Assay Detail
Functional
CHEMBL825005
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Effective concentration in KXalpha-3-beta-4R2 cells expressing rat nicotinic acetylcholine receptor alpha3-beta4 subunits
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha3/beta4 (CHEMBL1907593) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Halogenated and isosteric cytisine derivatives with increased affinity and functional activity at nicotinic acetylcholine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 8.68 | 10.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | — | 1 | 10.43 |
| CHEMBL62858 | — | — | 1 | 9.26 |
| CHEMBL305106 | — | — | 1 | 9.06 |
| CHEMBL64496 | — | — | 1 | 8.29 |
| CHEMBL497939 | CYTISINICLINE | 3.0 | 1 | 7.60 |
| CHEMBL432712 | — | — | 1 | 7.41 |
| CHEMBL65324 | — | — | 1 | - |
| CHEMBL292054 | — | — | 1 | - |
| CHEMBL291398 | — | — | 1 | - |
| CHEMBL293649 | — | — | 1 | - |
| CHEMBL181840 | — | — | 1 | - |
| CHEMBL294311 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | EC50 | = | 0.037 | nM | 10.43 |
| CHEMBL62858 | — | EC50 | = | 0.55 | nM | 9.26 |
| CHEMBL305106 | — | EC50 | = | 0.88 | nM | 9.06 |
| CHEMBL64496 | — | EC50 | = | 5.1 | nM | 8.29 |
| CHEMBL497939 | CYTISINICLINE | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL432712 | — | EC50 | = | 39.0 | nM | 7.41 |
| CHEMBL65324 | — | EC50 | > | 100.0 | nM | - |
| CHEMBL292054 | — | EC50 | > | 100.0 | nM | - |
| CHEMBL291398 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL293649 | — | EC50 | > | 100.0 | nM | - |
| CHEMBL181840 | — | EC50 | > | 100.0 | nM | - |
| CHEMBL294311 | — | EC50 | > | 100.0 | nM | - |