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. 2016 Oct 28;7(12):1161–1166. doi: 10.1021/acsmedchemlett.6b00356

Table 7. Biochemical and in Vitro ADME Results for (+)-32 and (−)-32.

  kinase selectivity (ratio)
in vitro metabolismd (%R)
   
No. PI3Kαa PI3Kβa PI3Kγa BMXb TECc hLM mLM rLM dLM hUGT mUGT Caco-2e PPBf (%)
(+)-32 6 34 2 4 20 71 28 45 65 91 93 1.3 98
(−)-32 17 44 7 1 7 63 11 46 32 91 99 1.7 98
a

Ratio of PI3K IC50/PI3Kδ IC50.

b

Ratio of BMX IC50/BTK IC50.

c

Ratio of TEC IC50/BTK IC50.

d

Percent parent remaining (%R) after 30 min.

e

Efflux ratio, PappB → A/PappA → B.

f

Percent mouse plasma protein binding (PPB).