Table 1. Inhibition Data for Compounds 11–20 (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 |
ND = Not determined.
ksecond values [M–1 s–1] for inhibition by K11777: RD: 6.6 × 105; CL: 9.2 × 105; CB: 2.3 × 104.