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Assay Detail

CHEMBL4413387

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Binding
Inhibition of OST-tagged DGKalpha (unknown origin) expressed in MDCK cell homogenates using DAG as substrate measured after 5 mins in presence of [gamma-32P]ATP by TLC analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MDCK
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Diacylglycerol kinase alpha (CHEMBL4105787)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of a novel DGKα inhibitor for XLP-1 therapy by virtual screening.
Velnati S, Ruffo E, Massarotti A, Talmon M, Varma KSS, Gesu A, Fresu LG, Snow AL, Bertoni A, Capello D, Tron GC, Graziani A, Baldanzi G.
Eur J Med Chem (2019) 164 : 378 -390
PubMed 30611057 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 4.96 5.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1494303 1 5.37
CHEMBL261131 DIACYLGLYCEROL KINASE INHIBITOR II 1 4.97
CHEMBL267777 RITANSERIN 2.0 1 4.78
CHEMBL259388 1 4.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1494303 IC50 = 4281.0 nM 5.37
CHEMBL261131 DIACYLGLYCEROL KINASE INHIBITOR II IC50 = 10600.0 nM 4.97
CHEMBL267777 RITANSERIN IC50 = 16700.0 nM 4.78
CHEMBL259388 IC50 = 19700.0 nM 4.71