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Assay Detail

CHEMBL5138014

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

Binding
Inhibition of EGFR in human A-431 cell membrane vesicles using phospholipase C-gamma-1 as substrate incubated for 10 mins by scintillation counter method
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type A-431
Subcellular Membrane vesicle
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Epidermal growth factor receptor (CHEMBL203)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

How the structural properties of the indole derivatives are important in kinase targeted drug design?: A case study on tyrosine kinase inhibitors.
Mondal D, Amin SA, Moinul M, Das K, Jha T, Gayen S.
Bioorg Med Chem (2022) 53 : 116534 -116534
PubMed 34864496 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.48 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL153206 1 8.92
CHEMBL423224 1 7.51
CHEMBL5198809 1 7.14
CHEMBL5173075 1 6.34
CHEMBL5195327 1 -
CHEMBL5179320 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL153206 IC50 = 1.2 nM 8.92
CHEMBL423224 IC50 = 31.0 nM 7.51
CHEMBL5198809 IC50 = 72.0 nM 7.14
CHEMBL5173075 IC50 = 460.0 nM 6.34
CHEMBL5195327 IC50 > 10000.0 nM -
CHEMBL5179320 IC50 > 10000.0 nM -