- Guide to PHARMACOLOGY
Compound class: Synthetic organic
Comment: WEHI-842 was developed as a potent inhibitor of Plasmodium plasmepsin V, a promising target for antimalarial drug development .
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.✖
1. Boddey J, Cowman A, Czabotar P, Hodder T, Sleebs B. (2016)
Structure of plasmepsin v in complex with an inhibitor and uses thereof.
Patent number: WO2016197190A1. Assignee: The Walter and Eliza Hall Institute of Medical Research. Priority date: 09/06/2015. Publication date: 15/12/2016.
2. Hodder AN, Sleebs BE, Czabotar PE, Gazdik M, Xu Y, O'Neill MT, Lopaticki S, Nebl T, Triglia T, Smith BJ et al.. (2015)
Structural basis for plasmepsin V inhibition that blocks export of malaria proteins to human erythrocytes.
Nat. Struct. Mol. Biol., 22 (8): 590-6. [PMID:26214367]
3. Jennison C, Lucantoni L, O'Neill MT, McConville R, Erickson SM, Cowman AF, Sleebs BE, Avery VM, Boddey JA. (2019)
Inhibition of Plasmepsin V Activity Blocks Plasmodium falciparum Gametocytogenesis and Transmission to Mosquitoes.
Cell Rep, 29 (12): 3796-3806.e4. [PMID:31851913]