Assay Detail
Binding
CHEMBL905461
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Displacement of [3H]cytisine from human alpha-4-beta-2 nAChR expressed in SH-EP1 cells
14
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SH-EP1 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Aporphine metho salts as neuronal nicotinic acetylcholine receptor blockers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 4.93 | 5.52 |
| Ki | 7 | 5.31 | 6.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL112640 | — | — | 2 | 6.04 |
| CHEMBL225851 | PREDICENTRINE METHIODIDE | — | 2 | 6.01 |
| CHEMBL388341 | BOLDINE METHIODIDE | — | 2 | 5.60 |
| CHEMBL388342 | BOLDINE | — | 2 | 5.52 |
| CHEMBL225852 | GLAUCINE METHIODIDE | — | 2 | 5.00 |
| CHEMBL225853 | 3-BROMOBOLDINE | — | 2 | 4.52 |
| CHEMBL388564 | — | — | 2 | 4.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL112640 | — | Ki | = | 910.0 | nM | 6.04 |
| CHEMBL225851 | PREDICENTRINE METHIODIDE | Ki | = | 970.0 | nM | 6.01 |
| CHEMBL388341 | BOLDINE METHIODIDE | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL388342 | BOLDINE | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL112640 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL225851 | PREDICENTRINE METHIODIDE | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL388341 | BOLDINE METHIODIDE | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL388342 | BOLDINE | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL225852 | GLAUCINE METHIODIDE | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL225853 | 3-BROMOBOLDINE | Ki | = | 30000.0 | nM | 4.52 |
| CHEMBL388564 | — | Ki | = | 31000.0 | nM | 4.51 |
| CHEMBL225852 | GLAUCINE METHIODIDE | IC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL225853 | 3-BROMOBOLDINE | IC50 | = | 99000.0 | nM | 4.00 |
| CHEMBL388564 | — | IC50 | = | 101000.0 | nM | - |