Table 2. Biological Activity of A-1293102 and Compound 5a.
|
Ki (nM) |
10%
HS EC50 (μM) |
||||
|---|---|---|---|---|---|
| compound | BCL-XL | BCL-2 | MCL-1 | MOLT-4 | RS4;11 |
| 4 (A-1293102) | 0.43 | 193 | >3900 | 0.08 | >5 |
| 5 | 0.14 | 31 | >1560 | >5 | >5 |
| A-11554637,25 | <0.1 | 80 | >444 | 0.07 | >5 |
| A-13318527,26 | <0.1 | 6.1 | 142 | 0.006 | >5 |
| navitoclax7 | <0.1 | <0.1 | >224 | 0.30 | 0.11 |
All assays were run at least in quadruplicate.