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Compound class: Synthetic organic
Comment: Analog 18 is the lead from a class of antimalarial compounds based on the naturally derived tripeptide molecule carmaphycin B . Functionally these compounds inhibit the Plasmodium proteasome.
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|
|Carmaphycin B has potent activity against multiple stages of the malaria parasite lifecycle (liver, asexual and sexual blood stages) but is toxic to mammalian cells in vitro . Using the carmaphycin B scaffold, the same study describes the design of analog 18 that retains blood stage antimalarial activity and with a 123-fold increase in selectivity.
Potential Target/Mechanism Of Action: analog 18 is an inhibitor of the β5 subunit of the of P. falciparum proteasome .