Assay Detail
Binding
CHEMBL4629361
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Reversible inhibition of human MAGL L179S/L186S mutant using 4-methylumbelliferyl butyrate as substrate measured after 5 mins by fluorescence assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
The discovery of diazetidinyl diamides as potent and reversible inhibitors of monoacylglycerol lipase (MAGL).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.47 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4647633 | — | — | 1 | 8.22 |
| CHEMBL4643128 | — | — | 1 | 8.15 |
| CHEMBL1615314 | — | — | 1 | 8.00 |
| CHEMBL4642828 | — | — | 1 | 7.82 |
| CHEMBL4642478 | — | — | 1 | 7.82 |
| CHEMBL4645891 | — | — | 1 | 7.82 |
| CHEMBL4645008 | — | — | 1 | 7.75 |
| CHEMBL4639530 | — | — | 1 | 7.72 |
| CHEMBL4649797 | — | — | 1 | 7.55 |
| CHEMBL4641944 | — | — | 1 | 7.51 |
| CHEMBL4633650 | — | — | 1 | 7.32 |
| CHEMBL4646726 | — | — | 1 | 6.57 |
| CHEMBL4638423 | — | — | 1 | 6.34 |
| CHEMBL4633969 | — | — | 1 | 6.03 |
| CHEMBL4647248 | — | — | 1 | - |
| CHEMBL4649126 | — | — | 1 | - |
| CHEMBL4637281 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4647633 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4643128 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1615314 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4642828 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4642478 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4645891 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4645008 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4639530 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4649797 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4641944 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4633650 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4646726 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4638423 | — | IC50 | = | 458.0 | nM | 6.34 |
| CHEMBL4633969 | — | IC50 | = | 939.0 | nM | 6.03 |
| CHEMBL4647248 | — | IC50 | < | 5.0 | nM | - |
| CHEMBL4649126 | — | IC50 | < | 5.0 | nM | - |
| CHEMBL4637281 | — | IC50 | < | 5.0 | nM | - |