Synonyms: MMV000147
Compound class:
Synthetic organic
Comment: The antifolate compound P218 is a potent and selective inhibitor of P. falciparum bifunctional dihydrofolate reductase-thymidylate synthase (PfDHFR-TS) and was designed to overcome the emergence of parasite resistance to this class of antimalarial compound [7].
The Malaria tab on this ligand page provides additional curator comments of relevance to the Guide to MALARIA PHARMACOLOGY. Ligand Activity Visualisation ChartsThese 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. ✖ |
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Guide to Malaria Pharmacology Comments |
P218 was selected from a structure-informed drug discovery process to develop inhibitors of the clinically validated target P. falciparum bifunctional dihydrofolate reductase-thymidylate synthase (PfDHFR-TS) [7]. The compound is example 8 from patent WO2009048957 [6]. Potential Target/Mechanism Of Action: P218 inhibits both wild-type and clinically relevant mutated forms of PfDHFR-TS. |
Target Candidate Profiles | ||||
Profile | Intended Use | Target Stage | Comment | References |
TCP-1 | reduce parasite burden | asexual blood stages | 7 | |
TCP-4 | chemoprotection | hepatic schizonts | 4 | |
TCP-5 | transmission reduction | gametocytes | 3 |