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. 2022 Sep 3;23(17):10070. doi: 10.3390/ijms231710070

Table 1.

In vitro activity of FAMs with possibly relevant side-target activity and with potential for SOSA 1.

Drug
(Structure, INN)		 Activity
Inline graphic
Oxaprozin		 partial RXR agonist [22]
EC50 = 16.1 ± 0.6 µM (23 ± 1% max. act.) (RXRα)
Inline graphic
Tianeptine		 partial PPARδ agonist
EC50 = 28 ± 4 µM (43 ± 4% max. act.)
Inline graphic
Bortezomib		 partial RAR agonist
EC50 = 0.8 ± 0.3 µM (<10% max. act.) (RARα)
Inline graphic
Mycophenolic acid		 partial RAR agonist
EC50 = 1.5 ± 0.6 µM (<10% max. act.) (RARα)

1 Activities were determined in Gal4 hybrid reporter gene assays. Maximum relative activation refers to the activity of the reference agonists bexarotene (RXR), L165041 (PPARδ), and tretinoin (RAR), each at 1 µM. Data are the mean ± S.E.M., n = 3.