Assay Detail
Binding
CHEMBL3376072
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Non-competitive inhibition of rat alpha3beta4 nAChR expressed in KX cells assessed as reduction in current by whole-cell patch clamp assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | KX |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha3/beta4 (CHEMBL1907593) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Synthesis, in vitro and in vivo studies, and molecular modeling of N-alkylated dextromethorphan derivatives as non-competitive inhibitors of α3β4 nicotinic acetylcholine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 5.11 | 5.71 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3356771 | — | — | 1 | 5.71 |
| CHEMBL3356773 | — | — | 1 | 5.60 |
| CHEMBL3356775 | — | — | 1 | 5.59 |
| CHEMBL1638 | — | — | 1 | 5.51 |
| CHEMBL3356774 | — | — | 1 | 5.18 |
| CHEMBL3356772 | — | — | 1 | 5.15 |
| CHEMBL3356767 | — | — | 1 | 4.98 |
| CHEMBL52440 | DEXTROMETHORPHAN | 4.0 | 1 | 4.96 |
| CHEMBL3356770 | — | — | 1 | 4.38 |
| CHEMBL3356769 | — | — | 1 | 4.06 |
| CHEMBL3356768 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3356771 | — | IC50 | = | 1950.0 | nM | 5.71 |
| CHEMBL3356773 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3356775 | — | IC50 | = | 2570.0 | nM | 5.59 |
| CHEMBL1638 | — | IC50 | = | 3080.0 | nM | 5.51 |
| CHEMBL3356774 | — | IC50 | = | 6610.0 | nM | 5.18 |
| CHEMBL3356772 | — | IC50 | = | 7140.0 | nM | 5.15 |
| CHEMBL3356767 | — | IC50 | = | 10470.0 | nM | 4.98 |
| CHEMBL52440 | DEXTROMETHORPHAN | IC50 | = | 11050.0 | nM | 4.96 |
| CHEMBL3356770 | — | IC50 | = | 41400.0 | nM | 4.38 |
| CHEMBL3356769 | — | IC50 | = | 87000.0 | nM | 4.06 |
| CHEMBL3356768 | — | IC50 | = | 176000.0 | nM | - |