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Assay Detail

CHEMBL5392480

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Functional
Antiproliferative activity against human NCI-H3255 cells harboring EGFR L858R mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type NCI-H3255
Confidence 1 — Organism
Curated By Autocuration

Target

NCI-H3255 (CHEMBL4296476)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of a Hydroxylamine-Based Brain-Penetrant EGFR Inhibitor for Metastatic Non-Small-Cell Lung Cancer.
Hill J, Jones RM, Crich D.
J Med Chem (2023) 66 : 15477 -15492
PubMed 37934858 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.67 8.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5394686 1 8.14
CHEMBL939 GEFITINIB 4.0 1 7.96
CHEMBL5420585 1 7.77
CHEMBL5430456 1 7.43
CHEMBL5430101 1 7.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5394686 IC50 = 7.2 nM 8.14
CHEMBL939 GEFITINIB IC50 = 11.0 nM 7.96
CHEMBL5420585 IC50 = 17.0 nM 7.77
CHEMBL5430456 IC50 = 37.0 nM 7.43
CHEMBL5430101 IC50 = 88.0 nM 7.06