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Assay Detail

CHEMBL4718827

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

Functional
Antiproliferative activity against mouse Ba/F3 cells expressing EGFR-L858R mutant assessed as inhibition of cell growth incubated for 48 hrs by XTT assay
11
Total Activities
11
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

Balancing potency, metabolic stability and permeability in pyrrolopyrimidine-based EGFR inhibitors.
Han J,Henriksen S,Nørsett KG,Sundby E,Hoff BH
Eur J Med Chem (2016) 124 : 583 -607
PubMed 27614407 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.92 7.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4786776 1 7.12
CHEMBL4784258 1 7.11
CHEMBL553 ERLOTINIB 4.0 1 7.06
CHEMBL4759003 1 7.05
CHEMBL4776396 1 7.01
CHEMBL4760328 1 7.00
CHEMBL4780286 1 6.90
CHEMBL4783569 1 6.87
CHEMBL4748367 1 6.85
CHEMBL4789027 1 6.80
CHEMBL4742081 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4786776 IC50 = 75.0 nM 7.12
CHEMBL4784258 IC50 = 77.0 nM 7.11
CHEMBL553 ERLOTINIB IC50 = 87.0 nM 7.06
CHEMBL4759003 IC50 = 90.0 nM 7.05
CHEMBL4776396 IC50 = 98.0 nM 7.01
CHEMBL4760328 IC50 = 99.0 nM 7.00
CHEMBL4780286 IC50 = 127.0 nM 6.90
CHEMBL4783569 IC50 = 134.0 nM 6.87
CHEMBL4748367 IC50 = 142.0 nM 6.85
CHEMBL4789027 IC50 = 158.0 nM 6.80
CHEMBL4742081 IC50 = 396.0 nM 6.40