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Assay Detail

CHEMBL4480181

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

Binding
Inhibition of recombinant full length human N-terminal GST-tagged C-terminal His6-tagged MEK1 expressed in Escherichia coli using myelin basic protein as substrate in presence of activated BRAF and ERK2 by ELISA
13
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Discovery of N-(benzyloxy)-1,3-diphenyl-1H-pyrazole-4-carboxamide derivatives as potential antiproliferative agents by inhibiting MEK.
Lv XH, Ren ZL, Zhou BG, Li QS, Chu MJ, Liu DH, Mo K, Zhang LS, Yao XK, Cao HQ.
Bioorg Med Chem (2016) 24 : 4652 -4659
PubMed 27515719 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Inhibition 11 - -
IC50 2 7.05 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL34704 1 7.05
CHEMBL4575118 1 7.04
CHEMBL4545932 1 -
CHEMBL4586091 1 -
CHEMBL4528906 1 -
CHEMBL4556810 1 -
CHEMBL4560047 1 -
CHEMBL4580386 1 -
CHEMBL4577383 1 -
CHEMBL4575979 1 -
CHEMBL4580566 1 -
CHEMBL4568694 1 -
CHEMBL4575359 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL34704 IC50 = 89.0 nM 7.05
CHEMBL4575118 IC50 = 91.0 nM 7.04
CHEMBL4545932 Inhibition - % -
CHEMBL4586091 Inhibition - % -
CHEMBL4528906 Inhibition - % -
CHEMBL4556810 Inhibition - % -
CHEMBL4560047 Inhibition - % -
CHEMBL4580386 Inhibition - % -
CHEMBL4577383 Inhibition - % -
CHEMBL4575979 Inhibition - % -
CHEMBL4580566 Inhibition - % -
CHEMBL4568694 Inhibition - % -
CHEMBL4575359 Inhibition - % -