- Guide to PHARMACOLOGY
Synonyms: (+)-SJ000557733 | (+)-SJ557733
Compound class: Synthetic organic
Comment: (+)-SJ733 is the optimized lead for the dihydroisoquinolones (DHIQ), a novel chemotype with antimalarial activity .
The (+)-enantiomer, shown here, has a significantly higher antimalarial potency .
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. Gaur AH, McCarthy JS, Panetta JC, Dallas RH, Woodford J, Tang L, Smith AM, Stewart TB, Branum KC, Freeman 3rd BB et al.. (2020)
Safety, tolerability, pharmacokinetics, and antimalarial efficacy of a novel Plasmodium falciparum ATP4 inhibitor SJ733: a first-in-human and induced blood-stage malaria phase 1a/b trial.
Lancet Infect Dis, 20 (8): 964-975. [PMID:32275867]
2. Jiménez-Díaz MB, Ebert D, Salinas Y, Pradhan A, Lehane AM, Myrand-Lapierre ME, O'Loughlin KG, Shackleford DM, Justino de Almeida M, Carrillo AK et al.. (2014)
(+)-SJ733, a clinical candidate for malaria that acts through ATP4 to induce rapid host-mediated clearance of Plasmodium.
Proc Natl Acad Sci USA, 111 (50): E5455-62. [PMID:25453091]
MMV Annual Report 2018, Chapter 7, R&D platforms and discovery.
Accessed on 27/01/2020. Modified on 27/01/2020. https://www.mmv.org/sites/default/files/uploads/docs/publications/2018/MMV_AR2018_Chapter7.pdf