Assay Detail
Binding
CHEMBL982702
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant DAGL-alpha-mediated sn-1-[14C]oleoyl-2-arachidonoyl-glycerol hydrolysis to 2-AG overexpressed in african green monkey COS7 cell membrane by scintillation counting
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | COS-7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Tetrahydrolipstatin analogues as modulators of endocannabinoid 2-arachidonoylglycerol metabolism.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 6.08 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL521157 | — | — | 1 | 7.80 |
| CHEMBL457232 | — | — | 1 | 7.46 |
| CHEMBL516323 | — | — | 1 | 7.37 |
| CHEMBL484393 | — | — | 1 | 7.00 |
| CHEMBL484215 | — | — | 1 | 6.37 |
| CHEMBL521467 | — | — | 1 | 6.34 |
| CHEMBL514886 | — | — | 1 | 6.22 |
| CHEMBL458828 | — | — | 1 | 6.10 |
| CHEMBL175247 | ORLISTAT | 4.0 | 1 | 6.00 |
| CHEMBL484392 | — | — | 1 | 5.96 |
| CHEMBL458827 | — | — | 1 | 5.55 |
| CHEMBL458622 | — | — | 1 | 5.30 |
| CHEMBL458972 | — | — | 1 | 4.60 |
| CHEMBL484371 | — | — | 1 | 4.60 |
| CHEMBL520494 | — | — | 1 | 4.60 |
| CHEMBL453289 | — | — | 1 | - |
| CHEMBL457736 | — | — | 1 | - |
| CHEMBL451312 | — | — | 1 | - |
| CHEMBL458108 | — | — | 1 | - |
| CHEMBL458090 | — | — | 1 | - |
| CHEMBL443980 | — | — | 1 | - |
| CHEMBL458623 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL521157 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL457232 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL516323 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL484393 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL484215 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL521467 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL514886 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL458828 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL175247 | ORLISTAT | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL484392 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL458827 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL458622 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL458972 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL484371 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL520494 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL453289 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL457736 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL451312 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL458108 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL458090 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL443980 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL458623 | — | IC50 | > | 25000.0 | nM | - |