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Assay Detail

CHEMBL5367528

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

Functional
Antiproliferative activity against mouse Ba/F3 EGFR-A763_Y764insFQEA cells incubated for 3 days by Cell Titer-Glo assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type Ba/F3 EGFR-A763_Y764insFQEA
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 6 7.53 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1173655 AFATINIB 4.0 1 8.57
CHEMBL4650281 CLN-081 3.0 1 8.30
CHEMBL4650319 MOBOCERTINIB 4.0 1 7.93
CHEMBL3353410 OSIMERTINIB 4.0 1 7.06
CHEMBL553 ERLOTINIB 4.0 1 6.67
CHEMBL939 GEFITINIB 4.0 1 6.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1173655 AFATINIB IC50 = 2.7 nM 8.57
CHEMBL4650281 CLN-081 IC50 = 5.0 nM 8.30
CHEMBL4650319 MOBOCERTINIB IC50 = 11.8 nM 7.93
CHEMBL3353410 OSIMERTINIB IC50 = 87.0 nM 7.06
CHEMBL553 ERLOTINIB IC50 = 214.0 nM 6.67
CHEMBL939 GEFITINIB IC50 = 233.0 nM 6.63