Assay Detail
Functional
CHEMBL953567
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human alpha3beta4 nAChR expressed in HEK293 cells by calcium influx assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha3/beta4 (CHEMBL1907594) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Gamma-lactams--a novel scaffold for highly potent and selective alpha 7 nicotinic acetylcholine receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.74 | 6.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL459900 | — | — | 1 | 6.10 |
| CHEMBL459689 | — | — | 1 | 6.00 |
| CHEMBL503427 | — | — | 1 | 6.00 |
| CHEMBL454407 | — | — | 1 | 5.90 |
| CHEMBL499536 | — | — | 1 | 4.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL459900 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL459689 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL503427 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL454407 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL499536 | — | IC50 | = | 19952.62 | nM | 4.70 |