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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

Figure 3. In vitro characterization of 37.

Figure 3

(a) Selectivity profiling of 37 on constitutively active nuclear receptors in uniform Gal4-hybrid reporter gene assays. Data are the mean±S.E.M. fold activation vs. DMSO ctrl; n=3. (b) Selectivity profiling of 37 on lipid-activated nuclear receptors in uniform Gal4-hybrid reporter gene assays. Data are the mean±S.E.M. relative activation vs. reference ligands; n=3. Reference ligands are listed in the methods section. (c) Dose-response curves of 37 on the NR4A receptors. Data are the mean±S.E.M., n≥3. (d) Effects of 37 in a multiplex toxicity assay measuring confluence, metabolic activity, necrosis and apoptosis in HEK293T and COS-7 cells. Bexarotene (100 μM) as positive control. Data are the mean±S.E.M., n≥3. (e) Stability of 37 against degradation by rat liver microsomes. Propranolol for comparison. Data are the mean±S.E.M., n=3.