Table 5. In vitro ADME properties for 66 (Cyprotex Discovery, Macclesfield, UK).
Microsomal stability | |||||||
Microsomal stability (human) |
Microsomal stability (mouse) |
||||||
CLint (μL min–1 mg–1) | S.E. CLint | T 1/2 (min) | n | CLint (μL min–1 mg–1) | S.E. CLint | T 1/2 (min) | n |
6.21 | 0.681 | 223 | 5 | 10.2 | 1.82 | 136 | 5 |
Solubility | |||||||
Estimated precipitation range (μM) | |||||||
Lower bound |
Upper bound |
Calculated mid-range |
|||||
100 | >100 | >100 |
Caco-2 permeability | |||||||
Direction | Papp (× 10–6 cm–1) |
Mean Papp (× 10–6 cm–1) | SD | n | Mean recovery (%) |
||
1 | 2 | ||||||
A → B | 0.0534 | 0.0421 | 0.0477 | 0.00799 | 2 | 57.6 | |
B → A | 4.88 | 5.29 | 5.08 | 0.293 | 2 | 64.0 |