Assay Detail
Binding
CHEMBL868992
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]epibatidine from rat alpha-2-beta-4 nACHR expressed in human HEK293 cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha2/beta4 (CHEMBL1907590) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 6.35 | 10.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | — | 1 | 10.05 |
| CHEMBL497939 | CYTISINICLINE | 3.0 | 1 | 8.27 |
| CHEMBL205644 | — | — | 1 | 8.05 |
| CHEMBL379303 | — | — | 1 | 6.75 |
| CHEMBL208438 | — | — | 1 | 6.52 |
| CHEMBL208066 | — | — | 1 | 5.77 |
| CHEMBL382845 | — | — | 1 | 5.09 |
| CHEMBL378809 | — | — | 1 | 4.55 |
| CHEMBL205379 | — | — | 1 | 4.30 |
| CHEMBL205330 | — | — | 1 | 4.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.09 | nM | 10.05 |
| CHEMBL497939 | CYTISINICLINE | Ki | = | 5.41 | nM | 8.27 |
| CHEMBL205644 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL379303 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL208438 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL208066 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL382845 | — | Ki | = | 8100.0 | nM | 5.09 |
| CHEMBL378809 | — | Ki | = | 28000.0 | nM | 4.55 |
| CHEMBL205379 | — | Ki | = | 50000.0 | nM | 4.30 |
| CHEMBL205330 | — | Ki | = | 75000.0 | nM | 4.12 |