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. Author manuscript; available in PMC: 2017 Dec 8.
Published in final edited form as: J Med Chem. 2016 Nov 16;59(23):10601–10618. doi: 10.1021/acs.jmedchem.6b01208

Table 4.

Radioligand binding affinity of compounds 1, 24, 46, 49, 53 and 54 at select GPCRs.a

Receptor Binding affinity Ki (nM)
1 24 46 49 53 54
D2R 150 60 170 45 30 99
D1R N/A 1100 1700 2000 2000 1100
D3R 13 35 100 64 31 69
D4R 82 280 1800 7100 77 430
D5R N/A 1500 N/A 1500 1100 1800
5-HT1A 86 55 100 14 1.4 66
5-HT1B 1700 1400 N/A 1600 420 2600
5-HT1D 320 390 820 94 100 410
5-HT2A 120 72 140 110 29 70
5-HT2B 38 12 71 43 32 18
5-HT2C 160 58 210 140 92 73
5-HT3 130 330 1500 N/A 2600 370
5-HT5A N/A 1300 1600 1400 330 810
5-HT6 720 350 960 2200 2300 410
5-HT7 140 100 160 69 31 95
DAT 690 2800 4000 N/A 2500 2100
SERT 340 450 580 480 330 62
H1 57 56 690 N/A 52 28
H2 680 310 2100 430 240 330
a

Ki values are the average of at least 2 duplicate experiments. SEM: < ± 20%.

N/A: not active.