Assay Detail
Binding
CHEMBL1059680
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Displacement of [3H]rimonabant from human CB1 receptor expressed in HEK293 cells by liquid scintillation counting
33
Total Activities
33
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 | Intermediate |
Publication
Discovery and functional evaluation of diverse novel human CB(1) receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 33 | 6.32 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL220360 | TARANABANT | 3.0 | 1 | 9.52 |
| CHEMBL111 | RIMONABANT | 4.0 | 1 | 8.72 |
| CHEMBL230356 | — | — | 1 | 8.66 |
| CHEMBL412262 | IBIPINABANT | 2.0 | 1 | 8.11 |
| CHEMBL554943 | — | — | 1 | 6.64 |
| CHEMBL560462 | — | — | 1 | 6.59 |
| CHEMBL560463 | — | — | 1 | 6.58 |
| CHEMBL555341 | — | — | 1 | 6.56 |
| CHEMBL557921 | — | — | 1 | 6.54 |
| CHEMBL565190 | — | — | 1 | 6.51 |
| CHEMBL560383 | — | — | 1 | 6.49 |
| CHEMBL550309 | — | — | 1 | 6.28 |
| CHEMBL563400 | — | — | 1 | 6.28 |
| CHEMBL559035 | — | — | 1 | 6.21 |
| CHEMBL562123 | — | — | 1 | 6.06 |
| CHEMBL549501 | — | — | 1 | 6.00 |
| CHEMBL550514 | — | — | 1 | 5.99 |
| CHEMBL563830 | — | — | 1 | 5.98 |
| CHEMBL561663 | — | — | 1 | 5.96 |
| CHEMBL551122 | — | — | 1 | 5.93 |
| CHEMBL562519 | — | — | 1 | 5.83 |
| CHEMBL555873 | — | — | 1 | 5.79 |
| CHEMBL564177 | — | — | 1 | 5.75 |
| CHEMBL556422 | — | — | 1 | 5.71 |
| CHEMBL549366 | — | — | 1 | 5.64 |
| CHEMBL564929 | — | — | 1 | 5.64 |
| CHEMBL552122 | — | — | 1 | 5.64 |
| CHEMBL551462 | — | — | 1 | 5.62 |
| CHEMBL564343 | — | — | 1 | 5.59 |
| CHEMBL562654 | — | — | 1 | 5.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL220360 | TARANABANT | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL111 | RIMONABANT | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL230356 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL412262 | IBIPINABANT | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL554943 | — | Ki | = | 227.0 | nM | 6.64 |
| CHEMBL560462 | — | Ki | = | 256.0 | nM | 6.59 |
| CHEMBL560463 | — | Ki | = | 264.0 | nM | 6.58 |
| CHEMBL555341 | — | Ki | = | 273.0 | nM | 6.56 |
| CHEMBL557921 | — | Ki | = | 287.0 | nM | 6.54 |
| CHEMBL565190 | — | Ki | = | 308.0 | nM | 6.51 |
| CHEMBL560383 | — | Ki | = | 325.0 | nM | 6.49 |
| CHEMBL550309 | — | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL563400 | — | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL559035 | — | Ki | = | 611.0 | nM | 6.21 |
| CHEMBL562123 | — | Ki | = | 875.0 | nM | 6.06 |
| CHEMBL549501 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL550514 | — | Ki | = | 1030.0 | nM | 5.99 |
| CHEMBL563830 | — | Ki | = | 1049.0 | nM | 5.98 |
| CHEMBL561663 | — | Ki | = | 1086.0 | nM | 5.96 |
| CHEMBL551122 | — | Ki | = | 1177.0 | nM | 5.93 |
| CHEMBL562519 | — | Ki | = | 1473.0 | nM | 5.83 |
| CHEMBL555873 | — | Ki | = | 1606.0 | nM | 5.79 |
| CHEMBL564177 | — | Ki | = | 1764.0 | nM | 5.75 |
| CHEMBL556422 | — | Ki | = | 1943.0 | nM | 5.71 |
| CHEMBL549366 | — | Ki | = | 2269.0 | nM | 5.64 |
| CHEMBL564929 | — | Ki | = | 2299.0 | nM | 5.64 |
| CHEMBL552122 | — | Ki | = | 2314.0 | nM | 5.64 |
| CHEMBL551462 | — | Ki | = | 2396.0 | nM | 5.62 |
| CHEMBL564343 | — | Ki | = | 2593.0 | nM | 5.59 |
| CHEMBL562654 | — | Ki | = | 2716.0 | nM | 5.57 |
| CHEMBL557442 | — | Ki | = | 2785.0 | nM | 5.55 |
| CHEMBL559476 | — | Ki | = | 3949.0 | nM | 5.40 |
| CHEMBL555869 | — | Ki | = | 7490.0 | nM | 5.13 |