Table 1.
Plasmin inhibition by sulfated small molecules. a
| Plasmin Inhibitor | IC50 (μM) | HS | ΔY% |
|---|---|---|---|
| 28 | 149 ± 5.6 b | 3.3 ± 0.7 | 82 ± 4 |
| 29 | 157 ± 5.0 | 3.6 ± 0.7 | 88 ± 4 |
| 30 | 220 ± 11 | 3.0 ± 1.3 | 74 ± 7 |
| 31 | 56 ± 2 | 3.2 ± 0.8 | 87 ± 4 |
| 32 | 45 ± 2 | 2.3 ± 0.7 | 105 ± 6 |
| 33 | 128 ± 8 | 1.8 ± 0.4 | 89 ± 7 |
| 34 | 130 ± 6 | 3.9 ± 1.0 | 83 ± 5 |
| 35 | 642 ± 78 | 1.4 ± 0.4 | 88 ± 11 |
| 36 | >1000 | ND c | ND |
| 37 | 84 ± 4 | 2.1 ± 0.4 | 76 ± 3 |
| 38 | >400 | ND | ND |
| 39 | >400 | ND | ND |
| 40 | 239 ± 73 | 1.1 ± 0.6 | 87 ±29 |
| 41 | 125 ± 9 | 4.0 ± 1.8 | 54 ± 5 |
| 42 | 161 ± 24 | 1.0 ± 0.2 | 92 ± 4 |
| 43 | 183 ± 43 | 1.0 ± 0.3 | 94 ± 21 |
| 44 | 137 ± 11 | 1.0 ± 0.2 | 102 ± 9 |
| 45 | 98 ± 9 | 1.7 ± 0.6 | 94 ± 6 |
| 46 | 111 ± 7 | 2.4 ± 0.4 | 95 ± 2 |
| 47 | 89 ± 7 | 1.9 ± 0.6 | 98 ± 7 |
| 48 | 621 ± 185 | 1.3 ± 0.4 | 89 ± 36 |
| 49 | 277 ± 61 | 1.8 ± 1.0 | 75 ± 22 |
| 50 | 185 ± 68 | 1.4 ± 0.2 | 38 ± 15 |
| 51 | ~2830 | ND | ND |
| 52 | 76 ± 12 | 1.0 ± 0.2 | 72 ± 9 |
| 53 | 209 ± 25 | 0.6 ± 0.1 | 105 ± 8 |
| 54 | 75 ± 25 | 0.7 ± 0.3 | 71 ± 18 |
| 55 | >400 | ND | ND |
Notes: a IC50, HS, and ΔY values were obtained following non-linear regression analysis of direct inhibition of human plasmin in pH 7.4 buffer at 37 °C. Inhibition was monitored by spectrophotometric measurement of the residual enzyme activity. See details under Experimental Section. b Errors represent standard error calculated using global fit of the data. c ND means not determined.