Assay Detail
Functional
CHEMBL1059682
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inverse agonist activity at human CB1 receptor by [35S]GTPgammaS incorporation assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| 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 |
|---|---|---|---|
| EC50 | 12 | 6.36 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL111 | RIMONABANT | 4.0 | 1 | 8.40 |
| CHEMBL560462 | — | — | 1 | 6.70 |
| CHEMBL557921 | — | — | 1 | 6.70 |
| CHEMBL428779 | — | — | 1 | 6.52 |
| CHEMBL560383 | — | — | 1 | 6.40 |
| CHEMBL559035 | — | — | 1 | 6.30 |
| CHEMBL554943 | — | — | 1 | 6.22 |
| CHEMBL550309 | — | — | 1 | 5.96 |
| CHEMBL550514 | — | — | 1 | 5.96 |
| CHEMBL560463 | — | — | 1 | 5.92 |
| CHEMBL565190 | — | — | 1 | 5.82 |
| CHEMBL562123 | — | — | 1 | 5.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL111 | RIMONABANT | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL560462 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL557921 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL428779 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL560383 | — | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL559035 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL554943 | — | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL550309 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL550514 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL560463 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL565190 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL562123 | — | EC50 | = | 4400.0 | nM | 5.36 |