- Guide to PHARMACOLOGY
Compound class: Synthetic organic
Comment: TCMDC-135051 is a probe molecule identified as a selective inhibitor of P. falciparum cyclin-dependent-like kinase CLK3 (PfCLK3) and is being developed in a hit-to-lead programme [1-2].
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. Alam MM, Sanchez-Azqueta A, Janha O, Flannery EL, Mahindra A, Mapesa K, Char AB, Sriranganadane D, Brancucci NMB, Antonova-Koch Y et al.. (2019)
Validation of the protein kinase PfCLK3 as a multistage cross-species malarial drug target.
Science, 365 (6456). [PMID:31467193]
2. Mahindra A, Janha O, Mapesa K, Sanchez-Azqueta A, Alam MM, Amambua-Ngwa A, Nwakanma DC, Tobin AB, Jamieson AG. (2020)
Development of Potent PfCLK3 Inhibitors Based on TCMDC-135051 as a New Class of Antimalarials.
J Med Chem, 63 (17): 9300-9315. [PMID:32787140]