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Assay Detail

CHEMBL3614949

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

Binding
Inhibition of human ABHD6 expressed in HEK293 cells at 1 uM pre-incubated for 10 mins before 2-AG substrate addition followed by rapid 40 fold compound dilution measured after 10 mins by HPLC method
3
Total Activities
3
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

Monoacylglycerol lipase ABHD6 (CHEMBL2189127)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Revisiting 1,3,4-Oxadiazol-2-ones: Utilization in the Development of ABHD6 Inhibitors.
Patel JZ, van Bruchem J, Laitinen T, Kaczor AA, Navia-Paldanius D, Parkkari T, Savinainen JR, Laitinen JT, Nevalainen TJ.
Bioorg Med Chem (2015) 23 : 6335 -6345
PubMed 26344596 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.77 7.88

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL175247 ORLISTAT 4.0 1 7.88
CHEMBL3613671 1 7.04
CHEMBL3613003 1 5.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL175247 ORLISTAT IC50 = 13.18 nM 7.88
CHEMBL3613671 IC50 = 91.2 nM 7.04
CHEMBL3613003 IC50 = 4073.8 nM 5.39