Assay Detail
Functional
CHEMBL861409
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [35S]GTP-gamma-S binding to human CB2 receptor expressed in CHO cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis and SAR studies of 2-oxoquinoline derivatives as CB2 receptor inverse agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.74 | 9.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL381314 | — | — | 1 | 9.20 |
| CHEMBL204433 | — | — | 1 | 9.10 |
| CHEMBL381689 | SR-144528 | — | 1 | 8.50 |
| CHEMBL382676 | — | — | 1 | 8.50 |
| CHEMBL203924 | — | — | 1 | 8.30 |
| CHEMBL204387 | — | — | 1 | 8.00 |
| CHEMBL206492 | — | — | 1 | 7.90 |
| CHEMBL381313 | — | — | 1 | 7.70 |
| CHEMBL381969 | — | — | 1 | 7.60 |
| CHEMBL178372 | — | — | 1 | 7.60 |
| CHEMBL202852 | — | — | 1 | 7.20 |
| CHEMBL201989 | — | — | 1 | 7.00 |
| CHEMBL203560 | — | — | 1 | 6.40 |
| CHEMBL204760 | — | — | 1 | 5.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL381314 | — | IC50 | = | 0.631 | nM | 9.20 |
| CHEMBL204433 | — | IC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL381689 | SR-144528 | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL382676 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL203924 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL204387 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL206492 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL381313 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL381969 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL178372 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL202852 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL201989 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL203560 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL204760 | — | IC50 | = | 3981.07 | nM | 5.40 |