Assay Detail
Binding
CHEMBL4356492
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Inhibition of recombinant rat MGL 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
23
Total Activities
23
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 | 23 | 6.82 | 7.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4536072 | — | — | 1 | 7.94 |
| CHEMBL4448448 | — | — | 1 | 7.78 |
| CHEMBL4463191 | — | — | 1 | 7.71 |
| CHEMBL4560077 | — | — | 1 | 7.66 |
| CHEMBL2391916 | — | — | 1 | 7.47 |
| CHEMBL4515209 | — | — | 1 | 7.27 |
| CHEMBL3219170 | — | — | 1 | 7.26 |
| CHEMBL1922513 | — | — | 1 | 7.23 |
| CHEMBL1710047 | — | — | 1 | 7.22 |
| CHEMBL4439900 | — | — | 1 | 7.03 |
| CHEMBL4558017 | — | — | 1 | 6.87 |
| CHEMBL4445264 | — | — | 1 | 6.79 |
| CHEMBL4514686 | — | — | 1 | 6.72 |
| CHEMBL4450432 | — | — | 1 | 6.71 |
| CHEMBL4544505 | — | — | 1 | 6.62 |
| CHEMBL4449771 | — | — | 1 | 6.56 |
| CHEMBL297304 | — | — | 1 | 6.51 |
| CHEMBL4553365 | — | — | 1 | 6.49 |
| CHEMBL4530292 | — | — | 1 | 6.29 |
| CHEMBL4438540 | — | — | 1 | 6.25 |
| CHEMBL4576162 | — | — | 1 | 6.12 |
| CHEMBL4548018 | — | — | 1 | 5.59 |
| CHEMBL4545305 | — | — | 1 | 4.88 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4536072 | — | IC50 | = | 11.5 | nM | 7.94 |
| CHEMBL4448448 | — | IC50 | = | 16.8 | nM | 7.78 |
| CHEMBL4463191 | — | IC50 | = | 19.5 | nM | 7.71 |
| CHEMBL4560077 | — | IC50 | = | 21.8 | nM | 7.66 |
| CHEMBL2391916 | — | IC50 | = | 34.1 | nM | 7.47 |
| CHEMBL4515209 | — | IC50 | = | 54.2 | nM | 7.27 |
| CHEMBL3219170 | — | IC50 | = | 55.5 | nM | 7.26 |
| CHEMBL1922513 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL1710047 | — | IC50 | = | 59.5 | nM | 7.22 |
| CHEMBL4439900 | — | IC50 | = | 93.9 | nM | 7.03 |
| CHEMBL4558017 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL4445264 | — | IC50 | = | 163.4 | nM | 6.79 |
| CHEMBL4514686 | — | IC50 | = | 189.4 | nM | 6.72 |
| CHEMBL4450432 | — | IC50 | = | 195.2 | nM | 6.71 |
| CHEMBL4544505 | — | IC50 | = | 237.9 | nM | 6.62 |
| CHEMBL4449771 | — | IC50 | = | 277.7 | nM | 6.56 |
| CHEMBL297304 | — | IC50 | = | 306.5 | nM | 6.51 |
| CHEMBL4553365 | — | IC50 | = | 322.1 | nM | 6.49 |
| CHEMBL4530292 | — | IC50 | = | 512.2 | nM | 6.29 |
| CHEMBL4438540 | — | IC50 | = | 568.0 | nM | 6.25 |
| CHEMBL4576162 | — | IC50 | = | 758.6 | nM | 6.12 |
| CHEMBL4548018 | — | IC50 | = | 2547.0 | nM | 5.59 |
| CHEMBL4545305 | — | IC50 | = | 13069.5 | nM | 4.88 |