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Assay Detail

CHEMBL5367531

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

Functional
Antiproliferative activity against mouse BaF3 cells harboring EGFR-D770-N771insNPG mutant incubated for 3 days by Cell Titer-Glo assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type BaF3
Confidence 1 — Organism
Curated By Autocuration

Target

BaF3 (CHEMBL614524)
Type CELL-LINE
Organism Mus musculus

Publication

Structural Mechanism and Inhibitors Targeting EGFR Exon 20 Insertion (Ex20ins) Mutations.
Chen H, Hu S, Patterson AV, Smaill JB, Ding K, Lu X.
J Med Chem (2023) 66 : 11656 -11671
PubMed 37669428 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.85 8.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4650319 MOBOCERTINIB 4.0 1 8.37
CHEMBL1173655 AFATINIB 4.0 1 7.40
CHEMBL3353410 OSIMERTINIB 4.0 1 7.24
CHEMBL553 ERLOTINIB 4.0 1 5.63
CHEMBL939 GEFITINIB 4.0 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4650319 MOBOCERTINIB IC50 = 4.3 nM 8.37
CHEMBL1173655 AFATINIB IC50 = 40.0 nM 7.40
CHEMBL3353410 OSIMERTINIB IC50 = 57.0 nM 7.24
CHEMBL553 ERLOTINIB IC50 = 2320.0 nM 5.63
CHEMBL939 GEFITINIB IC50 = 2500.0 nM 5.60