Assay Detail
Binding
CHEMBL854080
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Binding affinity at the CB2 receptor
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis of functionalized 1,8-naphthyridinones and their evaluation as novel, orally active CB1 receptor inverse agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 5.72 | 6.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL204391 | — | — | 1 | 6.42 |
| CHEMBL265787 | — | — | 1 | 6.14 |
| CHEMBL201102 | — | — | 1 | 5.96 |
| CHEMBL203811 | — | — | 1 | 5.96 |
| CHEMBL202202 | — | — | 1 | 5.85 |
| CHEMBL202064 | — | — | 1 | 5.85 |
| CHEMBL203152 | — | — | 1 | 5.85 |
| CHEMBL370388 | — | — | 1 | 5.85 |
| CHEMBL202013 | — | — | 1 | 5.82 |
| CHEMBL380483 | — | — | 1 | 5.82 |
| CHEMBL371252 | — | — | 1 | 5.75 |
| CHEMBL202659 | — | — | 1 | 5.60 |
| CHEMBL201552 | — | — | 1 | 5.50 |
| CHEMBL202201 | — | — | 1 | 5.44 |
| CHEMBL204232 | NAPHTHYRIDINONE | — | 1 | 5.39 |
| CHEMBL202169 | — | — | 1 | 5.29 |
| CHEMBL381677 | — | — | 1 | 5.27 |
| CHEMBL201388 | — | — | 1 | 5.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL204391 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL265787 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL201102 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL203811 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL202202 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL202064 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL203152 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL370388 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL202013 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL380483 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL371252 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL202659 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL201552 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL202201 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL204232 | NAPHTHYRIDINONE | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL202169 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL381677 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL201388 | — | IC50 | = | 6200.0 | nM | 5.21 |