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. Author manuscript; available in PMC: 2023 Nov 15.
Published in final edited form as: Bioorg Med Chem Lett. 2022 Sep 29;76:129013. doi: 10.1016/j.bmcl.2022.129013

Table 4.

Methylated linker 2 analogs

graphic file with name nihms-1903262-t0011.jpg
No. * R Modea IC50 / EC50 (µM)b Efficacy (%)b,c
60 S Cl Inh 4.4 93
61 S CF3 Inh 3.4 95
62 R Cl Inh 4.9 98
63 R CF3 Inh 3.5 100
a

Inh = inhibitor; Act = activator; NA = not active

b

CRC from Tl+ flux assay in HEK-293 cells expressing WT Slack

c

Amplitude of response in the presence of 30 µM test compound as a percentage of the maximum response for VU0606170