Assay Detail
Binding
CHEMBL838862
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Binding affinity against nicotinic acetylcholine receptor alpha4-beta2 in human HEK293 cells using [3H]- nicotine as radioligand
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
In pursuit of alpha4beta2 nicotinic receptor partial agonists for smoking cessation: carbon analogs of (-)-cytisine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 7.97 | 9.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL497939 | CYTISINICLINE | 3.0 | 1 | 9.64 |
| CHEMBL365965 | — | — | 1 | 9.36 |
| CHEMBL187992 | — | — | 1 | 8.85 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 8.80 |
| CHEMBL191867 | — | — | 1 | 8.70 |
| CHEMBL190502 | — | — | 1 | 8.54 |
| CHEMBL191174 | — | — | 1 | 8.31 |
| CHEMBL373359 | — | — | 1 | 8.24 |
| CHEMBL191988 | — | — | 1 | 8.19 |
| CHEMBL190826 | — | — | 1 | 8.19 |
| CHEMBL189968 | — | — | 1 | 8.15 |
| CHEMBL264986 | — | — | 1 | 7.89 |
| CHEMBL190192 | — | — | 1 | 7.89 |
| CHEMBL365578 | — | — | 1 | 7.85 |
| CHEMBL191784 | — | — | 1 | 7.47 |
| CHEMBL373144 | — | — | 1 | 7.47 |
| CHEMBL193889 | — | — | 1 | 7.14 |
| CHEMBL425906 | — | — | 1 | 7.05 |
| CHEMBL189973 | — | — | 1 | 6.70 |
| CHEMBL192726 | — | — | 1 | 6.58 |
| CHEMBL189898 | — | — | 1 | 6.43 |
| CHEMBL190749 | — | — | 1 | - |
| CHEMBL193144 | — | — | 1 | - |
| CHEMBL190013 | — | — | 1 | - |
| CHEMBL371397 | — | — | 1 | - |
| CHEMBL190754 | — | — | 1 | - |
| CHEMBL193005 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL497939 | CYTISINICLINE | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL365965 | — | Ki | = | 0.44 | nM | 9.36 |
| CHEMBL187992 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL3 | NICOTINE | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL191867 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL190502 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL191174 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL373359 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL191988 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL190826 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL189968 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL264986 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL190192 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL365578 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL191784 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL373144 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL193889 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL425906 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL189973 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL192726 | — | Ki | = | 264.0 | nM | 6.58 |
| CHEMBL189898 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL190749 | — | Ki | > | 500.0 | nM | - |
| CHEMBL193144 | — | Ki | > | 500.0 | nM | - |
| CHEMBL190013 | — | Ki | > | 500.0 | nM | - |
| CHEMBL371397 | — | Ki | > | 500.0 | nM | - |
| CHEMBL190754 | — | Ki | > | 500.0 | nM | - |
| CHEMBL193005 | — | Ki | > | 500.0 | nM | - |