. 2014 Oct 23;6(1):73–78. doi: 10.1021/ml5003376

Table 2. SGK1 Activity of Selected 1H-Pyrazolo[3,4-b]pyrazines 14, 16, and 21.

	sulfonamide Ar	X	IC₅₀ (μM) 10 μM (ATP)	IC₅₀ (μM) 500 μM (ATP)
14a	1-naphtyl	H	0.016	0.760
14b	3-(2,5-dichlorothienyl)	H	0.004	0.183
14c	3-Cl-5-hydrazino-Ph	H	0.196	0.639
14d	2-ClPh	H	0.014	0.910
14e	2-Cl-3-FPh	H	0.021	1.26
14f	2,4-diClPh	H		4.76
14g	2,3-diClPh	H	0.003	0.442
14h	2,5-diClPh	H	0.005	0.025
14i	2-Cl-5-MeOPh	H	0.002	0.034
14j	2-Cl-4-CF₃Ph	H	0.407	18.9
14k	2-FPh	H	0.022	1.49
14l	2,5-diFPh	H	0.015	0.730
14m	5-Cl-2,4-diFPh	H	<0.002	0.041
14n	5-Cl-2-FPh	H	0.001	0.041
14o	2-F-5-MePh	H	0.002	0.039
14p	2-F-5-MeOPh	H	<0.002	0.004
14q	5-Cl-2-CNPh	H	0.01	0.293
14r	5-Me-2-CNPh	H	0.003	0.061
14s	5-MeO-2-CNPh	H	0.002	0.040
14t	2,3-diClPh	F	0.003	0.182
14u	2,5-diClPh	F	0.002	0.013
14v	5-Cl,2-FPh	F	0.002	0.050
16a	2,5-diClPh	H	0.439	4.55
16b	2,5-diClPh	F	0.496	3.33
16c	2,3-diClPh	F	0.419	5.73
21a	2,3-diClPh		0.013	0.605
21b	2,5-diClPh		0.002	0.011
21c	5-Cl-2-FPh		0.004	0.088
21d	5-Cl-2-CNPh		0.003	0.150
21e	5-Me-2-CNPh		0.003	0.58
21f	2-F-5-MePh		0.002	0.029
21g	2-Cl-5-MeOPh		0.002	0.034
21h	2,5-diFPh		0.029	1.34