Skip to main content
. 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 3.

Ring D library compounds

graphic file with name nihms-1936972-t0012.jpg
No. R Modea IC50 / EC50 (μM)b Efficacy (%)b,c
40 H Inh >10 51
41 2-F Inh 7.9 88
42 3-F Inactive
43 4-F Inh 3.2 105
44 2-Cl Inh 8.0 81
45 3-Cl Inactive
46 4-Cl Inh 11 94
47 2-CF3 Act 1.9 66
48 3-CF3 Inh 11 48
49 4-CF3 Inh 3.8 95
50 2-Me Act >10 <10
51 3- Me Inh >10 <10
52 4- Me Inactive
53 2-OMe Act >10 18
54 3-OMe Act >10 <10
55 4-OMe Act 7.1 21
56 2,4-difluoro Inh 6.5 93
57 4-Cl,2-F Inh 7.2 99
58 2-Cl,4-F Inh 2.1 95
59 thiophen-2-yl Inh 6.9 99
60 5-fluorothiophen-2-yl Inh 4.8 105
61 2-thiazolyl Inactive
62 4-isothiazolyl Inh 6.6 106
63 2-furanyl Inh >10 44
64 2-pyridyl Inactive
65 3-pyridyl Inactive
66 4-pyridyl Inactive
67 4-fluoro-2-pyridyl Inactive
68 2-pyrimidinyl 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)