Table 1 Summary of compounds tested.
Cpd | Substrate ligand (“warhead”) | E3 ligand target | Linker length (Mr)* |
|---|---|---|---|
A | MLN8237 (alisertib) | VHL | 288 |
B | MLN8237 | CRBN | 272 |
C | MLN8237 | VHL | 200 |
D | MLN8237 | CRBN | 316 |
DX | MLN8237 | CRBN | 404 |
E | MLN8237 | VHL | 244 |
F | MLN8237 | CRBN | 228 |
G | MLN8237 | VHL | 156 |
H | MLN8237 | CRBN | 184 |