femtomolar EZH2 hist. methyltransferase inh.
oral activity (10-25 mg/kg QD) in xenograft
from opt. of prior ligand
J. Bio. Chem., Jan. 30, 2021
Constellation Pharma, Cambridge, MA
12. The 2nd generation Constellation EZH2 histone methyltransferase inhibitor, CPI-1328, is an extremely potent tool compound with reversible femtomolar activity against EZH2, and is one of the most potent…