Table 6. Pharmacokinetic Properties of Compounds CCT369260 (2) and CCT373566 (12a).
| BCL6 TR-FRET IC50 (nM)a | MSD degrader assay [OCI-Ly1] DC50 (nM) [Dmax]a | calculated free DC50 [OCI-Ly1](nM) | Cmax (nM/L) | CL (mL/min/kg) | CLu (mL/min/kg) | t1/2 (h) | Vss (L) | F (%) | mouse (BALB\c) PPB | |
|---|---|---|---|---|---|---|---|---|---|---|
| 2 CCT369260 | 523 | 54 [100%] | 1.2 | 1577 | 19.8 (22% Qh) | 46731 | 1.4 | 2.1 | 54 | 99.96 |
| 12a CCT373566 | 2.2 | 0.7 [96%] | 0.09 | 3947 | 5.7 (6% Qh) | 4670 | 1.15 | 0.47 | 44 | 99.88 |
a
Data represent the geometric mean of at least three replicates. See Tables S1 and S2 for full statistics.