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Assay Detail

CHEMBL828023

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Binding
Inhibitory concentration against recombinant human Protein kinase C epsilon
14
Total Activities
14
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 epsilon type (CHEMBL3582)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of anilino-monoindolylmaleimides as potent and selective PKCbeta inhibitors.
Tanaka M, Sagawa S, Hoshi J, Shimoma F, Matsuda I, Sakoda K, Sasase T, Shindo M, Inaba T.
Bioorg Med Chem Lett (2004) 14 : 5171 -5174
PubMed 15380221 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.57 7.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL540357 1 7.24
CHEMBL364337 1 5.58
CHEMBL366266 1 5.55
CHEMBL369114 1 5.46
CHEMBL187235 1 5.46
CHEMBL365656 1 5.46
CHEMBL184647 1 5.41
CHEMBL184548 1 5.23
CHEMBL185221 1 5.20
CHEMBL266487 RO-316233 1 5.12
CHEMBL184042 1 -
CHEMBL184146 1 -
CHEMBL183310 1 -
CHEMBL184649 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL540357 IC50 = 58.0 nM 7.24
CHEMBL364337 IC50 = 2605.0 nM 5.58
CHEMBL366266 IC50 = 2807.0 nM 5.55
CHEMBL369114 IC50 = 3455.0 nM 5.46
CHEMBL187235 IC50 = 3425.0 nM 5.46
CHEMBL365656 IC50 = 3456.0 nM 5.46
CHEMBL184647 IC50 = 3905.0 nM 5.41
CHEMBL184548 IC50 = 5866.0 nM 5.23
CHEMBL185221 IC50 = 6322.0 nM 5.20
CHEMBL266487 RO-316233 IC50 = 7516.0 nM 5.12
CHEMBL184042 IC50 > 10000.0 nM -
CHEMBL184146 IC50 > 10000.0 nM -
CHEMBL183310 IC50 > 10000.0 nM -
CHEMBL184649 IC50 > 10000.0 nM -