Assay Detail
Binding
CHEMBL840076
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Inhibition of alpha beta[3H]epibatidine binding to Nicotinic acetylcholine receptor alpha4-beta2 of rat cerebral cortex
17
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2'-fluoro-3'-(substituted phenyl)deschloroepibatidine analogues. Novel nicotinic antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 10.04 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL298826 | (-)-EPIBATIDINE | — | 1 | 11.00 |
| CHEMBL298517 | (+)-EPIBATIDINE | — | 1 | 10.70 |
| CHEMBL56682 | — | — | 1 | 10.70 |
| CHEMBL185060 | — | — | 1 | 10.70 |
| CHEMBL185612 | — | — | 1 | 10.40 |
| CHEMBL185591 | — | — | 1 | 10.30 |
| CHEMBL181428 | — | — | 1 | 10.22 |
| CHEMBL185061 | — | — | 1 | 10.15 |
| CHEMBL184809 | — | — | 1 | 10.05 |
| CHEMBL184320 | — | — | 1 | 9.92 |
| CHEMBL184633 | — | — | 1 | 9.80 |
| CHEMBL58935 | — | — | 3 | 9.62 |
| CHEMBL362415 | — | — | 1 | 9.06 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 8.82 |
| CHEMBL361465 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL298826 | (-)-EPIBATIDINE | Ki | = | 0.01 | nM | 11.00 |
| CHEMBL298517 | (+)-EPIBATIDINE | Ki | = | 0.02 | nM | 10.70 |
| CHEMBL185060 | — | Ki | = | 0.02 | nM | 10.70 |
| CHEMBL56682 | — | Ki | = | 0.02 | nM | 10.70 |
| CHEMBL185612 | — | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL185591 | — | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL181428 | — | Ki | = | 0.06 | nM | 10.22 |
| CHEMBL185061 | — | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL184809 | — | Ki | = | 0.09 | nM | 10.05 |
| CHEMBL184320 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL184633 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL58935 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL58935 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL58935 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL362415 | — | Ki | = | 0.87 | nM | 9.06 |
| CHEMBL3 | NICOTINE | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL361465 | — | Ki | = | 0.0009 | nM | - |