Assay Detail
Binding
CHEMBL1058165
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]epibatidine from alpha3 nAChR in human IMR32 cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | IMR-32 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Neuronal acetylcholine receptor subunit alpha-3 (CHEMBL3068) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and SAR studies of 1,4-diazabicyclo[3.2.2]nonane phenyl carbamates--subtype selective, high affinity alpha7 nicotinic acetylcholine receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 5.77 | 7.81 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL365956 | — | — | 1 | 7.81 |
| CHEMBL564825 | — | — | 1 | 5.86 |
| CHEMBL561469 | — | — | 1 | 5.68 |
| CHEMBL551330 | — | — | 1 | 5.40 |
| CHEMBL552994 | — | — | 1 | 5.32 |
| CHEMBL564850 | — | — | 1 | 5.31 |
| CHEMBL555703 | — | — | 1 | 5.00 |
| CHEMBL559478 | SSR180711 | 2.0 | 1 | - |
| CHEMBL561933 | — | — | 1 | - |
| CHEMBL551404 | — | — | 1 | - |
| CHEMBL561070 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL365956 | — | IC50 | = | 15.6 | nM | 7.81 |
| CHEMBL564825 | — | IC50 | = | 1390.0 | nM | 5.86 |
| CHEMBL561469 | — | IC50 | = | 2090.0 | nM | 5.68 |
| CHEMBL551330 | — | IC50 | = | 4020.0 | nM | 5.40 |
| CHEMBL552994 | — | IC50 | = | 4750.0 | nM | 5.32 |
| CHEMBL564850 | — | IC50 | = | 4910.0 | nM | 5.31 |
| CHEMBL555703 | — | IC50 | = | 9960.0 | nM | 5.00 |
| CHEMBL559478 | SSR180711 | IC50 | > | 6480.0 | nM | - |
| CHEMBL561933 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL551404 | — | IC50 | - | — | - | |
| CHEMBL561070 | — | IC50 | - | — | - |