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Assay Detail

CHEMBL1249168

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

Binding
Inhibition of EGFR
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Development of a new epidermal growth factor receptor positron emission tomography imaging agent based on the 3-cyanoquinoline core: synthesis and biological evaluation.
Pisaneschi F, Nguyen QD, Shamsaei E, Glaser M, Robins E, Kaliszczak M, Smith G, Spivey AC, Aboagye EO.
Bioorg Med Chem (2010) 18 : 6634 -6645
PubMed 20797871 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 9.32 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1243316 1 10.52
CHEMBL607707 PELITINIB 2.0 1 9.62
CHEMBL1243255 1 9.60
CHEMBL1243284 1 9.54
CHEMBL1243254 1 9.24
CHEMBL1243345 1 9.10
CHEMBL328216 1 9.09
CHEMBL1243283 1 8.74
CHEMBL1243346 1 8.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1243316 IC50 = 0.03 nM 10.52
CHEMBL607707 PELITINIB IC50 = 0.24 nM 9.62
CHEMBL1243255 IC50 = 0.25 nM 9.60
CHEMBL1243284 IC50 = 0.29 nM 9.54
CHEMBL1243254 IC50 = 0.57 nM 9.24
CHEMBL1243345 IC50 = 0.8 nM 9.10
CHEMBL328216 IC50 = 0.81 nM 9.09
CHEMBL1243283 IC50 = 1.81 nM 8.74
CHEMBL1243346 IC50 = 4.05 nM 8.39