Table 3.
Enzymatic and cellular activities profile of compounds varying R1
Entry | R1 | mTOR IC50(nM) mTORC1 | mTOR IC50(nM) Cellular |
---|---|---|---|
8 |
![]() |
13.5 | 40 |
9 |
![]() |
78.9 | 100 |
10 |
![]() |
93.8 | >300 |
11 |
![]() |
3440 | >300 |
12 |
![]() |
33.2 | >300 |
13 |
![]() |
662 | >300 |
14 |
![]() |
213 | >300 |
15 |
![]() |
66.5 | 150 |
16 |
![]() |
82.6 | 40 |
17 |
![]() |
45.9 | >300 |
18 |
![]() |
214 | >300 |
IC50 determinations are the mean of two of independent measurement with standard error of <20%, None of the tested compounds exhibited IC50 for inhibition of cellular PI3K activity of less than 300 nM.