Drug intelligence / Profile preview

TCMDC-135051

Development stage
Preclinical
Lead developer
GSK
Modality
Small Molecules
01

Overview

TCMDC-135051 is a highly selective and potent small molecule inhibitor of the Plasmodium falciparum cyclin-dependent-like kinase 3 (PfCLK3), an essential protein kinase involved in RNA splicing and parasite survival. It acts as a reversible inhibitor with low off-target toxicity and demonstrates activity against multiple life stages of malaria parasites—including blood stage trophozoite-to-schizont transition, gametocyte development, and liver stage parasites. The compound has shown efficacy against both chloroquine-sensitive and resistant P. falciparum strains as well as other Plasmodium species. Its mechanism offers potential for curative treatment, transmission blocking, and prophylaxis in malaria[1][2][3][4][8].

Other names
TCMDC-135051 hydrochlorideTCMDC135051 hydrochlorideTCMDC 135051 hydrochlorideTCMDC-135051 (hydrochloride)HY-126323BHY126323BHY 126323BMS-29440MS29440MS 294402705545-47-5CHEMBL4798421CHEMBL-4798421CHEMBL 4798421PubChem CID 139035060
02

Targets

PfCLK3 (Plasmodium falciparum CDC-like kinase 3)

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