Assay Detail
Binding
CHEMBL1042698
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Displacement of [3H]SR141716A from rat brain CB1 receptor
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Bioisosteric replacement of the hydrazide pharmacophore of the cannabinoid-1 receptor antagonist SR141716A. Part I: potent, orally-active 1,4-disubstituted imidazoles.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 8.07 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL111 | RIMONABANT | 4.0 | 1 | 9.05 |
| CHEMBL578969 | — | — | 1 | 8.96 |
| CHEMBL584889 | — | — | 1 | 8.74 |
| CHEMBL578576 | — | — | 1 | 8.31 |
| CHEMBL584261 | — | — | 1 | 8.28 |
| CHEMBL577040 | — | — | 1 | 8.24 |
| CHEMBL565742 | — | — | 1 | 8.14 |
| CHEMBL583229 | — | — | 1 | 8.13 |
| CHEMBL585095 | — | — | 1 | 8.07 |
| CHEMBL568230 | — | — | 1 | 8.02 |
| CHEMBL579196 | — | — | 1 | 8.00 |
| CHEMBL576618 | — | — | 1 | 7.85 |
| CHEMBL576230 | — | — | 1 | 7.85 |
| CHEMBL568221 | — | — | 1 | 7.72 |
| CHEMBL567811 | — | — | 1 | 7.72 |
| CHEMBL565733 | — | — | 1 | 7.70 |
| CHEMBL577477 | — | — | 1 | 7.60 |
| CHEMBL568229 | — | — | 1 | 7.51 |
| CHEMBL568007 | — | — | 1 | 7.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL111 | RIMONABANT | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL578969 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL584889 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL578576 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL584261 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL577040 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL565742 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL583229 | — | Ki | = | 7.4 | nM | 8.13 |
| CHEMBL585095 | — | Ki | = | 8.6 | nM | 8.07 |
| CHEMBL568230 | — | Ki | = | 9.5 | nM | 8.02 |
| CHEMBL579196 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL576618 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL576230 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL568221 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL567811 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL565733 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL577477 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL568229 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL568007 | — | Ki | = | 38.0 | nM | 7.42 |