Assay Detail
Binding
CHEMBL1040738
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]CP-55940 from human CB1 receptor expressed in CHO cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Design, synthesis, biological properties, and molecular modeling investigations of novel tacrine derivatives with a combination of acetylcholinesterase inhibition and cannabinoid CB1 receptor antagonism.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 7.60 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL567228 | — | — | 1 | 8.51 |
| CHEMBL570623 | — | — | 1 | 8.02 |
| CHEMBL583855 | — | — | 1 | 7.85 |
| CHEMBL566388 | — | — | 1 | 7.72 |
| CHEMBL158784 | RAC-IBIPINABANT | — | 1 | 7.60 |
| CHEMBL558598 | RIMONABANT HYDROCHLORIDE | — | 1 | 7.60 |
| CHEMBL576673 | — | — | 1 | 7.57 |
| CHEMBL585736 | — | — | 1 | 7.51 |
| CHEMBL571730 | — | — | 1 | 7.38 |
| CHEMBL569547 | — | — | 1 | 7.37 |
| CHEMBL570159 | — | — | 1 | 7.32 |
| CHEMBL570158 | — | — | 1 | 7.27 |
| CHEMBL567532 | — | — | 1 | 7.06 |
| CHEMBL95 | TACRINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL567228 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL570623 | — | Ki | = | 9.6 | nM | 8.02 |
| CHEMBL583855 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL566388 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL158784 | RAC-IBIPINABANT | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL558598 | RIMONABANT HYDROCHLORIDE | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL576673 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL585736 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL571730 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL569547 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL570159 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL570158 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL567532 | — | Ki | = | 88.0 | nM | 7.06 |
| CHEMBL95 | TACRINE | Ki | > | 1000.0 | nM | - |