Table 1 Biological activity of rapalogs

From: Diversity oriented biosynthesis via accelerated evolution of modular gene clusters

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

  1. Comparison of FKBP12 PPIase inhibition, mTORC1 pathway inhibition (p-S6) and S. cerevisiae MIC values for a selection of rapalogs.