Assay Detail
Binding
CHEMBL2168995
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Displacement of [3H]epibatidine from rat alpha4beta2 nACHR
17
Total Activities
17
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/beta2 (CHEMBL1907596) ↗| 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 | 17 | 7.75 | 10.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1076903 | VARENICLINE | 4.0 | 1 | 10.30 |
| CHEMBL59986 | — | — | 1 | 10.30 |
| CHEMBL2165444 | — | — | 1 | 8.34 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 8.31 |
| CHEMBL2165443 | — | — | 1 | 8.14 |
| CHEMBL274525 | ABT-418 | — | 1 | 8.13 |
| CHEMBL2165442 | — | — | 1 | 7.88 |
| CHEMBL2165440 | — | — | 1 | 7.71 |
| CHEMBL2165452 | — | — | 1 | 7.62 |
| CHEMBL2165441 | — | — | 1 | 7.51 |
| CHEMBL2165439 | — | — | 1 | 7.31 |
| CHEMBL2165438 | — | — | 1 | 7.12 |
| CHEMBL2165445 | — | — | 1 | 6.89 |
| CHEMBL2165451 | — | — | 1 | 6.86 |
| CHEMBL2165453 | — | — | 1 | 6.80 |
| CHEMBL2165446 | — | — | 1 | 6.75 |
| CHEMBL2165450 | — | — | 1 | 5.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1076903 | VARENICLINE | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL59986 | — | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL2165444 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL3 | NICOTINE | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL2165443 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL274525 | ABT-418 | Ki | = | 7.4 | nM | 8.13 |
| CHEMBL2165442 | — | Ki | = | 13.1 | nM | 7.88 |
| CHEMBL2165440 | — | Ki | = | 19.7 | nM | 7.71 |
| CHEMBL2165452 | — | Ki | = | 23.8 | nM | 7.62 |
| CHEMBL2165441 | — | Ki | = | 31.2 | nM | 7.51 |
| CHEMBL2165439 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL2165438 | — | Ki | = | 75.9 | nM | 7.12 |
| CHEMBL2165445 | — | Ki | = | 129.0 | nM | 6.89 |
| CHEMBL2165451 | — | Ki | = | 137.0 | nM | 6.86 |
| CHEMBL2165453 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL2165446 | — | Ki | = | 176.0 | nM | 6.75 |
| CHEMBL2165450 | — | Ki | = | 1950.0 | nM | 5.71 |