- Guide to PHARMACOLOGY
Compound class: Synthetic organic
Comment: Compound 34c is from a series of benzo[b]thiophhene inhibitors with antimalarial activity.
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|
|Compound 34c inhibits N-Myristoyltransferase (NMT) an essential eukaryotic enzyme and an attractive drug target in parasitic infections such as malaria. 34c displays antimalarial activity against the asexual blood stage of P. falciparum and liver stage of P. berghei .
The compound is example 118 in  that includes assay data for 138 structures.
There is a PDB structure 2YNE of this compound in the P. vivax enzyme.
Potential Target/Mechanism Of Action: 34c is a high affinity inhibitor of both P. falciparum and P. vivax NMT.