Assay Detail
Binding
CHEMBL3603305
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Antagonist activity at rat alpha-7 nicotinic acetylcholine receptor expressed in Xenopus oocytes assessed as inhibition of acetylcholine-induced currents preincubated for 10 mins followed by nicotine induction by two-electrode voltage-clamp electrophysiology assay
8
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL4980) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Pharmacological profile of zacopride and new quaternarized fluorobenzamide analogues on mammalian α7 nicotinic acetylcholine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 4.80 | 5.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL18041 | ZACOPRIDE | 2.0 | 2 | 5.15 |
| CHEMBL3600666 | — | — | 2 | 5.09 |
| CHEMBL3600667 | — | — | 2 | 4.55 |
| CHEMBL3600668 | — | — | 2 | 4.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL18041 | ZACOPRIDE | IC50 | = | 7079.46 | nM | 5.15 |
| CHEMBL18041 | ZACOPRIDE | IC50 | = | 7040.0 | nM | 5.15 |
| CHEMBL3600666 | — | IC50 | = | 8128.31 | nM | 5.09 |
| CHEMBL3600666 | — | IC50 | = | 8070.0 | nM | 5.09 |
| CHEMBL3600667 | — | IC50 | = | 28183.83 | nM | 4.55 |
| CHEMBL3600667 | — | IC50 | = | 28400.0 | nM | 4.55 |
| CHEMBL3600668 | — | IC50 | = | 38904.51 | nM | 4.41 |
| CHEMBL3600668 | — | IC50 | = | 39300.0 | nM | 4.41 |