Assay Detail
Binding
CHEMBL2154447
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Displacement of [3H]CP55940 from human CB2 receptor expressed in CHO cell membranes after 1 hr by scintillation counting
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Scaffold hopping strategy toward original pyrazolines as selective CB₂ receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 6.73 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL188 | WIN-552122 | — | 1 | 8.51 |
| CHEMBL381689 | SR-144528 | — | 1 | 7.67 |
| CHEMBL2151380 | — | — | 1 | 6.60 |
| CHEMBL2151379 | — | — | 1 | 6.42 |
| CHEMBL2151370 | — | — | 1 | 6.30 |
| CHEMBL2151377 | — | — | 1 | 6.16 |
| CHEMBL2151381 | — | — | 1 | 5.44 |
| CHEMBL2151368 | — | — | 1 | - |
| CHEMBL2151369 | — | — | 1 | - |
| CHEMBL2151371 | — | — | 1 | - |
| CHEMBL2151372 | — | — | 1 | - |
| CHEMBL2151373 | — | — | 1 | - |
| CHEMBL2151374 | — | — | 1 | - |
| CHEMBL2151375 | — | — | 1 | - |
| CHEMBL2151376 | — | — | 1 | - |
| CHEMBL2151378 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL188 | WIN-552122 | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL381689 | SR-144528 | Ki | = | 21.6 | nM | 7.67 |
| CHEMBL2151380 | — | Ki | = | 251.0 | nM | 6.60 |
| CHEMBL2151379 | — | Ki | = | 385.0 | nM | 6.42 |
| CHEMBL2151370 | — | Ki | = | 504.0 | nM | 6.30 |
| CHEMBL2151377 | — | Ki | = | 689.0 | nM | 6.16 |
| CHEMBL2151381 | — | Ki | = | 3639.0 | nM | 5.44 |
| CHEMBL2151368 | — | Ki | > | 3000.0 | nM | - |
| CHEMBL2151369 | — | Ki | > | 3000.0 | nM | - |
| CHEMBL2151371 | — | Ki | > | 3000.0 | nM | - |
| CHEMBL2151372 | — | Ki | > | 3000.0 | nM | - |
| CHEMBL2151373 | — | Ki | > | 3000.0 | nM | - |
| CHEMBL2151374 | — | Ki | > | 3000.0 | nM | - |
| CHEMBL2151375 | — | Ki | > | 3000.0 | nM | - |
| CHEMBL2151376 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL2151378 | — | Ki | > | 1000.0 | nM | - |