Table 1 Summary of binary (PROTAC:p38δ or PROTAC:VHL) and ternary (p38δ:PROTAC:VHL) affinity and kinetic measurements

From: Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase

 

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

  1. The last protein listed in each list above represents that which was immobilized on the SPR instrument. See Methods section for further descriptions
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