Assay Detail
Binding
CHEMBL867841
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]epibatidine from rat alpha-4-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; alpha4/beta4 (CHEMBL1907595) ↗| 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 | 6.75 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | — | 1 | 9.80 |
| CHEMBL497939 | CYTISINICLINE | 3.0 | 1 | 8.68 |
| CHEMBL205644 | — | — | 1 | 8.64 |
| CHEMBL379303 | — | — | 1 | 7.42 |
| CHEMBL208438 | — | — | 1 | 7.17 |
| CHEMBL208066 | — | — | 1 | 6.23 |
| CHEMBL382845 | — | — | 1 | 5.48 |
| CHEMBL378809 | — | — | 1 | 4.89 |
| CHEMBL205379 | — | — | 1 | 4.70 |
| CHEMBL205330 | — | — | 1 | 4.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL497939 | CYTISINICLINE | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL205644 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL379303 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL208438 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL208066 | — | Ki | = | 590.0 | nM | 6.23 |
| CHEMBL382845 | — | Ki | = | 3300.0 | nM | 5.48 |
| CHEMBL378809 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL205379 | — | Ki | = | 20000.0 | nM | 4.70 |
| CHEMBL205330 | — | Ki | = | 33000.0 | nM | 4.48 |