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RAGER lead profiling screen assay results. Primary assays were performed at 10 μM RAGER to determine the percent inhibition; secondary dose response determined IC50 and Ki.
| Assay name | %Inhibition at 10 μM | Ki (μM) |
|---|---|---|
| MT1 (h) | 96 | 0.093a |
| MT2 (h) | 82 | 0.70b |
| Kappa opioid receptor | 69 | n.d.c |
| Peripheral benzodiazepine receptor | 64 | 8.5 |
| Androgen receptor (h) | 59 | 2.6 |
| Dopamine transporter | 52 | 6.8 |
MT1 (IC50 = 0.26 μM).
MT2 (IC50 = 1.1 μM).
n.d. = not determined.
