Assay Detail
Functional
CHEMBL2168998
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human alpha4beta2 nACHR expressed in SH-EP1 cells by 86Rb+ efflux assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | SH-EP1 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha3/beta4 (CHEMBL1907594) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Identification of novel α4β2-nicotinic acetylcholine receptor (nAChR) agonists based on an isoxazole ether scaffold that demonstrate antidepressant-like activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 6.07 | 6.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3 | NICOTINE | 4.0 | 1 | 6.54 |
| CHEMBL2165443 | — | — | 1 | 5.96 |
| CHEMBL2165444 | — | — | 1 | 5.93 |
| CHEMBL1076903 | VARENICLINE | 4.0 | 1 | 5.85 |
| CHEMBL2165445 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3 | NICOTINE | EC50 | = | 290.0 | nM | 6.54 |
| CHEMBL2165443 | — | EC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL2165444 | — | EC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL1076903 | VARENICLINE | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL2165445 | — | EC50 | > | 3000.0 | nM | - |