Assay Detail
Binding
CHEMBL854079
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Binding affinity at the CB1 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 | 7.67 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL201388 | — | — | 1 | 8.64 |
| CHEMBL202169 | — | — | 1 | 8.64 |
| CHEMBL371252 | — | — | 1 | 8.43 |
| CHEMBL202064 | — | — | 1 | 8.28 |
| CHEMBL204232 | NAPHTHYRIDINONE | — | 1 | 8.12 |
| CHEMBL381677 | — | — | 1 | 7.82 |
| CHEMBL202659 | — | — | 1 | 7.70 |
| CHEMBL201102 | — | — | 1 | 7.62 |
| CHEMBL201552 | — | — | 1 | 7.62 |
| CHEMBL202013 | — | — | 1 | 7.58 |
| CHEMBL380483 | — | — | 1 | 7.50 |
| CHEMBL265787 | — | — | 1 | 7.46 |
| CHEMBL202201 | — | — | 1 | 7.34 |
| CHEMBL202202 | — | — | 1 | 7.26 |
| CHEMBL203152 | — | — | 1 | 7.11 |
| CHEMBL370388 | — | — | 1 | 7.02 |
| CHEMBL204391 | — | — | 1 | 6.96 |
| CHEMBL203811 | — | — | 1 | 6.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL201388 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL202169 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL371252 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL202064 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL204232 | NAPHTHYRIDINONE | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL381677 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL202659 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL201102 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL201552 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL202013 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL380483 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL265787 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL202201 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL202202 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL203152 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL370388 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL204391 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL203811 | — | IC50 | = | 120.0 | nM | 6.92 |