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. 2015 Jan 15;6(3):282–286. doi: 10.1021/ml500463t

Table 3. In Vitro PDE2 and PDE10 Inhibition and Metabolic Stability Data for Compounds 6 and 9–18.

graphic file with name ml-2014-00463t_0005.jpg

  R hPDE2 IC50 (nM)a rPDE10 IC50 (nM)a rLMb hLMb
6 H 29 480 13 7
9 On-Bu 6 5500 98 34
10 O(CH2)2OMe 95 9120 18 5
11 CH2On-Pr 21 3890 98 78
12 CH2OCH2CF3 3 2450 77 12
13 CH2Oi-Pr 10 6030 98 57
14 morpholine 310 >10000 53 14
15 OCF3 150 8910 11 3
16 5-Cl 5750 n.m. n.m. n.m.
17 4-Me 2450 n.m. n.m. n.m.
18 5-On-Bu 54 3800 46 6
a

Average value of at least two independent experiments.

b

Percent metabolized after incubating 1 μM solution 15 min with rLM or hLM at 37 °C.