Assay Detail
Binding
CHEMBL4376250
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mouse DAGL-alpha expressed in HEK293T cell membranes pre-incubated for 20 mins before PNP-butyrate substrate addition and measured after 30 mins by surrogate substrate assay
10
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure Kinetics Relationships and Molecular Dynamics Show Crucial Role for Heterocycle Leaving Group in Irreversible Diacylglycerol Lipase Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.12 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4447844 | — | — | 1 | 8.60 |
| CHEMBL3954476 | — | — | 1 | 8.52 |
| CHEMBL4437021 | — | — | 1 | 8.42 |
| CHEMBL4572363 | — | — | 2 | 6.68 |
| CHEMBL4532055 | — | — | 2 | 5.47 |
| CHEMBL4545496 | — | — | 1 | - |
| CHEMBL3895863 | — | — | 1 | - |
| CHEMBL2144065 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4447844 | — | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL3954476 | — | IC50 | = | 3.02 | nM | 8.52 |
| CHEMBL4437021 | — | IC50 | = | 3.802 | nM | 8.42 |
| CHEMBL4572363 | — | IC50 | = | 208.93 | nM | 6.68 |
| CHEMBL4572363 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4532055 | — | IC50 | = | 3388.44 | nM | 5.47 |
| CHEMBL4532055 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL4545496 | — | IC50 | > | 31622.78 | nM | - |
| CHEMBL3895863 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL2144065 | — | IC50 | < | 1.0 | nM | - |