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Assay Detail

CHEMBL680027

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

Functional
Concentration required to inhibit autophosphorylation of cytoplasmic domain of epidermal growth factor receptor (EGFR)
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Binding modes of 6,7 di-substituted 4-anilinoquinoline-3-carbonitriles to EGFR.
Akula N, Bhalla J, Sridhar J, Pattabiraman N.
Bioorg Med Chem Lett (2004) 14 : 3397 -3400
PubMed 15177440 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 5.92 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL607707 PELITINIB 2.0 1 7.10
CHEMBL116853 1 7.05
CHEMBL115187 1 6.89
CHEMBL117324 1 6.82
CHEMBL113900 1 6.60
CHEMBL30973 1 6.51
CHEMBL441279 1 6.48
CHEMBL327023 1 6.26
CHEMBL117326 1 6.25
CHEMBL281300 1 6.23
CHEMBL323630 1 6.19
CHEMBL263788 1 6.10
CHEMBL326280 1 6.10
CHEMBL324718 1 6.09
CHEMBL116525 1 6.04
CHEMBL283682 1 6.03
CHEMBL115440 1 6.03
CHEMBL114593 1 6.02
CHEMBL114728 1 5.80
CHEMBL326811 1 5.79
CHEMBL424252 1 5.72
CHEMBL118000 1 5.64
CHEMBL114490 1 5.63
CHEMBL421047 1 5.58
CHEMBL114392 1 5.57
CHEMBL116857 1 5.54
CHEMBL332497 1 5.42
CHEMBL325156 1 5.32
CHEMBL113901 1 5.28
CHEMBL113985 1 5.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL607707 PELITINIB IC50 = 80.0 nM 7.10
CHEMBL116853 IC50 = 90.0 nM 7.05
CHEMBL115187 IC50 = 130.0 nM 6.89
CHEMBL117324 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
CHEMBL117326 IC50 = 560.0 nM 6.25
CHEMBL281300 IC50 = 590.0 nM 6.23
CHEMBL323630 IC50 = 650.0 nM 6.19
CHEMBL263788 IC50 = 790.0 nM 6.10
CHEMBL326280 IC50 = 790.0 nM 6.10
CHEMBL324718 IC50 = 810.0 nM 6.09
CHEMBL116525 IC50 = 910.0 nM 6.04
CHEMBL283682 IC50 = 940.0 nM 6.03
CHEMBL115440 IC50 = 930.0 nM 6.03
CHEMBL114593 IC50 = 960.0 nM 6.02
CHEMBL114728 IC50 = 1600.0 nM 5.80
CHEMBL326811 IC50 = 1620.0 nM 5.79
CHEMBL424252 IC50 = 1910.0 nM 5.72
CHEMBL118000 IC50 = 2290.0 nM 5.64
CHEMBL114490 IC50 = 2320.0 nM 5.63
CHEMBL421047 IC50 = 2640.0 nM 5.58
CHEMBL114392 IC50 = 2700.0 nM 5.57
CHEMBL116857 IC50 = 2880.0 nM 5.54
CHEMBL332497 IC50 = 3830.0 nM 5.42
CHEMBL325156 IC50 = 4840.0 nM 5.32
CHEMBL113901 IC50 = 5220.0 nM 5.28
CHEMBL113985 IC50 = 5390.0 nM 5.27
CHEMBL113902 IC50 = 7500.0 nM 5.12
CHEMBL116012 IC50 = 10300.0 nM 4.99
CHEMBL114073 IC50 = 10600.0 nM 4.97
CHEMBL113996 IC50 = 13600.0 nM 4.87