Table 1. Initial GPCR Screen^a.

	pKia
receptor	compound 3a	compound 3b	compound 3c
5-HT1A	6.2 ± 0.1b	5.7 ± 0.1b	7.13 ± 0.06b
5-HT1B	<5	<5	<5
5-HT1D	<5	<5	<5
5-HT1E	<5	<5	<5
5-HT2A	<5	<5	<5
5-HT2B	6.84 ± 0.06b	6.75 ± 0.06b	6.1 ± 0.1b
5-HT2C	5.6 ± 1.0b	5.6 ± 3.5b	5.4 ± 1.3b
5-HT3	<5	<5	<5
5-HT5A	5.7 ± 1.5b	<5	<5
5-HT6	<5	<5	<5
5-HT7	<5	<5	6.0 ± 0.1b
Alpha1A	<5	<5	5.8 ± 0.1b
Alpha1B	<5	<5	<5
Alpha1D	<5	<5	<5
Alpha2A	5.2 ± 0.2b	<5	6.4 ± 0.1b
Alpha2B	5.3 ± 0.1b	<5	6.4 ± 0.1b
Alpha2C	<5	<5	<5
Beta1	<5	<5	<5
Beta2	5.3 ± 0.1b	<5	<5
Beta3	<5	<5	6.0 ± 0.1b
BZP	5.8 ± 0.1b	<5	5.1 ± 0.1b
D1	<5	<5	<5
D2	<5	<5	<5
D3	<5	<5	<5
D4	<5	<5	5.7 ± 0.1b
D5	<5	<5	<5
DAT	5.3 ± 0.2b	<5	5.5 ± 0.2b
GABAA	<5	<5	<5
H1	5.5 ± 0.5b	<5	<5
H2	<5	<5	<5
H3	<5	<5	5.4 ± 0.2b
H4	<5	<5	<5
M1	<5	<5	<5
M2	<5	<5	<5
M3	<5	<5	<5
M4	<5	<5	<5
M5	<5	<5	<5
NET	5.6 ± 0.1b	6.5 ± 0.1b	6.4 ± 0.1c
δ-OR	<5	<5	<5
κ-OR	6.5 ± 0.1b	<5	<5
μ-OR	5.7 ± 0.1b	<5	<5
PBR	<5	<5	<5
σ1	6.9 ± 0.1b	6.0 ± 0.1b	6.5 ± 0.1b
σ2	<5	<5	6.2 ± 0.1b

^aFor pK_i values reported as <5, the compound did not demonstrate ≥50% binding in an initial assay at 10 μM concentration.

^bThese data reflect triplicate measurements of a single experiment. The error reflects the error in the sigmoidal curve fit.

^cThese data reflect the average of triplicate experiments run in triplicate. The error reflects the standard deviation of the three calculated pK_i values. Values in italic type are noted for the reader’s convenience.