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Assay Detail

CHEMBL805368

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

Binding
Inhibition of Src protein tyrosine kinase
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

Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCbeta.
Faul MM, Gillig JR, Jirousek MR, Ballas LM, Schotten T, Kahl A, Mohr M.
Bioorg Med Chem Lett (2003) 13 : 1857 -1859
PubMed 12749884 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.55 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388978 STAUROSPORINE 1 9.00
CHEMBL54382 1 4.96
CHEMBL55394 1 4.17
CHEMBL52654 1 4.08
CHEMBL432130 1 -
CHEMBL300138 ENZASTAURIN 3.0 1 -
CHEMBL300549 1 -
CHEMBL53596 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388978 STAUROSPORINE IC50 = 1.0 nM 9.00
CHEMBL54382 IC50 = 11000.0 nM 4.96
CHEMBL55394 IC50 = 68000.0 nM 4.17
CHEMBL52654 IC50 = 83000.0 nM 4.08
CHEMBL432130 IC50 > 100000.0 nM -
CHEMBL300138 ENZASTAURIN IC50 > 100000.0 nM -
CHEMBL300549 IC50 > 100000.0 nM -
CHEMBL53596 IC50 > 100000.0 nM -