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Assay Detail

CHEMBL5707346

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

Functional
Antiproliferative activity against human PC-9 cells harboring EGFR Del E746_A750 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS 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

Novel mutant-selective EGFR kinase inhibitors against EGFR T790M.
Zhou W, Ercan D, Chen L, Yun CH, Li D, Capelletti M, Cortot AB, Chirieac L, Iacob RE, Padera R, Engen JR, Wong KK, Eck MJ, Gray NS, Jänne PA.
Nature (2009) 462 : 1070 -1074
PubMed 20033049 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.83 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL91867 1 8.70
CHEMBL1643989 1 8.22
CHEMBL1643976 1 7.82
CHEMBL939 GEFITINIB 4.0 1 7.77
CHEMBL1229592 1 7.44
CHEMBL180022 NERATINIB 4.0 1 7.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL91867 IC50 = 2.0 nM 8.70
CHEMBL1643989 IC50 = 6.0 nM 8.22
CHEMBL1643976 IC50 = 15.0 nM 7.82
CHEMBL939 GEFITINIB IC50 = 17.0 nM 7.77
CHEMBL1229592 IC50 = 36.0 nM 7.44
CHEMBL180022 NERATINIB IC50 = 96.0 nM 7.02