Assay Detail
Binding
CHEMBL2168993
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Displacement of [3H]epibatidine from rat alpha3beta2 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; alpha3/beta2 (CHEMBL1907587) ↗| 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 | 6.46 | 8.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2165444 | — | — | 1 | 8.06 |
| CHEMBL2165443 | — | — | 1 | 7.76 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 7.54 |
| CHEMBL2165440 | — | — | 1 | 6.91 |
| CHEMBL2165441 | — | — | 1 | 6.50 |
| CHEMBL2165452 | — | — | 1 | 6.44 |
| CHEMBL2165442 | — | — | 1 | 6.43 |
| CHEMBL2165438 | — | — | 1 | 6.33 |
| CHEMBL2165451 | — | — | 1 | 6.28 |
| CHEMBL2165446 | — | — | 1 | 6.00 |
| CHEMBL2165445 | — | — | 1 | 5.99 |
| CHEMBL2165453 | — | — | 1 | 5.69 |
| CHEMBL2165448 | — | — | 1 | 5.39 |
| CHEMBL2165450 | — | — | 1 | 5.18 |
| CHEMBL2165439 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2165444 | — | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL2165443 | — | Ki | = | 17.3 | nM | 7.76 |
| CHEMBL3 | NICOTINE | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL2165440 | — | Ki | = | 123.0 | nM | 6.91 |
| CHEMBL2165441 | — | Ki | = | 315.0 | nM | 6.50 |
| CHEMBL2165452 | — | Ki | = | 362.0 | nM | 6.44 |
| CHEMBL2165442 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL2165438 | — | Ki | = | 462.0 | nM | 6.33 |
| CHEMBL2165451 | — | Ki | = | 521.0 | nM | 6.28 |
| CHEMBL2165446 | — | Ki | = | 990.0 | nM | 6.00 |
| CHEMBL2165445 | — | Ki | = | 1030.0 | nM | 5.99 |
| CHEMBL2165453 | — | Ki | = | 2040.0 | nM | 5.69 |
| CHEMBL2165448 | — | Ki | = | 4100.0 | nM | 5.39 |
| CHEMBL2165450 | — | Ki | = | 6670.0 | nM | 5.18 |
| CHEMBL2165439 | — | Ki | - | — | - |