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. Author manuscript; available in PMC: 2016 Sep 24.
Published in final edited form as: J Med Chem. 2015 Sep 10;58(18):7485–7500. doi: 10.1021/acs.jmedchem.5b01005

Table 10.

P450 Inhibition and Permeability Profile of Compound 106

graphic file with name nihms-766653-f0019.jpg
P450 inhibitiona
 permeabilityb
CYP1A2 IC50 >30 μM A–B Papp 45.0 × 10–6 cm/s
CYP2C9 IC50 25.6 μM B–A Papp 49.9 × 10–6 cm/s
CYP2D6 IC50 >30 μM efflux ratio 1.1
CYP3A4 IC50 >30 μM
a

Cocktail assay in HLM.

b

MDR1-MDCK cells.