Assay Detail
Binding
CHEMBL4059304
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]cytisine from human alpha4beta2 nAChR expressed in human SH-EP1 cell membranes after 75 mins by liquid scintillation spectrometry
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Dual Nicotinic Acetylcholine Receptor α4β2 Antagonists/α7 Agonists: Synthesis, Docking Studies, and Pharmacological Evaluation of Tetrahydroisoquinolines and Tetrahydroisoquinolinium Salts.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 2 | 6.76 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL446533 | ERYSODINE | — | 1 | 7.30 |
| CHEMBL442947 | ERYSOTRINE | — | 1 | 6.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL446533 | ERYSODINE | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL442947 | ERYSOTRINE | Ki | = | 600.0 | nM | 6.22 |