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Assay Detail

CHEMBL3879169

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

Binding
Inhibition of MB064 probe binding to DAGLalpha in mouse brain membrane proteome preincubated for 30 mins followed by MB064 probe addition measured after 20 mins by gel-based competitive activity based protein profiling assay
12
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Tissue Brain
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Diacylglycerol lipase-alpha (CHEMBL5180)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Triazole Ureas Act as Diacylglycerol Lipase Inhibitors and Prevent Fasting-Induced Refeeding.
Deng H, Kooijman S, van den Nieuwendijk AM, Ogasawara D, van der Wel T, van Dalen F, Baggelaar MP, Janssen FJ, van den Berg RJ, den Dulk H, Cravatt BF, Overkleeft HS, Rensen PC, van der Stelt M.
J Med Chem (2017) 60 : 428 -440
PubMed 27992221 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.87 9.20
Inhibition 5 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3895863 2 9.20
CHEMBL3897587 2 8.70
CHEMBL3913807 2 8.70
CHEMBL3906477 1 8.10
CHEMBL3967137 2 7.10
CHEMBL3922787 2 7.10
CHEMBL3934441 1 6.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3895863 IC50 = 0.631 nM 9.20
CHEMBL3897587 IC50 = 1.995 nM 8.70
CHEMBL3913807 IC50 = 1.995 nM 8.70
CHEMBL3906477 IC50 = 7.943 nM 8.10
CHEMBL3967137 IC50 = 79.43 nM 7.10
CHEMBL3922787 IC50 = 79.43 nM 7.10
CHEMBL3934441 IC50 = 630.96 nM 6.20
CHEMBL3895863 Inhibition - % -
CHEMBL3967137 Inhibition - % -
CHEMBL3922787 Inhibition - % -
CHEMBL3897587 Inhibition - % -
CHEMBL3913807 Inhibition - % -