Assay Detail
Functional
CHEMBL1069388
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Inverse agonist activity at human CB2 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation after 4 hrs
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and SAR of novel imidazoles as potent and selective cannabinoid CB2 receptor antagonists with high binding efficiencies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 8.70 | 9.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL600683 | — | — | 1 | 9.60 |
| CHEMBL599071 | — | — | 1 | 9.10 |
| CHEMBL381689 | SR-144528 | — | 1 | 8.30 |
| CHEMBL382728 | — | — | 1 | 8.30 |
| CHEMBL604120 | — | — | 1 | 8.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL600683 | — | EC50 | = | 0.2512 | nM | 9.60 |
| CHEMBL599071 | — | EC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL381689 | SR-144528 | EC50 | = | 5.012 | nM | 8.30 |
| CHEMBL382728 | — | EC50 | = | 5.012 | nM | 8.30 |
| CHEMBL604120 | — | EC50 | = | 6.31 | nM | 8.20 |