Assay Detail
Binding
CHEMBL932400
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]CP-55940 from human CB1R expressed in HEK293 cells
33
Total Activities
33
Compounds Tested
2
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
Benzodioxoles: novel cannabinoid-1 receptor inverse agonists for the treatment of obesity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 32 | 7.70 | 9.00 |
| IC50 | 1 | 9.52 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL220360 | TARANABANT | 3.0 | 1 | 9.52 |
| CHEMBL410339 | — | — | 1 | 9.00 |
| CHEMBL263391 | — | — | 1 | 8.70 |
| CHEMBL409471 | — | — | 1 | 8.52 |
| CHEMBL258539 | — | — | 1 | 8.48 |
| CHEMBL258753 | — | — | 1 | 8.40 |
| CHEMBL259656 | — | — | 1 | 8.40 |
| CHEMBL408427 | — | — | 1 | 8.40 |
| CHEMBL111 | RIMONABANT | 4.0 | 1 | 8.22 |
| CHEMBL259654 | — | — | 1 | 8.22 |
| CHEMBL409472 | — | — | 1 | 8.15 |
| CHEMBL409217 | — | — | 1 | 8.15 |
| CHEMBL412262 | IBIPINABANT | 2.0 | 1 | 8.10 |
| CHEMBL262857 | — | — | 1 | 8.05 |
| CHEMBL260625 | — | — | 1 | 7.96 |
| CHEMBL262858 | — | — | 1 | 7.89 |
| CHEMBL259339 | — | — | 1 | 7.89 |
| CHEMBL410248 | — | — | 1 | 7.82 |
| CHEMBL259699 | — | — | 1 | 7.75 |
| CHEMBL410247 | — | — | 1 | 7.60 |
| CHEMBL259425 | — | — | 1 | 7.55 |
| CHEMBL260810 | — | — | 1 | 7.52 |
| CHEMBL261037 | — | — | 1 | 7.46 |
| CHEMBL411054 | — | — | 1 | 7.42 |
| CHEMBL409441 | — | — | 1 | 7.34 |
| CHEMBL260284 | — | — | 1 | 7.30 |
| CHEMBL259651 | — | — | 1 | 6.96 |
| CHEMBL405888 | — | — | 1 | 6.67 |
| CHEMBL263128 | — | — | 1 | 6.56 |
| CHEMBL263129 | — | — | 1 | 6.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL220360 | TARANABANT | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL410339 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL263391 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL409471 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL258539 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL258753 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL259656 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL408427 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL111 | RIMONABANT | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL259654 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL409472 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL409217 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL412262 | IBIPINABANT | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL262857 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL260625 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL259339 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL262858 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL410248 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL259699 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL410247 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL259425 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL260810 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL261037 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL411054 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL409441 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL260284 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL259651 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL405888 | — | Ki | = | 216.0 | nM | 6.67 |
| CHEMBL263128 | — | Ki | = | 277.0 | nM | 6.56 |
| CHEMBL263129 | — | Ki | = | 509.0 | nM | 6.29 |
| CHEMBL263390 | — | Ki | = | 873.0 | nM | 6.06 |
| CHEMBL259652 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL428257 | — | Ki | > | 1000.0 | nM | - |