Table 1.
Activity (IC50) and kinetics data for β-hematin formation at a lipid-water interface (37 °C, pH 4.8) in 24-well plates in the presence of antimalarial drugs.a
Drug | IC50 | 100Y | z (min−1) | Kads (mM−1) | k2 (M−2min−1) | |
---|---|---|---|---|---|---|
| ||||||
Parasite | β-H (μM) | |||||
CQ | 14.0b 15.0 ± 2.9c 10.6 ± 1.7d |
18.8 ± 0.6 | 67.6 ± 0.8 | 0.015 ± 0.001 | 102.0 ± 4.7 | 0.12 ± 0.01 |
AQ | 7.8b 16.0 ± 2.1c 20.4 ± 0.7d |
5.9 ± 0.3 | 70.1 ± 1.4 | 0.023 ± 0.003 | 566.4 ± 44.9 | 1.7 ± 0.4 |
QD | 21.5b 47.0 ± 11.3c 48.0 ± 10.9d |
20.1 ± 4.1 | 73.6 ± 1.3 | 0.015 ± 0.001 | 32.7 ± 2.3 | 0.032 ± 0.005 |
QN | 34.2b 141.0 ± 7.9c 109.8 ± 25.6d |
31.0 ± 8.3 | 68.1 ± 1.8 | 0.020 ± 0.003 | 61.2 ± 3.4 | 0.0014 ± 0.0007 |
Error calculated as standard error of the mean (SEM), following three experimental repeats, each including triplicate data points.
Data (nM, 3D7) reported by Hawley et al.40
Data (nM, D10) determined by Dr J.M. Combrinck, University of Cape Town, and communicated privately.
Data (nM, NF54) determined by Dr J.M. Combrinck, University of Cape Town, and communicated privately.