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Assay Detail

CHEMBL3879162

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

Binding
Inhibition of full length recombinant human DAGLalpha expressed in HEK293T cell membranes using PNP butyrate as substrate by colorimetric assay
31
Total Activities
31
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

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 31 7.73 9.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3897587 1 9.20
CHEMBL3954476 1 9.10
CHEMBL3906477 1 9.10
CHEMBL3913807 1 9.10
CHEMBL3970032 1 9.00
CHEMBL3895863 1 8.90
CHEMBL3964338 1 8.60
CHEMBL3941507 1 8.50
CHEMBL3916842 1 8.30
CHEMBL3903742 1 8.30
CHEMBL3921538 1 8.30
CHEMBL2144065 1 8.20
CHEMBL3986579 1 8.20
CHEMBL3922787 1 8.10
CHEMBL3897762 1 8.10
CHEMBL3925845 1 7.90
CHEMBL3931744 1 7.90
CHEMBL3967137 1 7.70
CHEMBL3912754 1 7.70
CHEMBL3904310 1 7.70
CHEMBL3966016 1 7.70
CHEMBL3974512 1 7.60
CHEMBL3934441 1 7.40
CHEMBL1891894 1 7.20
CHEMBL3929394 1 7.00
CHEMBL3945819 1 6.80
CHEMBL3907846 1 6.40
CHEMBL3956962 1 5.80
CHEMBL3894652 1 5.40
CHEMBL3978360 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3897587 IC50 = 0.631 nM 9.20
CHEMBL3954476 IC50 = 0.7943 nM 9.10
CHEMBL3906477 IC50 = 0.7943 nM 9.10
CHEMBL3913807 IC50 = 0.7943 nM 9.10
CHEMBL3970032 IC50 = 1.0 nM 9.00
CHEMBL3895863 IC50 = 1.259 nM 8.90
CHEMBL3964338 IC50 = 2.512 nM 8.60
CHEMBL3941507 IC50 = 3.162 nM 8.50
CHEMBL3916842 IC50 = 5.012 nM 8.30
CHEMBL3903742 IC50 = 5.012 nM 8.30
CHEMBL3921538 IC50 = 5.012 nM 8.30
CHEMBL2144065 IC50 = 6.31 nM 8.20
CHEMBL3986579 IC50 = 6.31 nM 8.20
CHEMBL3922787 IC50 = 7.943 nM 8.10
CHEMBL3897762 IC50 = 7.943 nM 8.10
CHEMBL3925845 IC50 = 12.59 nM 7.90
CHEMBL3931744 IC50 = 12.59 nM 7.90
CHEMBL3967137 IC50 = 19.95 nM 7.70
CHEMBL3912754 IC50 = 19.95 nM 7.70
CHEMBL3904310 IC50 = 19.95 nM 7.70
CHEMBL3966016 IC50 = 19.95 nM 7.70
CHEMBL3974512 IC50 = 25.12 nM 7.60
CHEMBL3934441 IC50 = 39.81 nM 7.40
CHEMBL1891894 IC50 = 63.1 nM 7.20
CHEMBL3929394 IC50 = 100.0 nM 7.00
CHEMBL3945819 IC50 = 158.49 nM 6.80
CHEMBL3907846 IC50 = 398.11 nM 6.40
CHEMBL3956962 IC50 = 1584.89 nM 5.80
CHEMBL3894652 IC50 = 3981.07 nM 5.40
CHEMBL3978360 IC50 = 5011.87 nM 5.30
CHEMBL3983619 IC50 = 6309.57 nM 5.20