TABLE 2.
Ki and functional inhibition at 12 off-target sites. The Ki values for 11 off targets that were first identified as hits (>50% radioligand displacement by 10 μM NP10679) in a screen of 41 targets are given. Ki values were determined from full binding displacement curves. The functional IC50 values for several targets were also determined. All assays were conducted at pH 7.4.
| Target | K i | Functional IC50 |
|---|---|---|
| μM | ||
| 5-HT1B | >10 | nd |
| 5-HT1D | 2.29 | nd |
| 5-HT2A | 0.638 | 1.71 |
| 5-HT2B | 1.92 | nd |
| α1A | 0.603 | 0.154 |
| α1B | 1.92 | nd |
| α1D | 0.495 | nd |
| α2C | 3.09 | nd |
| H1 | 0.040 | 0.073 |
| SERT | 0.135 | nd |
| σ2 | 1.98 | nd |
| hERG | nd | 0.617 |
α1A, α adrenergic receptor-1A; α1B, α adrenergic receptor-1B; α2C, α adrenergic receptor-2C; α1D, α adrenergic receptor-1D; 5-HT1B, serotonin receptor-1B; 5-HT2A, serotonin receptor-2A; 5-HT2B, serotonin receptor-2B; 5-HT1D, serotonin receptor-1D; nd, not done.