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Biological activity of rapalogs
| Compound ID | Module organisation | FKBP12 K i (nM) | p-S6 IC 50 (nM) | S. cerevisiae MIC (μg mL −1 ) |
|---|---|---|---|---|
| Rapamycin | Natural | 5.4 | <1 | <0.25 |
| 1 | Natural | 2.5 | N/A | <0.25 |
| 8 | +1 | 6.5 | N/A | <2 |
| 7 | −1 | 7.9 | 100 | <2 |
| 5 | −3 | 370 | 300 | <64 |
| 3 | −5 | 460 | >1900 | >64 |
| 2 | −6 | >1000 | 1000 | >64 |
Comparison of FKBP12 PPIase inhibition, mTORC1 pathway inhibition (p-S6) and S. cerevisiae MIC values for a selection of rapalogs.
