Table 1:

Chemical structure and activity of EZH2 inhibitors in clinical trials

Compound	Structure	In vitro IC50(nM)	Methylation IC50 (nM)	Route of administration	Ref.
EPZ6438 (Tazemetostat)		2–38	2–90	Oral	[24]
GSK126		10–29	7–252	Intravenous	[25]
CPI-1205		2.2–3.1	32	Oral	[23]