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Assay Detail

CHEMBL3889077

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Binding
In Vitro Activity Assay: In vitro PLD activity is measured with an exogenous substrate assay as previously described (Brown, H. A. et al. (1993) Cell 75:1137-1144). Briefly, PLD activity was measured as the release of [methyl-3H]choline from [choline-methyl-3H]dipalmitoylphosphatidylcholine. PLD enzyme (PLD1=3 nM, or PLD2=15 nM) is reconstituted with phospholipid vesicle substrates. Lipid solutions were dried and resuspended, and small unilamellar vesicles were prepared by bath sonication. All assays were performed at 37° C. with agitation for 30 min. Reactions were stopped by addition of trichloroacetic acid and bovine serum albumin. Free [methyl-3H]choline was separated from precipitated lipids and proteins by centrifugation and analyzed by liquid scintillation counting.
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Phospholipase D2 (CHEMBL2734)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Antiviral therapies with phospholipase D inhibitors
(2016)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.53 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3925090 1 7.00
CHEMBL492797 1 6.62
CHEMBL3947795 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3925090 IC50 = 100.0 nM 7.00
CHEMBL492797 IC50 = 240.0 nM 6.62
CHEMBL3947795 IC50 = 1100.0 nM 5.96