Description
A mutant ERα antagonist and ligand used for bump and hole; is selective for ERα containing three substitutions, ErαL384M, ErαM421G, and ErαG521R, over the wild-type ERα and ERβ (IC50s= 29, 1,085, and 2,232 nM, respectively); reduces reporter gene expression in HeLa cells expressing the triple mutant ERα (EC50 = 41 nM)