Assay Detail
Functional
CHEMBL1815451
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against human alpha4beta2 nAChR in SHEP1 cells assessed as inhibition of carbamylcholine induced 86Rb+ efflux
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | SHEP1 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Nicotinic acetylcholine receptor efficacy and pharmacological properties of 3-(substituted phenyl)-2β-substituted tropanes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 4.96 | 5.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1812744 | — | — | 1 | 5.75 |
| CHEMBL1812747 | — | — | 1 | 5.11 |
| CHEMBL1812745 | — | — | 1 | 5.01 |
| CHEMBL1812750 | — | — | 1 | 4.96 |
| CHEMBL1812740 | — | — | 1 | 4.96 |
| CHEMBL1812739 | — | — | 1 | 4.92 |
| CHEMBL894 | BUPROPION | 4.0 | 1 | 4.92 |
| CHEMBL1812748 | — | — | 1 | 4.85 |
| CHEMBL1812743 | — | — | 1 | 4.82 |
| CHEMBL1812741 | — | — | 1 | 4.82 |
| CHEMBL1812746 | — | — | 1 | 4.80 |
| CHEMBL1812749 | — | — | 1 | 4.54 |
| CHEMBL1812742 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1812744 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL1812747 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL1812745 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL1812750 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL1812740 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL1812739 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL894 | BUPROPION | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL1812748 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL1812743 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL1812741 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL1812746 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL1812749 | — | IC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL1812742 | — | IC50 | = | 942000.0 | nM | - |