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Assay Detail

CHEMBL821536

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Binding
Tested for inhibition of protein tyrosine kinase c-Src phosphorylation in intact cells
8
Total Activities
8
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

Substituted 5,7-diphenyl-pyrrolo[2,3d]pyrimidines: potent inhibitors of the tyrosine kinase c-Src.
Missbach M, Altmann E, Widler L, Susa M, Buchdunger E, Mett H, Meyer T, Green J.
Bioorg Med Chem Lett (2000) 10 : 945 -949
PubMed 10853665 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.84 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL105436 1 6.70
CHEMBL424375 1 6.30
CHEMBL173453 1 6.16
CHEMBL172973 1 5.48
CHEMBL169757 1 5.46
CHEMBL175409 1 5.41
CHEMBL176702 1 5.40
CHEMBL173478 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL105436 IC50 = 200.0 nM 6.70
CHEMBL424375 IC50 = 500.0 nM 6.30
CHEMBL173453 IC50 = 700.0 nM 6.16
CHEMBL172973 IC50 = 3300.0 nM 5.48
CHEMBL169757 IC50 = 3500.0 nM 5.46
CHEMBL175409 IC50 = 3900.0 nM 5.41
CHEMBL176702 IC50 = 4000.0 nM 5.40
CHEMBL173478 IC50 > 5000.0 nM -