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Assay Detail

CHEMBL5663178

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

Functional
Cytotoxicity against mouse BaF3 cells harboring EGFR Del L747_A750InsP mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type BaF3
Confidence 1 — Organism
Curated By Autocuration

Target

BaF3 (CHEMBL614524)
Type CELL-LINE
Organism Mus musculus

Publication

PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinib.
Engelman JA, Zejnullahu K, Gale CM, Lifshits E, Gonzales AJ, Shimamura T, Zhao F, Vincent PW, Naumov GN, Bradner JE, Althaus IW, Gandhi L, Shapiro GI, Nelson JM, Heymach JV, Meyerson M, Wong KK, Jänne PA.
Cancer Res (2007) 67 : 11924 -11932
PubMed 18089823 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.47 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2110732 DACOMITINIB ANHYDROUS 4.0 1 8.80
CHEMBL939 GEFITINIB 4.0 1 8.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2110732 DACOMITINIB ANHYDROUS IC50 = 1.6 nM 8.80
CHEMBL939 GEFITINIB IC50 = 7.4 nM 8.13