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Assay Detail

CHEMBL871845

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Binding
Inhibition of [3H]PDBu binding to C1b domain of protein kinase C delta with phosphatidylserine
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 delta type (CHEMBL2996)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Conformationally constrained analogues of diacylglycerol (DAG). 25. Exploration of the sn-1 and sn-2 carbonyl functionality reveals the essential role of the sn-1 carbonyl at the lipid interface in the binding of DAG-lactones to protein kinase C.
Kang JH, Peach ML, Pu Y, Lewin NE, Nicklaus MC, Blumberg PM, Marquez VE.
J Med Chem (2005) 48 : 5738 -5748
PubMed 16134942 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.22 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL137386 1 9.05
CHEMBL370130 1 8.50
CHEMBL434938 1 7.69
CHEMBL194257 1 6.66
CHEMBL363418 1 5.72
CHEMBL194357 1 5.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL137386 Ki = 0.9 nM 9.05
CHEMBL370130 Ki = 3.13 nM 8.50
CHEMBL434938 Ki = 20.6 nM 7.69
CHEMBL194257 Ki = 219.0 nM 6.66
CHEMBL363418 Ki = 1890.0 nM 5.72
CHEMBL194357 Ki = 2140.0 nM 5.67