Assay Detail
Binding
CHEMBL3384490
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Inhibition of human recombinant MAGL expressed in HEK293 cells using 2-AG as substrate
39
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Piperazine and piperidine carboxamides and carbamates as inhibitors of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 7.37 | 9.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3087181 | — | — | 2 | 9.44 |
| CHEMBL3356971 | — | — | 2 | 9.26 |
| CHEMBL3356985 | — | — | 1 | 9.16 |
| CHEMBL1232635 | — | — | 2 | 9.07 |
| CHEMBL3356956 | — | — | 2 | 8.89 |
| CHEMBL3356957 | — | — | 2 | 8.77 |
| CHEMBL3356975 | — | — | 2 | 8.26 |
| CHEMBL3356974 | — | — | 2 | 8.11 |
| CHEMBL3356981 | — | — | 2 | 7.38 |
| CHEMBL3356979 | — | — | 2 | 7.16 |
| CHEMBL3356976 | — | — | 2 | 7.13 |
| CHEMBL3356960 | — | — | 2 | 6.88 |
| CHEMBL3352862 | — | — | 2 | 6.59 |
| CHEMBL3356959 | — | — | 2 | 6.56 |
| CHEMBL602499 | — | — | 2 | 6.46 |
| CHEMBL3356980 | — | — | 2 | 6.18 |
| CHEMBL3356978 | — | — | 2 | 5.96 |
| CHEMBL3356962 | — | — | 2 | 5.78 |
| CHEMBL3356961 | — | — | 2 | 5.72 |
| CHEMBL3356977 | — | — | 2 | 5.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3087181 | — | IC50 | = | 0.3631 | nM | 9.44 |
| CHEMBL3087181 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3356971 | — | IC50 | = | 0.5495 | nM | 9.26 |
| CHEMBL3356971 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3356985 | — | IC50 | = | 0.6918 | nM | 9.16 |
| CHEMBL1232635 | — | IC50 | = | 0.8511 | nM | 9.07 |
| CHEMBL1232635 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3356956 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3356956 | — | IC50 | = | 1.318 | nM | 8.88 |
| CHEMBL3356957 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3356957 | — | IC50 | = | 1.698 | nM | 8.77 |
| CHEMBL3356975 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL3356975 | — | IC50 | = | 5.495 | nM | 8.26 |
| CHEMBL3356974 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL3356974 | — | IC50 | = | 7.762 | nM | 8.11 |
| CHEMBL3356981 | — | IC50 | = | 41.69 | nM | 7.38 |
| CHEMBL3356981 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL3356979 | — | IC50 | = | 69.18 | nM | 7.16 |
| CHEMBL3356979 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3356976 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL3356976 | — | IC50 | = | 74.13 | nM | 7.13 |
| CHEMBL3356960 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL3356960 | — | IC50 | = | 131.83 | nM | 6.88 |
| CHEMBL3352862 | — | IC50 | = | 257.04 | nM | 6.59 |
| CHEMBL3352862 | — | IC50 | = | 257.0 | nM | 6.59 |
| CHEMBL3356959 | — | IC50 | = | 275.42 | nM | 6.56 |
| CHEMBL3356959 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL602499 | — | IC50 | = | 346.74 | nM | 6.46 |
| CHEMBL602499 | — | IC50 | = | 347.0 | nM | 6.46 |
| CHEMBL3356980 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL3356980 | — | IC50 | = | 660.69 | nM | 6.18 |
| CHEMBL3356978 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3356978 | — | IC50 | = | 1122.02 | nM | 5.95 |
| CHEMBL3356962 | — | IC50 | = | 1660.0 | nM | 5.78 |
| CHEMBL3356962 | — | IC50 | = | 1659.59 | nM | 5.78 |
| CHEMBL3356961 | — | IC50 | = | 1905.46 | nM | 5.72 |
| CHEMBL3356961 | — | IC50 | = | 1905.0 | nM | 5.72 |
| CHEMBL3356977 | — | IC50 | = | 2844.0 | nM | 5.55 |
| CHEMBL3356977 | — | IC50 | = | 2818.38 | nM | 5.55 |