- Guide to PHARMACOLOGY
Molecular properties generated using the CDK
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 . From this series, UCT943 was optimized for antiplasmodial activity by structural modification of the clinical candidate MMV048 and shown to have asexual blood stage, transmission-blocking, and liver stage activities [1-2]. UCT943 was being developed as a back-up compound to MMV048 but has been withdrawn due to preclinical toxicity concerns .
The compound formulation is claimed in patent WO2013121387 .
Potential Target/Mechanism Of Action: Genomic experiments provide evidence that the molecular target of UCT943 is the Plasmodium lipid kinase, phosphatidylinositol 4-kinase (PfPI4K) . This lipid kinase has been proposed to act at the Golgi to regulate essential membrane trafficking events .