Table 1.
Compound | GGDPS IC50 (μM) | Cellular LEC (μM)1 |
---|---|---|
1 15 | 2.2 ± 0.6 | 0.5 |
3 20 | 1.3 ± 0.3 | 0.1 |
4 20 | 5.9 ± 1.3 | 2.5 |
7 | 3.0 ± 0.9 | 0.25 |
11 | >100 μM | No activity up to 100 μM |
17 | 2.0 ± 0.5 | 0.5 |
27 | >100 μM | No activity up to 100 μM |
29 | 2.7 ± 1.6 | 0.25 |
31 | 1.6 ± 0.7 | 0.5 |
37 | 1.4 ± 0.5 | 0.1 |
Cellular LEC (lowest effective concentration) is defined as the lowest concentration for which an unmodified Rap1a band is visible in the immunoblot and a statistically significant increase in intracellular lambda light chain is observed in the ELISA.