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Assay Detail

CHEMBL3373886

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

Binding
Inhibition of human DAGLalpha expressed in HEK293T cell membranes
21
Total Activities
21
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
IC50 21 6.80 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3319620 1 7.75
CHEMBL3319619 1 7.25
CHEMBL3319622 1 7.19
CHEMBL3319625 1 7.18
CHEMBL3319623 1 7.04
CHEMBL3319621 1 6.84
CHEMBL3319618 1 6.73
CHEMBL3319629 1 6.52
CHEMBL3319637 1 6.29
CHEMBL3319626 1 6.16
CHEMBL3319624 1 5.80
CHEMBL3319630 1 -
CHEMBL3319628 1 -
CHEMBL3319627 1 -
CHEMBL3319631 1 -
CHEMBL3319632 1 -
CHEMBL3319633 1 -
CHEMBL3319634 1 -
CHEMBL3319635 1 -
CHEMBL3319636 1 -
CHEMBL3319638 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3319620 IC50 = 18.0 nM 7.75
CHEMBL3319619 IC50 = 56.0 nM 7.25
CHEMBL3319622 IC50 = 65.0 nM 7.19
CHEMBL3319625 IC50 = 66.0 nM 7.18
CHEMBL3319623 IC50 = 91.0 nM 7.04
CHEMBL3319621 IC50 = 143.0 nM 6.84
CHEMBL3319618 IC50 = 185.0 nM 6.73
CHEMBL3319629 IC50 = 302.0 nM 6.52
CHEMBL3319637 IC50 = 512.0 nM 6.29
CHEMBL3319626 IC50 = 695.0 nM 6.16
CHEMBL3319624 IC50 = 1600.0 nM 5.80
CHEMBL3319630 IC50 > 10000.0 nM -
CHEMBL3319628 IC50 > 10000.0 nM -
CHEMBL3319627 IC50 > 10000.0 nM -
CHEMBL3319631 IC50 > 10000.0 nM -
CHEMBL3319632 IC50 > 10000.0 nM -
CHEMBL3319633 IC50 > 10000.0 nM -
CHEMBL3319634 IC50 > 10000.0 nM -
CHEMBL3319635 IC50 > 10000.0 nM -
CHEMBL3319636 IC50 > 10000.0 nM -
CHEMBL3319638 IC50 > 10000.0 nM -