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. 2019 Feb 7;62(5):2521–2540. doi: 10.1021/acs.jmedchem.8b01854

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
a

Permeability measured in a Madin Darby canine kidney cell monolayer transfected with the multidrug resistance 1 (mdr1) gene encoding P-glycoprotein MDR1.

b

Protein binding measured at 1 μM.

c

NT = not tested.