Assay Detail
Binding
CHEMBL950044
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]nicotine from alpha4beta2 nAChR in Sprague-Dawley rat brain membrane
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Deconstructing cytisine: The syntheses of (+/-)-cyfusine and (+/-)-cyclopropylcyfusine, fused ring analogs of cytisine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 8.00 | 9.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL497939 | CYTISINICLINE | 3.0 | 1 | 9.37 |
| CHEMBL404660 | CYFUSINE | — | 1 | 7.80 |
| CHEMBL401532 | CYCLOPROPYLCYFUSINE | — | 1 | 6.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL497939 | CYTISINICLINE | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL404660 | CYFUSINE | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL401532 | CYCLOPROPYLCYFUSINE | Ki | = | 144.0 | nM | 6.84 |