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. Author manuscript; available in PMC: 2017 Aug 15.
Published in final edited form as: Bioorg Med Chem. 2016 Jun 11;24(16):3758–3770. doi: 10.1016/j.bmc.2016.06.018

Table 3.

Structural modification at Site C

graphic file with name nihms800702t11.jpg
Compd. R EC50 *
(µM)
±SEM
Ki *
(µM)±
SEM
16 graphic file with name nihms800702t12.jpg >30
17 graphic file with name nihms800702t13.jpg >30
18 graphic file with name nihms800702t14.jpg >30
19 graphic file with name nihms800702t15.jpg >30
20 graphic file with name nihms800702t16.jpg 9.4 ± 3.4 0.6 ± 0.10
21 graphic file with name nihms800702t17.jpg 9.9 ± 2.6 1.4 ± 0.2
22 graphic file with name nihms800702t18.jpg 0.8 ± 0.1 1.3 ± 0.3
23 graphic file with name nihms800702t19.jpg >30
24 graphic file with name nihms800702t20.jpg >30
25 graphic file with name nihms800702t21.jpg >30
26 graphic file with name nihms800702t22.jpg >30
27 graphic file with name nihms800702t23.jpg >30
28 graphic file with name nihms800702t24.jpg >30
29 graphic file with name nihms800702t25.jpg >30
30 graphic file with name nihms800702t26.jpg >30
31 graphic file with name nihms800702t27.jpg 3 ± 0.2 3 ± 0.6
*

EC50 and Ki values are averages of multiple experiments (where n = 3, unless otherwise stated) ± standard error of the mean.