TABLE 3.
Second-order binding constants for binding of peptidyl vinyl sulfonyl compounds to falcipain-2 and falcipain-3
| Compound | R1′ |
kass (M−1 s−1)
|
|
|---|---|---|---|
| Falcipain-2 | Falcipain-3 | ||
| 325 | Sulfone | 21,600 | 39,600 |
| 326 | Sulfone | 29,700 | 31,300 |
| 327 | Sulfone | 78,600 | 57,100 |
| 328 | Sulfone | 111,000 | 127,000 |
| 344 | Sulfone | 54,600 | 61,700 |
| 345 | Sulfone | 102,000 | 55,700 |
| 290 | Sulfonamide | 74,700 | 147,000 |
| 291 | Sulfonamide | 411,000 | 407,000 |
| 340 | Sulfonamide | 120,000 | 179,000 |
| 341 | Sulfonamide | 245,000 | 711,000 |
| 348 | Sulfonate ester | >106 | >106 |
| 349 | Sulfonate ester | 288,000 | 160,000 |
| 351 | Sulfonate ester | >106 | >106 |
| 354 | Sulfonate ester | >106 | >106 |
| 364 | Sulfonate ester | >106 | >106 |