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. 2021 Aug 26;64(17):12603–12629. doi: 10.1021/acs.jmedchem.1c00497

Table 4. Off-Target Activity Data for the Selected Molecules.

  % activity at 1.0 × 10–6 Ma
compd H1R (%) α1R (%) M1R (%) hERGb (%)
2 39 48 –15 23
3 58 66 5 34
5 54 39 4 31
7 29 56 –7 28
11 24 43 –5 29
15 10 13 11 29
16 2 14 –1 40
18 19 19 7 38
21 4 15 –6 47
Phentolamine 91 76    
Mepyramine 95   55  
Amitriptyline 99 82 78  
Doxepin 97   92  
Quetiapine 76 75 88  
Olanzapine 89 82 89  
Verapamil       91
a

% inhibition of control specific binding at the concentration of 1.0 × 10–6 M. Assays carried out in duplicate (n = 2). Blank spaces—compounds not tested in the assay.

b

% inhibition of hERG-mediated potassium currents at a concentration of 1.0 × 10–6 M.