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. Author manuscript; available in PMC: 2012 Mar 15.
Published in final edited form as: Bioorg Med Chem Lett. 2011 Jan 22;21(6):1719–1723. doi: 10.1016/j.bmcl.2011.01.079

Table 1.

Biochemical and Cell-based IC50 Values, and Mouse Plasma and Brain levels for a series of 2,7-substituted quinazolinesa

graphic file with name nihms274084t1.jpg
compound R' R JNK3
IC50
(µM)		 JNK1
IC50
(µM)		 c-jun
IC50
(µM)		 bmouse
[plasma]		 (µM)
[brain]
3 graphic file with name nihms274084t2.jpg graphic file with name nihms274084t3.jpg 0.09 0.05 0.31 17.8 7.17
8a graphic file with name nihms274084t4.jpg graphic file with name nihms274084t5.jpg 0.05 0.04 0.12 42.9 1.31
8b graphic file with name nihms274084t6.jpg graphic file with name nihms274084t7.jpg 0.7 nt nt nt nt
8c graphic file with name nihms274084t8.jpg graphic file with name nihms274084t9.jpg 4.4 nt nt nt nt
8d graphic file with name nihms274084t10.jpg graphic file with name nihms274084t11.jpg 0.21 nt nt 26.7 8.1
8e graphic file with name nihms274084t12.jpg graphic file with name nihms274084t13.jpg 0.73 nt nt nt nt
8f graphic file with name nihms274084t14.jpg graphic file with name nihms274084t15.jpg >20 nt nt nt nt
8g graphic file with name nihms274084t16.jpg graphic file with name nihms274084t17.jpg 0.05 nt 0.04 nt nt
8h graphic file with name nihms274084t18.jpg graphic file with name nihms274084t19.jpg 0.06 0.1 0.29 13.1 1.37
a

JNK3 biochemical IC50 values are the averages of four or more experiments, and the JNK1 and cell-based IC50 values are the averages of two or more experiments. All standard deviations are ≤44% for the biochemical and ≤81% for the cell-based assays.

b

10 mg/kg ip 2h.

nt = not tested.