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Assay Detail

CHEMBL5711668

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

Functional
Anticancer activity against human PC-9 cells harboring del19 mutant assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay
6
Total Activities
6
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

Brigatinib combined with anti-EGFR antibody overcomes osimertinib resistance in EGFR-mutated non-small-cell lung cancer.
Uchibori K, Inase N, Araki M, Kamada M, Sato S, Okuno Y, Fujita N, Katayama R.
Nat Commun (2017) 8 : 14768 -14768
PubMed 28287083 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.66 9.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1173655 AFATINIB 4.0 1 9.20
CHEMBL3353410 OSIMERTINIB 4.0 1 8.13
CHEMBL939 GEFITINIB 4.0 1 7.79
CHEMBL3397300 1 7.34
CHEMBL3545311 BRIGATINIB 4.0 1 6.88
CHEMBL4203266 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1173655 AFATINIB IC50 = 0.638 nM 9.20
CHEMBL3353410 OSIMERTINIB IC50 = 7.463 nM 8.13
CHEMBL939 GEFITINIB IC50 = 16.38 nM 7.79
CHEMBL3397300 IC50 = 46.18 nM 7.34
CHEMBL3545311 BRIGATINIB IC50 = 132.8 nM 6.88
CHEMBL4203266 IC50 = 253.0 nM 6.60