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Assay Detail

CHEMBL4394780

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

Binding
Inhibition of purified Escherichia coli BL21 (DE3) leuRS incubated for 10 mins in presence of 14C-labeled leucine by radiolabel transfer assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Escherichia coli BL21(DE3)
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Leucine--tRNA ligase (CHEMBL4295566)
Type SINGLE PROTEIN
Organism Escherichia coli (strain K12)

Publication

Comparative analysis of pyrimidine substituted aminoacyl-sulfamoyl nucleosides as potential inhibitors targeting class I aminoacyl-tRNA synthetases.
Nautiyal M, De Graef S, Pang L, Gadakh B, Strelkov SV, Weeks SD, Van Aerschot A.
Eur J Med Chem (2019) 173 : 154 -166
PubMed 30995568 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 7.74 8.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4465674 1 8.01
CHEMBL4467328 1 7.68
CHEMBL4451258 1 7.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4465674 Ki = 9.8 nM 8.01
CHEMBL4467328 Ki = 20.8 nM 7.68
CHEMBL4451258 Ki = 29.5 nM 7.53