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Assay Detail

CHEMBL3815405

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

Binding
Inhibition of recombinant human EGFR expressed in baculovirus by fluorescence based assay
23
Total Activities
23
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

Toward discovery of mutant EGFR inhibitors; Design, synthesis and in vitro biological evaluation of potent 4-arylamino-6-ureido and thioureido-quinazoline derivatives.
Mowafy S, Galanis A, Doctor ZM, Paranal RM, Lasheen DS, Farag NA, Jänne PA, Abouzid KA.
Bioorg Med Chem (2016) 24 : 3501 -3512
PubMed 27288180 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 8.76 9.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL939 GEFITINIB 4.0 1 9.29
CHEMBL3814257 1 9.18
CHEMBL3814882 1 9.11
CHEMBL3814959 1 9.10
CHEMBL3814211 1 9.07
CHEMBL2031296 1 9.00
CHEMBL3814956 1 8.97
CHEMBL3814320 1 8.85
CHEMBL3814812 1 8.82
CHEMBL3815163 1 8.74
CHEMBL3815074 1 8.69
CHEMBL3633928 1 8.69
CHEMBL3814447 1 8.65
CHEMBL3814445 1 8.65
CHEMBL3813728 1 8.65
CHEMBL3815161 1 8.54
CHEMBL3814694 1 8.43
CHEMBL3814846 1 8.40
CHEMBL3814816 1 8.30
CHEMBL3814182 1 8.04
CHEMBL3814460 1 -
CHEMBL3815115 1 -
CHEMBL3813876 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL939 GEFITINIB IC50 = 0.509 nM 9.29
CHEMBL3814257 IC50 = 0.662 nM 9.18
CHEMBL3814882 IC50 = 0.772 nM 9.11
CHEMBL3814959 IC50 = 0.803 nM 9.10
CHEMBL3814211 IC50 = 0.854 nM 9.07
CHEMBL2031296 IC50 = 1.01 nM 9.00
CHEMBL3814956 IC50 = 1.06 nM 8.97
CHEMBL3814320 IC50 = 1.43 nM 8.85
CHEMBL3814812 IC50 = 1.5 nM 8.82
CHEMBL3815163 IC50 = 1.81 nM 8.74
CHEMBL3815074 IC50 = 2.04 nM 8.69
CHEMBL3633928 IC50 = 2.03 nM 8.69
CHEMBL3814447 IC50 = 2.22 nM 8.65
CHEMBL3814445 IC50 = 2.25 nM 8.65
CHEMBL3813728 IC50 = 2.26 nM 8.65
CHEMBL3815161 IC50 = 2.92 nM 8.54
CHEMBL3814694 IC50 = 3.7 nM 8.43
CHEMBL3814846 IC50 = 3.96 nM 8.40
CHEMBL3814816 IC50 = 5.06 nM 8.30
CHEMBL3814182 IC50 = 9.05 nM 8.04
CHEMBL3814460 IC50 - -
CHEMBL3815115 IC50 - -
CHEMBL3813876 IC50 < 0.495 nM -