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Assay Detail

CHEMBL890489

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

Binding
Displacement of [3H]PDBu from mouse recombinant PKCalpha expressed in Escherichia coli
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Protein kinase C alpha type (CHEMBL2567)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Conformationally constrained analogues of diacylglycerol (DAG). 28. DAG-dioxolanones reveal a new additional interaction site in the C1b domain of PKC delta.
Choi Y, Pu Y, Peach ML, Kang JH, Lewin NE, Sigano DM, Garfield SH, Blumberg PM, Marquez VE.
J Med Chem (2007) 50 : 3465 -3481
PubMed 17591763 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 8.27 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL96766 1 8.54
CHEMBL230048 1 8.51
CHEMBL231617 1 8.46
CHEMBL2096884 1 8.24
CHEMBL2096883 1 8.19
CHEMBL231141 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL96766 Ki = 2.9 nM 8.54
CHEMBL230048 Ki = 3.07 nM 8.51
CHEMBL231617 Ki = 3.49 nM 8.46
CHEMBL2096884 Ki = 5.78 nM 8.24
CHEMBL2096883 Ki = 6.41 nM 8.19
CHEMBL231141 Ki = 19.83 nM 7.70