Table 25.
enzyme assays k3/Ki, M−1s−1 | cellular assays IC50, μM | Ref | |||||||
---|---|---|---|---|---|---|---|---|---|
mCasp-1 | Casp-3 | Casp-6 | Casp-8 | Con A | Monocyte | Jurkat | |||
-F | 246 | 129000 | 207000 | 36842 | 71667 | 3.05 | 0.95 | 0.24 | 274 |
-OPh | 247 | 3630 | 19152 | 2399 | 4258 | 38.00 | 11.17 | 13.95 | |
-OCO(2,6-Cl2-Ph) | 248 | 52109 | 725222 | 56883 | 17010 | 2.15 | 11.50 | 10.61 | |
-O(1-Naphthylyl) | 249 | 354241 | 1958905 | 0 | 0 | 2.65 | 19 | > 100 | |
-O(2-Naphthylyl) | 250 | 263 | 7521 | 0 | 0 | > 50 | 15.90 | > 100 | |
-O(2,6-F2-Ph) | 251 | 53875 | 200052 | 9979 | 9075 | 2.40 | > 100 | 2.04 | |
-O(2,3,6-F3-Ph) | 252 | 47081 | 187700 | 81749 | 16972 | 2.433 | - | 1.195 | |
-O(2,3,5,6-F4-Ph) | 253 | 77528 | 267953 | 78887 | 30173 | 2.17 | 6.25 | 4.50 | |
-O(2,6-Cl2-Ph) | 254 | 25259 | 178629 | 87715 | 2713 | 2.75 | 15.32 | 3.00 | |
255 | 7572 | 71138 | 23909 | 2266 | n.d. | n.d. | 28 | 297 | |
256 | 9396 | 35478 | 509 | 295 | n.d. | n.d. | 46 | ||
257 | 42463 | 143850 | 5804 | 6344 | n.d. | n.d. | 71 | ||
258 | 1191 | 38119 | 975 | 3059 | n.d. | n.d. | 102 | ||
259 | 24834 | 113766 | 5147 | 3199 | n.d. | n.d. | 37 | ||
260 | 45379 | 168736 | 44007 | 18230 | n.d. | n.d. | 137 |