Table 1.

SAR of the 4-Amino Moiety.

Compound	R1 Group	SETD8 IC50 (µM)a
1		7.3 ± 1.0b
2		7.9 ± 0.8b
3		7.9 ± 1.2
4		7.9 ± 1.4b
5		26 ± 5
6		40 ± 1
7		40 ± 6
8		43 ± 5
9		> 250
10		> 250
11		63 ± 19
12		> 250
13		32 ± 8b
14		> 250
15		> 250

^aIC₅₀ determination experiments were performed in duplicate.

^bIC₅₀ value was reported previously.⁴²