Assay Detail
Binding
CHEMBL750053
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Inhibitory activity against nicotinic acetylcholine receptor alpha3-beta4
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha3/beta4 (CHEMBL1907594) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Structure activity studies of ring E analogues of methyllycaconitine. Part 2: Synthesis of antagonists to the alpha3beta4* nicotinic acetylcholine receptors through modifications to the ester.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 6.35 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL267936 | MECAMYLAMINE | 4.0 | 1 | 7.00 |
| CHEMBL1687 | — | — | 1 | 5.70 |
| CHEMBL121721 | HEXAMETHONIUM HYDROXIDE | — | 1 | - |
| CHEMBL1190 | DECAMETHONIUM | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL267936 | MECAMYLAMINE | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1687 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL121721 | HEXAMETHONIUM HYDROXIDE | IC50 | ~ | 1700.0 | nM | - |
| CHEMBL1190 | DECAMETHONIUM | IC50 | ~ | 1700.0 | nM | - |