Table 5. Biochemical and ADME Profiling of Compounds 23, 33, 34, 46, and 47a.
Cmpd | USP7 IC50 (μM) | HLM/MLM CLhep | logD7.4/Ksol | Caco-2 Papp A/B |
---|---|---|---|---|
23 | 0.030 | 19/84 | 2.3/175 | 1.93 |
33 | 0.040 | 19/86 | 1.7/200 | 0.15 |
34 | 0.006 | 18/62 | –0.1/191 | 0.28 |
46 | 0.087 | 11/34 | 0/200 | 0.26 |
47 | 0.022 | 7/28 | 0.1/179 | 0.14 |
See Supporting Information for assay conditions. HLM/MLM units: mL/min/kg. Ksol units: μM. Caco-2 units: 10–6 cm/s