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Assay Detail

CHEMBL963131

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

Binding
Inhibition of MEK-stimulated ERK phosphorylation in PDGF-stimulated mouse C26 cells treated as single oral dose before PDGF challenge by whole cell assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type C26
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901.
Barrett SD, Bridges AJ, Dudley DT, Saltiel AR, Fergus JH, Flamme CM, Delaney AM, Kaufman M, LePage S, Leopold WR, Przybranowski SA, Sebolt-Leopold J, Van Becelaere K, Doherty AM, Kennedy RM, Marston D, Howard WA, Smith Y, Warmus JS, Tecle H.
Bioorg Med Chem Lett (2008) 18 : 6501 -6504
PubMed 18952427 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 8.96 10.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL244488 1 10.15
CHEMBL507361 MIRDAMETINIB 2.0 1 9.48
CHEMBL450775 1 9.32
CHEMBL507836 1 9.09
CHEMBL508526 1 9.00
CHEMBL105442 CI-1040 2.0 1 8.46
CHEMBL452600 1 8.46
CHEMBL447345 1 7.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL244488 IC50 = 0.07 nM 10.15
CHEMBL507361 MIRDAMETINIB IC50 = 0.33 nM 9.48
CHEMBL450775 IC50 = 0.48 nM 9.32
CHEMBL507836 IC50 = 0.82 nM 9.09
CHEMBL508526 IC50 = 1.0 nM 9.00
CHEMBL105442 CI-1040 IC50 = 3.5 nM 8.46
CHEMBL452600 IC50 = 3.5 nM 8.46
CHEMBL447345 IC50 = 19.0 nM 7.72