Assay Detail
Binding
CHEMBL909736
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Inhibition of [3H]MLA binding to alpha-7 nAChR in rat brain membrane
9
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL4980) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Des-keto lobeline analogs with increased potency and selectivity at dopamine and serotonin transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | - | - |
| Ki | 4 | 5.33 | 5.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL125511 | 8R-hydroxylobelane | — | 1 | 5.92 |
| CHEMBL425617 | — | — | 1 | 5.77 |
| CHEMBL122270 | LOBELINE | 2.0 | 1 | 5.20 |
| CHEMBL122317 | — | — | 1 | 4.41 |
| CHEMBL213613 | — | — | 1 | - |
| CHEMBL213148 | — | — | 1 | - |
| CHEMBL377539 | — | — | 1 | - |
| CHEMBL217815 | — | — | 1 | - |
| CHEMBL124219 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL125511 | 8R-hydroxylobelane | Ki | = | 1210.0 | nM | 5.92 |
| CHEMBL425617 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL122270 | LOBELINE | Ki | = | 6260.0 | nM | 5.20 |
| CHEMBL122317 | — | Ki | = | 39300.0 | nM | 4.41 |
| CHEMBL213613 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL213148 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL377539 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL217815 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL124219 | — | IC50 | > | 100000.0 | nM | - |