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. Author manuscript; available in PMC: 2024 Nov 15.
Published in final edited form as: Bioorg Med Chem. 2023 Sep 30;95:117487. doi: 10.1016/j.bmc.2023.117487

Table 4.

Ring B library compoundsd

graphic file with name nihms-1936972-t0013.jpg
No. B Modea IC50 / EC50 (μM)b Efficacy (%)b,c
69 graphic file with name nihms-1936972-t0014.jpg Act 4.0 14
70 graphic file with name nihms-1936972-t0015.jpg Inh 9.2 98
71 graphic file with name nihms-1936972-t0016.jpg Inh >10 24
73a graphic file with name nihms-1936972-t0017.jpg Inactive
73b graphic file with name nihms-1936972-t0018.jpg Inh >10 52
74 graphic file with name nihms-1936972-t0019.jpg Inh >10 31
75 graphic file with name nihms-1936972-t0020.jpg Inh >10 63
76 graphic file with name nihms-1936972-t0021.jpg Inh 4.9 105
77 graphic file with name nihms-1936972-t0022.jpg Inactive
a

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

b

Concentration-response curve (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 (inhibitors) or loxapine (activators)

d

Synthesis described in Supplementary Material