Assay Detail
Binding
CHEMBL859079
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Displacement of [3H]SR-141716 from human CB1 receptor transfected in HEK293 cells
21
Total Activities
21
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 | Expert |
Publication
New bicyclic cannabinoid receptor-1 (CB1-R) antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 8.48 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL425047 | — | — | 1 | 9.70 |
| CHEMBL204188 | — | — | 1 | 9.52 |
| CHEMBL201565 | — | — | 1 | 9.22 |
| CHEMBL201602 | — | — | 1 | 9.22 |
| CHEMBL201520 | — | — | 1 | 9.00 |
| CHEMBL425762 | — | — | 1 | 9.00 |
| CHEMBL379246 | — | — | 1 | 9.00 |
| CHEMBL204339 | — | — | 1 | 8.74 |
| CHEMBL203925 | — | — | 1 | 8.70 |
| CHEMBL111 | RIMONABANT | 4.0 | 1 | 8.68 |
| CHEMBL202583 | — | — | 1 | 8.52 |
| CHEMBL202419 | — | — | 1 | 8.40 |
| CHEMBL379667 | — | — | 1 | 8.30 |
| CHEMBL201582 | — | — | 1 | 8.22 |
| CHEMBL381858 | — | — | 1 | 8.10 |
| CHEMBL201923 | — | — | 1 | 7.92 |
| CHEMBL370560 | — | — | 1 | 7.70 |
| CHEMBL201862 | — | — | 1 | 7.68 |
| CHEMBL201924 | — | — | 1 | 7.58 |
| CHEMBL380937 | — | — | 1 | 7.55 |
| CHEMBL201929 | — | — | 1 | 7.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL425047 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL204188 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL201565 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL201602 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL201520 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL425762 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL379246 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL204339 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL203925 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL111 | RIMONABANT | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL202583 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL202419 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL379667 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL201582 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL381858 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL201923 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL370560 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL201862 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL201924 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL380937 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL201929 | — | Ki | = | 38.0 | nM | 7.42 |