Table 4. Quantification of the Degradation Profile of Heterotetravalent PROTAC AB3124 (86) and Heterotrivalent PROTACs AB3063 (26) and AB3067 (27) Against BET Proteins and CRBN in HEK293 Cells.
| Western
Blot DC50 (nM)a |
HiBiT Dmax 50 (nM)b |
||||||
|---|---|---|---|---|---|---|---|
| Compound | BRD4Long | BRD4Short | BRD3 | BRD2 | CRBN | BRD4 | 95% CI |
| AB3124 (86) | 2.2 ± 0.1 | 2.9 ± 0.3 | 3.5 ± 0.3 | 1.0 ± 0.2 | 113 ± 3.2 | 1.1 | 0.91 to 1.4 |
| AB3063 (26) | 0.76 ± 0.1 | 3.2 ± 0.9 | 4.8 ± 2.4 | 14 ± 4.6 | 200 ± 31 | 3.0 | 2.6 to 3.3 |
| AB3067 (27) | 2.3 ± 0.4 | 2.1 ± 0.3 | 1.6 ± 0.3 | 15 ± 2.1 | 75 ± 14 | 0.64 | 0.50 to 0.80 |
a
Calculated as mean (±S.E) from three independent biological experiments.
b
Calculated as mean from two independent biological experiments.