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Assay Detail

CHEMBL677391

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

Binding
Inhibition of tyrosine phosphorylation activity of the epidermal growth factor receptor (EGFR) tyrosine kinase from human A-431 carcinoma cell-shed membrane vesicles
33
Total Activities
33
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

Tyrosine kinase inhibitors. 3. Structure-activity relationships for inhibition of protein tyrosine kinases by nuclear-substituted derivatives of 2,2'-dithiobis(1-methyl-N-phenyl-1H-indole-3-carboxamide).
Rewcastle GW, Palmer BD, Dobrusin EM, Fry DW, Kraker AJ, Denny WA.
J Med Chem (1994) 37 : 2033 -2042
PubMed 8027985 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 4.87 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL62176 1 6.00
CHEMBL60472 1 5.44
CHEMBL293889 1 5.37
CHEMBL64430 1 5.30
CHEMBL61119 1 5.28
CHEMBL292323 1 5.19
CHEMBL291359 1 5.00
CHEMBL304414 1 5.00
CHEMBL293251 1 4.94
CHEMBL59812 1 4.70
CHEMBL62701 1 4.65
CHEMBL293250 1 4.39
CHEMBL293913 1 4.36
CHEMBL291979 1 4.27
CHEMBL62843 1 4.00
CHEMBL293986 1 4.00
CHEMBL303127 1 -
CHEMBL291667 1 -
CHEMBL64459 1 -
CHEMBL294341 1 -
CHEMBL63009 1 -
CHEMBL64781 1 -
CHEMBL61278 1 -
CHEMBL292287 1 -
CHEMBL60200 1 -
CHEMBL64068 1 -
CHEMBL62067 1 -
CHEMBL63455 1 -
CHEMBL64814 1 -
CHEMBL64165 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL62176 IC50 = 1000.0 nM 6.00
CHEMBL60472 IC50 = 3600.0 nM 5.44
CHEMBL293889 IC50 = 4300.0 nM 5.37
CHEMBL64430 IC50 = 5000.0 nM 5.30
CHEMBL61119 IC50 = 5300.0 nM 5.28
CHEMBL292323 IC50 = 6500.0 nM 5.19
CHEMBL291359 IC50 = 9900.0 nM 5.00
CHEMBL304414 IC50 = 10000.0 nM 5.00
CHEMBL293251 IC50 = 11400.0 nM 4.94
CHEMBL59812 IC50 = 20000.0 nM 4.70
CHEMBL62701 IC50 = 22300.0 nM 4.65
CHEMBL293250 IC50 = 40500.0 nM 4.39
CHEMBL293913 IC50 = 44000.0 nM 4.36
CHEMBL291979 IC50 = 54100.0 nM 4.27
CHEMBL293986 IC50 = 100000.0 nM 4.00
CHEMBL62843 IC50 = 100000.0 nM 4.00
CHEMBL64231 IC50 > 100000.0 nM -
CHEMBL62699 IC50 > 100000.0 nM -
CHEMBL294205 IC50 > 100000.0 nM -
CHEMBL64165 IC50 > 100000.0 nM -
CHEMBL64814 IC50 > 100000.0 nM -
CHEMBL63455 IC50 > 100000.0 nM -
CHEMBL62067 IC50 > 100000.0 nM -
CHEMBL64068 IC50 > 100000.0 nM -
CHEMBL60200 IC50 > 100000.0 nM -
CHEMBL292287 IC50 > 100000.0 nM -
CHEMBL61278 IC50 > 100000.0 nM -
CHEMBL64781 IC50 > 100000.0 nM -
CHEMBL63009 IC50 > 100000.0 nM -
CHEMBL294341 IC50 > 100000.0 nM -
CHEMBL64459 IC50 > 100000.0 nM -
CHEMBL291667 IC50 > 100000.0 nM -
CHEMBL303127 IC50 > 100000.0 nM -