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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 2. Evaluation of alternative m/p-substituents.

ID graphic file with name EMS203174-i001.jpg EC50(Nurr1)
(max. activation) a
19 graphic file with name EMS203174-i017.jpg inactive (10 μM)
20 graphic file with name EMS203174-i018.jpg 1.1±0.2 μM
(1.4±0.1-fold)
21 graphic file with name EMS203174-i019.jpg inactive (10 μM)
22 graphic file with name EMS203174-i020.jpg inactive (10 μM)
23 graphic file with name EMS203174-i021.jpg inactive (10 μM)
24 graphic file with name EMS203174-i022.jpg 0.26±0.04 μM
(1.6±0.1-fold)
25 graphic file with name EMS203174-i023.jpg 0.5±0.2 μM
(1.4±0.1-fold)
26 graphic file with name EMS203174-i024.jpg 0.04±0.01 μM
(1.5±0.1-fold)
27 graphic file with name EMS203174-i025.jpg 0.32±0.08 μM
(1.4±0.1-fold)
28 graphic file with name EMS203174-i026.jpg 0.7±0.1 μM
(1.9±0.1-fold)
29 graphic file with name EMS203174-i027.jpg 0.07±0.02 μM
(1.5±0.1-fold)
30 graphic file with name EMS203174-i028.jpg 0.9±0.2 μM
(1.5±0.1-fold)
31 graphic file with name EMS203174-i029.jpg 0.2±0.1 μM
(1.5±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.