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Assay Detail

CHEMBL5386735

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

Binding
Inhibition of EGFR (unknown origin)
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Epidermal growth factor receptor (CHEMBL203)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and biological evaluation of novel quinoline derivatives as small molecule mutant EGFR inhibitors targeting resistance in NSCLC: In vitro screening and ADME predictions.
Kardile RA, Sarkate AP, Lokwani DK, Tiwari SV, Azad R, Thopate SR.
Eur J Med Chem (2023) 245 : 114889 -114889
PubMed 36375337 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.86 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL248392 1 8.30
CHEMBL111038 1 8.12
CHEMBL5416668 1 6.31
CHEMBL4447196 1 6.30
CHEMBL3613691 1 5.28
CHEMBL5206476 1 -
CHEMBL607707 PELITINIB 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL248392 IC50 = 5.0 nM 8.30
CHEMBL111038 IC50 = 7.5 nM 8.12
CHEMBL5416668 IC50 = 490.0 nM 6.31
CHEMBL4447196 IC50 = 500.0 nM 6.30
CHEMBL3613691 IC50 = 5283.0 nM 5.28
CHEMBL5206476 IC50 = 5300000.0 nM -
CHEMBL607707 PELITINIB IC50 = 83000000.0 nM -