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Assay Detail

CHEMBL766778

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

Binding
Displacement of phorbol 12,13-dibutyrate (PDBU) from Protein kinase C alpha
6
Total Activities
6
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. 11. Ultrapotent protein kinase C ligands based on a chiral 5-disubstituted tetrahydro-2-furanone template.
Lee J, Wang S, Milne GW, Sharma R, Lewin NE, Blumberg PM, Marquez VE.
J Med Chem (1996) 39 : 29 -35
PubMed 8568819 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.48 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL116029 1 7.92
CHEMBL119303 1 7.89
CHEMBL321823 1 7.62
CHEMBL94718 1 7.55
CHEMBL119907 1 7.02
CHEMBL299225 1 6.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL116029 Ki = 12.0 nM 7.92
CHEMBL119303 Ki = 13.0 nM 7.89
CHEMBL321823 Ki = 24.0 nM 7.62
CHEMBL94718 Ki = 28.0 nM 7.55
CHEMBL119907 Ki = 96.0 nM 7.02
CHEMBL299225 Ki = 138.0 nM 6.86