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Assay Detail

CHEMBL4773310

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

Binding
Inhibition of recombinant human 10His-tagged eIF4E expressed in Escherichia coli BL21 (DE3) cells by catalytic enzyme-linked click chemistry assay
3
Total Activities
3
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

Eukaryotic translation initiation factor 4E (CHEMBL4848)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A cell-penetrant lactam-stapled peptide for targeting eIF4E protein-protein interactions.
Gallagher EE,Menon A,Chmiel AF,Deprey K,Kritzer JA,Garner AL
Eur J Med Chem (2020) 205 : 112655 -112655
PubMed 32739551 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.69 8.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4780117 1 8.19
CHEMBL4777401 1 7.66
CHEMBL4461497 1 7.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4780117 IC50 = 6.5 nM 8.19
CHEMBL4777401 IC50 = 22.0 nM 7.66
CHEMBL4461497 IC50 = 60.0 nM 7.22