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Assay Detail

CHEMBL3373887

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

Binding
Inhibition of human DAGLalpha expressed in HEK293T cell membranes assessed as reduction in hydrolysis of inhibition of [14C]-sn-1-oleoyl-2-arachidonoyl-glycerol
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of glycine sulfonamides as dual inhibitors of sn-1-diacylglycerol lipase α and α/β-hydrolase domain 6.
Janssen FJ, Deng H, Baggelaar MP, Allarà M, van der Wel T, den Dulk H, Ligresti A, van Esbroeck AC, McGuire R, Di Marzo V, Overkleeft HS, van der Stelt M.
J Med Chem (2014) 57 : 6610 -6622
PubMed 24988361 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 6.16 6.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3319620 1 6.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3319620 Ki = 700.0 nM 6.16