Table 1.

Inhibiting activity of compounds 1a–r against EZH2/PRC2.

compound	n	R1	R2	% inhibition at 50 µM	IC50 (μM)
1a	0	1H-pyrrol-1-yl	isopropyl	0
1b	0	1H-pyrrol-1-yl	cyclopentyl	4.7
1c	0	1H-pyrrol-1-yl	phenyl	0
1d	0	1H-pyrrol-1-yl	benzyl	5.8
1e	0	phenyl	isopropyl	0
1f	0	phenyl	cyclopentyl	2.7
1g	0	phenyl	phenyl	6.9
1h	0	phenyl	benzyl	20
1i	0	styryl	isopropyl	0
1j	0	styryl	cyclopentyl	2.9
1k	0	styryl	phenyl	0
1l	0	styryl	benzyl	11.8
1m	0	H	phenyl	25.3	>400
1n	0	methyl	isopropyl	16.7	342.7
1o	0	methyl	phenyl	71.5	15.4
1p	0	methyl	benzyl	68.3	19.6
1q	0	n-propyl	phenyl	29.0	151
1r	1	methyl	phenyl	4.5	>400
SAH					34.7
GSK126					0.009