Assay Detail
Binding
CHEMBL1068116
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Displacement of [3H]nicotine from alpha4beta2 nAChR in rat brain homogenate by liquid scintillation spectrophotometry
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Lobeline esters as novel ligands for neuronal nicotinic acetylcholine receptors and neurotransmitter transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 7.34 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3 | NICOTINE | 4.0 | 1 | 8.85 |
| CHEMBL122270 | LOBELINE | 2.0 | 1 | 8.40 |
| CHEMBL597085 | — | — | 1 | 8.30 |
| CHEMBL596683 | — | — | 1 | 8.10 |
| CHEMBL599267 | — | — | 1 | 8.00 |
| CHEMBL603692 | — | — | 1 | 7.96 |
| CHEMBL597298 | — | — | 1 | 7.92 |
| CHEMBL605748 | — | — | 1 | 7.89 |
| CHEMBL604306 | — | — | 1 | 7.89 |
| CHEMBL597299 | — | — | 1 | 7.89 |
| CHEMBL599268 | — | — | 1 | 7.82 |
| CHEMBL597297 | — | — | 1 | 7.80 |
| CHEMBL605420 | — | — | 1 | 7.77 |
| CHEMBL596682 | — | — | 1 | 7.22 |
| CHEMBL597067 | — | — | 1 | 7.16 |
| CHEMBL597270 | — | — | 1 | 6.82 |
| CHEMBL597271 | — | — | 1 | 6.30 |
| CHEMBL606378 | — | — | 1 | 6.07 |
| CHEMBL599081 | — | — | 1 | 5.79 |
| CHEMBL599693 | — | — | 1 | 5.54 |
| CHEMBL603904 | — | — | 1 | 4.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3 | NICOTINE | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL122270 | LOBELINE | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL597085 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL596683 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL599267 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL603692 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL597298 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL605748 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL604306 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL597299 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL599268 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL597297 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL605420 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL596682 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL597067 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL597270 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL597271 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL606378 | — | Ki | = | 860.0 | nM | 6.07 |
| CHEMBL599081 | — | Ki | = | 1620.0 | nM | 5.79 |
| CHEMBL599693 | — | Ki | = | 2870.0 | nM | 5.54 |
| CHEMBL603904 | — | Ki | = | 19300.0 | nM | 4.71 |