pone.0248034.s003.tif (10.36 MB)

Selectivity of human RORγt inhibitors.

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posted on 2021-11-09, 18:32 authored by Steven A. Saenz, Andrea Local, Tiffany Carr, Arvind Shakya, Shivsmriti Koul, Haiqing Hu, Lisa Chourb, Justin Stedman, Jenna Malley, Laura Akullian D’Agostino, Veerabahu Shanmugasundaram, John Malona, C. Eric Schwartz, Lisa Beebe, Meghan Clements, Ganesh Rajaraman, John Cho, Lan Jiang, Alex Dubrovskiy, Matt Kreilein, Roman Shimanovich, Lawrence G. Hamann, Laure Escoubet, J. Michael Ellis

RORγt inhibitor selectivity of Compound 1, Compound 2 or Compound 3 was assessed in nuclear hormone receptor binding assays, as measured by percent inhibition. Assays utilized reporter cells (HEK293) harboring a receptor hybrid in which the native N-terminal DNA binding domain (DBD) has been replaced with that of the yeast Gal4 DBD, with a firefly luciferase reporter gene functionally linked to a Gal4 upstream activation sequence. All compounds were dosed at 10 μM and percent inhibition calculated by relative light units (RLUs) compared to vehicle. *, repeat dose response curves failed to generate reliable IC50 values for compounds tested. RAR, RAR-related orphan receptor alpha; PPARγ, peroxisome proliferator-activated receptor gamma; TRα, thyroid hormone receptor alpha; GR, glucocorticoid receptor; LXR, liver X receptor.

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Selectivity of human RORγt inhibitors.

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