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Assay Detail

CHEMBL3769290

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

Binding
Inhibition of Mycobacterium tuberculosis 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
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mycobacterium tuberculosis
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 32 4.98 5.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3764310 1 5.64
CHEMBL3764493 1 5.34
CHEMBL3763921 1 5.22
CHEMBL3765025 1 5.10
CHEMBL2436531 1 4.94
CHEMBL3765180 1 4.80
CHEMBL3764864 1 4.71
CHEMBL3199451 1 4.70
CHEMBL3763231 1 4.70
CHEMBL1320974 1 4.65
CHEMBL3764428 1 -
CHEMBL3763642 1 -
CHEMBL3763922 1 -
CHEMBL3763960 1 -
CHEMBL3763240 1 -
CHEMBL3763212 1 -
CHEMBL3765018 1 -
CHEMBL3764700 1 -
CHEMBL3763938 1 -
CHEMBL3765282 1 -
CHEMBL3765458 1 -
CHEMBL3765364 1 -
CHEMBL3764842 1 -
CHEMBL3763977 1 -
CHEMBL3765792 1 -
CHEMBL3190031 1 -
CHEMBL3764109 1 -
CHEMBL3763845 1 -
CHEMBL3764304 1 -
CHEMBL3764978 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3764310 IC50 = 2270.0 nM 5.64
CHEMBL3764493 IC50 = 4540.0 nM 5.34
CHEMBL3763921 IC50 = 6000.0 nM 5.22
CHEMBL3765025 IC50 = 8000.0 nM 5.10
CHEMBL2436531 IC50 = 11400.0 nM 4.94
CHEMBL3765180 IC50 = 15900.0 nM 4.80
CHEMBL3764864 IC50 = 19300.0 nM 4.71
CHEMBL3199451 IC50 = 20000.0 nM 4.70
CHEMBL3763231 IC50 = 20000.0 nM 4.70
CHEMBL1320974 IC50 = 22200.0 nM 4.65
CHEMBL3763642 IC50 > 20000.0 nM -
CHEMBL3763922 IC50 > 20000.0 nM -
CHEMBL3763960 IC50 > 20000.0 nM -
CHEMBL3763240 IC50 > 20000.0 nM -
CHEMBL3763212 IC50 > 20000.0 nM -
CHEMBL3765018 IC50 > 20000.0 nM -
CHEMBL3764700 IC50 > 20000.0 nM -
CHEMBL3763938 IC50 > 20000.0 nM -
CHEMBL3765282 IC50 > 20000.0 nM -
CHEMBL3763208 IC50 > 20000.0 nM -
CHEMBL3764492 IC50 > 20000.0 nM -
CHEMBL3764428 IC50 > 20000.0 nM -
CHEMBL3765458 IC50 > 20000.0 nM -
CHEMBL3765364 IC50 > 20000.0 nM -
CHEMBL3764842 IC50 > 20000.0 nM -
CHEMBL3763977 IC50 > 20000.0 nM -
CHEMBL3765792 IC50 > 20000.0 nM -
CHEMBL3190031 IC50 > 20000.0 nM -
CHEMBL3764109 IC50 > 20000.0 nM -
CHEMBL3763845 IC50 > 20000.0 nM -
CHEMBL3764304 IC50 > 20000.0 nM -
CHEMBL3764978 IC50 > 50000.0 nM -