LeuRS-IN-1 is a highly potent and orally active inhibitor of the leucyl-tRNA synthetase enzyme derived from Mycobacterium tuberculosis (M.tb LeuRS). It exhibits significant inhibitory activity against M.tb LeuRS with IC 50 and Kd values of 0.06 uM and 0.075 uM, respectively. Additionally, LeuRS-IN-1 effectively inhibits human cytoplasmic LeuRS with an IC 50 value of 38.8 uM and suppresses protein synthesis in HepG2 cells with an EC 50 value of 19.6 uM.