Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3077166

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

Binding
Inhibition of autophosphorylation of His6-tagged EGFR cytoplasmic domain (unknown origin) expressed in Sf9 cells by DELFIA time resolved fluorometry
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis, structure, and biological assay of cinnamic amides as potential EGFR kinase inhibitors
Zhang M, Lu X, Zhang H, Li N, Xiao Y, Zhu H, Ye Y
Med Chem Res (2013) 22 : 986 -994
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 4.95 6.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL553 ERLOTINIB 4.0 1 6.47
CHEMBL2336355 N-(2-METHOXYPHENYL)CINNAMAMIDE 1 5.29
CHEMBL1998736 N-(2-FLUOROPHENYL)CINNAMAMIDE 1 5.13
CHEMBL2336357 N-(4-METHOXYPHENYL)CINNAMAMIDE 1 5.04
CHEMBL2283248 1 5.03
CHEMBL1981977 N-(2-CHLOROPHENYL)CINNAMAMIDE 1 5.01
CHEMBL2336361 N-(4-FLUOROPHENYL)CINNAMAMIDE 1 5.00
CHEMBL2283249 1 4.99
CHEMBL2283251 1 4.93
CHEMBL2336358 N-O-TOLYLCINNAMAMIDE 1 4.91
CHEMBL2336359 N-P-TOLYLCINNAMAMIDE 1 4.90
CHEMBL2283253 1 4.89
CHEMBL2283252 1 4.88
CHEMBL2336335 N-(4-CHLOROPHENYL)CINNAMAMIDE 1 4.86
CHEMBL2283256 1 4.86
CHEMBL1830131 N-(3-CHLOROPHENYL)CINNAMAMIDE 1 4.84
CHEMBL2283245 1 4.84
CHEMBL2283257 1 4.80
CHEMBL2283255 1 4.79
CHEMBL1830130 N-M-TOLYLCINNAMAMIDE 1 4.71
CHEMBL1830129 N-PHENYLCINNAMAMIDE 1 4.63
CHEMBL2283259 N-TERT-BUTYLCINNAMAMIDE 1 4.53
CHEMBL2283258 N-DODECYLCINNAMAMIDE 1 4.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL553 ERLOTINIB IC50 = 340.0 nM 6.47
CHEMBL2336355 N-(2-METHOXYPHENYL)CINNAMAMIDE IC50 = 5160.0 nM 5.29
CHEMBL1998736 N-(2-FLUOROPHENYL)CINNAMAMIDE IC50 = 7370.0 nM 5.13
CHEMBL2336357 N-(4-METHOXYPHENYL)CINNAMAMIDE IC50 = 9050.0 nM 5.04
CHEMBL2283248 IC50 = 9350.0 nM 5.03
CHEMBL1981977 N-(2-CHLOROPHENYL)CINNAMAMIDE IC50 = 9860.0 nM 5.01
CHEMBL2336361 N-(4-FLUOROPHENYL)CINNAMAMIDE IC50 = 10020.0 nM 5.00
CHEMBL2283249 IC50 = 10230.0 nM 4.99
CHEMBL2283251 IC50 = 11690.0 nM 4.93
CHEMBL2336358 N-O-TOLYLCINNAMAMIDE IC50 = 12290.0 nM 4.91
CHEMBL2336359 N-P-TOLYLCINNAMAMIDE IC50 = 12690.0 nM 4.90
CHEMBL2283253 IC50 = 12880.0 nM 4.89
CHEMBL2283252 IC50 = 13230.0 nM 4.88
CHEMBL2336335 N-(4-CHLOROPHENYL)CINNAMAMIDE IC50 = 13710.0 nM 4.86
CHEMBL2283256 IC50 = 13930.0 nM 4.86
CHEMBL1830131 N-(3-CHLOROPHENYL)CINNAMAMIDE IC50 = 14590.0 nM 4.84
CHEMBL2283245 IC50 = 14580.0 nM 4.84
CHEMBL2283257 IC50 = 15740.0 nM 4.80
CHEMBL2283255 IC50 = 16170.0 nM 4.79
CHEMBL1830130 N-M-TOLYLCINNAMAMIDE IC50 = 19690.0 nM 4.71
CHEMBL1830129 N-PHENYLCINNAMAMIDE IC50 = 23160.0 nM 4.63
CHEMBL2283259 N-TERT-BUTYLCINNAMAMIDE IC50 = 29850.0 nM 4.53
CHEMBL2283258 N-DODECYLCINNAMAMIDE IC50 = 38460.0 nM 4.42