- Guide to PHARMACOLOGY
Compound class: Synthetic organic
Comment: MMV048 is the optimised lead compound for the 2-aminopyridines, a class of small molecules with promising antimalarial activity .
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|
|Phenotypic whole cell high-throughput screening has identified the 2-aminopyridines as a class of small molecules with promising antimalarial activity . MMV048, the optimised lead compound from this class, has activity against all lifecycle stages of the Plasmodium parasite, with the exception of late stage hypnozoites . UCT943 is another compound from this screen, that was being developed as a back-up for MMV048, but was withdrawn due to preclinical toxicity concerns.
MMV048 has progressed to clinical evaluation and was awarded MMV Project of the Year award (2012).
Potential Target/Mechanism Of Action: Genomic and chemoproteomic experiments provide significant evidence that the molecular target of MMV048 is the Plasmodium lipid kinase, phosphatidylinositol 4-kinase (PfPI4K) .
|Target Candidate Profiles|
|Profile||Intended Use||Target Stage||Comment||References|
|TCP-1||reduce parasite burden||asexual blood stages|