Assay Detail
Functional
CHEMBL1068974
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Antagonist activity at nicotinic acetylcholine receptor in rat striatal slices assessed as inhibition of S-(-)-nicotine-induced [3H]dopamine release
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Novel bis-2,2,6,6-tetramethylpiperidine (bis-TMP) and bis-mecamylamine antagonists at neuronal nicotinic receptors mediating nicotine-evoked dopamine release.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.98 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL239844 | — | — | 1 | 9.70 |
| CHEMBL54331 | — | — | 1 | 8.70 |
| CHEMBL600214 | — | — | 1 | 8.66 |
| CHEMBL605784 | — | — | 1 | 7.34 |
| CHEMBL589476 | — | — | 1 | 6.97 |
| CHEMBL600418 | — | — | 1 | 6.50 |
| CHEMBL602685 | — | — | 1 | - |
| CHEMBL602686 | — | — | 1 | - |
| CHEMBL601877 | — | — | 1 | - |
| CHEMBL601446 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL239844 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL54331 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL600214 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL605784 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL589476 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL600418 | — | IC50 | = | 319.0 | nM | 6.50 |
| CHEMBL602685 | — | IC50 | - | — | - | |
| CHEMBL602686 | — | IC50 | - | — | - | |
| CHEMBL601877 | — | IC50 | - | — | - | |
| CHEMBL601446 | — | IC50 | - | — | - |