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. Author manuscript; available in PMC: 2013 Mar 7.
Published in final edited form as: J Med Chem. 2012 Feb 16;55(5):2406–2415. doi: 10.1021/jm201690h

Table 1.

Ki values of compounds 9 and 12 determined from in vitro competitive binding assays.

Receptor or binding site Ki (nM)
9 12
H1 5,440 7,055
H2 1,708 923
H3 1.9 ± 0.23 0.4 ± 0.04
H4 >10,000 >10,000
5-HT1A 432 >10,000
5-HT1B >10,000 >10,000
5-HT1D 6,380 5,237
5-HT2A 2,718 1,355
5-HT2B 3,152 >10,000
DAT >10,000 137
M1 3,266 931
M2 462 681
M3 204 512
M4 351 415
M5 437 336
All othersa >10,000 >10,000
a

5-HT1E,2C,3,5A,6 and 7, α1A,1B,1D,2A,2B and 2C, β1–3, D1–5, σ1,2, SERT and NET