Table 3. In Vitro ADME Assessment of Compounds 7h and 7c.
| Cmpd | hERa | rERb | MDCKcPapp (1 × 10–6 cm/s) | MDCK ratio (BA/AB) | hPPBd (%free) | rPPBe (%free) | rBBf (%free) |
|---|---|---|---|---|---|---|---|
| 7h | 0.3 | 0.8 | 16 | 5.5 | 14 | 36 | 16 |
| 7c | 0.3 | 0.4 | 32 | 1.7 | 10 | 25 | 9 |
a
Human extraction ratio.
b
Rat extraction ratio. Extraction ratios are calculated as in vitro CL/Q where Q is species specific hepatic blood flow.
c
MDR1-MDCK from Madin Darby canine kidney cells.
d
Human plasma protein binding.
e
Rat plasma protein binding.
f
Rat brain tissue binding.