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Assay Detail

CHEMBL821534

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Binding
Inhibitory activity against c-src tyrosine kinase
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Proto-oncogene tyrosine-protein kinase Src (CHEMBL267)
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 10 4.88 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL7775 1 6.00
CHEMBL267019 1 5.10
CHEMBL268868 DAPH 1 4.80
CHEMBL7939 CGP-53353 1 4.30
CHEMBL8095 1 4.19
CHEMBL266969 1 -
CHEMBL267941 1 -
CHEMBL7914 1 -
CHEMBL266255 1 -
CHEMBL8223 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL7775 IC50 = 1000.0 nM 6.00
CHEMBL267019 IC50 = 8000.0 nM 5.10
CHEMBL268868 DAPH IC50 = 16000.0 nM 4.80
CHEMBL7939 CGP-53353 IC50 = 50000.0 nM 4.30
CHEMBL8095 IC50 = 64000.0 nM 4.19
CHEMBL266969 IC50 > 50000.0 nM -
CHEMBL267941 IC50 > 100000.0 nM -
CHEMBL7914 IC50 > 100000.0 nM -
CHEMBL266255 IC50 > 50000.0 nM -
CHEMBL8223 IC50 > 100000.0 nM -