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Assay Detail

CHEMBL4350375

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

Binding
Inhibition of recombinant GST-tagged MNK1 (unknown origin) using eIF4E-derived peptide as substrate in presence of ATP at km concentration by ADP-Glo assay
6
Total Activities
6
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

Synthesis and evaluation of 2'H-spiro[cyclohexane-1,3'-imidazo[1,5-a]pyridine]-1',5'-dione derivatives as Mnk inhibitors.
Abdelaziz AM, Basnet SKC, Islam S, Li M, Tadesse S, Albrecht H, Gerber C, Yu M, Wang S.
Bioorg Med Chem Lett (2019) 29 : 2650 -2654
PubMed 31362920 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.46 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4439094 1 8.70
CHEMBL4073443 TOMIVOSERTIB 2.0 1 8.30
CHEMBL4449736 1 7.50
CHEMBL4535537 1 7.12
CHEMBL4454334 1 6.66
CHEMBL4466664 1 6.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4439094 Ki = 2.0 nM 8.70
CHEMBL4073443 TOMIVOSERTIB Ki = 5.0 nM 8.30
CHEMBL4449736 Ki = 32.0 nM 7.50
CHEMBL4535537 Ki = 76.0 nM 7.12
CHEMBL4454334 Ki = 221.0 nM 6.66
CHEMBL4466664 Ki = 341.0 nM 6.47