4):4829–4847. doi: 10.1021/acs.jmedchem.4c03104

Table 1. Deconstruction of the 5-chloro-2-(2-(dimethylamino)ethoxy)aniline substituent.

ID graphic file with name EMS203174-i001.jpg EC50(Nurr1)
(max. activation) a
4 graphic file with name EMS203174-i002.jpg 3±1 μM
(1.3±0.1-fold)
5 graphic file with name EMS203174-i003.jpg inactive (10 μM)
6 graphic file with name EMS203174-i004.jpg inactive (10 μM)
7 graphic file with name EMS203174-i005.jpg inactive (10 μM)
8 graphic file with name EMS203174-i006.jpg 0.06±0.03 μM
(1.5±0.1-fold)
9 graphic file with name EMS203174-i007.jpg 0.7±0.1 μM
(1.4±0.1-fold)
10 graphic file with name EMS203174-i008.jpg 0.6±0.2 μM
(1.5±0.1-fold)
11 graphic file with name EMS203174-i009.jpg 1.5±0.1 μM
(1.6±0.1-fold)
12 graphic file with name EMS203174-i010.jpg 0.08±0.02 μM
(1.4±0.1-fold)
13 graphic file with name EMS203174-i011.jpg inactive (10 μM)
14 graphic file with name EMS203174-i012.jpg 0.5±0.2 μM
(1.5±0.1-fold)
15 graphic file with name EMS203174-i013.jpg 0.33±0.09 μM
(1.6±0.1-fold)
16 graphic file with name EMS203174-i014.jpg 1.0±0.2 μM
(1.4±0.1-fold)
17 graphic file with name EMS203174-i015.jpg 1.0±0.2 μM
(1.3±0.1-fold)
18 graphic file with name EMS203174-i016.jpg 1.7±0.5 μM
(1.3±0.1-fold)
a

Nurr1 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.