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Assay Detail

CHEMBL5224778

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

Functional
Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M double mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
8
Total Activities
8
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

Design, synthesis and biological evaluation of novel macrocyclic derivatives bearing aniline pyrimidine scaffolds as EGFR-TKIs.
Shen Y, Xiao X, Zhang P, Wang Q, Zhu X, Yang Y, Chen Y.
Bioorg Med Chem Lett (2022) 75 : 128970 -128970
PubMed 36064123 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.03 7.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3353410 OSIMERTINIB 4.0 1 7.48
CHEMBL5290583 1 7.46
CHEMBL5269317 1 7.29
CHEMBL5273197 1 7.20
CHEMBL5289304 1 6.83
CHEMBL5287438 1 6.67
CHEMBL5286636 1 6.67
CHEMBL5274514 1 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3353410 OSIMERTINIB IC50 = 33.0 nM 7.48
CHEMBL5290583 IC50 = 35.0 nM 7.46
CHEMBL5269317 IC50 = 51.0 nM 7.29
CHEMBL5273197 IC50 = 63.0 nM 7.20
CHEMBL5289304 IC50 = 148.0 nM 6.83
CHEMBL5287438 IC50 = 215.0 nM 6.67
CHEMBL5286636 IC50 = 213.0 nM 6.67
CHEMBL5274514 IC50 = 218.0 nM 6.66