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. Author manuscript; available in PMC: 2022 Aug 15.
Published in final edited form as: Bioorg Med Chem. 2021 Jul 11;44:116307. doi: 10.1016/j.bmc.2021.116307

Table 1.

Summary of the bioassay results.

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
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.