FIGURE 6.

Cytotoxicity, solubility, and permeability of MSNB analogs. The heat map shows IC₅₀ values for the TRβ-SRC2-2 FP assay, cell cytotoxicity (Raji, BJ, HEK293, and HepG2), solubility, and permeability. Cytotoxicity potencies were determined by the measurement of total ATP content using CellTiter-Glo® (Promega) after incubation with compound for 72 h. Solubility was measured using the Millipore method in PBS (pH 7.4). Permeability was measured using PAMPA (pH 7.4). The solubility and permeability assay conditions reflect the conditions required for activity in cell-based assays. Compounds are ordered by potency of antagonism of the TRβ and SRC2-2 interaction. The numerical values underlying this heat map are presented in supplemental Table 1.