Assay Detail
Binding
CHEMBL2168994
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Displacement of [3H]epibatidine from rat alpha3beta4 nACHR
13
Total Activities
13
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; alpha3/beta4 (CHEMBL1907593) ↗| 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 | 13 | 6.22 | 7.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1076903 | VARENICLINE | 4.0 | 1 | 7.07 |
| CHEMBL2165439 | — | — | 1 | 6.77 |
| CHEMBL2165452 | — | — | 1 | 6.73 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 6.58 |
| CHEMBL2165444 | — | — | 1 | 6.16 |
| CHEMBL2165438 | — | — | 1 | 6.11 |
| CHEMBL2165453 | — | — | 1 | 6.09 |
| CHEMBL2165443 | — | — | 1 | 5.90 |
| CHEMBL2165440 | — | — | 1 | 5.75 |
| CHEMBL2165445 | — | — | 1 | 5.06 |
| CHEMBL2165451 | — | — | 1 | - |
| CHEMBL2165450 | — | — | 1 | - |
| CHEMBL2165446 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1076903 | VARENICLINE | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL2165439 | — | Ki | = | 171.0 | nM | 6.77 |
| CHEMBL2165452 | — | Ki | = | 186.0 | nM | 6.73 |
| CHEMBL3 | NICOTINE | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL2165444 | — | Ki | = | 692.0 | nM | 6.16 |
| CHEMBL2165438 | — | Ki | = | 771.0 | nM | 6.11 |
| CHEMBL2165453 | — | Ki | = | 809.0 | nM | 6.09 |
| CHEMBL2165443 | — | Ki | = | 1270.0 | nM | 5.90 |
| CHEMBL2165440 | — | Ki | = | 1760.0 | nM | 5.75 |
| CHEMBL2165445 | — | Ki | = | 8780.0 | nM | 5.06 |
| CHEMBL2165451 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2165450 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2165446 | — | Ki | > | 10000.0 | nM | - |