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Assay Detail

CHEMBL4197607

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

Binding
Inhibition of Escherichia coli BL21(DE3) Isoleucyl-tRNA synthetase assessed as reduction in tRNA aminoacylation preincubated for 10 mins with Escherichia coli tRNA and 14C-labeled isoleucine followed by ATP addition by liquid scintillation counting method
2
Total Activities
2
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 Intermediate

Target

Isoleucine--tRNA ligase (CHEMBL3657)
Type SINGLE PROTEIN
Organism Escherichia coli K-12

Publication

Family-wide analysis of aminoacyl-sulfamoyl-3-deazaadenosine analogues as inhibitors of aminoacyl-tRNA synthetases.
Zhang B, De Graef S, Nautiyal M, Pang L, Gadakh B, Froeyen M, Van Mellaert L, Strelkov SV, Weeks SD, Van Aerschot A.
Eur J Med Chem (2018) 148 : 384 -396
PubMed 29477072 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 7.70 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1163069 1 8.72
CHEMBL4215986 1 6.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1163069 Ki = 1.92 nM 8.72
CHEMBL4215986 Ki = 213.0 nM 6.67