IC50, Ki and α values derived from the displacement curves measured by competitive 19F NMR for compound 15b and VHL homo-PROTACs. The respective α values previously reported by ITC were added for comparison.
| PROTAC | Target | 19F NMR | ITC | ||
|---|---|---|---|---|---|
| IC50 (nM) | K i (nM) | α | α | ||
| 15b | — | 3022 | 2058 | — | — |
| Brd4(2) | 346 | 71 | 29 | 15 | |
| CMP99 | — | 888 | 287 | — | — |
| CM11 | — | 277 | 39 | 7 | 13 |