Synonyms: DDD107498 | DDD498 | MMV121
Compound class:
Synthetic organic
Comment: M5717 (formerly DDD498) is a quinoline-4-carboxamide derivative that is the optimised lead developed from a phenotypic screen for novel antimalarial drugs and has advanced to clinical evaluation. The compound was awarded MMV Project of the Year (2014).
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 |
M5717 has comparable activity against multiple stages of the malaria parasite lifecycle and is indicated for use as a combination therapy for acute uncomplicated malaria, with potential to be a single-exposure radical cure (SERC) treatment [1]. Preclinical asessment of M5717 in combination with pyronaridine, reports rapid clearance of asexual blood stage parasites with exoerythrocytic activity and shows promise as an effective, long-lasting antimalarial therapy [4]. The compound is example 1A from patent WO2013153357 [2]. Potential Target/Mechanism Of Action: Evidence from genetic experiments indicates that P. falciparum elongation factor 2 (PfeEF2) may be the molecular target [1]. |
Target Candidate Profiles | ||||
Profile | Intended Use | Target Stage | Comment | References |
TCP-1 | reduce parasite burden | asexual blood stages | 1 | |
TCP-4 | chemoprotection | hepatic schizonts | 1 | |
TCP-5 | transmission reduction | gametocytes | 1 |