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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 3. SAR of bicyclic amide substituents.

ID graphic file with name EMS203174-i001.jpg EC50(Nurr1)
(max. activation) a
32 graphic file with name EMS203174-i030.jpg 0.4±0.1 μM
(2.0±0.1-fold)
33 graphic file with name EMS203174-i031.jpg 0.12±0.04 μM
(1.5±0.1-fold)
34 graphic file with name EMS203174-i032.jpg 0.10±0.03 μM
(1.8±0.1-fold)
35 graphic file with name EMS203174-i033.jpg 0.13±0.04 μM
(1.7±0.1-fold)
36 graphic file with name EMS203174-i034.jpg 0.13±0.04 μM
(1.8±0.1-fold)
37 graphic file with name EMS203174-i035.jpg 0.06±0.02 μM
(1.9±0.1-fold)
38 graphic file with name EMS203174-i036.jpg 1.4±0.5 μM
(1.5±0.1-fold)
39 graphic file with name EMS203174-i037.jpg inactive (10 μM)
40 graphic file with name EMS203174-i038.jpg inactive (10 μM)
41 graphic file with name EMS203174-i039.jpg inactive (10 μM)
42 graphic file with name EMS203174-i040.jpg 0.5±0.2 μM
(1.4±0.1-fold)
43 graphic file with name EMS203174-i041.jpg 0.24±0.07 μM
(1.5±0.1-fold)
44 graphic file with name EMS203174-i042.jpg 0.31±0.05 μM
(2.1±0.1-fold)
45 graphic file with name EMS203174-i043.jpg 0.4±0.2 μM
(2.1±0.1-fold)
46 graphic file with name EMS203174-i044.jpg 0.10±0.04 μM
(2.0±0.1-fold)
47 graphic file with name EMS203174-i045.jpg 0.10±0.04 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.