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. Author manuscript; available in PMC: 2021 Jul 27.
Published in final edited form as: J Med Chem. 2018 Sep 28;61(19):8875–8894. doi: 10.1021/acs.jmedchem.8b01108

Table 3.

5,6-Substituents

graphic file with name nihms-1712951-t0012.jpg
Compd R5 R6 EC50 (μM) Act. (%)a
10 Me Me 2.2 ± 0.52 211 ± 20.5
22 Me Cl 3.0 ± 0.56 200 ± 13.3
23 H H 5.4 ± 1.22 109 ± 4.2
24 H Me 2.4 ± 0.33 106 ± 13.1
25 H CF3 4.4 ± 0.54 78 ± 2.2
26 H graphic file with name nihms-1712951-t0013.jpg 24.3 ± 5.33 65 ± 2.2
27 H Br 1.3 ± 0.3 115 ± 5.4
28 H Cl 1.0 ± 0.16 109 ± 1.0

Measurements are reported as the mean ± SD of two or more independent experiments, each conducted in duplicate.

a

Activation values represent percentage relative to control.25