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