Table 1.
Analogs of the head group on the 4-aminoquinoline series.
 | ||||||
|---|---|---|---|---|---|---|
| ID | R | P. fal. D6 EC50 (μM)a | HepG2 TC50 (μM)b,c,d | SI | cLogP | LLE |
| 3 |  |
0.019 | >4 | >210 | 6.4 | 1.3 |
| 7 |  |
0.012 | 2.8 | 230 | 4.6 | 3.3 |
| 8 |  |
0.20 | >5.5 | >28 | 4.7 | 2.0 |
| 9 |  |
0.018 | 20 | 1100 | 3.9 | 3.8 |
| 10 |  |
0.085 | 7.1 | 84 | 5.5 | 1.5 |
| 11 |  |
0.064 | >30 | >470 | 5.2 | 2.0 |
| 12 |  |
0.13 | >36 | >280 | 2.9 | 4.0 |
| 13 |  |
2.1 | >36 | >17 | 1.9 | 3.8 |
| 14 |  |
0.20 | >33 | >170 | 2.3 | 4.4 |
| 15 |  |
0.022 | >29 | >1300 | 3.0 | 4.6 |
| 16 |  |
0.16 | 22 | >140 | 4.2 | 2.6 |
| 17 |  |
0.050 | 21 | 420 | 2.7 | 4.6 |
| 18 |  |
0.13 | >31 | >240 | 2.7 | 4.2 |
| 19 |  |
0.12 | >31 | >260 | 2.5 | 3.6 |
| 20 |  |
0.25 | 10 | 40 | 4.1 | 2.5 |
| 21 |  |
0.058 | >31 | 540 | 3.5 | 3.8 |
| 22 |  |
0.027 | >28 | >1000 | 3.5 | 4.2 |
| 23 |  |
0.16 | >6 | >38 | 2.2 | 4.7 |
| 24 |  |
0.11 | >35 | >320 | 3.4 | 3.6 |
| Chloroquine | 0.005 | 3.3 | 660 | |||
a
All r2 values >0.9 unless noted otherwise
b
n = 1 biological replicate made up of 2 technical replicates
c
concentration which is toxic to 50% of the cell population
d
tested concentration ranges were determined based on compound solubility