Assay Detail
Binding
CHEMBL840083
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Inhibition of [3H]epibatidine binding to Nicotinic acetylcholine receptor alpha3-beta2
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha3/beta2 (CHEMBL2109234) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
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 | 8.19 | 10.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | — | 1 | 10.46 |
| CHEMBL366991 | — | — | 1 | 9.64 |
| CHEMBL175428 | — | — | 1 | 8.15 |
| CHEMBL84149 | — | — | 1 | 8.11 |
| CHEMBL360881 | — | — | 1 | 8.09 |
| CHEMBL346301 | — | — | 1 | 8.07 |
| CHEMBL174531 | — | — | 1 | 7.89 |
| CHEMBL176171 | — | — | 1 | 7.85 |
| CHEMBL174543 | — | — | 1 | 7.68 |
| CHEMBL180525 | — | — | 1 | 7.64 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 7.33 |
| CHEMBL175639 | — | — | 1 | 7.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.035 | nM | 10.46 |
| CHEMBL366991 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL175428 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL84149 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL360881 | — | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL346301 | — | Ki | = | 8.6 | nM | 8.07 |
| CHEMBL174531 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL176171 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL174543 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL180525 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL3 | NICOTINE | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL175639 | — | Ki | = | 48.0 | nM | 7.32 |