Table 5.
Broad-Panel Counter Screening of 12c against Other GPCRs and Transportersa
| GPCRs | % inhibition (10 μM)b | Ki (μM)b | GPCRs, transporters, ion channels | % inhibition (10 μM) | Ki (μM)b |
|---|---|---|---|---|---|
| 5-HT1A | 8.68 | ND | D1 | 12.29 | ND |
| 5-HT1B | 6.3 | ND | D2 | 2.51 | ND |
| 5-HT1D | 29.64 | ND | D3 | 10.64 | ND |
| 5-HT1E | 7.71 | ND | D4 | 29.91 | ND |
| 5-HT2A | 10.62 | ND | D5 | −7.17 | ND |
| 5-HT2B | 28.69 | ND | DAT | 24.83 | ND |
| 5-HT2C | 52.62 | >10 | GABAA | 5.98 | ND |
| 5-HT3 | 26.82 | ND | H1 | 6.43 | ND |
| 5-HTSA | 13.95 | ND | H2 | 22.36 | ND |
| 5-HT6 | 7.98 | ND | KOR | 1.48 | ND |
| 5-HT7A | 5.16 | ND | M1 | 2.86 | ND |
| Alpha1A | 13.56 | ND | M2 | −1.87 | ND |
| Alpha1B | −5.42 | ND | M3 | 45.38 | ND |
| Alpha2A | 4.45 | ND | M4 | 29.26 | ND |
| Beta1 | 17.2 | ND | M5 | 0.82 | ND |
| Beta2 | −14.07 | ND | MOR | 16.24 | ND |
| hERG | 11.04 | ND |
a
The broad-panel counter screening of 12c against a panel of GPCRs and transporters was generously provided by the NIMH Psychoactive Drug Screening Program.
b
The values are the mean percent inhibition of binding from at least three independent experiments, SEM < 20%. “ND” means that a Ki binding affinity was not detected.