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. 2020 Feb 12;11(4):485–490. doi: 10.1021/acsmedchemlett.9b00611

Table 1. In Vitro and in Vivo Data for 3 and Analogs 5–11.

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a

Biochemical assay.

b

Inhibition of ASK1 autophosphorylation. IC50 results are the geometric mean of a minimum of two determinations.

c

MDCK-MDR1 human P-gp transfected cell line. Papp = apparent permeability, apical-to-basolateral (10–6 cm/s); ER = (B–A)/(A–B) efflux ratio.

d

Clu = Cl/fu.

e

DMSO/PG (1:1) used as vehicle. Vdss = 1.8 L/kg; t1/2 = 0.9 h.

f

DMSO/PG (1:1) used as vehicle. Vdss = 2.7 L/kg; t1/2 = 0.7 h.

g

DMA/EtOH/PG/water (1:1:3:5) used as vehicle. Vdss = 3.5 L/kg; t1/2 = 2.0 h.