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. 2016 Sep 21;7(12):1073–1076. doi: 10.1021/acsmedchemlett.6b00276

Table 1. Inhibition Data for Compounds 1120 (Ki in nM).

inhibitor rhodesain (RD) cruzain (CRZ) cathepsin B (CB) cathepsin L (CL)
11 0.49 0.44 8 11
12 6.5 16 68 30
13 29 130 310 110
14 4.2 11 34 19.6
15 50 NDa 6300 280
16 30 130 310 200
17 18.4 25 210 46
18 18 28 710 49
19 14 17 72 27
20 544 ND 3200 2020
K11777b 20 ND 390 80
a

ND = Not determined.

b

ksecond values [M–1 s–1] for inhibition by K11777: RD: 6.6 × 105; CL: 9.2 × 105; CB: 2.3 × 104.