Assay Detail
Binding
CHEMBL1016398
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Displacement of [3H]SR141716A from CB1 receptor in rat brain
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 8.38 | 9.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL111 | RIMONABANT | 4.0 | 1 | 9.19 |
| CHEMBL522235 | — | — | 1 | 8.68 |
| CHEMBL562668 | OTENABANT | 3.0 | 1 | 8.55 |
| CHEMBL496770 | — | — | 1 | 8.44 |
| CHEMBL496352 | — | — | 1 | 8.38 |
| CHEMBL498411 | — | — | 1 | 8.23 |
| CHEMBL524087 | — | — | 1 | 7.92 |
| CHEMBL496555 | — | — | 1 | 7.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL111 | RIMONABANT | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL522235 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL562668 | OTENABANT | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL496770 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL496352 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL498411 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL524087 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL496555 | — | Ki | = | 24.0 | nM | 7.62 |