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. Author manuscript; available in PMC: 2019 Oct 11.
Published in final edited form as: J Med Chem. 2019 Mar 27;62(7):3753–3772. doi: 10.1021/acs.jmedchem.9b00351

Table 7.

Radioligand Binding Affinities of Compounds 1, 17, 41, and 46 at Select GPCRs, Ion Channels, and Transportersa

receptor binding affinity Ki (nM)
compound 1 compound 17 compound 41 compound 46
D1  110  140  150  130
D2  8300  9600  7600  8700
D3  7900  8100  >10 000  6200
D4  4500  6900  6900  4900
D5  38  82  47  27
5-HT1A  1200  6900  2500  3700
5-HT1B  9300  8800  9300  9900
5-HT1D  9300  8100  8900  4100
5-HT1E  9800  8900  9900  7800
5-HT2A  4900  8700  4300  3400
5-HT2B  4100  6700  830  1100
5-HT3  7900  9100  9300  7600
5-HT4  9100  >10 000  >10 000  3700
5-HT5A  >10 000  9500  7400  6200
5-HT6  8100  7900  6900  7200
5-HT7A  7800  8100  4100  3800
alpha1A  3400  8700  7000  2900
alpha1B  9200  8800  7400  4800
alpha2A  3400  6800  5100  2600
beta1  7600  9600  8500  8500
beta2  9300  >10 000  8600  5900
MOR  8200  9400  4400  2100
KOR  3100  7200  1500  3200
M1  8800  8500  9000  6600
M2  7700  7300  8100  1700
M3  >10 000  9200  >10 000  2700
sigma1  8200  8000  6900  8800
H1  >10 000  >10 000  9800  2600
H2  8000  8200  6700  2500
DAT  8300  >10 000  9100  4500
SERT  >10 000  >10 000  9700  >10 000
a

Ki values represent the average of at least three triplicate experiments. SEM <±20%.