Assay Detail
Binding
CHEMBL821653
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Binding affinity towards alpha4-beta2 measured by using the inhibition of [3H]NIC binding to rat striatal membrane
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Striatum |
| Subcellular | Membrane |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
N,N-disubstituted piperazines: synthesis and affinities at alpha4beta2(*) and alpha7(*) neuronal nicotinic acetylcholine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 5.29 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3 | NICOTINE | 4.0 | 1 | 9.00 |
| CHEMBL6200 | NORNICOTINE | 1.0 | 1 | 7.48 |
| CHEMBL510275 | METHYLLYCACONITINE | — | 1 | 5.84 |
| CHEMBL267915 | — | — | 1 | 4.50 |
| CHEMBL268830 | — | — | 1 | 4.49 |
| CHEMBL268831 | — | — | 1 | 4.41 |
| CHEMBL6277 | — | — | 1 | 4.38 |
| CHEMBL6334 | — | — | 1 | 4.34 |
| CHEMBL6346 | SCR01020 | — | 1 | 4.26 |
| CHEMBL266220 | — | — | 1 | 4.22 |
| CHEMBL6233 | — | — | 1 | - |
| CHEMBL268598 | — | — | 1 | - |
| CHEMBL414181 | — | — | 1 | - |
| CHEMBL6284 | — | — | 1 | - |
| CHEMBL6283 | — | — | 1 | - |
| CHEMBL216458 | ALPHA-BUNGAROTOXIN | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3 | NICOTINE | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL6200 | NORNICOTINE | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL510275 | METHYLLYCACONITINE | Ki | = | 1460.0 | nM | 5.84 |
| CHEMBL267915 | — | Ki | = | 31700.0 | nM | 4.50 |
| CHEMBL268830 | — | Ki | = | 32100.0 | nM | 4.49 |
| CHEMBL268831 | — | Ki | = | 38900.0 | nM | 4.41 |
| CHEMBL6277 | — | Ki | = | 42000.0 | nM | 4.38 |
| CHEMBL6334 | — | Ki | = | 46000.0 | nM | 4.34 |
| CHEMBL6346 | SCR01020 | Ki | = | 54800.0 | nM | 4.26 |
| CHEMBL266220 | — | Ki | = | 60500.0 | nM | 4.22 |
| CHEMBL6233 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL268598 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL414181 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL6284 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL6283 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL216458 | ALPHA-BUNGAROTOXIN | Ki | > | 10000.0 | nM | - |