Assay Detail
Binding
CHEMBL1211577
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Displacement of [3H]epibatidine from alpha4beta2 nicotinic receptor expressed in human HEK293 cells
24
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
A novel series of [3.2.1] azabicyclic biaryl ethers as alpha3beta4 and alpha6/4beta4 nicotinic receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 6.76 | 9.53 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1076903 | VARENICLINE | 4.0 | 1 | 9.53 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 8.02 |
| CHEMBL1209125 | — | — | 1 | 6.83 |
| CHEMBL1209124 | — | — | 2 | 6.60 |
| CHEMBL1209186 | — | — | 1 | 6.60 |
| CHEMBL1209187 | — | — | 2 | 6.47 |
| CHEMBL1209072 | — | — | 1 | 6.32 |
| CHEMBL1209244 | — | — | 1 | 6.13 |
| CHEMBL1209126 | — | — | 1 | 5.73 |
| CHEMBL1209242 | — | — | 1 | 5.54 |
| CHEMBL1209071 | — | — | 1 | - |
| CHEMBL1209073 | — | — | 1 | - |
| CHEMBL1209123 | — | — | 1 | - |
| CHEMBL1209183 | — | — | 1 | - |
| CHEMBL1209184 | — | — | 1 | - |
| CHEMBL1209070 | — | — | 2 | - |
| CHEMBL1209243 | — | — | 1 | - |
| CHEMBL1209305 | — | — | 1 | - |
| CHEMBL1209306 | — | — | 1 | - |
| CHEMBL1209307 | — | — | 1 | - |
| CHEMBL1209185 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1076903 | VARENICLINE | Ki | = | 0.295 | nM | 9.53 |
| CHEMBL3 | NICOTINE | Ki | = | 9.46 | nM | 8.02 |
| CHEMBL1209125 | — | Ki | = | 149.0 | nM | 6.83 |
| CHEMBL1209124 | — | Ki | = | 252.0 | nM | 6.60 |
| CHEMBL1209186 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL1209124 | — | Ki | = | 255.0 | nM | 6.59 |
| CHEMBL1209187 | — | Ki | = | 336.0 | nM | 6.47 |
| CHEMBL1209072 | — | Ki | = | 477.0 | nM | 6.32 |
| CHEMBL1209244 | — | Ki | = | 745.0 | nM | 6.13 |
| CHEMBL1209126 | — | Ki | = | 1860.0 | nM | 5.73 |
| CHEMBL1209242 | — | Ki | = | 2905.0 | nM | 5.54 |
| CHEMBL1209070 | — | Ki | > | 832.0 | nM | - |
| CHEMBL1209071 | — | Ki | > | 614.0 | nM | - |
| CHEMBL1209073 | — | Ki | > | 309.0 | nM | - |
| CHEMBL1209123 | — | Ki | > | 419.0 | nM | - |
| CHEMBL1209183 | — | Ki | > | 1503.0 | nM | - |
| CHEMBL1209184 | — | Ki | > | 1040.0 | nM | - |
| CHEMBL1209070 | — | Ki | > | 1307.0 | nM | - |
| CHEMBL1209187 | — | Ki | > | 424.0 | nM | - |
| CHEMBL1209243 | — | Ki | > | 604.0 | nM | - |
| CHEMBL1209305 | — | Ki | > | 615.5 | nM | - |
| CHEMBL1209306 | — | Ki | > | 962.5 | nM | - |
| CHEMBL1209307 | — | Ki | - | — | - | |
| CHEMBL1209185 | — | Ki | > | 575.0 | nM | - |