Table 1. Relevant activity parameters of SC81458 and SC83288.
SC81458 | SC83288 | |
---|---|---|
IC50, IC90, IC99 (nM) | 8, 18, 50 | 3, 8, 20 |
In vitro PCT99.9% (h) | 37±4 (4) | 51±6 (4) |
In vitro logPRR | 3.4±0.4 (4) | 3.0±0.5 (4) |
In vitro lag phase (h) | <5 | <5 |
In vivo PCT99.9% (h)* | <48 | 48 |
In vivo logPRR* | 5.3 (W2), 3.2 (3D7) | 3.0 |
IC50/90/99, inhibitory concentration of 50, 90 or 99% of the maximal effect; PCT99.9%, clearance time of 99.9% of the original parasite population; PRR, parasite reduction ratio.
For the in vitro PCT99.9% and the in vitro logPRR the means±s.e. of the means of (n) independent determinations are shown.
*Obtained in the P. falciparum-infected humanized NSG mouse model system.