Assay Detail
Functional
CHEMBL1815456
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against human muscle-type alpha1beta1gammadelta nAChR in TE671/RD 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 | TE671/RD |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Acetylcholine receptor; alpha1/beta1/delta/gamma (CHEMBL1907588) ↗| 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 | 4.93 | 5.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1812748 | — | — | 1 | 5.52 |
| CHEMBL1812744 | — | — | 1 | 5.33 |
| CHEMBL1812750 | — | — | 1 | 5.14 |
| CHEMBL894 | BUPROPION | 4.0 | 1 | 5.10 |
| CHEMBL1812740 | — | — | 1 | 5.02 |
| CHEMBL1812741 | — | — | 1 | 5.00 |
| CHEMBL1812746 | — | — | 1 | 4.96 |
| CHEMBL1812739 | — | — | 1 | 4.92 |
| CHEMBL1812749 | — | — | 1 | 4.89 |
| CHEMBL1812747 | — | — | 1 | 4.89 |
| CHEMBL1812743 | — | — | 1 | 4.72 |
| CHEMBL1812745 | — | — | 1 | 4.58 |
| CHEMBL1812742 | — | — | 1 | 4.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1812748 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL1812744 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL1812750 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL894 | BUPROPION | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL1812740 | — | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL1812741 | — | IC50 | = | 9900.0 | nM | 5.00 |
| CHEMBL1812746 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL1812739 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL1812749 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL1812747 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL1812743 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL1812745 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL1812742 | — | IC50 | = | 95000.0 | nM | 4.02 |