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Assay Detail

CHEMBL3815441

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

Binding
Inhibition of wild type EGFR (unknown origin) expressed in mouse BaF/3 cells assessed as cell growth inhibition after 72 hrs by MTS assay
25
Total Activities
25
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 25 6.80 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3814882 1 7.68
CHEMBL3815074 1 7.41
CHEMBL2031296 1 7.39
CHEMBL3814956 1 7.21
CHEMBL3814816 1 7.18
CHEMBL3815163 1 7.12
CHEMBL3814694 1 7.10
CHEMBL3815161 1 7.06
CHEMBL939 GEFITINIB 4.0 1 6.90
CHEMBL3814445 1 6.82
CHEMBL3633928 1 6.73
CHEMBL3814447 1 6.71
CHEMBL3815115 1 6.61
CHEMBL3814460 1 6.59
CHEMBL3814257 1 6.58
CHEMBL3814320 1 6.57
CHEMBL3814812 1 6.57
CHEMBL3814959 1 6.56
CHEMBL3814940 1 6.53
CHEMBL3814211 1 6.50
CHEMBL3813728 1 6.48
CHEMBL3813876 1 6.41
CHEMBL3814846 1 6.39
CHEMBL3814182 1 6.11
CHEMBL3814021 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3814882 IC50 = 21.0 nM 7.68
CHEMBL3815074 IC50 = 39.0 nM 7.41
CHEMBL2031296 IC50 = 41.0 nM 7.39
CHEMBL3814956 IC50 = 62.0 nM 7.21
CHEMBL3814816 IC50 = 66.0 nM 7.18
CHEMBL3815163 IC50 = 76.0 nM 7.12
CHEMBL3814694 IC50 = 80.0 nM 7.10
CHEMBL3815161 IC50 = 87.0 nM 7.06
CHEMBL939 GEFITINIB IC50 = 127.0 nM 6.90
CHEMBL3814445 IC50 = 150.0 nM 6.82
CHEMBL3633928 IC50 = 186.0 nM 6.73
CHEMBL3814447 IC50 = 194.0 nM 6.71
CHEMBL3815115 IC50 = 247.0 nM 6.61
CHEMBL3814460 IC50 = 259.0 nM 6.59
CHEMBL3814257 IC50 = 264.0 nM 6.58
CHEMBL3814320 IC50 = 269.0 nM 6.57
CHEMBL3814812 IC50 = 271.0 nM 6.57
CHEMBL3814959 IC50 = 273.0 nM 6.56
CHEMBL3814940 IC50 = 296.0 nM 6.53
CHEMBL3814211 IC50 = 315.0 nM 6.50
CHEMBL3813728 IC50 = 332.0 nM 6.48
CHEMBL3813876 IC50 = 390.0 nM 6.41
CHEMBL3814846 IC50 = 410.0 nM 6.39
CHEMBL3814182 IC50 = 772.0 nM 6.11
CHEMBL3814021 IC50 > 500.0 nM -