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. Author manuscript; available in PMC: 2015 Aug 14.
Published in final edited form as: J Med Chem. 2014 Jul 29;57(15):6531–6552. doi: 10.1021/jm500561a

Table 7.

Caco-2 Cell Permeability and CYP450 Isoform Inhibition of Compound 22

compd Papp (nm/s)a
CYP450 isoform (% inhibition at 1 μM)
PA→B PB→A CYP1A2 CYP2C19 CYP2C9 CYP2D6 CYP3A4
22 123.2 107.3 66.8 72.6 28.9 <5.0 12.2
a

Papp (nm/s): >50, high; 10–50, medium; <10, low; caffeine PA–B reference control, 206 ± 35 nm/s; cimetidine PA–B and PB–A reference control, 1.1 ± 0.1 and 21.3 ± 3.4 nm/s, respectively.