Assay Detail
Binding
CHEMBL838852
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Inhibition of [3H]epibatidine binding to rat Nicotinic acetylcholine receptor alpha4-beta2
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
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 | 11 | 8.89 | 10.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | — | 1 | 10.21 |
| CHEMBL346301 | — | — | 1 | 9.29 |
| CHEMBL174531 | — | — | 1 | 9.07 |
| CHEMBL175428 | — | — | 1 | 9.03 |
| CHEMBL176171 | — | — | 1 | 9.02 |
| CHEMBL174543 | — | — | 1 | 8.85 |
| CHEMBL360881 | — | — | 1 | 8.80 |
| CHEMBL84149 | — | — | 1 | 8.72 |
| CHEMBL180525 | — | — | 1 | 8.54 |
| CHEMBL175639 | — | — | 1 | 8.21 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 8.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.061 | nM | 10.21 |
| CHEMBL346301 | — | Ki | = | 0.51 | nM | 9.29 |
| CHEMBL174531 | — | Ki | = | 0.85 | nM | 9.07 |
| CHEMBL175428 | — | Ki | = | 0.93 | nM | 9.03 |
| CHEMBL176171 | — | Ki | = | 0.95 | nM | 9.02 |
| CHEMBL174543 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL360881 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL84149 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL180525 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL175639 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL3 | NICOTINE | Ki | = | 10.0 | nM | 8.00 |