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Assay Detail

CHEMBL5363647

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

Binding
Inhibition of DGK in human whole blood cell assessed as increase in IFNgamma level incubated for 1 hr followed by anti-human CD3/ antiCD28 mAB stimulation and measure after 24 hrs by AlphaLISA assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Blood
Cell Type Whole blood cell
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of Potent, Dual-Inhibitors of Diacylglycerol Kinases Alpha and Zeta Guided by Phenotypic Optimization.
Chupak L, Wichroski M, Zheng X, Ding M, Martin S, Allard C, Shi J, Gentles R, Meanwell NA, Fang J, Tenney D, Tokarski J, Cao C, Wee S.
ACS Med Chem Lett (2023) 14 : 929 -935
PubMed 37465293 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 6.55 6.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5424446 1 6.55
CHEMBL5408449 1 -
CHEMBL261131 DIACYLGLYCEROL KINASE INHIBITOR II 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5424446 EC50 = 280.0 nM 6.55
CHEMBL5408449 EC50 > 20000.0 nM -
CHEMBL261131 DIACYLGLYCEROL KINASE INHIBITOR II EC50 > 10000.0 nM -