ganaplacide   Click here for help

GtoPdb Ligand ID: 9946

Synonyms: GNF156 | KAF156
Antimalarial Ligand
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 [1].

The Malaria tab on this ligand page provides additional curator comments of relevance to the Guide to MALARIA PHARMACOLOGY.
Click here for help
2D Structure
Click here for help
Click here for structure editor
Physico-chemical Properties
Click here for help
Hydrogen bond acceptors 5
Hydrogen bond donors 2
Rotatable bonds 5
Topological polar surface area 76.18
Molecular weight 411.19
XLogP 4.09
No. Lipinski's rules broken 0
Click here for help
Canonical SMILES NCC(=O)N1CCn2c(C1(C)C)nc(c2Nc1ccc(cc1)F)c1ccc(cc1)F
Isomeric SMILES NCC(=O)N1CCn2c(C1(C)C)nc(c2Nc1ccc(cc1)F)c1ccc(cc1)F
InChI InChI=1S/C22H23F2N5O/c1-22(2)21-27-19(14-3-5-15(23)6-4-14)20(26-17-9-7-16(24)8-10-17)28(21)11-12-29(22)18(30)13-25/h3-10,26H,11-13,25H2,1-2H3
Guide to Malaria Pharmacology Comments
Ganaplacide is an antimalarial drug candidate, under clinical development, with potent blood stage activity and the potential to prevent infection and block disease transmission [1]. The median parasite clearance times (PCT) for a multiple-dose regimen were 45 hours in patients with P. falciparum malaria, 24 hours in patients with P. vivax malaria and 49 hours in patients with P. falciparum malaria after treatment with a single dose [5].

Potential Target/Mechanism Of Action: As the precise mechanism of action of ganaplacide is not yet known, we do not have a molecular target for this compound. Further information about possible mechanistic insights is provided under the Clinical data tab.
Target Candidate Profiles
Profile Intended Use Target Stage Comment References
TCP-1 reduce parasite burden asexual blood stages
TCP-4 chemoprotection hepatic schizonts
TCP-5 transmission reduction gametocytes