Assay Detail
Functional
CHEMBL3124135
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at CB2 receptor (unknown origin) stably expressed in CHO cells co-expressing co-expressing Ga15/16 assessed as calcium current after 45 mins by fluo-4 AM assay
15
Total Activities
15
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 | Autocuration |
Publication
Design, synthesis, biological evaluation, and comparative docking study of 1,2,4-triazolones as CB1 receptor selective antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 5.42 | 6.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL178372 | — | — | 1 | 6.19 |
| CHEMBL3120198 | — | — | 1 | 5.82 |
| CHEMBL3120201 | — | — | 1 | 5.71 |
| CHEMBL3120203 | — | — | 1 | 5.39 |
| CHEMBL3120205 | — | — | 1 | 5.30 |
| CHEMBL3120210 | — | — | 1 | 5.22 |
| CHEMBL111 | RIMONABANT | 4.0 | 1 | 5.01 |
| CHEMBL3120199 | — | — | 1 | 4.70 |
| CHEMBL3120209 | — | — | 1 | - |
| CHEMBL3120208 | — | — | 1 | - |
| CHEMBL3120207 | — | — | 1 | - |
| CHEMBL3120206 | — | — | 1 | - |
| CHEMBL3120204 | — | — | 1 | - |
| CHEMBL3120202 | — | — | 1 | - |
| CHEMBL3120200 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL178372 | — | IC50 | = | 644.0 | nM | 6.19 |
| CHEMBL3120198 | — | IC50 | = | 1510.0 | nM | 5.82 |
| CHEMBL3120201 | — | IC50 | = | 1930.0 | nM | 5.71 |
| CHEMBL3120203 | — | IC50 | = | 4090.0 | nM | 5.39 |
| CHEMBL3120205 | — | IC50 | = | 5030.0 | nM | 5.30 |
| CHEMBL3120210 | — | IC50 | = | 6080.0 | nM | 5.22 |
| CHEMBL111 | RIMONABANT | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL3120199 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL3120209 | — | IC50 | - | — | - | |
| CHEMBL3120208 | — | IC50 | - | — | - | |
| CHEMBL3120207 | — | IC50 | - | — | - | |
| CHEMBL3120206 | — | IC50 | - | — | - | |
| CHEMBL3120204 | — | IC50 | - | — | - | |
| CHEMBL3120202 | — | IC50 | - | — | - | |
| CHEMBL3120200 | — | IC50 | - | — | - |