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Assay Detail

CHEMBL3769291

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of human leucyl-tRNA synthetase assessed as reduction of [14C]-L-leucine ligation to tRNA incubated for 5 mins by scintillation counting method in presence of ATP
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Leucine--tRNA ligase, cytoplasmic (CHEMBL3258)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of potent anti-tuberculosis agents targeting leucyl-tRNA synthetase.
Gudzera OI, Golub AG, Bdzhola VG, Volynets GP, Lukashov SS, Kovalenko OP, Kriklivyi IA, Yaremchuk AD, Starosyla SA, Yarmoluk SM, Tukalo MA.
Bioorg Med Chem (2016) 24 : 1023 -1031
PubMed 26822568 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 4.54 4.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3764310 1 4.73
CHEMBL3764493 1 4.56
CHEMBL3765025 1 4.34
CHEMBL2436531 1 -
CHEMBL3763921 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3764310 IC50 = 18700.0 nM 4.73
CHEMBL3764493 IC50 = 27600.0 nM 4.56
CHEMBL3765025 IC50 = 45800.0 nM 4.34
CHEMBL2436531 IC50 = 116300.0 nM -
CHEMBL3763921 IC50 = 115700.0 nM -