Assay Detail
Binding
CHEMBL756011
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Binding affinity for nicotinic acetylcholine receptor alpha4-beta2 was evaluated by its ability to inhibit [3H]NIC binding to rat brain membranes
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 7 — Homologous single protein target |
| Curated By | Intermediate |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
bis-Azaaromatic quaternary ammonium analogues: ligands for alpha4beta2* and alpha7* subtypes of neuronal nicotinic receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 38 | 5.09 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3 | NICOTINE | 4.0 | 1 | 8.85 |
| CHEMBL56296 | — | — | 1 | 7.19 |
| CHEMBL106542 | — | — | 1 | 6.48 |
| CHEMBL105342 | — | — | 1 | 6.37 |
| CHEMBL105440 | — | — | 1 | 5.81 |
| CHEMBL510275 | METHYLLYCACONITINE | — | 1 | 5.81 |
| CHEMBL420649 | — | — | 1 | 5.71 |
| CHEMBL320514 | — | — | 1 | 5.30 |
| CHEMBL1134 | DECAMETHONIUM BROMIDE | 4.0 | 1 | 5.24 |
| CHEMBL105537 | — | — | 1 | 5.21 |
| CHEMBL104553 | — | — | 1 | 5.10 |
| CHEMBL102757 | — | — | 1 | 5.04 |
| CHEMBL104613 | — | — | 1 | 5.04 |
| CHEMBL1687 | — | — | 1 | 5.01 |
| CHEMBL430886 | — | — | 1 | 4.85 |
| CHEMBL323144 | — | — | 1 | 4.75 |
| CHEMBL105794 | — | — | 1 | 4.73 |
| CHEMBL293527 | — | — | 1 | 4.71 |
| CHEMBL104461 | — | — | 1 | 4.70 |
| CHEMBL105608 | HEXAMETHONIUM CHLORIDE | — | 1 | 4.66 |
| CHEMBL105017 | — | — | 1 | 4.65 |
| CHEMBL105742 | — | — | 1 | 4.62 |
| CHEMBL105106 | — | — | 1 | 4.46 |
| CHEMBL105257 | — | — | 1 | 4.42 |
| CHEMBL430870 | — | — | 1 | 4.41 |
| CHEMBL54331 | — | — | 1 | 4.31 |
| CHEMBL104265 | — | — | 1 | 4.18 |
| CHEMBL52918 | — | — | 1 | 4.16 |
| CHEMBL53780 | — | — | 1 | 4.10 |
| CHEMBL104381 | — | — | 1 | 4.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3 | NICOTINE | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL56296 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL106542 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL105342 | — | Ki | = | 430.0 | nM | 6.37 |
| CHEMBL105440 | — | Ki | = | 1540.0 | nM | 5.81 |
| CHEMBL510275 | METHYLLYCACONITINE | Ki | = | 1560.0 | nM | 5.81 |
| CHEMBL420649 | — | Ki | = | 1950.0 | nM | 5.71 |
| CHEMBL320514 | — | Ki | = | 5030.0 | nM | 5.30 |
| CHEMBL1134 | DECAMETHONIUM BROMIDE | Ki | = | 5730.0 | nM | 5.24 |
| CHEMBL105537 | — | Ki | = | 6100.0 | nM | 5.21 |
| CHEMBL104553 | — | Ki | = | 7890.0 | nM | 5.10 |
| CHEMBL102757 | — | Ki | = | 9150.0 | nM | 5.04 |
| CHEMBL104613 | — | Ki | = | 9020.0 | nM | 5.04 |
| CHEMBL1687 | — | Ki | = | 9720.0 | nM | 5.01 |
| CHEMBL430886 | — | Ki | = | 14000.0 | nM | 4.85 |
| CHEMBL323144 | — | Ki | = | 17900.0 | nM | 4.75 |
| CHEMBL105794 | — | Ki | = | 18700.0 | nM | 4.73 |
| CHEMBL293527 | — | Ki | = | 19700.0 | nM | 4.71 |
| CHEMBL104461 | — | Ki | = | 20000.0 | nM | 4.70 |
| CHEMBL105608 | HEXAMETHONIUM CHLORIDE | Ki | = | 21700.0 | nM | 4.66 |
| CHEMBL105017 | — | Ki | = | 22500.0 | nM | 4.65 |
| CHEMBL105742 | — | Ki | = | 24200.0 | nM | 4.62 |
| CHEMBL105106 | — | Ki | = | 34300.0 | nM | 4.46 |
| CHEMBL105257 | — | Ki | = | 37800.0 | nM | 4.42 |
| CHEMBL430870 | — | Ki | = | 39300.0 | nM | 4.41 |
| CHEMBL54331 | — | Ki | = | 48600.0 | nM | 4.31 |
| CHEMBL104265 | — | Ki | = | 65500.0 | nM | 4.18 |
| CHEMBL52918 | — | Ki | = | 69200.0 | nM | 4.16 |
| CHEMBL53780 | — | Ki | = | 79900.0 | nM | 4.10 |
| CHEMBL104381 | — | Ki | = | 97800.0 | nM | 4.01 |
| CHEMBL103044 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL105538 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL276745 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL55181 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL419357 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL54117 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL104387 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL54954 | — | Ki | > | 100000.0 | nM | - |