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. 2021 Jun 22;29(8):823–833.e5. doi: 10.1016/j.str.2021.06.002

Table 1.

In vitro activities of perampanel analogs

Compound IC50 (μM)
Perampanel 100–250
2 9.99 ± 2.50
3 6.38 ± 1.21
4 4.02 ± 1.36
5 0.14 ± 0.02
6 0.47 ± 0.02
11 0.120 ± 0.016
14 0.128 ± 0.015
15 0.110 ± 0.013
16 0.100 ± 0.035
19 0.037 ± 0.007
21 0.018 ± 0.002
23 0.020 ± 0.005
25 0.025 ± 0.003
26 0.170 ± 0.022
29 0.25–0.50
31 0.037 ± 0.004
50 0.25–0.50

Activities of perampanel and analogs 2–50 with previously reported IC50s of perampanel and compounds 2–26 (Zhang et al., 2021) with standard deviation calculated from triplicate measurements. While IC50 values could not be calculated for compounds 29 and 50 due to incomplete inhibition at maximum concentrations tested, in vitro activity data demonstrate that both compounds reduce Mpro activity to 50% between 0.25 μM and 0. 5 μM (Figure S2).