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. Author manuscript; available in PMC: 2023 May 8.
Published in final edited form as: J Med Chem. 2013 Mar 15;56(6):2246–2255. doi: 10.1021/jm301280p

Table 5.

The potency of active-site-directed IDE inhibitors varies in a substrate-selective manner.

kiapp, nM
Cmpd. FRET1 FAßB Insulin
1a 2.96 ± 0.20 (n = 3) 21.7 ± 3.5 (n = 3) 37.9 ± 4.0 (n = 3)
8a 25.9 ± 1.2 (n = 3) 70.3 ± 12 (n = 3) 275 ± 25 (n = 3)
8b 103 ± 7.0 (n = 3) 927 ± 120 (n = 3) 1890 ± 410 (n = 3)
14a 86.9 ± 11 (n = 3) 107 ± 25 (n = 3) 1280 ± 300 (n = 3)
15 49.8 ± 3.7 (n = 3) 228 ± 67 (n = 3) 3260 ± 760 (n = 3)
16 85.1 ± 5.0 (n = 3) 365 ± 68 (n = 3) 833 ± 160 (n = 3)
17 43.7 ± 8.0 (n = 3) 1.40 ± 0.31 (n = 3) 410 ± 120 (n = 3)
18 23.1 ± 1.2 (n = 3) 246 ± 33 (n = 3) 171 ± 26 (n = 3)