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Assay Detail

CHEMBL679549

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

Binding
Inhibitory activity against recombinant tyrosine kinase EGF-R (EGF-R ICD)
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Dianilinophthalimides: potent and selective, ATP-competitive inhibitors of the EGF-receptor protein tyrosine kinase.
Trinks U, Buchdunger E, Furet P, Kump W, Mett H, Meyer T, Müller M, Regenass U, Rihs G, Lydon N.
J Med Chem (1994) 37 : 1015 -1027
PubMed 8151612 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 5.62 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL268868 DAPH 1 6.52
CHEMBL7939 CGP-53353 1 6.16
CHEMBL44 GENISTEIN 2.0 1 6.00
CHEMBL8095 1 5.70
CHEMBL267019 1 5.60
CHEMBL7914 1 5.60
CHEMBL7775 1 5.06
CHEMBL8223 1 4.30
CHEMBL8000 1 -
CHEMBL8091 1 -
CHEMBL8271 1 -
CHEMBL268368 STAUROSPORINE AGLYCON 1 -
CHEMBL266487 RO-316233 1 -
CHEMBL267941 1 -
CHEMBL7352 1 -
CHEMBL8222 1 -
CHEMBL7929 1 -
CHEMBL267869 1 -
CHEMBL266255 1 -
CHEMBL8163 1 -
CHEMBL268441 1 -
CHEMBL266969 1 -
CHEMBL8036 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL268868 DAPH IC50 = 300.0 nM 6.52
CHEMBL7939 CGP-53353 IC50 = 700.0 nM 6.16
CHEMBL44 GENISTEIN IC50 = 1000.0 nM 6.00
CHEMBL8095 IC50 = 2000.0 nM 5.70
CHEMBL267019 IC50 = 2500.0 nM 5.60
CHEMBL7914 IC50 = 2500.0 nM 5.60
CHEMBL7775 IC50 = 8700.0 nM 5.06
CHEMBL8223 IC50 = 50000.0 nM 4.30
CHEMBL8000 IC50 > 100000.0 nM -
CHEMBL8091 IC50 > 100000.0 nM -
CHEMBL8271 IC50 > 100000.0 nM -
CHEMBL268368 STAUROSPORINE AGLYCON IC50 > 100000.0 nM -
CHEMBL266487 RO-316233 IC50 > 50000.0 nM -
CHEMBL267941 IC50 > 50000.0 nM -
CHEMBL7352 IC50 > 50000.0 nM -
CHEMBL8222 IC50 > 100000.0 nM -
CHEMBL7929 IC50 > 50000.0 nM -
CHEMBL267869 IC50 > 100000.0 nM -
CHEMBL266255 IC50 > 100000.0 nM -
CHEMBL8163 IC50 > 50000.0 nM -
CHEMBL268441 IC50 > 50000.0 nM -
CHEMBL266969 IC50 > 50000.0 nM -
CHEMBL8036 IC50 > 50000.0 nM -