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Assay Detail

CHEMBL4427017

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

Binding
Inhibition of human DAGLalpha expressed in HEK293T cell membrane fractions using PNP butyrate as substrate preincubated for 20 mins followed by substrate addition by colorimetric surrogate substrate assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Diacylglycerol lipase-alpha (CHEMBL5545)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inhibitors of diacylglycerol lipases in neurodegenerative and metabolic disorders.
Janssen FJ, van der Stelt M.
Bioorg Med Chem Lett (2016) 26 : 3831 -3837
PubMed 27394666 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.95 8.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4447844 1 8.50
CHEMBL175854 1 7.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4447844 IC50 = 3.162 nM 8.50
CHEMBL175854 IC50 = 39.81 nM 7.40