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. 2016 Apr 7;7(6):618–622. doi: 10.1021/acsmedchemlett.6b00056

Table 1. Binding Data of the Synthesized Compounds 1131 for 5-HT6R.

graphic file with name ml-2016-00056b_0007.jpg

compd Q R R1 5-HT6Ki [nM]a
Ib 2-napthtyl H H 27 ± 6
11 3-quinolinyl H H 13 ± 3
12 6-quinolinyl H H 20 ± 4
13 7-quinolinyl H H 7 ± 2
14 3-isoquinolinyl H H 12 ± 1
15 4-isoquinolinyl H H 5 ± 1
16 3-quinolinyl 5-Cl H 11 ± 2
17 5-quinolinyl 5-Cl H 11 ± 3
18 7-quinolinyl 5-Cl H 9 ± 2
19 4-isoquinolinyl 5-Cl H 18 ± 3
IIb 2-napthtyl 5-MeO H 19 ± 2
20 3-quinolinyl 5-MeO H 8 ± 1
21 5-quinolinyl 5-MeO H 4 ± 1
22 6-quinolinyl 5-MeO H 14 ± 3
23 7-quinolinyl 5-MeO H 2 ± 0.4
24 3-isoquinolinyl 5-MeO H 6 ± 1
25 4-isoquinolinyl 5-MeO H 3 ± 0.2
26 3-quinolinyl 6-Cl H 37 ± 5
27 6-quinolinyl 6-Cl H 112 ± 9
28 7-quinolinyl 6-Cl H 22 ± 2
29 3-isoquinolinyl 6-Cl H 102 ± 12
30 7-quinolinyl H Me 18 ± 3
31 3-isoquinolinyl H Me 20 ± 2
a

Mean Ki values ± SEM based on three independent binding experiments.

b

Data from ref (13).