Assay Detail
Binding
CHEMBL981123
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Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel sterically hindered cannabinoid CB1 receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 6.10 | 8.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL381689 | SR-144528 | — | 1 | 8.27 |
| CHEMBL285932 | — | — | 1 | 6.96 |
| CHEMBL478624 | — | — | 1 | 6.54 |
| CHEMBL476576 | — | — | 1 | 6.19 |
| CHEMBL111 | RIMONABANT | 4.0 | 1 | 6.10 |
| CHEMBL478210 | — | — | 1 | 6.10 |
| CHEMBL479094 | — | — | 1 | 6.10 |
| CHEMBL518595 | — | — | 1 | 5.96 |
| CHEMBL479095 | — | — | 1 | 5.92 |
| CHEMBL517815 | — | — | 1 | 5.89 |
| CHEMBL476317 | — | — | 1 | 5.85 |
| CHEMBL478643 | — | — | 1 | 5.75 |
| CHEMBL478625 | — | — | 1 | 5.64 |
| CHEMBL476545 | — | — | 1 | 5.62 |
| CHEMBL478856 | — | — | 1 | 5.62 |
| CHEMBL476529 | — | — | 1 | 5.10 |
| CHEMBL476336 | — | — | 1 | - |
| CHEMBL502133 | — | — | 1 | - |
| CHEMBL475910 | — | — | 1 | - |
| CHEMBL475909 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL381689 | SR-144528 | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL285932 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL478624 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL476576 | — | Ki | = | 650.0 | nM | 6.19 |
| CHEMBL111 | RIMONABANT | Ki | = | 790.0 | nM | 6.10 |
| CHEMBL478210 | — | Ki | = | 790.0 | nM | 6.10 |
| CHEMBL479094 | — | Ki | = | 790.0 | nM | 6.10 |
| CHEMBL518595 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL479095 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL517815 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL476317 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL478643 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL478625 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL476545 | — | Ki | = | 2400.0 | nM | 5.62 |
| CHEMBL478856 | — | Ki | = | 2400.0 | nM | 5.62 |
| CHEMBL476529 | — | Ki | = | 7900.0 | nM | 5.10 |
| CHEMBL476336 | — | Ki | > | 7900.0 | nM | - |
| CHEMBL502133 | — | Ki | > | 7900.0 | nM | - |
| CHEMBL475910 | — | Ki | > | 7900.0 | nM | - |
| CHEMBL475909 | — | Ki | > | 7900.0 | nM | - |