Assay Detail
Binding
CHEMBL3768666
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Inhibition of full length human C-terminal HA-tagged DAGLalpha expressed in HEK293 cell membrane using DAG as substrate incubated for 20 mins by LC-MS analysis
31
Total Activities
31
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
Structure activity relationship studies on chemically non-reactive glycine sulfonamide inhibitors of diacylglycerol lipase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 7.52 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3764017 | — | — | 1 | 9.22 |
| CHEMBL3765578 | — | — | 1 | 9.05 |
| CHEMBL3764876 | — | — | 1 | 8.62 |
| CHEMBL3763826 | — | — | 1 | 8.52 |
| CHEMBL3765716 | — | — | 1 | 8.52 |
| CHEMBL3763853 | — | — | 1 | 8.52 |
| CHEMBL3763831 | — | — | 1 | 8.40 |
| CHEMBL3764093 | — | — | 1 | 8.22 |
| CHEMBL3765421 | — | — | 1 | 8.22 |
| CHEMBL3765022 | — | — | 1 | 8.10 |
| CHEMBL3763430 | — | — | 1 | 8.10 |
| CHEMBL3765158 | — | — | 1 | 7.96 |
| CHEMBL3765824 | — | — | 1 | 7.80 |
| CHEMBL3764778 | — | — | 1 | 7.77 |
| CHEMBL3764377 | — | — | 1 | 7.77 |
| CHEMBL3765573 | — | — | 1 | 7.75 |
| CHEMBL3765497 | — | — | 1 | 7.72 |
| CHEMBL3765546 | — | — | 1 | 7.52 |
| CHEMBL3764349 | — | — | 1 | 7.40 |
| CHEMBL3765562 | — | — | 1 | 7.35 |
| CHEMBL3764044 | — | — | 1 | 7.26 |
| CHEMBL3763964 | — | — | 1 | 7.22 |
| CHEMBL3765750 | — | — | 1 | 7.10 |
| CHEMBL3765634 | — | — | 1 | 7.10 |
| CHEMBL3764007 | — | — | 1 | 6.89 |
| CHEMBL3764430 | — | — | 1 | 6.79 |
| CHEMBL3763708 | — | — | 1 | 6.29 |
| CHEMBL3763737 | — | — | 1 | 4.87 |
| CHEMBL3764425 | — | — | 1 | 4.85 |
| CHEMBL3763376 | — | — | 1 | 4.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3764017 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3765578 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3764876 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3763826 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3765716 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3763853 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3763831 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3764093 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3765421 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3765022 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3763430 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3765158 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3765824 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3764778 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3764377 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3765573 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3765497 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3765546 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3764349 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3765562 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL3764044 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL3763964 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3765750 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3765634 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3764007 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3764430 | — | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL3763708 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL3763737 | — | IC50 | = | 13500.0 | nM | 4.87 |
| CHEMBL3764425 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL3763376 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL3764769 | — | IC50 | > | 30000.0 | nM | - |