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Assay Detail

CHEMBL2328801

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

Binding
Inhibition of human wild type EGFR expressed in Sf9 cells using [gamma32P]-ATP after 10 mins by scintillation counting
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Structure-Based Approach for the Discovery of Pyrrolo[3,2-d]pyrimidine-Based EGFR T790M/L858R Mutant Inhibitors.
Sogabe S, Kawakita Y, Igaki S, Iwata H, Miki H, Cary DR, Takagi T, Takagi S, Ohta Y, Ishikawa T.
ACS Med Chem Lett (2013) 4 : 201 -205
PubMed 24900643 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.38 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL180022 NERATINIB 4.0 1 8.60
CHEMBL1614725 TAK-285 1.0 1 8.40
CHEMBL2322329 1 8.34
CHEMBL2322330 1 8.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL180022 NERATINIB IC50 = 2.5 nM 8.60
CHEMBL1614725 TAK-285 IC50 = 4.0 nM 8.40
CHEMBL2322329 IC50 = 4.6 nM 8.34
CHEMBL2322330 IC50 = 6.9 nM 8.16