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Assay Detail

CHEMBL768824

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

Binding
Displacement of [20-3H]phorbol-12,13-dibutyrate (PDBu) from a recombinant protein kinase C alpha with phosphatidylserine
3
Total Activities
3
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 alpha type (CHEMBL299)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Conformationally constrained analogues of diacylglycerol. 21. A solid-phase method of synthesis of diacylglycerol lactones as a prelude to a combinatorial approach for the synthesis of protein kinase C isozyme-specific ligands.
Duan D, Lewin NE, Sigano DM, Blumberg PM, Marquez VE.
J Med Chem (2004) 47 : 3248 -3254
PubMed 15163204 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 7.25 7.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL110256 1 7.43
CHEMBL109354 1 7.28
CHEMBL321665 1 7.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL110256 Ki = 37.0 nM 7.43
CHEMBL109354 Ki = 52.4 nM 7.28
CHEMBL321665 Ki = 92.5 nM 7.03