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. 2014 Apr 14;13:143. doi: 10.1186/1475-2875-13-143

Table 2.

Most active compounds tested by St Jude’s Children’s Research Hospital

Compound Class (therapeutic area) EC 50 3D7 (μM) EC 50 K1 (μM)
Methylene blue
Nitric oxide/guanylate cyclase inhibitor (various)
<0.0003 (NA)
<0.0003 (NA)
Dactinomycin
Nucleoside reverse transcriptase inhibitor (oncology)
0.0009 (0, 0.13)
0.001 (0.0003, 0.006)
Sulfamerazine
Dihydrofolate synthetase inhibitor (anti-infective)
0.01 (0.01, 0.01)
0.01 (0.01, 0.01)
Methotrexate
Dihydrofolate reductase inhibitor (oncology)
0.01 (0.009, 0.01)
0.02 (0.01, 0.02)
Bortezomib
Proteasome inhibitor (oncology)
0.02 (0.01, 0.04)
0.08 (0.07, 0.09)
Thiothixene
Post-synaptic receptor agonista (anti-psychotic)
0.04 (0, 233.71)
0.02 (0.01, 0.05)
Dequalinium
Anti-septic
0.06 (0.002, 1.53)
0.06 (0.03, 0.12)
Doxorubicin
Topoisomerase II inhibitor, DNA intercalating agent (oncology)
0.21 (0.16, 0.27)
0.20 (0.14, 0.30)
Pentamidine
Inhibition of DNA, RNA, phospholipid and protein synthesisb (anti-infective)
0.22 (0.18, 0.27)
0.05 (0.04, 0.06)
Bosutinib
Tyrosine kinase inhibitor (oncology)
0.22 (0.016, 3.11)
0.65 (0.36, 1.19)
Aminopterin
Dihydrofolate reductase inhibitor (oncology)
0.32 (0.30, 0.33)
1.25 (1.11, 1.41)
Midostaurin
Multi-kinase inhibitor (oncology)
0.35 (0.17, 0.71)
0.15 (0.13, 0.17)
Lestaurtinib
FMS-like tyrosine kinase 3 inhibitor (oncology)
0.49 (0.28, 0.84)
0.34 (0.29, 0.41)
Demecarium
Cholinesterase inhibitor (ophthalmology)
0.51 (0.45, 0.57)
0.30 (0.26, 0.36)
Cyproterone
Steroidal anti-androgen (oncology)
0.56 (0.54, 0.58)
0.89 (0, 1501.50)
Lapatinib
Tyrosine kinase inhibitor (oncology)
0.56 (0.39, 0.80)
>7.37 (NA)
Pimozide
Dopamine receptor blocker (anti-psychotic)
0.70 (0.44, 1.11)
>12.76 (NA)
Pravastatin
HMG-CoA reductase inhibitor (anti-cholesterol)
0.75 (0.51, 1.09)
0.12 (0.10, 0.15)
Dipyrone
NSAIDb (pain)
0.84 (0.71, 0.98)
0.50 (0.21, 1.16)
Mitomycin
Inhibition of DNA synthesis (oncology)
0.97 (0.81, 1.17)
0.51 (0.45, 0.57)
Propafenone
Sodium channel modulator (cardiology)
1.22 (0.58, 2.55)
0.33 (0.31, 0.34)
Cyclosporin A
Immune suppressant (oncology)
1.23 (1.06, 1.44)
0.87 (0.62, 1.23)
Vorinostat
Histone deacetylase inhibitor (oncology)
1.47 (1.17, 1.84)
0.84 (0.76, 0.93)
Sorafenib Multi-kinase inhibitor (oncology) 2.71 (2.4, 3.1) 0.88 (0.7, 1.1)

NA, not available. EC50 values are shown as mean (95% CI). Compounds with an EC50 < 1 μM against either P. falciparum strain are shown. Relevant results from all compound sets tested at SJCRH are shown. Where compounds were duplicated across the consolidated test set, the results with the most potent in vitro activity are shown. Known anti-malarial drugs have been excluded.

aAgonist of dopaminergic-receptors, serotonergic-receptors, histaminergic-receptors, alpha1/alpha2-receptors, and muscarinic (cholinergic) M1/M2-receptors.

bMechanism unknown.

SYBR®I fluorescence assay for activity against P. falciparum strains 3D7 and K1.

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