Assay Detail
Binding
CHEMBL840081
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]epibatidine binding to Nicotinic acetylcholine receptor alpha2-beta2
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Novel pyridyl ring C5 substituted analogues of epibatidine and 3-(1-methyl-2(S)-pyrrolidinylmethoxy)pyridine (A-84543) as highly selective agents for neuronal nicotinic acetylcholine receptors containing beta2 subunits.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 8.65 | 10.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | — | 1 | 10.60 |
| CHEMBL366991 | — | — | 1 | 9.72 |
| CHEMBL180525 | — | — | 1 | 8.72 |
| CHEMBL174531 | — | — | 1 | 8.72 |
| CHEMBL360881 | — | — | 1 | 8.60 |
| CHEMBL84149 | — | — | 1 | 8.60 |
| CHEMBL175428 | — | — | 1 | 8.47 |
| CHEMBL176171 | — | — | 1 | 8.38 |
| CHEMBL346301 | — | — | 1 | 8.36 |
| CHEMBL174543 | — | — | 1 | 8.03 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 7.92 |
| CHEMBL175639 | — | — | 1 | 7.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.025 | nM | 10.60 |
| CHEMBL366991 | — | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL180525 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL174531 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL360881 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL84149 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL175428 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL176171 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL346301 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL174543 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL3 | NICOTINE | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL175639 | — | Ki | = | 22.0 | nM | 7.66 |