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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 4. Modification of the amide linker.

ID EC50(Nurr1)
(max. activation) a
37 graphic file with name EMS203174-i046.jpg 0.06±0.02 μM
(1.9±0.1-fold)
48 graphic file with name EMS203174-i047.jpg inactive (10 μM)
49 graphic file with name EMS203174-i048.jpg 1.2±0.2 μM
(1.5±0.1-fold)
50 graphic file with name EMS203174-i049.jpg inactive (10 μM)
51 graphic file with name EMS203174-i050.jpg 0.21±0.07 μM
(1.6±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.