Assay Detail
Functional
CHEMBL1815450
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Antagonist activity against human alpha4beta4 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/beta4 (CHEMBL1907591) ↗| 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 | 5.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1812744 | — | — | 1 | 5.37 |
| CHEMBL1812748 | — | — | 1 | 5.34 |
| CHEMBL1812747 | — | — | 1 | 5.24 |
| CHEMBL1812740 | — | — | 1 | 5.14 |
| CHEMBL1812739 | — | — | 1 | 5.06 |
| CHEMBL1812741 | — | — | 1 | 5.00 |
| CHEMBL1812746 | — | — | 1 | 4.92 |
| CHEMBL1812749 | — | — | 1 | 4.82 |
| CHEMBL894 | BUPROPION | 4.0 | 1 | 4.82 |
| CHEMBL1812745 | — | — | 1 | 4.62 |
| CHEMBL1812750 | — | — | 1 | 4.60 |
| CHEMBL1812742 | — | — | 1 | 4.24 |
| CHEMBL1812743 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1812744 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL1812748 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL1812747 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL1812740 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL1812739 | — | IC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL1812741 | — | IC50 | = | 9900.0 | nM | 5.00 |
| CHEMBL1812746 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL1812749 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL894 | BUPROPION | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL1812745 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL1812750 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL1812742 | — | IC50 | = | 57000.0 | nM | 4.24 |
| CHEMBL1812743 | — | IC50 | > | 100000.0 | nM | - |