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. Author manuscript; available in PMC: 2020 Apr 11.
Published in final edited form as: J Med Chem. 2019 Mar 22;62(7):3503–3512. doi: 10.1021/acs.jmedchem.8b01972

Table 1.

In vitro Profiling Data

Entry Cmpd Pf 3D7 IC50, nM BACE1 IC50, nM Pf PM-II IC50, nM Pf PM-IV IC50, nM hERG IC50, nM hERG/3D7 Ratio MLM t1/2, min MLM Clint, μL/min/mg
1 12 460 >10,000 >10,000 >10,000 8,950 19 161 1.4
2 14 200 >10,000 >10,000 >10,000 9,410 47 35 6.2
3 16 600 >10,000 >10,000 >10,000 4,740 8 n.d. n.d.
4 24 140 >10,000 >10,000 >10,000 8,540 61 34 6.4
5 26 83 >10,000 >10,000 >10,000 7,560 91 33 6.7
6 30 170 >10,000 >10,000 >10,000 2,110 12 31 7.2
7 34 230 >10,000 >10,000 >10,000 21,700 94 70 3.1
8 35 450 n.d. n.d. n.d. >50,000 >111 n.d. n.d.
9 54a 140 n.d. n.d. n.d. >50,000 >357 n.d. n.d.
10 54b 51 n.d. n.d. n.d. 32,000 627 38 n.d.

n.d. = not determined.