Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5738731

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

Binding
Biological Assay: The assay used to measure the in vitro activity of MGL is adapted from the assay used for another serine hydrolase (FAAH) described in Wilson et al., 2003 (A high-throughput-compatible assay for determining the activity of fatty acid amide hydrolase. Wilson S J, Lovenberg T W, Barbier A J. Anal Biochem. 2003 Jul. 15; 318(2):270-5). The assay consists of combining endogenously expressed MGL from HeLa cells with test compounds, adding [glycerol-1,3-3H]-oleoyl glycerol, incubating for one hour, and then measuring the amount of cleaved [1,3-3H]-glycerol that passes through an activated carbon filter. The amount of cleaved, tritiated glycerol passing through the carbon filter is proportional to the activity of the MGL enzyme in a particular well/test condition.
ChEMBL ↗
237
Total Activities
71
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Target

Monoglyceride lipase (CHEMBL4191) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Azaspirocycles as monoacylglycerol lipase modulators
(2022)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 79 9.05 10.85
kon 79 - -
k_off 79 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5785193 — — 3 10.85
CHEMBL5832941 — — 3 10.57
CHEMBL5892322 — — 3 10.41
CHEMBL5996643 — — 6 10.39
CHEMBL5793684 — — 3 10.32
CHEMBL5941658 — — 3 10.09
CHEMBL5901923 — — 3 10.07
CHEMBL5747079 — — 3 10.06
CHEMBL6030416 — — 3 10.03
CHEMBL5751521 — — 6 10.02
CHEMBL5783701 — — 3 10.01
CHEMBL6025412 — — 3 10.00
CHEMBL5977282 — — 3 10.00
CHEMBL5992406 — — 6 10.00
CHEMBL6043445 — — 3 9.96
CHEMBL5809976 — — 3 9.96
CHEMBL5766234 — — 6 9.96
CHEMBL6017690 — — 3 9.77
CHEMBL6029674 — — 3 9.68
CHEMBL5806570 — — 3 9.64
CHEMBL5856728 — — 6 9.60
CHEMBL5748180 — — 3 9.55
CHEMBL5924021 — — 3 9.55
CHEMBL5998656 — — 3 9.52
CHEMBL5903041 — — 3 9.49
CHEMBL6061710 — — 3 9.46
CHEMBL6034498 — — 3 9.40
CHEMBL5759972 — — 3 9.31
CHEMBL5861814 — — 3 9.27
CHEMBL5813078 — — 3 9.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5785193 — IC50 = 0.014 nM 10.85
CHEMBL5832941 — IC50 = 0.027 nM 10.57
CHEMBL5892322 — IC50 = 0.039 nM 10.41
CHEMBL5996643 — IC50 = 0.041 nM 10.39
CHEMBL5793684 — IC50 = 0.048 nM 10.32
CHEMBL5941658 — IC50 = 0.082 nM 10.09
CHEMBL5901923 — IC50 = 0.086 nM 10.07
CHEMBL5747079 — IC50 = 0.088 nM 10.06
CHEMBL6030416 — IC50 = 0.094 nM 10.03
CHEMBL5751521 — IC50 = 0.095 nM 10.02
CHEMBL5783701 — IC50 = 0.097 nM 10.01
CHEMBL5977282 — IC50 = 0.1 nM 10.00
CHEMBL5992406 — IC50 = 0.1 nM 10.00
CHEMBL6025412 — IC50 = 0.1 nM 10.00
CHEMBL6043445 — IC50 = 0.11 nM 9.96
CHEMBL5766234 — IC50 = 0.11 nM 9.96
CHEMBL5809976 — IC50 = 0.11 nM 9.96
CHEMBL6017690 — IC50 = 0.17 nM 9.77
CHEMBL6029674 — IC50 = 0.21 nM 9.68
CHEMBL5806570 — IC50 = 0.23 nM 9.64
CHEMBL5856728 — IC50 = 0.25 nM 9.60
CHEMBL5924021 — IC50 = 0.28 nM 9.55
CHEMBL5748180 — IC50 = 0.28 nM 9.55
CHEMBL5998656 — IC50 = 0.3 nM 9.52
CHEMBL5903041 — IC50 = 0.32 nM 9.49
CHEMBL6061710 — IC50 = 0.35 nM 9.46
CHEMBL5751521 — IC50 = 0.36 nM 9.44
CHEMBL6034498 — IC50 = 0.4 nM 9.40
CHEMBL5759972 — IC50 = 0.49 nM 9.31
CHEMBL5861814 — IC50 = 0.54 nM 9.27
CHEMBL5813078 — IC50 = 0.62 nM 9.21
CHEMBL5892929 — IC50 = 0.71 nM 9.15
CHEMBL5823173 — IC50 = 0.73 nM 9.14
CHEMBL5856182 — IC50 = 0.82 nM 9.09
CHEMBL5796272 — IC50 = 0.86 nM 9.07
CHEMBL5992406 — IC50 = 0.87 nM 9.06
CHEMBL5866689 — IC50 = 0.87 nM 9.06
CHEMBL6017398 — IC50 = 0.9 nM 9.05
CHEMBL6057035 — IC50 = 0.9 nM 9.05
CHEMBL6046201 — IC50 = 1.0 nM 9.00
CHEMBL5822201 — IC50 = 1.0 nM 9.00
CHEMBL5864923 — IC50 = 1.1 nM 8.96
CHEMBL5955363 — IC50 = 1.1 nM 8.96
CHEMBL6002098 — IC50 = 1.1 nM 8.96
CHEMBL5866293 — IC50 = 1.3 nM 8.89
CHEMBL5996643 — IC50 = 1.4 nM 8.85
CHEMBL6055648 — IC50 = 1.4 nM 8.85
CHEMBL5856728 — IC50 = 1.5 nM 8.82
CHEMBL5796666 — IC50 = 1.6 nM 8.80
CHEMBL5898827 — IC50 = 1.7 nM 8.77