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Assay Detail

CHEMBL4262256

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

Binding
Inhibition of recombinant human DAGLalpha expressed in HEK293 cells using PNP-butyrate as substrate pretreated for 20 to 30 mins followed by substrate addition measured every 60 secs for 20 mins by colorimetric method
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Chiral disubstituted piperidinyl ureas: a class of dual diacylglycerol lipase-α and ABHD6 inhibitors.
Deng H, van der Wel T, van den Berg RJBHN, van den Nieuwendijk AMCH, Janssen FJ, Baggelaar MP, Overkleeft HS, van der Stelt M.
Medchemcomm (2017) 8 : 982 -988
PubMed 30108813 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.59 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3906477 1 9.10
CHEMBL4279328 1 9.10
CHEMBL4294845 1 7.80
CHEMBL4287766 1 7.80
CHEMBL4281906 1 7.80
CHEMBL4284689 1 7.60
CHEMBL4281842 1 7.60
CHEMBL4289572 1 7.60
CHEMBL4277989 1 7.50
CHEMBL3934441 1 7.40
CHEMBL4279884 1 7.10
CHEMBL4291201 1 7.10
CHEMBL4288486 1 6.80
CHEMBL4289712 1 5.90
CHEMBL4283505 1 -
CHEMBL4294085 1 -
CHEMBL4290683 1 -
CHEMBL4286853 1 -
CHEMBL4278939 1 -
CHEMBL4276750 1 -
CHEMBL4277826 1 -
CHEMBL4278232 1 -
CHEMBL4290942 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3906477 IC50 = 0.7943 nM 9.10
CHEMBL4279328 IC50 = 0.7943 nM 9.10
CHEMBL4294845 IC50 = 15.85 nM 7.80
CHEMBL4287766 IC50 = 15.85 nM 7.80
CHEMBL4281906 IC50 = 15.85 nM 7.80
CHEMBL4284689 IC50 = 25.12 nM 7.60
CHEMBL4281842 IC50 = 25.12 nM 7.60
CHEMBL4289572 IC50 = 25.12 nM 7.60
CHEMBL4277989 IC50 = 31.62 nM 7.50
CHEMBL3934441 IC50 = 39.81 nM 7.40
CHEMBL4279884 IC50 = 79.43 nM 7.10
CHEMBL4291201 IC50 = 79.43 nM 7.10
CHEMBL4288486 IC50 = 158.49 nM 6.80
CHEMBL4289712 IC50 = 1258.93 nM 5.90
CHEMBL4283505 IC50 > 10000.0 nM -
CHEMBL4294085 IC50 > 10000.0 nM -
CHEMBL4290683 IC50 > 10000.0 nM -
CHEMBL4286853 IC50 > 10000.0 nM -
CHEMBL4278939 IC50 > 10000.0 nM -
CHEMBL4276750 IC50 > 10000.0 nM -
CHEMBL4277826 IC50 > 10000.0 nM -
CHEMBL4278232 IC50 > 10000.0 nM -
CHEMBL4290942 IC50 > 10000.0 nM -