|
In vitro potency |
PvPI4K IC50
|
3.4 nM |
23 nM |
| |
PfNF54 IC50
|
28 nM |
5.4 nM |
| |
PfK1 IC50
|
25 nM |
4.7 nM |
| physicochemical property |
log D7.4
|
2.60 (0.01) |
–0.27 (0.03) |
| |
thermodynamic solubility (pH)a
|
4.2 μg·mL−1 (6.5) |
110 μg·mL−1(6.0) |
| |
Mol wt |
393.4 g·mol–1
|
427.4 g·mol–1
|
| |
pKa (measured) |
4.0 (0.07) |
7.45 (0.05) |
| cardiotoxicity
risk |
hERG IC50
|
>11 μM |
10 μM |
| life cycle stage activity |
Pc liver hypnozoites/schizonts IC50
|
64 nM |
<10 nM |
| |
Pb liver schizonts IC50
|
46 nM |
0.92 nM |
| |
Pv liver hypnozoites/schizonts IC50
|
<100 nM |
<100 nM |
| |
Pf/Pv ex vivo
|
202 nM |
29 nM |
| |
Pf early gametocytes IC50
|
215 nM |
134 nM |
| |
Pf late/mature gametocytes IC50
|
140 nM |
66 nM |
| |
Pf gamete (male/female) IC50
|
91/139 nM |
83/87 nM |
| |
Pf oocyst reduction IC50
|
111 nM (indirect) |
96 nM |
| efficacy |
Pb ED90 (NOD-scid IL-2Rγnull mouse) |
1.1 mg·kg–1
|
1.0 mg·kg–1
|
| |
Pf ED90 (NOD-scid IL-2Rγnull mouse) |
0.57 mg·kg–1
|
0.25 mg·kg–1
|