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Assay Detail

CHEMBL5164562

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

Binding
Inhibition of human recombinant full length GST-tagged MNK1 expressed in baculovirus expression system using S6 peptide as substrate in presence of [gamma-33P]-ATP incubated for 60 mins by radiometric scintillation counting method
4
Total Activities
4
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

Publication

Overcoming Paradoxical Kinase Priming by a Novel MNK1 Inhibitor.
Bou-Petit E, Hümmer S, Alarcon H, Slobodnyuk K, Cano-Galietero M, Fuentes P, Guijarro PJ, Muñoz MJ, Suarez-Cabrera L, Santamaria A, Estrada-Tejedor R, Borrell JI, Ramón Y Cajal S.
J Med Chem (2022) 65 : 6070 -6087
PubMed 35417652 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.81 6.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5189796 1 6.16
CHEMBL5187079 1 5.89
CHEMBL1240885 1 5.82
CHEMBL5180935 1 5.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5189796 IC50 = 690.0 nM 6.16
CHEMBL5187079 IC50 = 1300.0 nM 5.89
CHEMBL1240885 IC50 = 1520.0 nM 5.82
CHEMBL5180935 IC50 = 4200.0 nM 5.38