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Assay Detail

CHEMBL698878

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

Binding
Compound tested for the inhibition of human isoleucyl-tRNA synthetase
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Isoleucine--tRNA ligase, cytoplasmic (CHEMBL3235)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationships of a series of novel thiazoles as inhibitors of aminoacyl-tRNA synthetases.
Yu XY, Hill JM, Yu G, Wang W, Kluge AF, Wendler P, Gallant P.
Bioorg Med Chem Lett (1999) 9 : 375 -380
PubMed 10091687 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.66 7.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL125075 1 7.47
CHEMBL538163 1 7.00
CHEMBL123796 1 6.92
CHEMBL333001 1 6.70
CHEMBL125820 1 6.52
CHEMBL264002 1 6.48
CHEMBL125221 1 6.43
CHEMBL340359 1 6.40
CHEMBL126515 1 5.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL125075 IC50 = 34.0 nM 7.47
CHEMBL538163 IC50 = 100.0 nM 7.00
CHEMBL123796 IC50 = 120.0 nM 6.92
CHEMBL333001 IC50 = 200.0 nM 6.70
CHEMBL125820 IC50 = 300.0 nM 6.52
CHEMBL264002 IC50 = 330.0 nM 6.48
CHEMBL125221 IC50 = 370.0 nM 6.43
CHEMBL340359 IC50 = 400.0 nM 6.40
CHEMBL126515 IC50 = 1020.0 nM 5.99