Assay Detail
Binding
CHEMBL3089194
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Displacement of [3H]epibatidine from rat alpha7 nAChR expressed in HEK293 cells after 4 hrs
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL4980) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Design, synthesis and discovery of picomolar selective α4β2 nicotinic acetylcholine receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 6.05 | 7.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1076903 | VARENICLINE | 4.0 | 1 | 7.21 |
| CHEMBL3086982 | — | — | 1 | 6.70 |
| CHEMBL3086984 | — | — | 1 | 6.60 |
| CHEMBL3086983 | — | — | 1 | 6.32 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 6.28 |
| CHEMBL3086991 | — | — | 1 | 6.24 |
| CHEMBL3086985 | — | — | 1 | 6.23 |
| CHEMBL2024096 | — | — | 1 | 6.17 |
| CHEMBL3086994 | — | — | 1 | 6.14 |
| CHEMBL3086993 | — | — | 1 | 5.96 |
| CHEMBL3086996 | — | — | 1 | 5.89 |
| CHEMBL3086986 | — | — | 1 | 5.82 |
| CHEMBL3086989 | — | — | 1 | 5.80 |
| CHEMBL3086995 | — | — | 1 | 5.75 |
| CHEMBL3086992 | — | — | 1 | 5.70 |
| CHEMBL3086990 | — | — | 1 | 5.11 |
| CHEMBL96201 | — | — | 1 | 4.96 |
| CHEMBL3086987 | — | — | 1 | - |
| CHEMBL3086988 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1076903 | VARENICLINE | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL3086982 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL3086984 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL3086983 | — | Ki | = | 480.0 | nM | 6.32 |
| CHEMBL3 | NICOTINE | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL3086991 | — | Ki | = | 580.0 | nM | 6.24 |
| CHEMBL3086985 | — | Ki | = | 590.0 | nM | 6.23 |
| CHEMBL2024096 | — | Ki | = | 670.0 | nM | 6.17 |
| CHEMBL3086994 | — | Ki | = | 720.0 | nM | 6.14 |
| CHEMBL3086993 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL3086996 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL3086986 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL3086989 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL3086995 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL3086992 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL3086990 | — | Ki | = | 7700.0 | nM | 5.11 |
| CHEMBL96201 | — | Ki | = | 11000.0 | nM | 4.96 |
| CHEMBL3086987 | — | Ki | > | 250000.0 | nM | - |
| CHEMBL3086988 | — | Ki | > | 25000.0 | nM | - |