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Assay Detail

CHEMBL3863078

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

Binding
Inhibition of rat brain PKC assessed as reduction in phosphatidyl serine/Ca2+-stimulated calf thymus histone H1 phosphorylation after 3 mins in presence of [gamma32P]ATP by liquid scintillation counting method
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Protein kinase C (PKC) (CHEMBL2094266)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Design and synthesis of triarylacrylonitrile analogues of tamoxifen with improved binding selectivity to protein kinase C.
Carpenter C, Sorenson RJ, Jin Y, Klossowski S, Cierpicki T, Gnegy M, Showalter HD.
Bioorg Med Chem (2016) 24 : 5495 -5504
PubMed 27647375 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 4.82 5.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL68236 1 5.52
CHEMBL83 TAMOXIFEN 4.0 1 4.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL68236 IC50 = 3000.0 nM 5.52
CHEMBL83 TAMOXIFEN IC50 = 75000.0 nM 4.12