- 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.✖
|The interaction table below provides data from an evaluation of asexual blood stage activity using a panel of culture-adapted P. falciparum strains, with no evidence of reduced potency against drug resistant strains. No significant change was observed in the potency (ED50) of (+)-SJ733 against different developmental forms of the asexual blood stage parasite. In addition, the compound demonstrates excellent efficacy in the SCID mouse model of P. falciparum malaria (ED90 of 1.9 mg/kg) and potent and efficacious transmission-blocking activity in a P. berghei mouse model (ED50 of 5 mg/kg) .|
|Whole organism assay data|
|Key to terms and symbols||Click on species/strain names for details||Click column headers to sort|