TABLE 1.
IC50s for heme polymerization and antimalarial drug potencies
Drug | IC50 (μM) for heme polymerization | Antimalarial drug potency (IC50 [nM] at an inoculum size of 1)
|
|||
---|---|---|---|---|---|
3D7 | HB3 | K1 | PH3 | ||
AQ | 15.1 | 7.8 | 8.5 | 18.5 | 13.8 |
CQ | 24.4 | 14.0 | 18.5 | 192.1 | 158.8 |
DesAQ | 42.8 | 6.9 | 6.5 | 38.8 | 33.4 |
BidesAQ | 72.9 | 21.3 | 18.6 | 166.0 | 119.8 |
DesCQ | 44.8 | 18.9 | 18.3 | 718.5 | 645.1 |
BidesCQ | 58.3 | 55.3 | 47.2 | 1,338.6 | 1,256.3 |
AMOPYR | 29.5 | 5.3 | 4.7 | 11.5 | 9.8 |
PYR | 64.4 | 5.7 | 6.2 | 9.1 | 10.1 |
MEP | 41.0 | 12.9 | 17.8 | 43.3 | 32.6 |
TBQ | 52.7 | 9.5 | 8.2 | 13.1 | 11.6 |
4-deOH TBQ | 50.6 | 42.1 | 57.2 | 69.3 | 75.2 |
4F-TBQ | 40.5 | 60.7 | 53.7 | 68.7 | 61.3 |
NTB-AQ | 31.6 | 5.5 | 4.8 | 9.1 | 10.5 |
CQ-PYROL | 43.6 | 19.5 | 17.3 | 89.6 | 76.3 |
AQ-PYRID | 72.5 | 682.3 | 794.1 | 1,337.5 | 1,298.0 |
CQ-PYRID | 91.6 | 11,660.5 | 10,224.5 | 15,119.4 | 14,612.3 |
De-SC-AQ | 19.0 | 1,398.1 | 1,546.8 | 2,264.7 | 2,139.3 |
QN | 64.8 | 34.2 | 36.8 | 81.2 | 74.3 |
QND | 24.0 | 21.5 | 23.9 | 50.6 | 43.6 |
CIN | 22.6 | 20.6 | 26.7 | 56.2 | 40.5 |
CIND | 27.2 | 40.1 | 35.1 | 90.6 | 75.4 |
HF | 184.5 | 5.8 | 5.2 | 2.8 | 3.2 |
MQ | 46.9 | 23.4 | 18.2 | 9.4 | 11.2 |
ARM | >1,000 | 2.3 | 1.6 | 1.2 | 2.2 |
ART | >1,000 | 4.3 | 3.4 | 5.8 | 4.2 |
DHA | >1,000 | 0.1 | 0.3 | 0.2 | 0.4 |
PQ | >1,000 | NDa | ND | ND | ND |
ND, not determined.