. 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 4.

Characterization of selected 3,5-diaryl-oxadiazoles from the qHTS


Analogue #	R₁	R₂	IC_{50Ultr aGlo}	IC_{50P. Pyralis}	IC_50KinGlo	IC_{50KinGlo Plus}	IC_{50KinGlo Max}
a	pyridin-2yl	pyridin-4yl	1.9± 0.6	14.4± 6.9	8.9±1.9	14.1± 0.0	25.3±4.1
b	pyridin-2yl	furan-2yl	1.3± 0.3	17.1±7.1	13.9±0.6	>50	>50
c	pyridin-2yl	biphenyl-4yl	0.038± 0.006	0.08±0.07	11.3±1.7	>50	>50
d	pyridin-2yl	4-phenyl benzoate	0.040± 0.006	1.4±1.2	10.0±3.4	13.4±2.4	13.1± 2.5
e	pyridin-2yl	2-methoxy phenyl	0.08± 0.01	2.8±1.6	5±1	13.5±0.8	12.7±1.7
f	phenyl	2,4-dimethoxy phenyl	0.054± 0.004	0.2±0.1	13.9±1.1	>50	>50
g	3-methyl phenyl	4-flouro phenyl	0.58± 0.1	1.7±0.5	14±7.7	Inactive	Inactive
h	4-methoxy phenyl	2-flouro phenyl	0.3 ± 0.05	2.8±1.6	>50	>50	Inactive
i	2-methoxy phenyl	phenyl	0.6 ± 0.1	8.3±3.7	>50	Inactive	Inactive
j	2-methoxy phenyl	pyridin-4yl	4.8 ± 0.7	24± 9.8	>50	Inactive	Inactive
k	pyridin-4yl	furan-2yl	2.4± 0.3	24± 10.7	>50	Inactive	Inactive
l	4-dimethyaminophenyl	2-methoxy phenyl	0.32± 0.04	0.5± 0.3	Inactive	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_{50K inGlo} , IC_{50KinGlo Plus} , IC_{50KinGlo Max}). Data shown are mean± SD for at least three replications.