Assay Detail
Binding
CHEMBL755331
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Affinity for Nicotinic acetylcholine receptor alpha4-beta2 tested by analogue-induced inhibition of [3H]NIC binding to rat striatal membranes
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Membrane |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha3/beta2 (CHEMBL1907587) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Neuronal nicotinic acetylcholine receptor binding affinities of boron-containing nicotine analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 6.48 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3 | NICOTINE | 4.0 | 1 | 9.00 |
| CHEMBL510275 | METHYLLYCACONITINE | — | 1 | 8.64 |
| CHEMBL6200 | NORNICOTINE | 1.0 | 1 | 7.33 |
| CHEMBL22285 | — | — | 1 | 6.66 |
| CHEMBL417278 | — | — | 1 | 6.40 |
| CHEMBL21553 | — | — | 1 | 5.62 |
| CHEMBL21816 | — | — | 1 | 4.98 |
| CHEMBL281410 | — | — | 1 | 4.91 |
| CHEMBL282473 | — | — | 1 | 4.82 |
| CHEMBL277416 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3 | NICOTINE | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL510275 | METHYLLYCACONITINE | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL6200 | NORNICOTINE | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL22285 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL417278 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL21553 | — | Ki | = | 2400.0 | nM | 5.62 |
| CHEMBL21816 | — | Ki | = | 10500.0 | nM | 4.98 |
| CHEMBL281410 | — | Ki | = | 12200.0 | nM | 4.91 |
| CHEMBL282473 | — | Ki | = | 15200.0 | nM | 4.82 |
| CHEMBL277416 | — | Ki | > | 100000.0 | nM | - |