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Assay Detail

CHEMBL689298

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

Functional
Antiproliferative activity determined by measuring the ability to block [3H]- thymidine uptake in HER-14 cells stimulated by EGF
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type HER-14
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Tyrphostins. 6. Dimeric benzylidenemalononitrile tyrophostins: potent inhibitors of EGF receptor tyrosine kinase in vitro.
Gazit A, Osherov N, Gilon C, Levitzki A.
J Med Chem (1996) 39 : 4905 -4911
PubMed 8960549 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 5.13 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL356324 1 5.70
CHEMBL67535 1 5.52
CHEMBL357400 1 5.52
CHEMBL144778 1 5.40
CHEMBL342792 1 5.40
CHEMBL358746 1 5.30
CHEMBL144760 1 5.30
CHEMBL144589 1 5.30
CHEMBL145209 1 5.24
CHEMBL144159 1 5.22
CHEMBL343887 1 5.21
CHEMBL144402 1 5.16
CHEMBL144770 1 5.14
CHEMBL144842 1 5.05
CHEMBL358494 1 5.00
CHEMBL144908 1 5.00
CHEMBL144791 1 4.96
CHEMBL147880 1 4.69
CHEMBL279138 1 4.62
CHEMBL424302 1 4.60
CHEMBL144632 1 4.46
CHEMBL145266 1 -
CHEMBL143108 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL356324 IC50 = 2000.0 nM 5.70
CHEMBL67535 IC50 = 3000.0 nM 5.52
CHEMBL357400 IC50 = 3000.0 nM 5.52
CHEMBL144778 IC50 = 4000.0 nM 5.40
CHEMBL342792 IC50 = 4000.0 nM 5.40
CHEMBL358746 IC50 = 5000.0 nM 5.30
CHEMBL144760 IC50 = 5000.0 nM 5.30
CHEMBL144589 IC50 = 5000.0 nM 5.30
CHEMBL145209 IC50 = 5800.0 nM 5.24
CHEMBL144159 IC50 = 6000.0 nM 5.22
CHEMBL343887 IC50 = 6200.0 nM 5.21
CHEMBL144402 IC50 = 7000.0 nM 5.16
CHEMBL144770 IC50 = 7300.0 nM 5.14
CHEMBL144842 IC50 = 9000.0 nM 5.05
CHEMBL358494 IC50 = 10000.0 nM 5.00
CHEMBL144908 IC50 = 10000.0 nM 5.00
CHEMBL144791 IC50 = 11000.0 nM 4.96
CHEMBL147880 IC50 = 20300.0 nM 4.69
CHEMBL279138 IC50 = 24000.0 nM 4.62
CHEMBL424302 IC50 = 25000.0 nM 4.60
CHEMBL144632 IC50 = 35000.0 nM 4.46
CHEMBL145266 IC50 > 80000.0 nM -
CHEMBL143108 IC50 > 100000.0 nM -