This study comprehensively investigates the scope of potential of Ormeloxifene to be developed as a better effective and prospective SERM, in comparison with other SERMS against ER dependent as well as ER independent cancers by in-vitro cytotoxicity assay on twenty six different cancer cell lines of different origin and predictive molecular docking studies on various important target genes involved in cancer progression and treatment responses. The gene discussed is ESR1; the disease is cancer.