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. Author manuscript; available in PMC: 2017 Jan 14.
Published in final edited form as: J Med Chem. 2015 Dec 30;59(1):219–237. doi: 10.1021/acs.jmedchem.5b01276

Figure 3.

Figure 3

Profiling ERα ligands: endogenous agonist E2 (1); SERM antagonist raloxifene (3); benzothiophene partial agonist (ShERPA) (30a). (A) Activation of ERE (estrogen response element) in MCF-7:ws8 cells. (B) RBAral from FP assay of displacement of fluorescent-E2 from ERα. (C) Cell viability of tamoxifen-resistant MCF-7:5C breast cancer cells 9 days after drug treatment, normalized to vehicle (100%). Data show mean and s.e.m.