Table 1.
Binding data of compounds 8−12 and reference compound PZ-1643 for 5-HT6 and D3 receptors.
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Compd | R |
Ki 5-HT6R
[nM] a |
%inh Binding
to D3R @1μM b |
PZ-1643 |
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27 c | 98% (7 nM) c |
8 |
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11 | – |
9 |
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6 | 54% |
10 |
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84 | – |
11 |
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17 | 25% |
12 |
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556 | – |
a Mean Ki values based on at least three independent binding experiments (SEM ≤ 18%) performed in HEK293 cells with stable expression of human 5-HT6R. b Percentage displacement values at 10−6 M; performed at Eurofins in CHO cells with stable expression of human D3R. c Data taken from [26].