Assay Detail
Binding
CHEMBL887658
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Displacement of [3H]CP-559440 from human CB1 receptor expressed in HEK293 cells
41
Total Activities
41
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 | Expert |
Publication
Optimization of imidazole amide derivatives as cannabinoid-1 receptor antagonists for the treatment of obesity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 41 | 7.65 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL111 | RIMONABANT | 4.0 | 1 | 8.96 |
| CHEMBL390543 | — | — | 1 | 8.72 |
| CHEMBL389175 | — | — | 1 | 8.66 |
| CHEMBL231118 | — | — | 1 | 8.43 |
| CHEMBL276312 | — | — | 1 | 8.41 |
| CHEMBL229749 | — | — | 1 | 8.34 |
| CHEMBL229583 | — | — | 1 | 8.31 |
| CHEMBL230800 | — | — | 1 | 8.30 |
| CHEMBL230801 | — | — | 1 | 8.24 |
| CHEMBL229967 | — | — | 1 | 8.20 |
| CHEMBL395026 | — | — | 1 | 8.16 |
| CHEMBL229698 | — | — | 1 | 8.14 |
| CHEMBL160963 | — | — | 1 | 8.11 |
| CHEMBL229584 | — | — | 1 | 8.09 |
| CHEMBL229750 | — | — | 1 | 8.05 |
| CHEMBL396984 | — | — | 1 | 8.00 |
| CHEMBL395322 | — | — | 1 | 7.77 |
| CHEMBL229802 | — | — | 1 | 7.77 |
| CHEMBL230802 | — | — | 1 | 7.75 |
| CHEMBL395321 | — | — | 1 | 7.75 |
| CHEMBL396739 | — | — | 1 | 7.72 |
| CHEMBL229751 | — | — | 1 | 7.70 |
| CHEMBL439375 | — | — | 1 | 7.68 |
| CHEMBL389198 | — | — | 1 | 7.66 |
| CHEMBL390545 | — | — | 1 | 7.66 |
| CHEMBL390544 | — | — | 1 | 7.60 |
| CHEMBL229965 | — | — | 1 | 7.54 |
| CHEMBL229914 | — | — | 1 | 7.54 |
| CHEMBL229803 | — | — | 1 | 7.47 |
| CHEMBL389174 | — | — | 1 | 7.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL111 | RIMONABANT | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL390543 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL389175 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL231118 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL276312 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL229749 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL229583 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL230800 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL230801 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL229967 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL395026 | — | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL229698 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL160963 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL229584 | — | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL229750 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL396984 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL395322 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL229802 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL230802 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL395321 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL396739 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL229751 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL439375 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL389198 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL390545 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL390544 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL229965 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL229914 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL229803 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL389174 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL387645 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL230583 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL229966 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL229801 | — | Ki | = | 95.0 | nM | 7.02 |
| CHEMBL229915 | — | Ki | = | 97.0 | nM | 7.01 |
| CHEMBL425662 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL229858 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL229859 | — | Ki | = | 620.0 | nM | 6.21 |
| CHEMBL229913 | — | Ki | = | 920.0 | nM | 6.04 |
| CHEMBL388987 | — | Ki | = | 940.0 | nM | 6.03 |
| CHEMBL387646 | — | Ki | = | 1100.0 | nM | 5.96 |