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. Author manuscript; available in PMC: 2015 Aug 1.

Published in final edited form as: Bioorg Med Chem Lett. 2014 Jun 11;24(15):3307–3314. doi: 10.1016/j.bmcl.2014.06.003

Table 5. In vitro DMPK Profile for 68 (VU0431316).

Protein Binding (F_u)^a,b				MDCK-WT Permeability
rat PPB		0.179		P_app (A-B)	50.4 × 10⁻⁶ cm/sec
cynomolgus PPB		0.167		P_app (B-A)	45.0 × 10⁻⁶ cm/sec
human PPB		0.120		efflux ratio	0.89

mouse BHB		0.054

				Caco-2 Permeability
CYP Inhibition IC₅₀ (μM)^c				P_app (A-B)	66.8 × 10⁻⁶ cm/sec
3A4	2D6	2C9	1A2	P_app (B-A)	71.4 × 10⁻⁶ cm/sec
>30	>30	>30	0.6	efflux ratio	1.07

^a

Fu = fraction unbound

^b

PPB = plasma protein binding; BHB = brain homogenate binding

^c

Assayed in pooled HLM in the presence of NADPH