Assay Detail
Binding
CHEMBL840059
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Inhibition of [3H]epibatidine binding to Nicotinic acetylcholine receptor alpha4-beta4
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 | 6.53 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | — | 1 | 9.80 |
| CHEMBL366991 | — | — | 1 | 8.00 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 7.40 |
| CHEMBL84149 | — | — | 1 | 6.66 |
| CHEMBL346301 | — | — | 1 | 6.28 |
| CHEMBL360881 | — | — | 1 | 6.15 |
| CHEMBL174531 | — | — | 1 | 5.92 |
| CHEMBL175428 | — | — | 1 | 5.89 |
| CHEMBL174543 | — | — | 1 | 5.72 |
| CHEMBL176171 | — | — | 1 | 5.70 |
| CHEMBL175639 | — | — | 1 | 5.62 |
| CHEMBL180525 | — | — | 1 | 5.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL366991 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL3 | NICOTINE | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL84149 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL346301 | — | Ki | = | 530.0 | nM | 6.28 |
| CHEMBL360881 | — | Ki | = | 710.0 | nM | 6.15 |
| CHEMBL174531 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL175428 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL174543 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL176171 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL175639 | — | Ki | = | 2400.0 | nM | 5.62 |
| CHEMBL180525 | — | Ki | = | 7000.0 | nM | 5.16 |