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Assay Detail

CHEMBL4359339

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

Binding
Inhibition of human EGFR L858R/T790M/C797S mutant using poly[Glu:Tyr] (4:1) as substrate measured in presence of [gamma-33P]ATP by radiometric assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structural Basis for EGFR Mutant Inhibition by Trisubstituted Imidazole Inhibitors.
Heppner DE, Günther M, Wittlinger F, Laufer SA, Eck MJ.
J Med Chem (2020) 63 : 4293 -4305
PubMed 32243152 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.05 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4098072 1 7.05
CHEMBL4441037 1 -
CHEMBL4575583 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4098072 IC50 = 90.0 nM 7.05
CHEMBL4441037 IC50 > 5000.0 nM -
CHEMBL4575583 IC50 > 5000.0 nM -