Assay Detail
Binding
CHEMBL1006412
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Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK293 cells
25
Total Activities
25
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
Investigations on the 4-quinolone-3-carboxylic acid motif. 2. Synthesis and structure-activity relationship of potent and selective cannabinoid-2 receptor agonists endowed with analgesic activity in vivo.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 25 | 8.02 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL525528 | — | — | 1 | 9.10 |
| CHEMBL507019 | — | — | 1 | 9.05 |
| CHEMBL498527 | — | — | 1 | 8.80 |
| CHEMBL524456 | — | — | 1 | 8.47 |
| CHEMBL496659 | — | — | 1 | 8.46 |
| CHEMBL497321 | — | — | 1 | 8.44 |
| CHEMBL523577 | — | — | 1 | 8.42 |
| CHEMBL201571 | — | — | 1 | 8.33 |
| CHEMBL381689 | SR-144528 | — | 1 | 8.27 |
| CHEMBL502276 | — | — | 1 | 8.20 |
| CHEMBL498132 | — | — | 1 | 8.04 |
| CHEMBL500415 | — | — | 1 | 8.03 |
| CHEMBL497325 | — | — | 1 | 7.97 |
| CHEMBL524884 | — | — | 1 | 7.94 |
| CHEMBL498297 | — | — | 1 | 7.84 |
| CHEMBL500414 | — | — | 1 | 7.79 |
| CHEMBL497326 | — | — | 1 | 7.77 |
| CHEMBL526153 | — | — | 1 | 7.62 |
| CHEMBL497681 | — | — | 1 | 7.62 |
| CHEMBL500925 | — | — | 1 | 7.59 |
| CHEMBL498131 | — | — | 1 | 7.28 |
| CHEMBL524731 | — | — | 1 | 7.25 |
| CHEMBL111 | RIMONABANT | 4.0 | 1 | 6.10 |
| CHEMBL497682 | — | — | 1 | - |
| CHEMBL524625 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL525528 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL507019 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL498527 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL524456 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL496659 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL497321 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL523577 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL201571 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL381689 | SR-144528 | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL502276 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL498132 | — | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL500415 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL497325 | — | Ki | = | 10.7 | nM | 7.97 |
| CHEMBL524884 | — | Ki | = | 11.6 | nM | 7.94 |
| CHEMBL498297 | — | Ki | = | 14.3 | nM | 7.84 |
| CHEMBL500414 | — | Ki | = | 16.1 | nM | 7.79 |
| CHEMBL497326 | — | Ki | = | 17.1 | nM | 7.77 |
| CHEMBL526153 | — | Ki | = | 23.8 | nM | 7.62 |
| CHEMBL497681 | — | Ki | = | 24.2 | nM | 7.62 |
| CHEMBL500925 | — | Ki | = | 25.5 | nM | 7.59 |
| CHEMBL498131 | — | Ki | = | 52.6 | nM | 7.28 |
| CHEMBL524731 | — | Ki | = | 55.9 | nM | 7.25 |
| CHEMBL111 | RIMONABANT | Ki | = | 790.0 | nM | 6.10 |
| CHEMBL497682 | — | Ki | - | — | - | |
| CHEMBL524625 | — | Ki | - | — | - |