Assay Detail
Functional
CHEMBL834065
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Change in membrane potential in TE-671 cells expressing acetylcholine neuromuscular receptors
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | TE-671 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Acetylcholine receptor; alpha1/beta1/delta/gamma (CHEMBL1907588) ↗| 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 | 8.01 | 10.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | — | 1 | 10.28 |
| CHEMBL497939 | CYTISINICLINE | 3.0 | 1 | 7.96 |
| CHEMBL64496 | — | — | 1 | 7.55 |
| CHEMBL305106 | — | — | 1 | 7.51 |
| CHEMBL181840 | — | — | 1 | 7.43 |
| CHEMBL62858 | — | — | 1 | 7.35 |
| CHEMBL432712 | — | — | 1 | - |
| CHEMBL65324 | — | — | 1 | - |
| CHEMBL292054 | — | — | 1 | - |
| CHEMBL291398 | — | — | 1 | - |
| CHEMBL293649 | — | — | 1 | - |
| CHEMBL294311 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | EC50 | = | 0.053 | nM | 10.28 |
| CHEMBL497939 | CYTISINICLINE | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL64496 | — | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL305106 | — | EC50 | = | 31.0 | nM | 7.51 |
| CHEMBL181840 | — | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL62858 | — | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL432712 | — | EC50 | > | 100.0 | nM | - |
| CHEMBL65324 | — | EC50 | > | 100.0 | nM | - |
| CHEMBL292054 | — | EC50 | > | 100.0 | nM | - |
| CHEMBL291398 | — | EC50 | > | 100.0 | nM | - |
| CHEMBL293649 | — | EC50 | > | 100.0 | nM | - |
| CHEMBL294311 | — | EC50 | > | 100.0 | nM | - |