Synonyms: ACT451840 | Actelion-451840
Compound class:
Synthetic organic
Comment: ACT-451840 is an investigational antimalarial drug, selected from a new class of compounds identified from a phenotypic screen [2,4]. Chemically it is a piperazine-containing compound.
The Malaria tab on this ligand page provides additional curator comments of relevance to the Guide to MALARIA PHARMACOLOGY. |
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Bioactivity Comments |
The interaction table below provides data from whole cell assays and gives the antiparasite activity of ACT-451840 against a number of Plasmodium lifecycle stages. The results include an evaluation of asexual blood stage activity using a panel of culture-adapted P. falciparum strains, with ACT-451840 demonstrating no evidence of reduced potency against drug resistant strains. Results from assays measuring the effect of ACT-451840 on the functional viability of mature gametocytes and oocysts of P. falciparum indicate that the transmission-blocking effect is dependent on the gametocytocidal activity of the compound. |
Whole organism assay data | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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