Assay Detail
Functional
CHEMBL838016
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Change in membrane potential in K-177 cells expressing acetylcholine central neuronal receptor alpha4-beta2 subunits
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | K-177 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
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 | 8.99 | 10.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL62858 | — | — | 1 | 10.44 |
| CHEMBL305106 | — | — | 1 | 10.30 |
| CHEMBL64496 | — | — | 1 | 9.96 |
| CHEMBL497939 | CYTISINICLINE | 3.0 | 1 | 9.38 |
| CHEMBL432712 | — | — | 1 | 8.96 |
| CHEMBL293649 | — | — | 1 | 8.66 |
| CHEMBL294311 | — | — | 1 | 8.40 |
| CHEMBL181840 | — | — | 1 | 7.39 |
| CHEMBL291398 | — | — | 1 | 7.38 |
| CHEMBL65324 | — | — | 1 | - |
| CHEMBL292054 | — | — | 1 | - |
| CHEMBL6623 | EPIBATIDINE | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL62858 | — | EC50 | = | 0.036 | nM | 10.44 |
| CHEMBL305106 | — | EC50 | = | 0.05 | nM | 10.30 |
| CHEMBL64496 | — | EC50 | = | 0.11 | nM | 9.96 |
| CHEMBL497939 | CYTISINICLINE | EC50 | = | 0.42 | nM | 9.38 |
| CHEMBL432712 | — | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL293649 | — | EC50 | = | 2.2 | nM | 8.66 |
| CHEMBL294311 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL181840 | — | EC50 | = | 41.0 | nM | 7.39 |
| CHEMBL291398 | — | EC50 | = | 42.0 | nM | 7.38 |
| CHEMBL65324 | — | EC50 | > | 100.0 | nM | - |
| CHEMBL292054 | — | EC50 | > | 100.0 | nM | - |
| CHEMBL6623 | EPIBATIDINE | EC50 | = | 0.0088 | nM | - |