Assay Detail
Functional
CHEMBL2187464
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human alpha4beta2 nAChR expressed in human SH-EP1 cells by whole cell voltage clamp based electrophysiology method
7
Total Activities
7
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; alpha4/beta2 (CHEMBL1907589) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Structure-activity studies of 7-heteroaryl-3-azabicyclo[3.3.1]non-6-enes: a novel class of highly potent nicotinic receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 7 | 6.12 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2177537 | — | — | 1 | 7.30 |
| CHEMBL2177538 | — | — | 1 | 7.00 |
| CHEMBL2177545 | — | — | 1 | 6.23 |
| CHEMBL2177543 | — | — | 1 | 5.85 |
| CHEMBL2177539 | — | — | 1 | 5.51 |
| CHEMBL2177544 | — | — | 1 | 5.46 |
| CHEMBL2177540 | — | — | 1 | 5.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2177537 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2177538 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2177545 | — | EC50 | = | 590.0 | nM | 6.23 |
| CHEMBL2177543 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL2177539 | — | EC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL2177544 | — | EC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL2177540 | — | EC50 | = | 3500.0 | nM | 5.46 |