Assay Detail
Binding
CHEMBL3089193
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Displacement of [3H]epibatidine from nAChR in rat forebrain
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Forebrain |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Design, synthesis and discovery of picomolar selective α4β2 nicotinic acetylcholine receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 8.92 | 9.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2024096 | — | — | 1 | 9.77 |
| CHEMBL3086994 | — | — | 1 | 9.36 |
| CHEMBL3086991 | — | — | 1 | 9.30 |
| CHEMBL3086992 | — | — | 1 | 9.30 |
| CHEMBL3086993 | — | — | 1 | 9.24 |
| CHEMBL1076903 | VARENICLINE | 4.0 | 1 | 9.15 |
| CHEMBL3086984 | — | — | 1 | 9.15 |
| CHEMBL3086995 | — | — | 1 | 9.14 |
| CHEMBL96201 | — | — | 1 | 8.96 |
| CHEMBL3086982 | — | — | 1 | 8.96 |
| CHEMBL3086989 | — | — | 1 | 8.96 |
| CHEMBL3086985 | — | — | 1 | 8.85 |
| CHEMBL3086983 | — | — | 1 | 8.77 |
| CHEMBL3086986 | — | — | 1 | 8.77 |
| CHEMBL3086996 | — | — | 1 | 8.46 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 7.92 |
| CHEMBL3086990 | — | — | 1 | 7.52 |
| CHEMBL3086987 | — | — | 1 | - |
| CHEMBL3086988 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2024096 | — | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL3086994 | — | Ki | = | 0.44 | nM | 9.36 |
| CHEMBL3086991 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3086992 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3086993 | — | Ki | = | 0.58 | nM | 9.24 |
| CHEMBL1076903 | VARENICLINE | Ki | = | 0.71 | nM | 9.15 |
| CHEMBL3086984 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL3086995 | — | Ki | = | 0.73 | nM | 9.14 |
| CHEMBL96201 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL3086982 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL3086989 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL3086985 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL3086983 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL3086986 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL3086996 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL3 | NICOTINE | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL3086990 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL3086987 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL3086988 | — | Ki | > | 50000.0 | nM | - |