Assay Detail
Functional
CHEMBL1815452
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against human ganglionic alpha3beta4alpha5beta2 nAChR in SHSY5Y 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 | SH-SY5Y |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Integrin alpha-5/Neuronal acetylcholine receptor subunit alpha-3/Neuronal acetylcholine receptor subunit beta-2/Neuronal acetylcholine receptor subunit beta-4 (CHEMBL3885595) ↗| 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 | 5.68 | 6.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1812744 | — | — | 1 | 6.24 |
| CHEMBL1812747 | — | — | 1 | 6.14 |
| CHEMBL1812740 | — | — | 1 | 5.89 |
| CHEMBL1812748 | — | — | 1 | 5.85 |
| CHEMBL1812741 | — | — | 1 | 5.77 |
| CHEMBL1812743 | — | — | 1 | 5.75 |
| CHEMBL1812739 | — | — | 1 | 5.75 |
| CHEMBL894 | BUPROPION | 4.0 | 1 | 5.75 |
| CHEMBL1812750 | — | — | 1 | 5.58 |
| CHEMBL1812746 | — | — | 1 | 5.51 |
| CHEMBL1812749 | — | — | 1 | 5.50 |
| CHEMBL1812745 | — | — | 1 | 5.44 |
| CHEMBL1812742 | — | — | 1 | 4.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1812744 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL1812747 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL1812740 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1812748 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL1812741 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL1812743 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL1812739 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL894 | BUPROPION | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL1812750 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL1812746 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL1812749 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL1812745 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL1812742 | — | IC50 | = | 20000.0 | nM | 4.70 |