Assay Detail
Binding
CHEMBL4356495
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant rat MGL 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 | 7.06 | 7.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4463191 | — | — | 1 | 7.35 |
| CHEMBL2391916 | — | — | 1 | 7.14 |
| CHEMBL4448448 | — | — | 1 | 7.08 |
| CHEMBL4536072 | — | — | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4463191 | — | IC50 | = | 44.9 | nM | 7.35 |
| CHEMBL2391916 | — | IC50 | = | 72.6 | nM | 7.14 |
| CHEMBL4448448 | — | IC50 | = | 82.7 | nM | 7.08 |
| CHEMBL4536072 | — | IC50 | = | 219.8 | nM | 6.66 |