4 research outputs found
Reawakening of Human Fetal Hemoglobin and an Epigenetic Path to the Clinic for Sickle Cell Disease and Beta-Thalassemia: Identification of an Orally-Available, Potent, and Selective Euchromatic Histone Lysine Methyltransferase 1 and 2 ( EHMT1/2) Inhibitor
No full textStructure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666
No full textThe recent publication of a potent
and selective inhibitor of protein
methyltransferase 5 (PRMT5) provides the scientific community with <i>in vivo</i>-active tool compound <b>EPZ015666</b> (<b>GSK3235025</b>) to probe the underlying pharmacology of this key
enzyme. Herein, we report the design and optimization strategies employed
on an initial hit compound with poor <i>in vitro</i> clearance
to yield <i>in vivo</i> tool compound <b>EPZ015666</b> and an additional potent <i>in vitro</i> tool molecule <b>EPZ015866</b> (<b>GSK3203591</b>)
