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Assay Detail

CHEMBL4829489

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

Binding
Inhibition of wild type EGFR L858R/T790M/C797S mutant (unknown origin) pretreated with substrate for 10 mins followed by ATP addition measured after 60 mins by mobility shift 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

The synthesis and bioactivity of pyrrolo[2,3-d]pyrimidine derivatives as tyrosine kinase inhibitors for NSCLC cells with EGFR mutations.
Xia Z, Huang R, Zhou X, Chai Y, Chen H, Ma L, Yu Q, Li Y, Li W, He Y.
Eur J Med Chem (2021) 224 : 113711 -113711
PubMed 34315040 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.52 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4847264 1 6.92
CHEMBL4297865 ABIVERTINIB 3.0 1 6.55
CHEMBL4850239 1 6.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4847264 IC50 = 119.0 nM 6.92
CHEMBL4297865 ABIVERTINIB IC50 = 279.0 nM 6.55
CHEMBL4850239 IC50 = 829.0 nM 6.08