Table 1.
Bioactivity of aminoquinolines in FP and WB assays
| ID | Comp. | IC50(µM)a (FP assay) | IC50(µM)b (Western Blot) |
|---|---|---|---|
| 5 | PU-H71 | 0.043 | 0.06–0.13 |
| 7 | 850375 | 5.8 | 5.0 |
| 8a | TG2-193-3 | 40 | NAc |
| 8c | TG2-205 | 40 | NA |
| 8 | 24724348 | 4.9 | 1.6 |
| 9 | 24724372 | 29 | 6.0 |
| 10 | 24724290 | 1.3 (0.73)d | 1.0(2–3)d |
| 11 | 24724310 | 2.4 | 6.0 |
| 18a | AS-222 | >50 | NA |
| 18d | AS-217 | >50 | NA |
| 19a | 24724364 | 3.1 | NA |
| 19b | 24724377 | 8.0 | NA |
| 19c | 24724374 | 40.0 | 13 |
| 19d | JM1-156b | >50 | 25 |
| 19e | 24724347 | >50 | NA |
| 19f | 24724365 | >50 | NA |
| 19g | 24724375 | 14.4 | NA |
| 19h | 24724350 | 44 | 25 |
| 19i | 24724357 | >50 | NA |
| 19j | 24724376 | >50 | NA |
| 19k | 24724346 | 2.1 | 25 |
| 19l | 24724369 | 14 | NA |
| 19m | 24724351 | >50 | NA |
| 20a | JM1-138b | 7.6 | NA |
| 20b | JM1-152c | <1.6 | NA |
| 20c | JM1-156c | <1.6 | NA |
| 20d | JM1-135c | <1.6 | NA |
| 20f | JM1-147d | <1.6 | 20 |
| 20g | 24724309 | <1.0 | 20 |
| 20h | 24724292 | 0.8 | 30 |
| 20i | 24724291 | <1.6 | NA |
| 20j | JM1-128a | 1.8 | NA |
| 20k | 24724363 | 1.1 | NA |
a
Mean of 2 determinations
b
Mean of 3 determinations
c
NA = Not Active
d
values in the parenthesis are from re-synthesized 10