Assay Detail
Binding
CHEMBL1168403
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Displacement of (+/-)-[3H]epibatidine from alpha4beta2 nAChR in rat cortical membrane
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; alpha4/beta2 (CHEMBL1907596) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Novel tricyclic Delta(2)-isoxazoline and 3-oxo-2-methyl-isoxazolidine derivatives: synthesis and binding affinity at neuronal nicotinic acetylcholine receptor subtypes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 5.95 | 10.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | — | 1 | 10.46 |
| CHEMBL497939 | CYTISINICLINE | 3.0 | 1 | 9.40 |
| CHEMBL1164304 | — | — | 1 | 7.03 |
| CHEMBL1163516 | — | — | 1 | 6.12 |
| CHEMBL1163244 | — | — | 1 | 6.04 |
| CHEMBL1164456 | — | — | 1 | 5.75 |
| CHEMBL1163249 | — | — | 1 | 5.35 |
| CHEMBL1794974 | — | — | 1 | 4.51 |
| CHEMBL1164458 | — | — | 1 | 4.30 |
| CHEMBL1163517 | — | — | 1 | 4.28 |
| CHEMBL1163515 | — | — | 1 | 4.10 |
| CHEMBL1164459 | — | — | 1 | 4.00 |
| CHEMBL1164404 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.035 | nM | 10.46 |
| CHEMBL497939 | CYTISINICLINE | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL1164304 | — | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL1163516 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL1163244 | — | Ki | = | 920.0 | nM | 6.04 |
| CHEMBL1164456 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL1163249 | — | Ki | = | 4500.0 | nM | 5.35 |
| CHEMBL1794974 | — | Ki | = | 31000.0 | nM | 4.51 |
| CHEMBL1164458 | — | Ki | = | 50000.0 | nM | 4.30 |
| CHEMBL1163517 | — | Ki | = | 53000.0 | nM | 4.28 |
| CHEMBL1163515 | — | Ki | = | 79000.0 | nM | 4.10 |
| CHEMBL1164459 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL1164404 | — | Ki | = | 260000.0 | nM | - |