Assay Detail
Binding
CHEMBL755329
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Binding affinity for Nicotinic acetylcholine receptor alpha4-beta2 by displacement of [3H](-)-cytisine from whole rat brain membranes
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Synthesis and structure-activity relationships of pyrrolidine-modified analogs of the potent cholinergic channel activator, ABT 418
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 6.13 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL274525 | ABT-418 | — | 1 | 8.52 |
| CHEMBL76773 | — | — | 1 | 7.15 |
| CHEMBL80575 | — | — | 1 | 6.08 |
| CHEMBL77175 | — | — | 1 | 5.99 |
| CHEMBL76631 | — | — | 1 | 5.46 |
| CHEMBL80497 | — | — | 1 | 5.44 |
| CHEMBL80526 | — | — | 1 | 5.30 |
| CHEMBL76999 | — | — | 1 | 5.10 |
| CHEMBL308341 | — | — | 1 | - |
| CHEMBL75870 | — | — | 1 | - |
| CHEMBL308268 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL274525 | ABT-418 | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL76773 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL80575 | — | Ki | = | 840.0 | nM | 6.08 |
| CHEMBL77175 | — | Ki | = | 1020.0 | nM | 5.99 |
| CHEMBL76631 | — | Ki | = | 3500.0 | nM | 5.46 |
| CHEMBL80497 | — | Ki | = | 3666.0 | nM | 5.44 |
| CHEMBL80526 | — | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL76999 | — | Ki | = | 8000.0 | nM | 5.10 |
| CHEMBL308341 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL75870 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL308268 | — | Ki | > | 10000.0 | nM | - |