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Assay Detail

CHEMBL4004559

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

Functional
Inhibition of human PBMC proliferation assessed as decrease in [3H]-TdR uptake after 6 days by mixed lymphocyte reaction assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type PBMC
Confidence 1 — Organism
Curated By Autocuration

Target

PBMC (CHEMBL613107)
Type CELL-LINE
Organism Homo sapiens

Publication

Indolyl-naphthyl-maleimides as potent and selective inhibitors of protein kinase C-α/β.
van Eis MJ, Evenou J, Schuler W, Zenke G, Vangrevelinghe E, Wagner J, von Matt P.
Bioorg Med Chem Lett (2017) 27 : 781 -786
PubMed 28131714 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.00 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL565612 SOTRASTAURIN 2.0 1 7.55
CHEMBL4064291 1 7.27
CHEMBL4085837 1 7.23
CHEMBL4077967 1 6.56
CHEMBL4102228 1 6.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL565612 SOTRASTAURIN IC50 = 28.0 nM 7.55
CHEMBL4064291 IC50 = 54.0 nM 7.27
CHEMBL4085837 IC50 = 59.0 nM 7.23
CHEMBL4077967 IC50 = 277.0 nM 6.56
CHEMBL4102228 IC50 = 406.0 nM 6.39