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Assay Detail

CHEMBL4413402

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Binding
Inhibition of pig FLAG3-tagged DGKalpha expressed in African green monkey COS7 cells using 1,2-dioleoyl-sn-glycerol as substrate measured after 30 mins by ADP-Glo luminescence assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Diacylglycerol kinase alpha (CHEMBL4523195)
Type SINGLE PROTEIN
Organism Sus scrofa

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 3 5.19 6.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4558937 1 6.22
CHEMBL261131 DIACYLGLYCEROL KINASE INHIBITOR II 1 4.75
CHEMBL259388 1 4.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4558937 IC50 = 600.0 nM 6.22
CHEMBL261131 DIACYLGLYCEROL KINASE INHIBITOR II IC50 = 18000.0 nM 4.75
CHEMBL259388 IC50 = 25000.0 nM 4.60