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Assay Detail

CHEMBL5255146

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

Binding
Inhibition of EGFR A763-Y764 ins FQEA mutant (unknown origin)
4
Total Activities
4
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

Structure optimization and discovery of novel compound for the treatment of insertion mutations within exon 20 of EGFR and HER2.
Cui Y, Wang R, Wei Y, Hou F, Li H, Jiang Y, Sun Y, Fu S, Zuo L, Wang X, Li M, Li J, Liu N, Zhang K, Wei M, Yang G.
Bioorg Med Chem (2023) 81 : 117202 -117202
PubMed 36804726 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 9.83 10.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5282641 1 10.01
CHEMBL5288888 1 9.94
CHEMBL1173655 AFATINIB 4.0 1 9.79
CHEMBL3545154 POZIOTINIB 3.0 1 9.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5282641 IC50 = 0.097 nM 10.01
CHEMBL5288888 IC50 = 0.116 nM 9.94
CHEMBL1173655 AFATINIB IC50 = 0.161 nM 9.79
CHEMBL3545154 POZIOTINIB IC50 = 0.262 nM 9.58