Table 5. In Vitro ADME Properties of Boronpleuromutilins.
ID | mouse S9 Clint (μL/min/mg) | mouse protein binding (funbound @ 2 μM) | MDR1-MDCK Pappa |
---|---|---|---|
2 | 4 | 0.218 | 0.2 |
3 | 41 | 0.154 | 6.7 |
4 | 131 | 0.26b | 22.1 |
5 | NT | 0.05b | 1.4 |
8 | 145 | 0.003 | 15.1 |
9 | 168 | 0.002 | NTc |
10 | 139 | 0.005 | NT |
11 | 77 | <0.001 | NT |
12 | 136 | 0.012 | NT |
14 | 117 | 0.003 | NT |
15 | 33 | 0.034 | 14.1 |
16 | 44 | 0.008 | NT |
19 | NT | 0.116 | 0.3 |
20 | 7 | 0.110 | 0.1 |
21 | NT | 0.119 | 0.5 |
23 | NT | 0.048 | 0.1 |
25 | 102 | 0.008 | 36.5 |
26 | 2 | 0.306 | 0.1 |
32 | NT | 0.005 | 22.6 |
33 | 142 | 0.008 | 9.0 |
40 | 226 | 0.058 | 6.6 |
41 | NT | 0.007 | NT |
42 | NT | 0.005 | NT |
44 | 80 | 0.008 | 2.3 |
45 | NT | 0.037 | NT |
46 | NT | <0.001 | 8.8 |
52 | 217 | 0.006 | NT |
53 | NT | <0.001 | NT |
55 | NT | NT | 8.7 |
59 | 53 | 0.033 | 3.7 |
Permeability measured in a Madin Darby canine kidney cell monolayer transfected with the multidrug resistance 1 (mdr1) gene encoding P-glycoprotein MDR1.
Protein binding measured at 1 μM.
NT = not tested.