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Assay Detail

CHEMBL4384426

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

Binding
Inhibition of wild type EGFR autophosphorylation in human A549 cells by Western blot analysis
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type A549
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Balancing reactivity and antitumor activity: heteroarylthioacetamide derivatives as potent and time-dependent inhibitors of EGFR.
Castelli R, Bozza N, Cavazzoni A, Bonelli M, Vacondio F, Ferlenghi F, Callegari D, Silva C, Rivara S, Lodola A, Digiacomo G, Fumarola C, Alfieri R, Petronini PG, Mor M.
Eur J Med Chem (2019) 162 : 507 -524
PubMed 30472599 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.68 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4562352 1 9.22
CHEMBL4530170 1 8.30
CHEMBL4440618 1 8.15
CHEMBL4572315 1 7.96
CHEMBL4556799 1 7.92
CHEMBL4530987 1 7.85
CHEMBL4435699 1 7.82
CHEMBL4437599 1 7.60
CHEMBL4558356 1 7.57
CHEMBL4449681 1 7.57
CHEMBL4526992 1 7.57
CHEMBL4439974 1 7.47
CHEMBL4538707 1 7.36
CHEMBL939 GEFITINIB 4.0 1 7.22
CHEMBL4521214 1 7.16
CHEMBL4473375 1 7.08
CHEMBL4559217 1 6.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4562352 IC50 = 0.6 nM 9.22
CHEMBL4530170 IC50 = 5.0 nM 8.30
CHEMBL4440618 IC50 = 7.0 nM 8.15
CHEMBL4572315 IC50 = 11.0 nM 7.96
CHEMBL4556799 IC50 = 12.0 nM 7.92
CHEMBL4530987 IC50 = 14.0 nM 7.85
CHEMBL4435699 IC50 = 15.0 nM 7.82
CHEMBL4437599 IC50 = 25.0 nM 7.60
CHEMBL4558356 IC50 = 27.0 nM 7.57
CHEMBL4449681 IC50 = 27.0 nM 7.57
CHEMBL4526992 IC50 = 27.0 nM 7.57
CHEMBL4439974 IC50 = 34.0 nM 7.47
CHEMBL4538707 IC50 = 44.0 nM 7.36
CHEMBL939 GEFITINIB IC50 = 60.0 nM 7.22
CHEMBL4521214 IC50 = 70.0 nM 7.16
CHEMBL4473375 IC50 = 83.0 nM 7.08
CHEMBL4559217 IC50 = 197.0 nM 6.71