Assay Detail
Binding
CHEMBL4424599
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Inhibition of human recombinant MAGL using 4-NPA as substrate after 30 mins
34
Total Activities
34
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
Optimization of a Benzoylpiperidine Class Identifies a Highly Potent and Selective Reversible Monoacylglycerol Lipase (MAGL) Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 6.19 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3901007 | — | — | 1 | 8.52 |
| CHEMBL576786 | — | — | 1 | 7.31 |
| CHEMBL4575018 | — | — | 1 | 7.13 |
| CHEMBL4536045 | — | — | 1 | 7.10 |
| CHEMBL4534867 | — | — | 1 | 6.96 |
| CHEMBL4436371 | — | — | 1 | 6.87 |
| CHEMBL570812 | — | — | 1 | 6.87 |
| CHEMBL4435479 | — | — | 1 | 6.86 |
| CHEMBL4449639 | — | — | 1 | 6.79 |
| CHEMBL4474818 | — | — | 1 | 6.71 |
| CHEMBL4472877 | — | — | 1 | 6.62 |
| CHEMBL4466342 | — | — | 1 | 6.58 |
| CHEMBL4559346 | — | — | 1 | 6.43 |
| CHEMBL4549211 | — | — | 1 | 6.41 |
| CHEMBL4471924 | — | — | 1 | 6.37 |
| CHEMBL4463252 | — | — | 1 | 6.34 |
| CHEMBL4282040 | — | — | 1 | 6.08 |
| CHEMBL4468362 | — | — | 1 | 6.02 |
| CHEMBL4542020 | — | — | 1 | 6.00 |
| CHEMBL4442280 | — | — | 1 | 5.96 |
| CHEMBL4468596 | — | — | 1 | 5.89 |
| CHEMBL4592963 | — | — | 1 | 5.89 |
| CHEMBL4530498 | — | — | 1 | 5.89 |
| CHEMBL4568297 | — | — | 1 | 5.85 |
| CHEMBL4475604 | — | — | 1 | 5.66 |
| CHEMBL4468106 | — | — | 1 | 5.62 |
| CHEMBL4527656 | — | — | 1 | 5.60 |
| CHEMBL4553078 | — | — | 1 | 5.58 |
| CHEMBL4577085 | — | — | 1 | 5.30 |
| CHEMBL4552228 | — | — | 1 | 5.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3901007 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL576786 | — | IC50 | = | 49.3 | nM | 7.31 |
| CHEMBL4575018 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL4536045 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4534867 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4436371 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL570812 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL4435479 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL4449639 | — | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL4474818 | — | IC50 | = | 194.0 | nM | 6.71 |
| CHEMBL4472877 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4466342 | — | IC50 | = | 262.0 | nM | 6.58 |
| CHEMBL4559346 | — | IC50 | = | 368.0 | nM | 6.43 |
| CHEMBL4549211 | — | IC50 | = | 389.0 | nM | 6.41 |
| CHEMBL4471924 | — | IC50 | = | 424.0 | nM | 6.37 |
| CHEMBL4463252 | — | IC50 | = | 457.0 | nM | 6.34 |
| CHEMBL4282040 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL4468362 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL4542020 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4442280 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4468596 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4592963 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4530498 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4568297 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4475604 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4468106 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL4527656 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4553078 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL4577085 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL4552228 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL4587797 | — | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL4451621 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL4465086 | — | IC50 | = | 10200.0 | nM | 4.99 |
| CHEMBL4587625 | — | IC50 | = | 12300.0 | nM | 4.91 |