Assay Detail
Binding
CHEMBL909735
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Inhibition of [3H]NIC binding to alpha-4-beta-2 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 | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596) ↗| Type | PROTEIN COMPLEX |
| 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 |
|---|---|---|---|
| Ki | 6 | 5.77 | 8.40 |
| IC50 | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL122270 | LOBELINE | 2.0 | 1 | 8.40 |
| CHEMBL122317 | — | — | 1 | 5.75 |
| CHEMBL125511 | 8R-hydroxylobelane | — | 1 | 5.63 |
| CHEMBL425617 | — | — | 1 | 5.38 |
| CHEMBL124219 | — | — | 1 | 5.01 |
| CHEMBL377539 | — | — | 1 | 4.47 |
| CHEMBL213613 | — | — | 1 | - |
| CHEMBL213148 | — | — | 1 | - |
| CHEMBL217815 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL122270 | LOBELINE | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL122317 | — | Ki | = | 1770.0 | nM | 5.75 |
| CHEMBL125511 | 8R-hydroxylobelane | Ki | = | 2360.0 | nM | 5.63 |
| CHEMBL425617 | — | Ki | = | 4190.0 | nM | 5.38 |
| CHEMBL124219 | — | Ki | = | 9750.0 | nM | 5.01 |
| CHEMBL377539 | — | Ki | = | 33600.0 | nM | 4.47 |
| CHEMBL213613 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL213148 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL217815 | — | IC50 | > | 100000.0 | nM | - |