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Assay Detail

CHEMBL4840155

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

Binding
Inhibition of human recombinant full length N-terminal GST tagged MEK7 expressed in Sf21 cells using JNK1 as substrate pre-incubated for 30 mins followed by addition of ATP and measured after 150 mins by ADP-Glo kinase assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf21
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Rational Design, Optimization, and Biological Evaluation of Novel MEK4 Inhibitors against Pancreatic Adenocarcinoma.
Kwong AJ, Pham TND, Oelschlager HE, Munshi HG, Scheidt KA.
ACS Med Chem Lett (2021) 12 : 1559 -1567
PubMed 34676038 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.86 7.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4866649 1 7.02
CHEMBL4879048 1 6.27
CHEMBL4872723 1 6.08
CHEMBL4865159 1 6.04
CHEMBL4871202 1 5.89
CHEMBL4875545 1 5.89
CHEMBL4875241 1 5.57
CHEMBL4875961 1 5.54
CHEMBL4871178 1 5.19
CHEMBL4871476 1 5.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4866649 IC50 = 96.0 nM 7.02
CHEMBL4879048 IC50 = 540.0 nM 6.27
CHEMBL4872723 IC50 = 840.0 nM 6.08
CHEMBL4865159 IC50 = 920.0 nM 6.04
CHEMBL4871202 IC50 = 1300.0 nM 5.89
CHEMBL4875545 IC50 = 1300.0 nM 5.89
CHEMBL4875241 IC50 = 2700.0 nM 5.57
CHEMBL4875961 IC50 = 2900.0 nM 5.54
CHEMBL4871178 IC50 = 6400.0 nM 5.19
CHEMBL4871476 IC50 = 8700.0 nM 5.06