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Assay Detail

CHEMBL1072161

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

Binding
Inhibition of EGFR autophosphorylation in human A431 cells after 8 hrs by Western blot
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel irreversible epidermal growth factor receptor inhibitors by chemical modulation of the cysteine-trap portion.
Carmi C, Cavazzoni A, Vezzosi S, Bordi F, Vacondio F, Silva C, Rivara S, Lodola A, Alfieri RR, La Monica S, Galetti M, Ardizzoni A, Petronini PG, Mor M.
J Med Chem (2010) 53 : 2038 -2050
PubMed 20151670 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.91 7.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL598007 1 7.36
CHEMBL2021576 1 7.17
CHEMBL597402 1 7.11
CHEMBL2021575 1 6.84
CHEMBL285063 1 6.82
CHEMBL604914 1 6.54
CHEMBL597200 1 6.54
CHEMBL606403 1 -
CHEMBL599047 1 -
CHEMBL603266 1 -
CHEMBL592617 1 -
CHEMBL599863 1 -
CHEMBL52765 1 -
CHEMBL599251 1 -
CHEMBL599453 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL598007 IC50 = 44.0 nM 7.36
CHEMBL2021576 IC50 = 68.0 nM 7.17
CHEMBL597402 IC50 = 78.0 nM 7.11
CHEMBL2021575 IC50 = 145.0 nM 6.84
CHEMBL285063 IC50 = 152.0 nM 6.82
CHEMBL604914 IC50 = 292.0 nM 6.54
CHEMBL597200 IC50 = 291.0 nM 6.54
CHEMBL606403 IC50 - -
CHEMBL599047 IC50 - -
CHEMBL603266 IC50 - -
CHEMBL592617 IC50 - -
CHEMBL599863 IC50 - -
CHEMBL52765 IC50 > 10000.0 nM -
CHEMBL599251 IC50 - -
CHEMBL599453 IC50 - -