Assay Detail
Binding
CHEMBL2161050
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Inhibition of human MAGL assessed as [3H]-2-OG hydrolysis preincubated for 30 mins before [3H]-2-OG addition measured after 10 mins by liquid scintillation counting
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development and characterization of endocannabinoid hydrolases FAAH and MAGL inhibitors bearing a benzotriazol-1-yl carboxamide scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 7.45 | 9.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2159781 | — | — | 1 | 9.27 |
| CHEMBL2159805 | — | — | 1 | 8.70 |
| CHEMBL2159780 | — | — | 1 | 8.52 |
| CHEMBL2159800 | — | — | 1 | 8.52 |
| CHEMBL2159812 | — | — | 1 | 8.15 |
| CHEMBL2159798 | — | — | 1 | 8.10 |
| CHEMBL2159806 | — | — | 1 | 8.10 |
| CHEMBL2159803 | — | — | 1 | 8.05 |
| CHEMBL2159779 | — | — | 1 | 8.05 |
| CHEMBL2159801 | — | — | 1 | 8.00 |
| CHEMBL2159802 | — | — | 1 | 7.96 |
| CHEMBL2159804 | — | — | 1 | 7.92 |
| CHEMBL2159811 | — | — | 1 | 7.89 |
| CHEMBL2159795 | — | — | 1 | 7.72 |
| CHEMBL2159788 | — | — | 1 | 7.70 |
| CHEMBL2159797 | — | — | 1 | 7.68 |
| CHEMBL2159777 | — | — | 1 | 7.64 |
| CHEMBL2159782 | — | — | 1 | 7.52 |
| CHEMBL2159787 | — | — | 1 | 7.50 |
| CHEMBL2159778 | — | — | 1 | 7.48 |
| CHEMBL2159799 | — | — | 1 | 7.48 |
| CHEMBL2159809 | — | — | 1 | 7.44 |
| CHEMBL576786 | — | — | 1 | 7.43 |
| CHEMBL2159790 | — | — | 1 | 7.42 |
| CHEMBL2159794 | — | — | 1 | 7.39 |
| CHEMBL2159813 | — | — | 1 | 7.21 |
| CHEMBL2159789 | — | — | 1 | 7.20 |
| CHEMBL2159783 | — | — | 1 | 7.15 |
| CHEMBL2159808 | — | — | 1 | 6.99 |
| CHEMBL2159792 | — | — | 1 | 6.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2159781 | — | IC50 | = | 0.54 | nM | 9.27 |
| CHEMBL2159805 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2159800 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2159780 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2159812 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2159798 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2159806 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2159803 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL2159779 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL2159801 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2159802 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2159804 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2159811 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2159795 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2159788 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2159797 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL2159777 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2159782 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2159787 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL2159778 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL2159799 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL2159809 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL576786 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL2159790 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL2159794 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL2159813 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL2159789 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL2159783 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL2159808 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL2159792 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL2159791 | — | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL2159784 | — | IC50 | = | 224.0 | nM | 6.65 |
| CHEMBL2159793 | — | IC50 | = | 234.0 | nM | 6.63 |
| CHEMBL2159810 | — | IC50 | = | 324.0 | nM | 6.49 |
| CHEMBL2159785 | — | IC50 | = | 372.0 | nM | 6.43 |
| CHEMBL2159807 | — | IC50 | = | 676.0 | nM | 6.17 |
| CHEMBL2159786 | — | IC50 | = | 955.0 | nM | 6.02 |
| CHEMBL2159796 | — | IC50 | = | 10471.0 | nM | 4.98 |