Assay Detail
Binding
CHEMBL3868322
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-cytisine from alpha4beta2-nACHR in rat whole brain
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Novel 5-substituted 3-hydroxyphenyl and 3-nitrophenyl ethers of S-prolinol as α4β2-nicotinic acetylcholine receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 8.70 | 9.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL156048 | — | — | 1 | 9.96 |
| CHEMBL84149 | — | — | 1 | 9.82 |
| CHEMBL82494 | — | — | 1 | 9.57 |
| CHEMBL73786 | — | — | 1 | 7.38 |
| CHEMBL305820 | — | — | 1 | 6.76 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL156048 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL84149 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL82494 | — | Ki | = | 0.27 | nM | 9.57 |
| CHEMBL73786 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL305820 | — | Ki | = | 175.0 | nM | 6.76 |