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Assay Detail

CHEMBL4427007

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

Binding
Inhibition of human C-terminal HA-tagged DAGLalpha expressed in HEK293F cell membrane fractions using PNP butyrate as substrate 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 7.45 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4476210 1 9.60
CHEMBL158897 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4476210 IC50 = 0.2512 nM 9.60
CHEMBL158897 IC50 = 5011.87 nM 5.30