Table 5.
Broad-Panel Counter Screening of Compound 15b against Other GPCRs, Ion Channels, and Transporters
| GPCRs, transporters, ion channels | % inhibition (10 μM)a | Ki (nM)a | GPCRs, transporters, ion channels | % inhibition (10 μM) | Ki (nM)a |
|---|---|---|---|---|---|
| 5-HT1A | 35.04 | ND | D1 | 7.92 | ND |
| 5-HT1B | 11.55 | ND | D2 | −0.64 | ND |
| 5-HT1D | 29.09 | ND | D3 | 10.45 | ND |
| 5-HT1E | 18.55 | ND | D4 | 20.65 | ND |
| 5-HT2A | 25.21 | ND | D5 | 8.29 | ND |
| 5-HT2B | 91.67 | 425.4 ± 81.4 | DAT | 15.46 | ND |
| 5-HT2C | 41.39 | ND | GABAA | −17.94 | ND |
| 5-HT3 | 22.6 | ND | H1 | 15.7 | ND |
| 5-HT5A | 20.55 | ND | H2 | 25.13 | ND |
| 5-HT6 | 15.34 | ND | KOR | 18.73 | ND |
| 5-HT7A | 20.68 | ND | M1 | −1.71 | ND |
| α 1A | 16.45 | ND | M2 | 3.15 | ND |
| α 1B | −5.51 | ND | M3 | 39.69 | ND |
| α 1D | −10.52 | ND | M4 | 28.71 | ND |
| α 2A | 23 | ND | M5 | −1.37 | ND |
| β 1 | 10.39 | ND | MOR | 20.45 | ND |
| β 2 | −7.69 | ND | hERG | 11.04 | ND |
a
Values are mean ± SEM of at least three independent experiments.
SEM < 20% where not listed. “ND” means that a Ki binding affinity was not determined because off-target inhibition at 10 μM did not reach 50%.