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Assay Detail

CHEMBL3616083

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

Binding
Inhibition of epidermal growth factor receptor kinase (unknown origin) using [33P]-ATP after 20 to 30 mins by radiometric assay
26
Total Activities
26
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

Molecular design and synthesis of certain new quinoline derivatives having potential anticancer activity.
Ibrahim DA, Abou El Ella DA, El-Motwally AM, Aly RM.
Eur J Med Chem (2015) 102 : 115 -131
PubMed 26256032 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 7.06 10.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL29197 1 10.54
CHEMBL3613702 1 10.43
CHEMBL91867 1 9.60
CHEMBL31965 CANERTINIB 3.0 1 9.10
CHEMBL553 ERLOTINIB 4.0 1 8.70
CHEMBL554 LAPATINIB 4.0 1 7.97
CHEMBL939 GEFITINIB 4.0 1 7.58
CHEMBL220037 1 7.52
CHEMBL607707 PELITINIB 2.0 1 7.41
CHEMBL180022 NERATINIB 4.0 1 7.04
CHEMBL115187 1 6.89
CHEMBL157128 1 6.82
CHEMBL113900 1 6.60
CHEMBL30973 1 6.51
CHEMBL441279 1 6.48
CHEMBL327023 1 6.26
CHEMBL281300 1 6.23
CHEMBL323630 1 6.19
CHEMBL115440 1 6.03
CHEMBL283682 1 6.03
CHEMBL114593 1 6.02
CHEMBL326811 1 5.79
CHEMBL118000 1 5.64
CHEMBL114392 1 5.57
CHEMBL3613695 1 5.32
CHEMBL3613691 1 5.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL29197 IC50 = 0.029 nM 10.54
CHEMBL3613702 IC50 = 0.037 nM 10.43
CHEMBL91867 IC50 = 0.25 nM 9.60
CHEMBL31965 CANERTINIB IC50 = 0.8 nM 9.10
CHEMBL553 ERLOTINIB IC50 = 2.0 nM 8.70
CHEMBL554 LAPATINIB IC50 = 10.8 nM 7.97
CHEMBL939 GEFITINIB IC50 = 26.0 nM 7.58
CHEMBL220037 IC50 = 30.0 nM 7.52
CHEMBL607707 PELITINIB IC50 = 39.0 nM 7.41
CHEMBL180022 NERATINIB IC50 = 92.0 nM 7.04
CHEMBL115187 IC50 = 130.0 nM 6.89
CHEMBL157128 IC50 = 150.0 nM 6.82
CHEMBL113900 IC50 = 250.0 nM 6.60
CHEMBL30973 IC50 = 310.0 nM 6.51
CHEMBL441279 IC50 = 330.0 nM 6.48
CHEMBL327023 IC50 = 550.0 nM 6.26
CHEMBL281300 IC50 = 590.0 nM 6.23
CHEMBL323630 IC50 = 650.0 nM 6.19
CHEMBL115440 IC50 = 930.0 nM 6.03
CHEMBL283682 IC50 = 940.0 nM 6.03
CHEMBL114593 IC50 = 960.0 nM 6.02
CHEMBL326811 IC50 = 1620.0 nM 5.79
CHEMBL118000 IC50 = 2290.0 nM 5.64
CHEMBL114392 IC50 = 2700.0 nM 5.57
CHEMBL3613695 IC50 = 4824.0 nM 5.32
CHEMBL3613691 IC50 = 5283.0 nM 5.28