Assay Detail
Binding
CHEMBL2168997
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Displacement of [3H]epibatidine from rat alpha4beta4 nACHR
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta4 (CHEMBL1907595) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
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 | 15 | 6.65 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2165439 | — | — | 1 | 8.00 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 7.64 |
| CHEMBL2165452 | — | — | 1 | 7.56 |
| CHEMBL2165438 | — | — | 1 | 7.48 |
| CHEMBL2165453 | — | — | 1 | 7.26 |
| CHEMBL2165440 | — | — | 1 | 7.22 |
| CHEMBL2165444 | — | — | 1 | 7.07 |
| CHEMBL1076903 | VARENICLINE | 4.0 | 1 | 6.96 |
| CHEMBL2165443 | — | — | 1 | 6.79 |
| CHEMBL2165441 | — | — | 1 | 5.91 |
| CHEMBL2165442 | — | — | 1 | 5.46 |
| CHEMBL2165445 | — | — | 1 | 5.38 |
| CHEMBL2165451 | — | — | 1 | 5.31 |
| CHEMBL2165446 | — | — | 1 | 5.12 |
| CHEMBL2165450 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2165439 | — | Ki | = | 9.9 | nM | 8.00 |
| CHEMBL3 | NICOTINE | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL2165452 | — | Ki | = | 27.5 | nM | 7.56 |
| CHEMBL2165438 | — | Ki | = | 33.2 | nM | 7.48 |
| CHEMBL2165453 | — | Ki | = | 55.1 | nM | 7.26 |
| CHEMBL2165440 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL2165444 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL1076903 | VARENICLINE | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL2165443 | — | Ki | = | 163.0 | nM | 6.79 |
| CHEMBL2165441 | — | Ki | = | 1240.0 | nM | 5.91 |
| CHEMBL2165442 | — | Ki | = | 3480.0 | nM | 5.46 |
| CHEMBL2165445 | — | Ki | = | 4140.0 | nM | 5.38 |
| CHEMBL2165451 | — | Ki | = | 4900.0 | nM | 5.31 |
| CHEMBL2165446 | — | Ki | = | 7530.0 | nM | 5.12 |
| CHEMBL2165450 | — | Ki | > | 10000.0 | nM | - |