Assay Detail
Binding
CHEMBL3089196
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Displacement of [3H]epibatidine from human alpha4beta2 nAChR after 4 hrs by cell-based assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Design, synthesis and discovery of picomolar selective α4β2 nicotinic acetylcholine receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 9.95 | 10.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3086984 | — | — | 1 | 10.51 |
| CHEMBL3086994 | — | — | 1 | 10.49 |
| CHEMBL3086985 | — | — | 1 | 10.37 |
| CHEMBL3086982 | — | — | 1 | 10.34 |
| CHEMBL3086991 | — | — | 1 | 10.31 |
| CHEMBL3086995 | — | — | 1 | 10.30 |
| CHEMBL2024096 | — | — | 1 | 10.21 |
| CHEMBL3086993 | — | — | 1 | 10.14 |
| CHEMBL3086986 | — | — | 1 | 10.12 |
| CHEMBL3086992 | — | — | 1 | 10.08 |
| CHEMBL3086983 | — | — | 1 | 10.03 |
| CHEMBL3086989 | — | — | 1 | 9.96 |
| CHEMBL1076903 | VARENICLINE | 4.0 | 1 | 9.89 |
| CHEMBL96201 | — | — | 1 | 9.85 |
| CHEMBL3086996 | — | — | 1 | 9.59 |
| CHEMBL3086990 | — | — | 1 | 8.92 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 8.00 |
| CHEMBL3086987 | — | — | 1 | - |
| CHEMBL3086988 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3086984 | — | Ki | = | 0.031 | nM | 10.51 |
| CHEMBL3086994 | — | Ki | = | 0.032 | nM | 10.49 |
| CHEMBL3086985 | — | Ki | = | 0.043 | nM | 10.37 |
| CHEMBL3086982 | — | Ki | = | 0.046 | nM | 10.34 |
| CHEMBL3086991 | — | Ki | = | 0.049 | nM | 10.31 |
| CHEMBL3086995 | — | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL2024096 | — | Ki | = | 0.062 | nM | 10.21 |
| CHEMBL3086993 | — | Ki | = | 0.072 | nM | 10.14 |
| CHEMBL3086986 | — | Ki | = | 0.076 | nM | 10.12 |
| CHEMBL3086992 | — | Ki | = | 0.083 | nM | 10.08 |
| CHEMBL3086983 | — | Ki | = | 0.093 | nM | 10.03 |
| CHEMBL3086989 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL1076903 | VARENICLINE | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL96201 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL3086996 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL3086990 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3 | NICOTINE | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL3086987 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL3086988 | — | Ki | > | 1000.0 | nM | - |