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. 2011 Oct 10;2(12):938–942. doi: 10.1021/ml200223s

Table 2. In Vitro Clearance in Human and Rat Liver Microsomes and Human CYP Inhibition Data for Selected Compounds.

compd Clint (HLM/RLM)a (μL/min/mg prot) CYP inhibition (2C8/2C9/2C19) IC50 (μM)
16 >1000/43 0.32/0.84/0.26
29 1700/30 0.47/0.34/0.90
39 >1000/125 0.57/0.64/0.68
48 <10/<10 0.086/0.28/0.038
51 <10/12 0.043/0.20/0.051
55 55/10 0.97/2.0/3.7
58 <10/<10 0.054/>20/0.15
60 17/17 0.079/1.7/7.5
61 92/40 0.22/7.4/12
63 28/20 0.050/0.29/0.17
a

HLM, human liver microsomes; RLM, rat liver microsomes.