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Compound class: Synthetic organic
Comment: DSM421 was being developed as a backup compound to DSM265, the clinical lead for the triazolopyrimidine structural class of antimalarial compounds, but it has not been progressed due to unpredicted off-target toxicity [1,3].
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|
|DSM421 retains the efficacy and pharmacokinetic properties of DSM265 that predict utility as single dose treatment or once-weekly chemopreventative. As a further advantage over DSM265, DSM421's physical and chemical properties indicate that it will be easier to formulate . The structure is one of those claimed in patent WO2016151521 .
Potential Target/Mechanism Of Action: DSM421 is a selective inhibitor of malarial DHODH in vitro.
|Target Candidate Profiles|
|Profile||Intended Use||Target Stage||Comment||References|
|TCP-1||reduce parasite burden||asexual blood stages|