Table 4.

In vitro TBK1 kinase inhibitory activity of the 15x–15ab.^a

Compd.	X	R2	R3	TBK1 inhibition（%）					IC50/nM
				1 μM	100 nM	10 nM	1 nM	0.1 nM
15x	N			75.8	80.5	34.1	18.6	N.T.	22.0
15y	N			53.9	102.4	93.8	88.8	33.6	0.2
15z	N			79.5	84.4	48.4	32.7	N.T.	24.4
15aa	N			48.3	36.8	14.10	N.T.b	N.T.	N.T.
15ab	C			90.3	72.9	70.9	60.1	43.1	3.6
BX795				N.T.	99.6	72.9	37.7	0.18	7.1
MRT67307				N.T.	92.8	29.6	2.4	<0	28.7

^aThe IC₅₀ values are shown as the mean (nM) values from two separate experiments.

^bN.T. = not tested.