. Author manuscript; available in PMC: 2012 Aug 29.

Published in final edited form as: J Med Chem. 2009 Mar 12;52(5):1450–1458. doi: 10.1021/jm8014525

Table 3.

Characterization of selected 2-phenylbenzothiazole analogs


Analogue #	R₁	R₂	R₃	R₄	IC_{50Ultr aGlo}	IC_50lucPpy	IC_50KinGlo	IC_{50KinGlo Plus}	IC_{50KinGlo Max}
a	H	H	H	dimethylamine	0.32± 0.0	0.2±0.0	10.7±3.4	Inactive	Inactive
b	H	H	H	Cl	1.4± 0.18	4.5±0.0	>50	Inactive	Inactive
c	OMe	H	H	F	0.86± 0.08	1.3±0.09	>50	Inactive	Inactive
d	OMe	H	F	H	1.1± 0.14	1.5±0.1	>50	Inactive	Inactive
e	OMe	F	H	H	0.5± 0.05	0.6±0.0	>50	Inactive	Inactive
f	OMe	Cl	H	F	4.9± 1.1	5.4±0.7	>50	Inactive	Inactive
g	OMe	H	H	Cl	3.8± 0.5	3.5±0.0	>50	Inactive	Inactive
h	OMe	O-methylbenzene	H	H	4.3± 0.2	8.9±0.6	>50	Inactive	Inactive
i	OMe	H	O-methylbenzene	H	30± 3	13.4±1	Inactive	Inactive	Inactive
j	OMe	H	H	CN	6.1± 1.3	5.7±0.9	Inactive	Inactive	Inactive
k	OMe	H	H	OMe	4.1± 0.4	2.2±0.0	>50	Inactive	Inactive
l	OMe	OMe	H	H	5.6± 1.3	3.2±0.0	>50	Inactive	Inactive
m	OMe	H	OMe	OMe	3.8± 0.6	2.8±0.0	>50	Inactive	Inactive
n	OMe	H	acetamide	H	1.9± 0.4	2.9±0.2	>50	Inactive	Inactive
o	OMe	H	Me	H	0.67± 0.07	1.5±0.1	>50	Inactive	Inactive
p	OMe	H	H	dimethylamine	2.7± 0.6	0.7±0.04	>50	Inactive	Inactive
q	H	H	F	H	7.8± 0.3	24.2±1.6	Inactive	Inactive	Inactive
r	H	H	OMe	OMe	1.9± 0.3	3.2±0.0	>50	Inactive	Inactive
s	H	H	H	OMe	0.36± 0.02	1.0±0.0	>50	Inactive	Inactive
t	H	OMe	H	H	7.7± 1.4	11.3±1.8	>50	Inactive	Inactive
u	H	H	H	CN	2.1± 0.2	6.3±0.0	>50	Inactive	Inactive
v	H	H	H	acetamide	3.1± 0.5	3.0±0.2	>50	Inactive	Inactive

Activity of compounds was determined by measurement of luminescence using either purified luciferase enzyme assays (IC_50UltraGlo or IC_50lucPpy) or formulations of UltraGlo (IC_50KinGlo , IC_{50K inGlo Plus} , IC_{50KinGlo Max}). Data shown are mean± SD for at least three replications.