Assay Detail
Binding
CHEMBL905460
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Displacement of [125I]alpha-bungarotoxin from human alpha-7 nAChR expressed in SH-SY5Y cells
14
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SH-SY5Y |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL2492) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Aporphine metho salts as neuronal nicotinic acetylcholine receptor blockers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 4.50 | 4.92 |
| Ki | 7 | 4.50 | 5.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL112640 | — | — | 2 | 5.00 |
| CHEMBL388341 | BOLDINE METHIODIDE | — | 2 | 4.82 |
| CHEMBL225852 | GLAUCINE METHIODIDE | — | 2 | 4.75 |
| CHEMBL225851 | PREDICENTRINE METHIODIDE | — | 2 | 4.68 |
| CHEMBL388342 | BOLDINE | — | 2 | 4.17 |
| CHEMBL225853 | 3-BROMOBOLDINE | — | 2 | 4.08 |
| CHEMBL388564 | — | — | 2 | 4.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL112640 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL112640 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL388341 | BOLDINE METHIODIDE | Ki | = | 15000.0 | nM | 4.82 |
| CHEMBL388341 | BOLDINE METHIODIDE | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL225852 | GLAUCINE METHIODIDE | Ki | = | 18000.0 | nM | 4.75 |
| CHEMBL225852 | GLAUCINE METHIODIDE | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL225851 | PREDICENTRINE METHIODIDE | Ki | = | 21000.0 | nM | 4.68 |
| CHEMBL225851 | PREDICENTRINE METHIODIDE | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL388342 | BOLDINE | Ki | = | 67000.0 | nM | 4.17 |
| CHEMBL388342 | BOLDINE | IC50 | = | 81000.0 | nM | 4.09 |
| CHEMBL225853 | 3-BROMOBOLDINE | Ki | = | 83000.0 | nM | 4.08 |
| CHEMBL388564 | — | Ki | = | 95000.0 | nM | 4.02 |
| CHEMBL225853 | 3-BROMOBOLDINE | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL388564 | — | IC50 | = | 114000.0 | nM | - |