Table 1. EPZ011989 in Vitro Data Summary.

property	analysis	units	EPZ011989
EZH2 activity	biochemical Ki	nM	<3 (WT) <3 (Y646)
	ELISA H3K27me3 IC50a	nM	94 ± 48 (n = 20)
liver microsome clearance	scaled microsomal clearanceb	mL/min/kg (%Eh)c	human	6 ± 0.5(29)
			rat	<10(<14)
			mouse	<10(<11)
plasma protein binding	equilibrium dialysis	percent unbound	human	97 ± 3
			rat	91 ± 6
			mouse	80 ± 11
LCC	11d proliferation WSU-DLCL2	nM	208 ± 75 (n = 4)
	predicted efficacious plasma exposured	nM (ng/mL)	human	214(130)
			rat	223(135)
			mouse	260(158)

^aEnzyme-linked immunoassay measure of cellular methyl mark reduction.

^bScaled according to the well-stirred liver model.

^cPercent hepatic extraction.

^dPlasma protein binding corrected LCC.