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Assay Detail

CHEMBL4616486

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

Binding
Inhibition of eIF4A1 in human MDA-MB-231 cells assessed as inhibition of cellular-translation incubated for 4 hrs by specific tandem sequence motif repeat AGAGAG in 5'- UTR containing luciferase reporter gene assay
5
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MDA-MB-231
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Eukaryotic initiation factor 4A-I (CHEMBL2052028)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design of Development Candidate eFT226, a First in Class Inhibitor of Eukaryotic Initiation Factor 4A RNA Helicase.
Ernst JT, Thompson PA, Nilewski C, Sprengeler PA, Sperry S, Packard G, Michels T, Xiang A, Tran C, Wegerski CJ, Eam B, Young NP, Fish S, Chen J, Howard H, Staunton J, Molter J, Clarine J, Nevarez A, Chiang GG, Appleman JR, Webster KR, Reich SH.
J Med Chem (2020) 63 : 5879 -5955
PubMed 32470302 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.54 8.82
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4303782 ZOTATIFIN 2.0 2 8.82
CHEMBL438139 ROCAGLAMIDE 1 8.33
CHEMBL123292 CYCLOHEXIMIDE 2.0 1 6.65
CHEMBL1098427 HIPPURISTANOL 1 6.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4303782 ZOTATIFIN IC50 = 1.5 nM 8.82
CHEMBL438139 ROCAGLAMIDE IC50 = 4.7 nM 8.33
CHEMBL123292 CYCLOHEXIMIDE IC50 = 226.0 nM 6.65
CHEMBL1098427 HIPPURISTANOL IC50 = 426.0 nM 6.37
CHEMBL4303782 ZOTATIFIN Inhibition - % -