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Assay Detail

CHEMBL770095

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Binding
Inhibition of Protein kinase C eta
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Protein kinase C eta type (CHEMBL3616)
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 12 6.98 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388978 STAUROSPORINE 1 8.30
CHEMBL54382 1 7.40
CHEMBL52654 1 7.40
CHEMBL291975 1 7.38
CHEMBL55394 1 7.30
CHEMBL53596 1 7.30
CHEMBL432130 1 7.28
CHEMBL301860 1 6.89
CHEMBL55788 1 6.70
CHEMBL300138 ENZASTAURIN 3.0 1 6.40
CHEMBL300549 1 6.30
CHEMBL293805 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388978 STAUROSPORINE IC50 = 5.0 nM 8.30
CHEMBL54382 IC50 = 40.0 nM 7.40
CHEMBL52654 IC50 = 40.0 nM 7.40
CHEMBL291975 IC50 = 42.0 nM 7.38
CHEMBL55394 IC50 = 50.0 nM 7.30
CHEMBL53596 IC50 = 50.0 nM 7.30
CHEMBL432130 IC50 = 52.0 nM 7.28
CHEMBL301860 IC50 = 130.0 nM 6.89
CHEMBL55788 IC50 = 200.0 nM 6.70
CHEMBL300138 ENZASTAURIN IC50 = 400.0 nM 6.40
CHEMBL300549 IC50 = 500.0 nM 6.30
CHEMBL293805 IC50 = 8000.0 nM 5.10