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Compound class: Synthetic organic
Comment: Compound 3 is the lead for a novel series of antimalarial compounds based on a benzimidazole core .
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|
|A phenotypic high-throughput screen of the Novartis chemical library, followed by a hit to lead effort, identified compound 3 as an early lead with promising antimalarial activity . SAR analysis was carried out but further optimization will be necessary to improve pharmacokinetic properties and address potential cardiotoxicity issues.
Potential Target/Mechanism Of Action: As the precise mechanism of action of compound 3 is not yet known, we do not have a molecular target for this compound.