Assay Detail
Binding
CHEMBL2168996
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Displacement of [3H]epibatidine from rat forebrain alpha4beta2* nACHR
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Identification of novel α4β2-nicotinic acetylcholine receptor (nAChR) agonists based on an isoxazole ether scaffold that demonstrate antidepressant-like activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 6.65 | 8.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3 | NICOTINE | 4.0 | 1 | 8.01 |
| CHEMBL2165444 | — | — | 1 | 7.92 |
| CHEMBL2165443 | — | — | 1 | 7.92 |
| CHEMBL2165442 | — | — | 1 | 6.83 |
| CHEMBL2165440 | — | — | 1 | 6.80 |
| CHEMBL2165452 | — | — | 1 | 6.76 |
| CHEMBL2165441 | — | — | 1 | 6.68 |
| CHEMBL2165438 | — | — | 1 | 6.41 |
| CHEMBL2165446 | — | — | 1 | 6.39 |
| CHEMBL2165439 | — | — | 1 | 6.38 |
| CHEMBL2165451 | — | — | 1 | 6.20 |
| CHEMBL2165445 | — | — | 1 | 5.96 |
| CHEMBL2165453 | — | — | 1 | 5.67 |
| CHEMBL2165450 | — | — | 1 | 5.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3 | NICOTINE | Ki | = | 9.8 | nM | 8.01 |
| CHEMBL2165444 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL2165443 | — | Ki | = | 11.9 | nM | 7.92 |
| CHEMBL2165442 | — | Ki | = | 149.0 | nM | 6.83 |
| CHEMBL2165440 | — | Ki | = | 157.0 | nM | 6.80 |
| CHEMBL2165452 | — | Ki | = | 172.0 | nM | 6.76 |
| CHEMBL2165441 | — | Ki | = | 207.0 | nM | 6.68 |
| CHEMBL2165438 | — | Ki | = | 386.0 | nM | 6.41 |
| CHEMBL2165446 | — | Ki | = | 405.0 | nM | 6.39 |
| CHEMBL2165439 | — | Ki | = | 417.0 | nM | 6.38 |
| CHEMBL2165451 | — | Ki | = | 637.0 | nM | 6.20 |
| CHEMBL2165445 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL2165453 | — | Ki | = | 2120.0 | nM | 5.67 |
| CHEMBL2165450 | — | Ki | = | 7380.0 | nM | 5.13 |