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Compound class: Synthetic organic
Comment: ELQ-300 is a late lead candidate from a novel class of 4(1H)-quinolone-based compounds with potent antimalarial activity . The ELQs (endochin-like quinolones) are structural derivatives of endochin (PubChem CID 100474), which has potent antiplasmodial activity, but is highly metabolically unstable in mammals [1,6].
The Malaria tab on this ligand page provides additional curator comments of relevance to the Guide to MALARIA PHARMACOLOGY.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
|Guide to Malaria Pharmacology Comments|
|Preclinical testing has found ELQ-300 to be active against P. falciparum and P. vivax and with the potential for both the prevention and treatment of malaria . However, further clinical development of ELQ-300 has been impeded by its physicochemical properties. Poor aqueous solubility and high crystallinity limit oral absorption of the higher doses required for a single-dose cure and to establish an acceptable therapeutic window. To address this challenge, a prodrug approach has been used to identify ELQ-300 prodrugs with improved physicochemical properties and the potential for clinical formulation [2-3].
Potential Target/Mechanism Of Action: ELQ-300 is an inhibitor of the Plasmodium mitochondrial cytochrome bc1 complex. It targets the highly divergent Qi-site and has a low resistance propensity compared to atovaquone, which targets the widely conserved Qo-site .