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. Author manuscript; available in PMC: 2023 Nov 24.
Published in final edited form as: J Med Chem. 2022 Nov 11;65(22):15238–15262. doi: 10.1021/acs.jmedchem.2c01170

Table 2.

Off-Target Analysis of Selected PAM Derivatives at 45 Other Receptors, Transporters, and Channels, As Determined in Radioligand Binding Assays by the PDSPa

derivative protein Ki (μM)
14 5HT2B 1.36
σ 1 1.48
σ 2 1.36
18 σ 1 4.64
σ 2 0.575
20 σ 1 5.15
σ 2 0.907
21 σ 2 3.62
22 D3 5.28
23 D3 7.63
σ 1 3.02
σ 2 2.84
26 σ 1 2.34
σ 2 1.34
27 MOR 7.22
σ 1 2.42
σ 2 3.43
KOR 5.50
DAT 0.467
5HT2B 3.25
35 D3 0.846
TSPO 0.427
σ 2 3.01
39 5HT2B 2.60
TSPO 0.123
σ 2 0.891
a

These are the only hits with >50% inhibition in the primary screen at 10 μM.