Assay Detail
Binding
CHEMBL1816969
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]SR141716A from rat brain CB1 receptor at pH 7.4 after 1 hr by liquid scintillation counting
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-activity relationship studies of novel pyrazole and imidazole carboxamides as cannabinoid-1 (CB1) antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 8.20 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1814154 | — | — | 1 | 10.00 |
| CHEMBL1814333 | — | — | 1 | 10.00 |
| CHEMBL1814329 | — | — | 1 | 10.00 |
| CHEMBL220360 | TARANABANT | 3.0 | 1 | 9.52 |
| CHEMBL1814331 | — | — | 1 | 9.40 |
| CHEMBL1814153 | — | — | 1 | 9.30 |
| CHEMBL1814330 | — | — | 1 | 9.10 |
| CHEMBL1814335 | — | — | 1 | 9.00 |
| CHEMBL1814155 | — | — | 1 | 8.96 |
| CHEMBL1814316 | — | — | 1 | 8.70 |
| CHEMBL1814338 | — | — | 1 | 8.52 |
| CHEMBL1814326 | — | — | 1 | 8.52 |
| CHEMBL1814332 | — | — | 1 | 8.40 |
| CHEMBL1814157 | — | — | 1 | 8.30 |
| CHEMBL1814327 | — | — | 1 | 8.22 |
| CHEMBL1814328 | — | — | 1 | 8.22 |
| CHEMBL1814318 | — | — | 1 | 8.00 |
| CHEMBL1814322 | — | — | 1 | 7.96 |
| CHEMBL1814320 | — | — | 1 | 7.92 |
| CHEMBL1814340 | — | — | 1 | 7.89 |
| CHEMBL1814315 | — | — | 1 | 7.82 |
| CHEMBL1814158 | — | — | 1 | 7.77 |
| CHEMBL111 | RIMONABANT | 4.0 | 1 | 7.75 |
| CHEMBL1814317 | — | — | 1 | 7.66 |
| CHEMBL1814156 | — | — | 1 | 7.66 |
| CHEMBL1814339 | — | — | 1 | 7.52 |
| CHEMBL1814313 | — | — | 1 | 7.51 |
| CHEMBL1814325 | — | — | 1 | 7.48 |
| CHEMBL1814337 | — | — | 1 | 7.44 |
| CHEMBL1814151 | — | — | 1 | 7.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1814154 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL1814329 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL1814333 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL220360 | TARANABANT | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL1814331 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL1814153 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL1814330 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL1814335 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1814155 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL1814316 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1814338 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1814326 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1814332 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1814157 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1814328 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1814327 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1814318 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1814322 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1814320 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1814340 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1814315 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1814158 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL111 | RIMONABANT | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1814317 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL1814156 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL1814339 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1814313 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL1814325 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL1814337 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL1814151 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL1814324 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL1814323 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL1814150 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL1814321 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL1814152 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL1814161 | — | IC50 | > | 1000.0 | nM | - |