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Assay Detail

CHEMBL4685759

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

Binding
Inhibition of EGFR (unknown origin) using poly (Glu,Tyr) 4:1 as substrate incubated for 8 mins in presence of ATP by colorimetric analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Comparative analysis of the dual EGFR-DNA targeting and growth inhibitory properties of 6-mono-alkylamino- and 6,6-dialkylaminoquinazoline-based type II combi-molecules.
Schmitt J,Goodfellow E,Huang S,Williams C,Gomes INF,Rosa MN,Reis RM,Yang R,Titi HM,Jean-Claude BJ
Eur J Med Chem (2020) 192 : 112185 -112185
PubMed 32145644 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.93 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL181617 1 8.00
CHEMBL939 GEFITINIB 4.0 1 7.51
CHEMBL4765122 1 6.30
CHEMBL4757104 1 5.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL181617 IC50 = 10.0 nM 8.00
CHEMBL939 GEFITINIB IC50 = 31.0 nM 7.51
CHEMBL4765122 IC50 = 504.0 nM 6.30
CHEMBL4757104 IC50 = 1257.0 nM 5.90