Table 2 Most active compounds tested by St Jude’s Children’s Research Hospital
From: Repositioning: the fast track to new anti-malarial medicines?
Compound | Class (therapeutic area) | EC503D7 (μM) | EC50K1 (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) |