Table 1.
Entry |
Compound |
R group and position |
Starvation‐ Induced IC50 [μm] |
Rapamycin‐ Induced IC50 [μm] |
---|---|---|---|---|
1 |
10 h |
5‐CF3 |
7.86±0.8 |
n/a |
2 |
10 i |
5‐NO2 |
7.33±1.5 |
n/a |
3 |
10 k |
5‐OCF3 |
4.68±1.4 |
n/a |
4 |
10 m |
5‐Cl |
5.54±2.5 |
n/a |
5 |
10 n |
5‐Br |
6.78±1.1 |
n/a |
6 |
10 r |
6‐CF3 |
5.82±3.0 |
n/a |
7 |
10 s |
6‐Cl |
8.12±1.5 |
n/a |
8 |
10 u |
7‐OMe |
2.46±0.6 |
2.37±0.7 |
9 |
10 w |
7‐azaindole |
4.33±1.7 |
4.95±0.7 |
10 |
10 w‐a |
4‐Cl‐7‐azaindole |
0.52±0.20 |
0.65±0.35 |
11 |
10 w‐b |
5‐Me‐7‐azaindole |
0.31±0.09 |
0.86±0.26 |
12 |
10 w‐c |
5‐Ar‐7‐azaindole |
9.00±1.1 |
n/a |
13 |
10 w‐d |
5‐CF3‐7‐azaindole |
0.12±0.03 |
0.77±0.29 |
14 |
10 w‐e |
5‐NO2‐7‐azaindole |
0.67±0.13 |
1.26±0.20 |
15 |
10 w‐f |
5‐F‐7‐azaindole |
n/a |
n/a |
16 |
10 w‐g |
5‐Cl‐7‐azaindole |
0.11±0.04 |
0.85±0.14 |
17 |
10 w‐h |
5‐Br‐7‐azaindole |
0.08±0.03 |
0.81±0.35 |
18 |
10 w‐i |
5‐I‐7‐azaindole |
0.08±0.02 |
1.24±0.20 |
19 |
10 w‐j (azaquindole‐1) |
5‐Br‐6‐Me‐7‐azaindole |
0.04±0.02 |
0.10±0.02 |
20 |
10 w‐k |
6‐Me‐7‐azaindole |
3.12±0.5 |
5.11±1.4 |
21 |
10 w‐l |
6‐Cl‐7‐azaindole |
3.06±0.9 |
6.21±2.2 |
22 |
9 w |
7‐azaindole |
n/a |
nd |
23 |
9 w‐b |
5‐Me‐7‐azaindole |
n/a |
nd |
All data are shown as mean ± SD of three independent experiments (N=3; n≥3). All compounds were initially assayed at a concentration of 10 μm. For hits reducing the number of LC3 puncta by more than 50 %, IC50 values were determined. n/a=inactive (no reduction of LC3 puncta at 10 μm). Ar=4‐Cl‐C6H4. nd=not determined.