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Assay Detail

CHEMBL4616478

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

Binding
Binding affinity to full length recombinant eIF4A1 (unknown origin) assessed as induction ternary complex formation in presence of AGAGAG by measuring Kd for AGAGAG + ATP complex formation SPR assay (Rvb = 8 +/- 0.9 microM)
2
Total Activities
2
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 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
Kd 2 7.25 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4303782 ZOTATIFIN 2.0 1 7.68
CHEMBL438139 ROCAGLAMIDE 1 6.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4303782 ZOTATIFIN Kd = 21.0 nM 7.68
CHEMBL438139 ROCAGLAMIDE Kd = 156.0 nM 6.81