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Assay Detail

CHEMBL3789495

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Binding
Inhibition of wild type EGFR phosphorylation in human LoVo cells preincubated for 2 hrs followed by EGF stimulation measured after 30 mins by ELISA
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Recent progress on third generation covalent EGFR inhibitors.
Cheng H, Nair SK, Murray BW.
Bioorg Med Chem Lett (2016) 26 : 1861 -1868
PubMed 26968253 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.64 7.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3353411 1 7.48
CHEMBL3353410 OSIMERTINIB 4.0 1 6.32
CHEMBL3353412 1 6.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3353411 IC50 = 33.0 nM 7.48
CHEMBL3353410 OSIMERTINIB IC50 = 480.0 nM 6.32
CHEMBL3353412 IC50 = 786.0 nM 6.11