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Assay Detail

CHEMBL5147204

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

Functional
Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth
29
Total Activities
29
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

Quinazolinones as allosteric fourth-generation EGFR inhibitors for the treatment of NSCLC.
Gero TW, Heppner DE, Beyett TS, To C, Azevedo SC, Jang J, Bunnell T, Feru F, Li Z, Shin BH, Soroko KM, Gokhale PC, Gray NS, Jänne PA, Eck MJ, Scott DA.
Bioorg Med Chem Lett (2022) 68 : 128718 -128718
PubMed 35378251 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 5.89 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5201543 1 7.30
CHEMBL5196360 1 6.50
CHEMBL5191510 1 6.31
CHEMBL4443062 1 6.21
CHEMBL5206902 1 6.11
CHEMBL5177272 1 6.09
CHEMBL5198812 1 6.00
CHEMBL5182553 1 5.97
CHEMBL5207108 1 5.94
CHEMBL5200988 1 5.91
CHEMBL5178865 1 5.90
CHEMBL5197154 1 5.89
CHEMBL5195912 1 5.83
CHEMBL5173701 1 5.82
CHEMBL5178754 1 5.81
CHEMBL5187605 1 5.80
CHEMBL5191674 1 5.77
CHEMBL5208065 1 5.73
CHEMBL5204970 1 5.70
CHEMBL5200637 1 5.70
CHEMBL5176460 1 5.70
CHEMBL5206436 1 5.67
CHEMBL5172573 1 5.63
CHEMBL5204270 1 5.61
CHEMBL5177306 1 5.59
CHEMBL5178571 1 5.52
CHEMBL5207462 1 5.46
CHEMBL5202129 1 5.44
CHEMBL4214567 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5201543 IC50 = 50.0 nM 7.30
CHEMBL5196360 IC50 = 320.0 nM 6.50
CHEMBL5191510 IC50 = 490.0 nM 6.31
CHEMBL4443062 IC50 = 610.0 nM 6.21
CHEMBL5206902 IC50 = 780.0 nM 6.11
CHEMBL5177272 IC50 = 810.0 nM 6.09
CHEMBL5198812 IC50 = 1000.0 nM 6.00
CHEMBL5182553 IC50 = 1070.0 nM 5.97
CHEMBL5207108 IC50 = 1140.0 nM 5.94
CHEMBL5200988 IC50 = 1240.0 nM 5.91
CHEMBL5178865 IC50 = 1270.0 nM 5.90
CHEMBL5197154 IC50 = 1280.0 nM 5.89
CHEMBL5195912 IC50 = 1470.0 nM 5.83
CHEMBL5173701 IC50 = 1500.0 nM 5.82
CHEMBL5178754 IC50 = 1540.0 nM 5.81
CHEMBL5187605 IC50 = 1600.0 nM 5.80
CHEMBL5191674 IC50 = 1710.0 nM 5.77
CHEMBL5208065 IC50 = 1850.0 nM 5.73
CHEMBL5204970 IC50 = 2000.0 nM 5.70
CHEMBL5200637 IC50 = 1990.0 nM 5.70
CHEMBL5176460 IC50 = 1990.0 nM 5.70
CHEMBL5206436 IC50 = 2160.0 nM 5.67
CHEMBL5172573 IC50 = 2320.0 nM 5.63
CHEMBL5204270 IC50 = 2430.0 nM 5.61
CHEMBL5177306 IC50 = 2560.0 nM 5.59
CHEMBL5178571 IC50 = 3000.0 nM 5.52
CHEMBL5207462 IC50 = 3460.0 nM 5.46
CHEMBL5202129 IC50 = 3660.0 nM 5.44
CHEMBL4214567 IC50 > 10000.0 nM -