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Assay Detail

CHEMBL3614931

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

Binding
Inhibition of human ABHD6 expressed in HEK293 cells assessed as reduction in glycerol production from 1-AG hydrolysis pre-incubated for 30 mins before 1-AG substrate addition and measured 90 mins post substrate addition by fluorescence method
14
Total Activities
7
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 14 6.60 7.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3613671 2 7.36
CHEMBL3613162 2 7.14
CHEMBL3613161 2 6.89
CHEMBL3613003 2 6.67
CHEMBL3613666 2 6.35
CHEMBL3613668 2 6.06
CHEMBL3401455 2 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3613671 IC50 = 43.65 nM 7.36
CHEMBL3613671 IC50 = 44.0 nM 7.36
CHEMBL3613162 IC50 = 73.0 nM 7.14
CHEMBL3613162 IC50 = 74.13 nM 7.13
CHEMBL3613161 IC50 = 130.0 nM 6.89
CHEMBL3613161 IC50 = 131.83 nM 6.88
CHEMBL3613003 IC50 = 216.0 nM 6.67
CHEMBL3613003 IC50 = 218.78 nM 6.66
CHEMBL3613666 IC50 = 446.68 nM 6.35
CHEMBL3613666 IC50 = 450.0 nM 6.35
CHEMBL3613668 IC50 = 870.96 nM 6.06
CHEMBL3613668 IC50 = 870.0 nM 6.06
CHEMBL3401455 IC50 = 1778.28 nM 5.75
CHEMBL3401455 IC50 = 1780.0 nM 5.75