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Compound class: Synthetic organic
Comment: Compound 55 is the drug-like lead discovered as a result of a SAR investigation and is a 2,8-Disubstituted-1,5-naphthyridine derivative of MMV024101 .
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. Angulo-Barturen I, Jiménez-Díaz MB, Mulet T, Rullas J, Herreros E, Ferrer S, Jiménez E, Mendoza A, Regadera J, Rosenthal PJ et al.. (2008)
A murine model of falciparum-malaria by in vivo selection of competent strains in non-myelodepleted mice engrafted with human erythrocytes.
PLoS ONE, 3 (5): e2252. [PMID:18493601]
2. Kandepedu N, Gonzàlez Cabrera D, Eedubilli S, Taylor D, Brunschwig C, Gibhard L, Njoroge M, Lawrence N, Paquet T, Eyermann CJ et al.. (2018)
Identification, Characterization, and Optimization of 2,8-Disubstituted-1,5-naphthyridines as Novel Plasmodium falciparum Phosphatidylinositol-4-kinase Inhibitors with in Vivo Efficacy in a Humanized Mouse Model of Malaria.
J Med Chem, 61 (13): 5692-5703. [PMID:29889526]