TABLE 1

Receptor affinities.

Panel screens of up to 105 radioligand-binding assays and 34 enzyme assays were performed, and the affinity of SEP-856 was determined for receptors at which >50% inhibition was seen at 10 μM. Details of radioligands, incubation conditions , and the targets in the screening panels are listed in the Supplemental Material. Data are shown as mean ± S.E.M. (n ≥ 3, n = 1 for 5-HT2B).

ReceptorKi (µM)
D2s21.3 ± 8.2
5-HT1A0.284 ± 0.056
5-HT1B1.90 ± 1.72
5-HT1D1.13 ± 0.21
5-HT2A17.25 ± 4.0
5-HT2B1.1
5-HT2C2.45 ± 0.82
5-HT70.031 ± 0.003
α2A0.59 ± 0.06
α2B1.9 ± 0.10