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. Author manuscript; available in PMC: 2013 Mar 1.

Published in final edited form as: Bioorg Med Chem. 2012 Jan 21;20(5):1671–1678. doi: 10.1016/j.bmc.2012.01.022

Table 1.

Binding affinity constants of compounds at selected DA, 5-HT and H-1 receptors

Compd #	>Binding data; K_i ± SEM (nM)
	5-HT_1A	5-HT_2A	5-HT_2C	D₂	D₃	D₄	H₁
Cloz^a	140	8.9	17.0	130	240	54	1.8
Hal^a	3600	120	4700	0.89	2.5	3.3	440
2^a	117.4 ± 32.6	23.6 ± 2.7	1425 ± 207	43.3 ± 13.3	158.8 ± 35.1	6.6 ± 0.6	188.6 ± 16.0
3^a	90.9 ± 21.0	109.6 ± 16.0	3552± 943	253.5 ± 38.9	ND	17.5 ± 2.0	157.6 ±36.0
4^a	ND	ND	ND	170	220	520	ND
5^a	2332 ± 470	194.8 ± 53.0	3513 ± 912	178.4 ± 29.2	548.1± 246.0	41.8 ± 9.0	1014 ± 206
6^a	27.7 ± 8.0	30.9 ± 6.0	872.1 ± 178.0	1.6 ± 0.1	5.1 ± 3.0	5.3 ± 1.0	8780 ± 1625
7	123.0 ± 12.9	236.0 ± 21.6	MP	22.0 ± 3.1	4.1± 0.6	49.0 ± 9.1	4,149 ± 924
8	102.0 ± 11.8	317.0 ± 29.2	2434 ± 583	33.0 ± 4.6	9.7 ± 1.1	9.4 ± 1.5	1719 ± 368
9	415.0 ± 48.1	411.5 ± 52.5	3775 ± 704	1021 ± 142	590.0 ± 54.3	37.0 ± 4.3	ND
10	168 ± 19	163.0 ± 20.0	2529 ± 223	751.1 ± 92.3	1,020 ± 25	32.1 ± 2.5	800.2 ± 69.9
11	73.0 ± 14.7	566.6 ± 91.9	>10,000	172.0 ± 28.1	208.8 ± 43.4	110.0 ± 12.6	509.0 ± 71.1
12	91.0 ± 10.5	510.3 ±76.9	4097 ± 754	139.0 ± 25.3	3043 ± 176	123.0 ± 19.9	1247 ± 204
13	263.0 ± 36.5	159.0 ± 11.0	1420 ± 295	258.7 ± 48.4	152.0 ± 21.0	28.6 ± 3.4	61.0 ± 8.5
14	216.0 ± 30.0	696.0 ± 51.3	ND	MP	863.0 ± 132.9	431.0 ± 40.7	665.0 ± 47.0
15	MP	MP	MP	MP	MP	MP	MP
16	495.0 ± 91.0	1003 ± 96	5920±769	1983 ± 163	1051 ± 174	1215 ± 67	129.0 ± 12.0
17	MP	1038^b	MP	MP	777.0 ± 125.7	126.0 ± 20.4	ND
18	MP	MP	MP	180.0 ± 29.5	16.0 ± 2.6	508.0 ± 1.2	ND
19	274.0 ± 52.7	>10,000	4623^b	44.0 ± 3.1	13.0 ± 1.8	432.0 ± 91.1	187.0 ± 34.5

Abbreviations: MP, Missed primary assay threshold of 50% inhibition; ND, Not determined; Cloz, Clozapine; Hal, Haloperidol.

^a

Results were previously reported in Ref. 7.

^b

Standard Errors are within 20% of the mean.