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…

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