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Assay Detail

CHEMBL923922

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

Binding
Inhibition of human EGFR autophosphorylation in A431 cells
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type A-431
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Synthesis and structure-activity relationship of 4-(2-aryl-cyclopropylamino)-quinoline-3-carbonitriles as EGFR tyrosine kinase inhibitors.
Pannala M, Kher S, Wilson N, Gaudette J, Sircar I, Zhang SH, Bakhirev A, Yang G, Yuen P, Gorcsan F, Sakurai N, Barbosa M, Cheng JF.
Bioorg Med Chem Lett (2007) 17 : 5978 -5982
PubMed 17827009 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.49 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL248392 1 8.30
CHEMBL248393 1 8.24
CHEMBL401251 1 7.28
CHEMBL248222 1 7.17
CHEMBL248044 1 7.05
CHEMBL248391 1 6.76
CHEMBL399438 1 6.63
CHEMBL245798 1 6.44
CHEMBL401054 1 6.39
CHEMBL248220 1 5.79
CHEMBL245800 1 5.68
CHEMBL247024 1 5.60
CHEMBL248045 1 5.59
CHEMBL245799 1 5.28
CHEMBL401644 1 5.08
CHEMBL248221 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL248392 IC50 = 5.0 nM 8.30
CHEMBL248393 IC50 = 5.7 nM 8.24
CHEMBL401251 IC50 = 52.8 nM 7.28
CHEMBL248222 IC50 = 68.0 nM 7.17
CHEMBL248044 IC50 = 90.0 nM 7.05
CHEMBL248391 IC50 = 173.0 nM 6.76
CHEMBL399438 IC50 = 234.0 nM 6.63
CHEMBL245798 IC50 = 360.0 nM 6.44
CHEMBL401054 IC50 = 405.0 nM 6.39
CHEMBL248220 IC50 = 1610.0 nM 5.79
CHEMBL245800 IC50 = 2100.0 nM 5.68
CHEMBL247024 IC50 = 2530.0 nM 5.60
CHEMBL248045 IC50 = 2580.0 nM 5.59
CHEMBL245799 IC50 = 5260.0 nM 5.28
CHEMBL401644 IC50 = 8270.0 nM 5.08
CHEMBL248221 IC50 - -