Fig. 3

Lead T6Is and clinically relevant SERMs and SERDs inhibit WT and Y537S ERα-Coactivator binding. HEK 293T cells were co-transfected with indicated plasmids (WT ERα or Y537S ERα and SRC3), charcoal stripped for 72-hours, followed by treated with increasing concentrations of drug for 48 h prior to bioluminescence reading. Clinically relevant (A) SERD and (B) SERM inhibition curves with WT-SRC3 binding. (C) Rad1901 and T6Is inhibition curves for WT-SRC3 binding. D-F) Same as A-C, but with Y537S-SRC3 binding. Data are shown as the mean ± s.d