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Assay Detail

CHEMBL701406

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

Functional
Inhibition of HER14 (human EGFR overexpressing) cell proliferation.
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases.
Gazit A, Osherov N, Posner I, Yaish P, Poradosu E, Gilon C, Levitzki A.
J Med Chem (1991) 34 : 1896 -1907
PubMed 1676428 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 4.94 5.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53898 1 5.60
CHEMBL55979 1 5.46
CHEMBL54471 1 5.16
CHEMBL56132 1 4.82
CHEMBL291313 1 4.70
CHEMBL55204 1 4.70
CHEMBL56542 1 4.60
CHEMBL56219 1 4.46
CHEMBL56879 1 -
CHEMBL56731 1 -
CHEMBL294213 1 -
CHEMBL57462 1 -
CHEMBL55360 1 -
CHEMBL56393 1 -
CHEMBL56964 1 -
CHEMBL293584 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53898 IC50 = 2500.0 nM 5.60
CHEMBL55979 IC50 = 3500.0 nM 5.46
CHEMBL54471 IC50 = 7000.0 nM 5.16
CHEMBL56132 IC50 = 15000.0 nM 4.82
CHEMBL291313 IC50 = 20000.0 nM 4.70
CHEMBL55204 IC50 = 20000.0 nM 4.70
CHEMBL56542 IC50 = 25000.0 nM 4.60
CHEMBL56219 IC50 = 35000.0 nM 4.46
CHEMBL56879 IC50 < 20000.0 nM -
CHEMBL56731 IC50 > 15000.0 nM -
CHEMBL294213 IC50 > 100000.0 nM -
CHEMBL57462 IC50 > 16000.0 nM -
CHEMBL55360 IC50 > 5000.0 nM -
CHEMBL56393 IC50 > 8000.0 nM -
CHEMBL56964 IC50 > 120000.0 nM -
CHEMBL293584 IC50 > 30000.0 nM -