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Assay Detail

CHEMBL5138507

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

Binding
Inhibition of EGFR (unknown origin)
16
Total Activities
16
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

Development of Dual Inhibitors Targeting Epidermal Growth Factor Receptor in Cancer Therapy.
Tan L, Zhang J, Wang Y, Wang X, Wang Y, Zhang Z, Shuai W, Wang G, Chen J, Wang C, Ouyang L, Li W.
J Med Chem (2022) 65 : 5149 -5183
PubMed 35311289 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.70 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4099329 1 8.96
CHEMBL31965 CANERTINIB 3.0 1 8.82
CHEMBL587723 AEE-788 2.0 1 8.70
CHEMBL4116552 1 8.64
CHEMBL4117373 1 8.31
CHEMBL5201054 1 7.99
CHEMBL554 LAPATINIB 4.0 1 7.97
CHEMBL4088718 1 7.76
CHEMBL1645462 AC-480 1.0 1 7.70
CHEMBL4065300 1 7.22
CHEMBL5194719 1 7.05
CHEMBL5203711 1 6.92
CHEMBL4286374 1 6.92
CHEMBL4073912 1 6.86
CHEMBL4294264 1 5.71
CHEMBL4569885 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4099329 IC50 = 1.1 nM 8.96
CHEMBL31965 CANERTINIB IC50 = 1.5 nM 8.82
CHEMBL587723 AEE-788 IC50 = 2.0 nM 8.70
CHEMBL4116552 IC50 = 2.3 nM 8.64
CHEMBL4117373 IC50 = 4.9 nM 8.31
CHEMBL5201054 IC50 = 10.3 nM 7.99
CHEMBL554 LAPATINIB IC50 = 10.8 nM 7.97
CHEMBL4088718 IC50 = 17.2 nM 7.76
CHEMBL1645462 AC-480 IC50 = 20.0 nM 7.70
CHEMBL4065300 IC50 = 60.1 nM 7.22
CHEMBL5194719 IC50 = 90.0 nM 7.05
CHEMBL5203711 IC50 = 120.0 nM 6.92
CHEMBL4286374 IC50 = 120.0 nM 6.92
CHEMBL4073912 IC50 = 137.0 nM 6.86
CHEMBL4294264 IC50 = 1935.0 nM 5.71
CHEMBL4569885 IC50 = 30000.0 nM -