Table 1.
Target protein | PROTAC (TL12–186) | Dmax50 (nM)a | # Surface lysine | # Ternary complex models | % Productive | Ubiquitination EC50 (nM) |
---|---|---|---|---|---|---|
CDK5 | 62 | 22 | 4157 | 57 | Not tested | |
CDK7 | 233 | 14 | 14,452 | 24 | 428 | |
CDK8 | >500 | 33 | 29,920 | 14 | 888 | |
CDK9 | 58 | 26 | 9802 | 33 | 297 | |
CDK12 | 7 | 31 | 4359 | 77 | 16 | |
CDK13 | 7 | 29 | 12,018 | 62 | 7 |
Dmax50 values are from Riching et al. (48).