Table 2.

Results of initial optimization of 2.

Cmpd	X	R1	R2	PKN3a	GAKb
				IC50 (μM)	Ki (μM)
2	CH	CF3	H	0.28	0.0039
4	N	CF3	H	4.4	0.037
5	CH	H	H	1.1	0.040
6	CH	F	H	0.70	0.0057
7	N	F	H	5.8	0.033
8	CH	Cl	H	0.070	0.0069
9	CH	Br	H	0.0093	0.0031
10	CH	I	H	0.098	0.0038
11	N	I	H	2.7	0.011
12	CH	H	F	0.39	0.0024
13	N	H	F	3.9	0.055
14	CH	H	Cl	0.027	0.0013
15	CH	H	Br	0.12	0.0049
16	CH	H	I	0.014	0.0044
17	N	H	I	0.93	0.021
18	CH	tBu	H	0.31	0.0081
19	CH	CN	H	0.21	0.0015
20	CH	SO2CH3	H	0.60	0.018
21	CH	OCH3	H	0.74	0.013
22	CH	OCH3	OCH3	0.48	0.00054
23	CH	H	OCH3	0.92	0.0026
24	CH	H	CF3	0.24	0.0062
25	N	H	CF3	2.6	0.079
26	CH	H	CN	0.079	0.0027

^aIC₅₀ values generated in SLCA assay (n=2)^[27-29]

^bGAK FRET K_i values are previously reported^[30-31,35].