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. Author manuscript; available in PMC: 2011 Aug 5.
Published in final edited form as: Bioorg Med Chem Lett. 2009 Mar 24;19(10):2865–2869. doi: 10.1016/j.bmcl.2009.03.080

Table 3.

Human and rat FAAH potency (kinact/Ki values)15 for compounds 13, 19–39 showing SAR of substituted benzothiophenes

graphic file with name nihms298813t6.jpg
R1 R2 R3 R4 R5 X hkinact/Ki (M−1 s−1) rkinact/Ki (M−1 s−1)
19 H H H H H N 695 174
6a Me H H H H N 2401 1083
20 Me H H H H C 5129 2613
21 Et H H H H N 1402 774
22 Et H H H H C 1668 1013
6b Me H H H Me N 1481 390
23 Cl H H H Me N 900 133
24 Me F H H H N 3321 1203
25 Me F H H H C 4147 1547
26 Me F H H Me N 1980 758
27 Me H F H H N 3134 779
13 Me H F H H C 4474 729
28 Me H Me H H N 2635 557
29 Me H Me H H C 3024 482
30 Me H Cl H H N 2822 1133
31 Me H CF3 H H N 1389 219
32 Me H OMe H H N 1381 500
33 Et H F H H N 1808 617
34 Et H F H H C 2292 1141
35 Me H F H Me N 1871 260
36 Me H Me H Me N 1169 183
37 Me H H OMe H N 73 113
38 Me H H OEt H N 14 <10
39 Cl H H Me Me N 73 14