3 research outputs found
Effects of Topical Application of Betamethasone on Imiquimod-induced Psoriasis-like Skin Inflammation in Mice
SAR Exploration Guided by LE and Fsp<sup>3</sup>: Discovery of a Selective and Orally Efficacious RORγ Inhibitor
A novel
series of RORγ inhibitors was identified starting with the HTS
hit <b>1</b>. After SAR investigation based on a prospective
consideration of two drug-likeness metrics, ligand efficiency (LE)
and fraction of sp<sup>3</sup> carbon atoms (Fsp<sup>3</sup>), significant
improvement of metabolic stability as well as reduction of CYP inhibition
was observed, which finally led to discovery of a selective and orally
efficacious RORγ inhibitor <b>3z</b>