Table 3.
inhibitor | enzyme | IC50 b (μM) | ΔY b,c (%) | SId |
---|---|---|---|---|
2 | plasmin | 7.2 ± 0.6 | 98 ± 5 | |
thrombin | 156 ± 14 | 77 ± 8 | 22 | |
FXa | ~505 | ND | 70 | |
FXIa | 180 ± 20 | 93 ± 11 | 26 | |
FIXa | >2000 | ND | >277 | |
FXIIa | >1000 | ND | >138 | |
trypsin | >440 | ND | >61 | |
chymotrypsin | 196 ± 39 | 92 ± 9 | 27 | |
1j | plasmin | 116 ± 9 | 111 ± 8 | |
thrombin | 267 ± 28 | 91 ± 11 | 2 | |
FXa | 212 ± 30 | 104 ± 17 | 2 | |
FXIa | 208 ± 32 | 109 ± 16 | 2 |
Direct inhibition of human enzymes was measured in appropriate Tris-HCl buffers of pH 7.4 at 37 °C. Inhibition was monitored spectrophotometrically. See Experimental Part for details.
Selectivity index.
Errors represent ±1 SE.
Not determined.