GSK-656 Three fluoroacetate

Description	GSK656, also known as GSK3036656, is a potent Mtb LeuRS inhibitor. GSK656 shows potent inhibition of Mtb LeuRS (IC50 = 0.20 μM) and in vitro antitubercular activity (Mtb H37Rv MIC = 0.08 μM). Additionally, it is highly selective for the Mtb LeuRS enzyme with IC50 of >300 μM and 132 μM for human mitochondrial LeuRS and human cytoplasmic LeuRS, respectively. In addition, it exhibits remarkable PK profiles and efficacy against Mtb in mouse TB infection models with superior tolerability over initial leads. GSK656 has been progressed to clinical development for the treatment of tuberculosis.
Pathways	Microbiology/Virology
Targets	Antibiotic

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