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Assay Detail

CHEMBL4413403

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

Binding
Inhibition of DGKalpha in human erythrocytes using OAG as substrate preincubated for 1 min followed by OAG addition and measured after 8 mins in presence of [gamma-32P]ATP
6
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
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
Ki 4 4.85 5.65
IC50 2 5.97 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL261131 DIACYLGLYCEROL KINASE INHIBITOR II 1 6.52
CHEMBL2288168 COCHLIOQUINONE A 1 5.65
CHEMBL2288178 STEMPHONE 1 5.48
CHEMBL259388 1 5.42
CHEMBL2268841 ETHYLENE GLYCOL DIOCTANOATE 1 4.24
CHEMBL428593 GLYCERYL MONOOLEATE -1.0 1 4.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL261131 DIACYLGLYCEROL KINASE INHIBITOR II IC50 = 300.0 nM 6.52
CHEMBL2288168 COCHLIOQUINONE A Ki = 2260.0 nM 5.65
CHEMBL2288178 STEMPHONE Ki = 3320.0 nM 5.48
CHEMBL259388 IC50 = 3800.0 nM 5.42
CHEMBL2268841 ETHYLENE GLYCOL DIOCTANOATE Ki = 58000.0 nM 4.24
CHEMBL428593 GLYCERYL MONOOLEATE Ki = 91000.0 nM 4.04