- Guide to PHARMACOLOGY
Synonyms: (+)-SJ000557733 | (+)-SJ557733
Compound class: Synthetic organic
Comment: (+)-SJ733 is the optimized lead for the dihydroisoquinolones (DHIQ), a novel chemotype with antimalarial activity .
The (+)-enantiomer, shown here, has a significantly higher antimalarial potency .
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|
|(+)-SJ733 is equally potent against all developmental forms of the asexual blood stage parasite and also has potential for transmission blockade . The compound was under clinical development as the fast clearance component of a single-exposure radical cure and prophylaxis (SERCaP) antimalarial drug but is no longer in the Medicines for Malaria (MMV) portfolio after it was found to have lower concentrations in humans than expected . A back-up series, that has been informed by (+)-SJ733, is being developed by the University of Kentucky.
Potential Target/Mechanism of Action: Evidence from genetic experiments indicates that Plasmodium non-SERCA-type Ca2+-transporting P-ATPase (PfATP4) may be the relevant molecular target . Further information about possible mechanistic insights is provided under the Clinical data tab.
|Target Candidate Profiles|
|Profile||Intended Use||Target Stage||Comment||References|
|TCP-1||reduce parasite burden||asexual blood stages||2|