Assay Detail
Binding
CHEMBL750930
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In vitro inhibition of 5-(125I)A-85380 binding to nicotinic acetylcholine receptor (nAChR) of rat brain
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Synthesis and evaluation of a novel series of 2-chloro-5-((1-methyl-2-(S)-pyrrolidinyl)methoxy)-3-(2-(4-pyridinyl)vinyl)pyridine analogues as potential positron emission tomography imaging agents for nicotinic acetylcholine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 10.38 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | — | 1 | 11.00 |
| CHEMBL97505 | — | — | 1 | 10.96 |
| CHEMBL98923 | — | — | 1 | 10.82 |
| CHEMBL95512 | — | — | 1 | 10.64 |
| CHEMBL99714 | — | — | 1 | 10.55 |
| CHEMBL316539 | — | — | 1 | 10.55 |
| CHEMBL320446 | — | — | 1 | 10.14 |
| CHEMBL95584 | — | — | 1 | 10.06 |
| CHEMBL316762 | — | — | 1 | 9.58 |
| CHEMBL95576 | — | — | 1 | 9.48 |
| CHEMBL97502 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.01 | nM | 11.00 |
| CHEMBL97505 | — | Ki | = | 0.011 | nM | 10.96 |
| CHEMBL98923 | — | Ki | = | 0.015 | nM | 10.82 |
| CHEMBL95512 | — | Ki | = | 0.023 | nM | 10.64 |
| CHEMBL99714 | — | Ki | = | 0.028 | nM | 10.55 |
| CHEMBL316539 | — | Ki | = | 0.028 | nM | 10.55 |
| CHEMBL320446 | — | Ki | = | 0.072 | nM | 10.14 |
| CHEMBL95584 | — | Ki | = | 0.088 | nM | 10.06 |
| CHEMBL316762 | — | Ki | = | 0.265 | nM | 9.58 |
| CHEMBL95576 | — | Ki | = | 0.331 | nM | 9.48 |
| CHEMBL97502 | — | Ki | = | 0.009 | nM | - |