Assay Detail
Binding
CHEMBL2065576
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Displacement of [3H]SR141716A form human CB1 receptor expressed in HEK293 cells after 60 mins by beta counting
23
Total Activities
23
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
Design of a Potent CB1 Receptor Antagonist Series: Potential Scaffold for Peripherally-Targeted Agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 9.07 | 10.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2063240 | — | — | 1 | 10.05 |
| CHEMBL2063245 | — | — | 1 | 9.92 |
| CHEMBL2063246 | — | — | 1 | 9.89 |
| CHEMBL2063237 | — | — | 1 | 9.85 |
| CHEMBL2063236 | — | — | 1 | 9.80 |
| CHEMBL2063243 | — | — | 1 | 9.60 |
| CHEMBL2063244 | — | — | 1 | 9.59 |
| CHEMBL2063235 | — | — | 1 | 9.39 |
| CHEMBL2063250 | — | — | 1 | 9.27 |
| CHEMBL2063248 | — | — | 1 | 9.26 |
| CHEMBL2063242 | — | — | 1 | 9.25 |
| CHEMBL2063239 | — | — | 1 | 9.23 |
| CHEMBL2063122 | — | — | 1 | 9.12 |
| CHEMBL484929 | — | — | 1 | 9.00 |
| CHEMBL2063252 | — | — | 1 | 9.00 |
| CHEMBL2063241 | — | — | 1 | 8.85 |
| CHEMBL2063247 | — | — | 1 | 8.80 |
| CHEMBL2063249 | — | — | 1 | 8.77 |
| CHEMBL111 | RIMONABANT | 4.0 | 1 | 8.74 |
| CHEMBL2063251 | — | — | 1 | 8.35 |
| CHEMBL2063238 | — | — | 1 | 8.29 |
| CHEMBL2063121 | — | — | 1 | 7.34 |
| CHEMBL2063120 | — | — | 1 | 7.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2063240 | — | Ki | = | 0.09 | nM | 10.05 |
| CHEMBL2063245 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL2063246 | — | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL2063237 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL2063236 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL2063243 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL2063244 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL2063235 | — | Ki | = | 0.41 | nM | 9.39 |
| CHEMBL2063250 | — | Ki | = | 0.54 | nM | 9.27 |
| CHEMBL2063248 | — | Ki | = | 0.55 | nM | 9.26 |
| CHEMBL2063242 | — | Ki | = | 0.56 | nM | 9.25 |
| CHEMBL2063239 | — | Ki | = | 0.59 | nM | 9.23 |
| CHEMBL2063122 | — | Ki | = | 0.75 | nM | 9.12 |
| CHEMBL484929 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL2063252 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL2063241 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL2063247 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL2063249 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL111 | RIMONABANT | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL2063251 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL2063238 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL2063121 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL2063120 | — | Ki | = | 57.0 | nM | 7.24 |