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Assay Detail

CHEMBL1949352

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

Binding
Inhibition of EGFR after 50 mins by HTRF assay
13
Total Activities
13
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

Synthesis and biological evaluation of quinazoline and quinoline bearing 2,2,6,6-tetramethylpiperidine-N-oxyl as potential epidermal growth factor receptor(EGFR) tyrosine kinase inhibitors and EPR bio-probe agents.
Li S, Guo C, Sun X, Li Y, Zhao H, Zhan D, Lan M, Tang Y.
Eur J Med Chem (2012) 49 : 271 -278
PubMed 22309911 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.65 8.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL939 GEFITINIB 4.0 1 8.14
CHEMBL1947124 1 7.82
CHEMBL242541 1 7.54
CHEMBL1946926 1 7.51
CHEMBL52765 1 7.28
CHEMBL1947125 1 7.19
CHEMBL343352 1 6.72
CHEMBL1947127 1 6.47
CHEMBL1947121 1 6.38
CHEMBL1947126 1 6.21
CHEMBL541988 1 5.06
CHEMBL1947122 1 5.04
CHEMBL1947123 1 5.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL939 GEFITINIB IC50 = 7.3 nM 8.14
CHEMBL1947124 IC50 = 15.0 nM 7.82
CHEMBL242541 IC50 = 29.0 nM 7.54
CHEMBL1946926 IC50 = 31.0 nM 7.51
CHEMBL52765 IC50 = 53.0 nM 7.28
CHEMBL1947125 IC50 = 65.0 nM 7.19
CHEMBL343352 IC50 = 189.0 nM 6.72
CHEMBL1947127 IC50 = 342.0 nM 6.47
CHEMBL1947121 IC50 = 422.0 nM 6.38
CHEMBL1947126 IC50 = 623.0 nM 6.21
CHEMBL541988 IC50 = 8719.0 nM 5.06
CHEMBL1947122 IC50 = 9021.0 nM 5.04
CHEMBL1947123 IC50 = 9284.0 nM 5.03