Assay Detail
Binding
CHEMBL963331
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Displacement of [3H]CP-55940 form human recombinant CB1 receptor expressed in HEK293 cells by liquid scintillation counting
15
Total Activities
15
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
Analogs of JHU75528, a PET ligand for imaging of cerebral cannabinoid receptors (CB1): development of ligands with optimized lipophilicity and binding affinity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 7.75 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL307696 | — | — | 1 | 8.82 |
| CHEMBL476404 | — | — | 1 | 8.70 |
| CHEMBL514361 | — | — | 1 | 8.33 |
| CHEMBL515022 | — | — | 1 | 7.99 |
| CHEMBL514215 | JHU-75528 | 1.0 | 1 | 7.96 |
| CHEMBL476232 | — | — | 1 | 7.89 |
| CHEMBL475977 | — | — | 1 | 7.85 |
| CHEMBL477642 | — | — | 1 | 7.62 |
| CHEMBL477004 | — | — | 1 | 7.50 |
| CHEMBL514845 | — | — | 1 | 7.48 |
| CHEMBL111 | RIMONABANT | 4.0 | 1 | 7.40 |
| CHEMBL476403 | — | — | 1 | 6.88 |
| CHEMBL476833 | — | — | 1 | 6.38 |
| CHEMBL476183 | — | — | 1 | - |
| CHEMBL514999 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL307696 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL476404 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL514361 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL515022 | — | Ki | = | 10.3 | nM | 7.99 |
| CHEMBL514215 | JHU-75528 | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL476232 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL475977 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL477642 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL477004 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL514845 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL111 | RIMONABANT | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL476403 | — | Ki | = | 131.0 | nM | 6.88 |
| CHEMBL476833 | — | Ki | = | 422.0 | nM | 6.38 |
| CHEMBL476183 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL514999 | — | Ki | > | 1000.0 | nM | - |