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Assay Detail

CHEMBL4324135

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Functional
Antiproliferative activity against human PC9 cells harboring EGFR del19/T790M/C797S triple mutant incubated for 96 hrs by Celltiter-Glo luminescent cell viability assay
2
Total Activities
2
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

Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors.
Engelhardt H, Böse D, Petronczki M, Scharn D, Bader G, Baum A, Bergner A, Chong E, Döbel S, Egger G, Engelhardt C, Ettmayer P, Fuchs JE, Gerstberger T, Gonnella N, Grimm A, Grondal E, Haddad N, Hopfgartner B, Kousek R, Krawiec M, Kriz M, Lamarre L, Leung J, Mayer M, Patel ND, Simov BP, Reeves JT, Schnitzer R, Schrenk A, Sharps B, Solca F, Stadtmüller H, Tan Z, Wunberg T, Zoephel A, McConnell DB.
J Med Chem (2019) 62 : 10272 -10293
PubMed 31689114 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.89 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4537790 1 8.89
CHEMBL3353410 OSIMERTINIB 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4537790 IC50 = 1.3 nM 8.89
CHEMBL3353410 OSIMERTINIB IC50 > 1000.0 nM -