Table 4.
InRAGER lead profiling screen assay results. Primary assays were performed at 10 μM InRAGER to determine the percent inhibition; secondary dose response determined IC50 and Ki.
| Assay name | %Inhibition at 10 μM | Ki (μM) | IC50 (μM) |
|---|---|---|---|
| Adenosine A3 receptor | 99 | 0.024 | 1.4 |
| 5-HT2B receptor | 97 | 0.55 | 0.26 |
| Norepinephrine transporter | 95 | 1.5 | |
| Kappa opioid receptor | 83 | 2.2 | |
| Urotensin (UT) receptor | 78 | 8.9 | 1.4 |
| Cholecystokinin A receptor | 76 | 3.6 | |
| Adenosine A2A receptor | 76 | 5.1 | |
| Prostaglandin receptor EP2 | 74 | 2.3 | |
| 5-HT2A receptor | 67 | 7.8 | |
| Translocator protein 18 kDa (TSPO) | 63 | 12.0 | 0.48 |