Assay Detail
Functional
CHEMBL2065579
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Antagonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP-55940-induced [35S]GTPgammaS binding incubated for 10 mins prior to CP-55940-challenge measured after 1 hr by beta counting
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| 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 | 21 | 9.41 | 10.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2063237 | — | — | 1 | 10.52 |
| CHEMBL2063236 | — | — | 1 | 10.40 |
| CHEMBL2063239 | — | — | 1 | 10.30 |
| CHEMBL2063240 | — | — | 1 | 10.15 |
| CHEMBL2063249 | — | — | 1 | 10.10 |
| CHEMBL2063246 | — | — | 1 | 10.10 |
| CHEMBL2063235 | — | — | 1 | 9.96 |
| CHEMBL2063245 | — | — | 1 | 9.96 |
| CHEMBL2063244 | — | — | 1 | 9.92 |
| CHEMBL2063248 | — | — | 1 | 9.64 |
| CHEMBL2063247 | — | — | 1 | 9.59 |
| CHEMBL2063243 | — | — | 1 | 9.14 |
| CHEMBL484929 | — | — | 1 | 9.09 |
| CHEMBL2063250 | — | — | 1 | 9.09 |
| CHEMBL2063122 | — | — | 1 | 9.06 |
| CHEMBL2063242 | — | — | 1 | 8.92 |
| CHEMBL111 | RIMONABANT | 4.0 | 1 | 8.80 |
| CHEMBL2063251 | — | — | 1 | 8.37 |
| CHEMBL2063241 | — | — | 1 | 8.25 |
| CHEMBL2063252 | — | — | 1 | 8.19 |
| CHEMBL2063238 | — | — | 1 | 8.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2063237 | — | Ki | = | 0.03 | nM | 10.52 |
| CHEMBL2063236 | — | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL2063239 | — | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL2063240 | — | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL2063249 | — | Ki | = | 0.08 | nM | 10.10 |
| CHEMBL2063246 | — | Ki | = | 0.08 | nM | 10.10 |
| CHEMBL2063235 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL2063245 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL2063244 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL2063248 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL2063247 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL2063243 | — | Ki | = | 0.72 | nM | 9.14 |
| CHEMBL484929 | — | Ki | = | 0.82 | nM | 9.09 |
| CHEMBL2063250 | — | Ki | = | 0.82 | nM | 9.09 |
| CHEMBL2063122 | — | Ki | = | 0.87 | nM | 9.06 |
| CHEMBL2063242 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL111 | RIMONABANT | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL2063251 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL2063241 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL2063252 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL2063238 | — | Ki | = | 7.5 | nM | 8.12 |