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Assay Detail

CHEMBL5165815

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

Functional
Antiproliferative activity against human osimertinib-resistant PC-9 cells harboring EGFR 19 del/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type PC-9
Confidence 1 — Organism
Curated By Autocuration

Target

PC-9 (CHEMBL614102)
Type CELL-LINE
Organism Homo sapiens

Publication

Conformational Constrained 4-(1-Sulfonyl-3-indol)yl-2-phenylaminopyrimidine Derivatives as New Fourth-Generation Epidermal Growth Factor Receptor Inhibitors Targeting T790M/C797S Mutations.
Chen H, Lai M, Zhang T, Chen Y, Tong L, Zhu S, Zhou Y, Ren X, Ding J, Xie H, Lu X, Ding K.
J Med Chem (2022) 65 : 6840 -6858
PubMed 35446588 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.77 9.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5193609 1 9.19
CHEMBL3545311 BRIGATINIB 4.0 1 8.84
CHEMBL3353410 OSIMERTINIB 4.0 1 8.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5193609 IC50 = 0.644 nM 9.19
CHEMBL3545311 BRIGATINIB IC50 = 1.454 nM 8.84
CHEMBL3353410 OSIMERTINIB IC50 = 5.431 nM 8.27