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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.✖
1. Lynch 3rd JJ, Rossignol E, Moehrle JJ, Van Vleet TR, Marsh KC, Parman T, Mirsalis J, Ottinger SE, Segreti JA, Rao M et al.. (2019)
Increased stress associated with head-out plethysmography testing can exacerbate respiratory effects and lead to mortality in rats.
J Pharmacol Toxicol Methods, 99: 106580. [PMID:31085318]
2. Phillips M, Charman SA, Rathod PK, Matthews D, Waterson D. (2016)
New substituted triazolopyrimidines as anti-malarial agents.
Patent number: WO2016151521A1. Assignee: Board of Regents of the University Of Texas System, University of Washington, Medicines for Malaria Venture. Priority date: 26/03/2015. Publication date: 29/09/2016.
3. Phillips MA, White KL, Kokkonda S, Deng X, White J, El Mazouni F, Marsh K, Tomchick DR, Manjalanagara K, Rudra KR et al.. (2016)
A Triazolopyrimidine-Based Dihydroorotate Dehydrogenase Inhibitor with Improved Drug-like Properties for Treatment and Prevention of Malaria.
ACS Infect Dis, 2 (12): 945-957. [PMID:27641613]