Table 1.
Summary of binary (PROTAC:p38δ or PROTAC:VHL) and ternary (p38δ:PROTAC:VHL) affinity and kinetic measurements
| SJFδ | SJFα | |
|---|---|---|
| PROTAC:p38δ Kd | 550 nM | 500 nM |
| PROTAC:VHL Kd | 3500 nM | 5000 nM |
| p38δ:PROTAC:VHL Kd | 436 nM | 1200 nM |
| p38δ:PROTAC:VHL koff | 0.018 s−1 | 0.072 s−1 |
| p38δ:PROTAC:VHL kon | 3.96 × 104 M−1 s−1 | 7.01 × 104 M−1 s−1 |
| p38δ:PROTAC:VHL t1/2 | 38 s | 8 s |
The last protein listed in each list above represents that which was immobilized on the SPR instrument. See Methods section for further descriptions