Table 3.
Compounds with Activity on Multiple Targets, as % Inhibition at 10uM
| Compound | RGS 4 | RGS 8 | RGS 16 |
|---|---|---|---|
| CCG-420854 | 33% | 3% | 8% |
| CCG-4388616 | 31% | 3% | 3% |
| CCG-462324a | 3% | 1% | 10% |
| CCG-500144 | 93% | 52% | 90% |
| CCG-510964a | 4% | 3% | 5% |
| CCG-5183116 | 15% | 10% | 15% |
| CCG-540848 | 76% | 9% | 42% |
| CCG-5591916 | 75% | 8% | 18% |
4
Initial RGS “active”
8
Initial RGS “active”
16
Initial RGS “active”
a
Lower potency at DRC
The table above shows individual compounds that had activity on more than one RGS as discovered in follow-up dose-response experiments. Superscripts after the compounds number indicate the RGS at which the compound was originally identified as having activity, and the percentages indicate the amount of inhibition at 10uM concentration of compound. For two compoundsa, the level of inhibition was quite low at 10uM, but these compounds did show dose-response activity, albeit with considerably higher IC50 values.