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Assay Detail

CHEMBL4196285

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

Binding
Inhibition of His6-tagged EGFR (unknown origin) cytoplasmic domain expressed in baculovirus infected Sf9 insect cells after 10 mins followed by addition of ATP-MgCl2 and measured after 1 hr by time-resolved fluorometric analysis
7
Total Activities
7
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

Design, synthesis, mechanistic and histopathological studies of small-molecules of novel indole-2-carboxamides and pyrazino[1,2-a]indol-1(2H)-ones as potential anticancer agents effecting the reactive oxygen species production.
Youssif BGM, Abdelrahman MH, Abdelazeem AH, Abdelgawad MA, Ibrahim HM, Salem OIA, Mohamed MFA, Treambleau L, Bukhari SNA.
Eur J Med Chem (2018) 146 : 260 -273
PubMed 29407956 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.05 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL553 ERLOTINIB 4.0 1 7.10
CHEMBL4209588 1 6.30
CHEMBL4214496 1 6.10
CHEMBL4207316 1 6.05
CHEMBL4208224 1 5.77
CHEMBL4208745 1 5.62
CHEMBL4213146 1 5.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL553 ERLOTINIB IC50 = 80.0 nM 7.10
CHEMBL4209588 IC50 = 500.0 nM 6.30
CHEMBL4214496 IC50 = 800.0 nM 6.10
CHEMBL4207316 IC50 = 900.0 nM 6.05
CHEMBL4208224 IC50 = 1700.0 nM 5.77
CHEMBL4208745 IC50 = 2400.0 nM 5.62
CHEMBL4213146 IC50 = 3900.0 nM 5.41