- Guide to PHARMACOLOGY
Synonyms: GNF156 | KAF156
Compound class: Synthetic organic
Comment: Ganaplacide is the optimised lead for the imidazolopiperazines (IZPs), a novel class of compounds identified from a phenotypic screen as having 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.✖
1. Kuhen KL, Chatterjee AK, Rottmann M, Gagaring K, Borboa R, Buenviaje J, Chen Z, Francek C, Wu T, Nagle A et al.. (2014)
KAF156 is an antimalarial clinical candidate with potential for use in prophylaxis, treatment, and prevention of disease transmission.
Antimicrob Agents Chemother, 58 (9): 5060-7. [PMID:24913172]
2. LaMonte G, Lim MY, Wree M, Reimer C, Nachon M, Corey V, Gedeck P, Plouffe D, Du A, Figueroa N et al.. (2016)
Mutations in the Plasmodium falciparum Cyclic Amine Resistance Locus (PfCARL) Confer Multidrug Resistance.
MBio, 7 (4). [PMID:27381290]
3. LaMonte GM, Rocamora F, Marapana DS, Gnädig NF, Ottilie S, Luth MR, Worgall TS, Goldgof GM, Mohunlal R, Santha Kumar TR et al.. (2020)
Pan-active imidazolopiperazine antimalarials target the Plasmodium falciparum intracellular secretory pathway.
Nat Commun, 11 (1): 1780. [PMID:32286267]
4. Lim MY, LaMonte G, Lee MCS, Reimer C, Tan BH, Corey V, Tjahjadi BF, Chua A, Nachon M, Wintjens R et al.. (2016)
UDP-galactose and acetyl-CoA transporters as Plasmodium multidrug resistance genes.
Nat Microbiol, 1: 16166. [PMID:27642791]
5. White NJ, Duong TT, Uthaisin C, Nosten F, Phyo AP, Hanboonkunupakarn B, Pukrittayakamee S, Jittamala P, Chuthasmit K, Cheung MS et al.. (2016)
Antimalarial Activity of KAF156 in Falciparum and Vivax Malaria.
N Engl J Med, 375 (12): 1152-60. [PMID:27653565]