TABLE 1.

Structures and potencies of MSNB analogs in TRB-SRC2 interaction assays

IC₅₀ values were determined using data from two independent experiments in triplicate.

^a Primary HTS hit compounds.

^b Competitive fluorescence polarization assay in the presence of TRβ-LBD (0.6 μm), T₃ (1 μm), and Texas Red-labeled SRC2–2 peptide (20 nm). The data were recorded after a 3-h incubation.

^c Competitive AlphaScreen assay in the presence of TRβ-LBD (0.1 μm), T3 (1 μm), and biotin-labeled SRC2–2 peptide (30 nm).

^d Percent efficacy is indicated within parentheses.