Assay Detail
Functional
CHEMBL954070
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Antagonist activity at human CB1 receptor expressed in SF9 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Aminopyrazine CB1 receptor inverse agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 8.77 | 9.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL497557 | — | — | 1 | 9.62 |
| CHEMBL111 | RIMONABANT | 4.0 | 1 | 9.37 |
| CHEMBL496507 | — | — | 1 | 9.17 |
| CHEMBL524804 | — | — | 1 | 9.10 |
| CHEMBL496091 | — | — | 1 | 9.08 |
| CHEMBL496508 | — | — | 1 | 9.06 |
| CHEMBL496293 | — | — | 1 | 9.04 |
| CHEMBL498783 | — | — | 1 | 8.92 |
| CHEMBL522720 | — | — | 1 | 8.78 |
| CHEMBL496919 | — | — | 1 | 8.76 |
| CHEMBL497556 | — | — | 1 | 8.71 |
| CHEMBL495892 | — | — | 1 | 8.55 |
| CHEMBL522395 | — | — | 1 | 8.01 |
| CHEMBL495891 | — | — | 1 | 7.83 |
| CHEMBL496506 | — | — | 1 | 7.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL497557 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL111 | RIMONABANT | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL496507 | — | Ki | = | 0.67 | nM | 9.17 |
| CHEMBL524804 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL496091 | — | Ki | = | 0.83 | nM | 9.08 |
| CHEMBL496508 | — | Ki | = | 0.87 | nM | 9.06 |
| CHEMBL496293 | — | Ki | = | 0.91 | nM | 9.04 |
| CHEMBL498783 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL522720 | — | Ki | = | 1.66 | nM | 8.78 |
| CHEMBL496919 | — | Ki | = | 1.75 | nM | 8.76 |
| CHEMBL497556 | — | Ki | = | 1.97 | nM | 8.71 |
| CHEMBL495892 | — | Ki | = | 2.84 | nM | 8.55 |
| CHEMBL522395 | — | Ki | = | 9.81 | nM | 8.01 |
| CHEMBL495891 | — | Ki | = | 14.96 | nM | 7.83 |
| CHEMBL496506 | — | Ki | = | 32.33 | nM | 7.49 |