Assay Detail
Binding
CHEMBL3385677
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Agonist activity at human alpha4beta2 nAChR expressed in SH-EP1 cells by [86Rb+] ion efflux assay
14
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SH-EP1 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Enantiopure Cyclopropane-Bearing Pyridyldiazabicyclo[3.3.0]octanes as Selective α4β2-nAChR Ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 14 | 7.58 | 8.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2024096 | — | — | 1 | 8.24 |
| CHEMBL3356148 | — | — | 2 | 7.90 |
| CHEMBL3356150 | — | — | 2 | 7.80 |
| CHEMBL2024094 | — | — | 1 | 7.75 |
| CHEMBL3356152 | — | — | 2 | 7.70 |
| CHEMBL3356151 | — | — | 2 | 7.60 |
| CHEMBL3 | NICOTINE | 4.0 | 2 | 6.52 |
| CHEMBL3356149 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2024096 | — | EC50 | = | 5.8 | nM | 8.24 |
| CHEMBL3356148 | — | EC50 | = | 12.59 | nM | 7.90 |
| CHEMBL3356148 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3356150 | — | EC50 | = | 15.85 | nM | 7.80 |
| CHEMBL2024094 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3356150 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3356152 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3356152 | — | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL3356151 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3356151 | — | EC50 | = | 25.12 | nM | 7.60 |
| CHEMBL3 | NICOTINE | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3 | NICOTINE | EC50 | = | 316.23 | nM | 6.50 |
| CHEMBL3356149 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL3356149 | — | EC50 | > | 1000.0 | nM | - |