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Assay Detail

CHEMBL4427014

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

Binding
Inhibition human DAGLalpha expressed in HEK293T cell membrane fractions using DAG as substrate preincubated for 30 mins followed by ABP HT01 probe addition measured after 30 mins in presence of probe by gel-based ABPP competition assay
5
Total Activities
5
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 5 7.46 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4581240 1 9.30
CHEMBL3895863 1 8.90
CHEMBL2136920 1 6.90
CHEMBL4476210 1 6.60
CHEMBL2144065 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4581240 IC50 = 0.5012 nM 9.30
CHEMBL3895863 IC50 = 1.259 nM 8.90
CHEMBL2136920 IC50 = 125.89 nM 6.90
CHEMBL4476210 IC50 = 251.19 nM 6.60
CHEMBL2144065 IC50 = 2511.89 nM 5.60