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Assay Detail

CHEMBL4030416

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

Binding
Inhibition of human ERG expressed in HEK293 cells by patch clamp method
6
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Discovery of N-{4-[5-(4-Fluorophenyl)-3-methyl-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-acetamide (CBS-3595), a Dual p38α MAPK/PDE-4 Inhibitor with Activity against TNFα-Related Diseases.
Albrecht W, Unger A, Bauer SM, Laufer SA.
J Med Chem (2017) 60 : 5290 -5305
PubMed 28613871 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 4.73 5.56
Inhibition 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL321494 2 5.56
CHEMBL432798 2 4.54
CHEMBL4075428 1 4.08
CHEMBL1773422 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL321494 IC50 = 2760.0 nM 5.56
CHEMBL432798 IC50 = 28600.0 nM 4.54
CHEMBL4075428 IC50 = 83000.0 nM 4.08
CHEMBL1773422 IC50 = 213000.0 nM -
CHEMBL432798 Inhibition - % -
CHEMBL321494 Inhibition - % -