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. 2023 Aug 3;66(16):11447–11463. doi: 10.1021/acs.jmedchem.3c00959

Table 2. S1R and S2R Binding Assays for Targeted Compounds.

graphic file with name jm3c00959_0011.jpg

            Ki (nM) ± SDa
ID R1 R2 X n m S1R S2R KiS2R/KiS1R
9a NO2 H   0 1 0.76 ± 0.17 12 ± 2.9 15.8
9b OCH3 H   0 1 6.2 ± 1.8 12 ± 1.2 1.9
9c COCH3 H   0 1 3.0 ± 0.46 10 ± 1.7 3.3
9d CN H   0 1 3.5 ± 0.7 2.6 ± 0.6 0.7
15a Cl Cl CO 1 1 7.5 ± 1.0 24 ± 3.6 3.2
15b OCH3 OCH3 CO 1 1 435 ± 35 736 ± 267 1.7
15d H H CO 0 1 209 ± 18 57 ± 3.3 0.3
15e H H CO 1 1 79 ± 3.8 99 ± 16 1.3
16a Cl Cl CH2 1 1 4.2 ± 0.8 11 ± 2.1 2.6
16b OCH3 OCH3 CH2 1 1 25 ± 5.3 23 ± 3.5 0.9
a

Each value is the mean ± SD of at least two experiments performed in duplicate.