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Assay Detail

CHEMBL676152

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

Binding
In vitro inhibition of HER1 autophosphorylation.
21
Total Activities
21
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

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 21 5.21 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56543 1 7.00
CHEMBL53898 1 6.16
CHEMBL56731 1 5.90
CHEMBL56219 1 5.68
CHEMBL55979 1 5.60
CHEMBL296407 1 5.35
CHEMBL440298 1 5.30
CHEMBL56393 1 5.30
CHEMBL417941 1 5.23
CHEMBL59145 1 5.18
CHEMBL55360 1 4.99
CHEMBL56879 1 4.96
CHEMBL56542 1 4.92
CHEMBL56132 1 4.85
CHEMBL54471 1 4.82
CHEMBL55993 1 4.62
CHEMBL55994 1 4.51
CHEMBL56319 1 4.31
CHEMBL291986 1 4.26
CHEMBL293749 1 -
CHEMBL57251 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56543 IC50 = 100.0 nM 7.00
CHEMBL53898 IC50 = 700.0 nM 6.16
CHEMBL56731 IC50 = 1250.0 nM 5.90
CHEMBL56219 IC50 = 2100.0 nM 5.68
CHEMBL55979 IC50 = 2500.0 nM 5.60
CHEMBL296407 IC50 = 4500.0 nM 5.35
CHEMBL440298 IC50 = 5000.0 nM 5.30
CHEMBL56393 IC50 = 5000.0 nM 5.30
CHEMBL417941 IC50 = 5900.0 nM 5.23
CHEMBL59145 IC50 = 6600.0 nM 5.18
CHEMBL55360 IC50 = 10300.0 nM 4.99
CHEMBL56879 IC50 = 11000.0 nM 4.96
CHEMBL56542 IC50 = 12000.0 nM 4.92
CHEMBL56132 IC50 = 14000.0 nM 4.85
CHEMBL54471 IC50 = 15000.0 nM 4.82
CHEMBL55993 IC50 = 24000.0 nM 4.62
CHEMBL55994 IC50 = 31000.0 nM 4.51
CHEMBL56319 IC50 = 49000.0 nM 4.31
CHEMBL291986 IC50 = 55000.0 nM 4.26
CHEMBL293749 IC50 < 625.0 nM -
CHEMBL57251 IC50 > 166000.0 nM -