Assay Detail
Binding
CHEMBL1016399
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]SR141716A from human CB1 receptor expressed in HEK293 cells
8
Total Activities
8
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
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 | 8.52 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL562668 | OTENABANT | 3.0 | 1 | 9.15 |
| CHEMBL111 | RIMONABANT | 4.0 | 1 | 9.05 |
| CHEMBL522235 | — | — | 1 | 8.64 |
| CHEMBL496555 | — | — | 1 | 8.55 |
| CHEMBL498411 | — | — | 1 | 8.28 |
| CHEMBL496352 | — | — | 1 | 8.21 |
| CHEMBL524087 | — | — | 1 | 8.15 |
| CHEMBL496770 | — | — | 1 | 8.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL562668 | OTENABANT | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL111 | RIMONABANT | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL522235 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL496555 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL498411 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL496352 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL524087 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL496770 | — | Ki | = | 7.4 | nM | 8.13 |