Assay Detail
Binding
CHEMBL4356496
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant rat MGL C201A/C208A mutant expressed in human HeLa cells using 2-oleoylglycerol as substrate preincubated for 10 mins followed by substrate addition and measured after 10 mins by LC-MS analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HeLa |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Benzisothiazolinone Derivatives as Potent Allosteric Monoacylglycerol Lipase Inhibitors That Functionally Mimic Sulfenylation of Regulatory Cysteines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 5.96 | 6.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2391916 | — | — | 1 | 6.22 |
| CHEMBL4463191 | — | — | 1 | 6.11 |
| CHEMBL4536072 | — | — | 1 | 5.83 |
| CHEMBL4448448 | — | — | 1 | 5.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2391916 | — | IC50 | = | 604.7 | nM | 6.22 |
| CHEMBL4463191 | — | IC50 | = | 782.0 | nM | 6.11 |
| CHEMBL4536072 | — | IC50 | = | 1460.7 | nM | 5.83 |
| CHEMBL4448448 | — | IC50 | = | 2079.6 | nM | 5.68 |