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Assay Detail

CHEMBL5357185

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Binding
Inhibition of eIF4E phosphorylation in human HeLa cells
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HeLa
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Medicinal chemistry approaches to target the MNK-eIF4E axis in cancer.
Fernandez A, Monsen PJ, Platanias LC, Schiltz GE.
RSC Med Chem (2023) 14 : 1060 -1087
PubMed 37360400 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.58 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4587832 1 6.70
CHEMBL3806189 1 6.55
CHEMBL4211649 TINODASERTIB 2.0 1 6.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4587832 IC50 = 200.0 nM 6.70
CHEMBL3806189 IC50 = 280.0 nM 6.55
CHEMBL4211649 TINODASERTIB IC50 = 321.0 nM 6.49