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Compound class: Synthetic organic
Comment: Compound 1u is the hit compound identified from a SAR study of peptoid-based histone deacetylase (HDAC) inhibitors for use as antimalarial agents .
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. Diedrich D, Stenzel K, Hesping E, Antonova-Koch Y, Gebru T, Duffy S, Fisher G, Schöler A, Meister S, Kurz T et al.. (2018)
One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.
Eur J Med Chem, 158: 801-813. [PMID:30245402]
2. Koehne E, Kreidenweiss A, Zoleko Manego R, McCall M, Mombo-Ngoma G, Mackwitz MKW, Hansen FK, Held J. (2019)
Histone deacetylase inhibitors with high in vitro activities against Plasmodium falciparum isolates collected from Gabonese children and adults.
Sci Rep, 9 (1): 17336. [PMID:31758015]