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Assay Detail

CHEMBL4144832

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Binding
Inhibition of human LeuRS assessed as reduction in ATP consumption
10
Total Activities
10
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

N-Leucinyl Benzenesulfonamides as Structurally Simplified Leucyl-tRNA Synthetase Inhibitors.
Charlton MH, Aleksis R, Saint-Leger A, Gupta A, Loza E, Ribas de Pouplana L, Kaula I, Gustina D, Madre M, Lola D, Jaudzems K, Edmund G, Randall CP, Kime L, O'Neill AJ, Goessens W, Jirgensons A, Finn PW.
ACS Med Chem Lett (2018) 9 : 84 -88
PubMed 29456792 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.18 7.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4174152 1 7.48
CHEMBL4163450 1 6.80
CHEMBL4171458 1 6.66
CHEMBL4172643 1 6.31
CHEMBL4159778 1 6.07
CHEMBL4160841 1 5.96
CHEMBL4163140 1 5.92
CHEMBL4167692 1 5.70
CHEMBL4171058 1 5.47
CHEMBL4161986 1 5.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4174152 IC50 = 33.0 nM 7.48
CHEMBL4163450 IC50 = 160.0 nM 6.80
CHEMBL4171458 IC50 = 220.0 nM 6.66
CHEMBL4172643 IC50 = 490.0 nM 6.31
CHEMBL4159778 IC50 = 850.0 nM 6.07
CHEMBL4160841 IC50 = 1100.0 nM 5.96
CHEMBL4163140 IC50 = 1200.0 nM 5.92
CHEMBL4167692 IC50 = 2000.0 nM 5.70
CHEMBL4171058 IC50 = 3400.0 nM 5.47
CHEMBL4161986 IC50 = 3900.0 nM 5.41