Tamoxifen: Selectivity & Specificity

Tamoxifen is a potent inhibitor of ER αLBD (10.46 nM), PKC β1 kinase (4900 nM), human recombinant CYP1A1 (12000 nM), PI3K α (19000 nM), PI3K β (14000 nM), PI3K δ (10000 nM), TGF-β, Collagen, ER, Cell proliferation, Breast cancer mortality, Acute bipolar mania, and Cryptococcus. Tamoxifen exhibits the greatest inhibitory potency toward ER αLBD (IC50 = 10.46 nM).