Assay Detail
Binding
CHEMBL750613
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]nicotine binding to Nicotinic acetylcholine receptor alpha4-beta2 from rat membranes
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
Epibatidine structure-activity relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 8.56 | 9.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL300996 | — | — | 1 | 9.96 |
| CHEMBL56806 | — | — | 1 | 9.89 |
| CHEMBL298826 | (-)-EPIBATIDINE | — | 1 | 9.59 |
| CHEMBL55003 | — | — | 1 | 9.59 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 9.00 |
| CHEMBL6623 | EPIBATIDINE | — | 1 | 8.12 |
| CHEMBL300837 | — | — | 1 | 8.07 |
| CHEMBL57337 | — | — | 1 | 7.97 |
| CHEMBL56677 | — | — | 1 | 7.58 |
| CHEMBL9732 | R-NICOTINE | — | 1 | 7.42 |
| CHEMBL54585 | — | — | 1 | 6.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL300996 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL56806 | — | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL298826 | (-)-EPIBATIDINE | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL55003 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL3 | NICOTINE | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL6623 | EPIBATIDINE | Ki | = | 7.6 | nM | 8.12 |
| CHEMBL300837 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL57337 | — | Ki | = | 10.8 | nM | 7.97 |
| CHEMBL56677 | — | Ki | = | 26.4 | nM | 7.58 |
| CHEMBL9732 | R-NICOTINE | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL54585 | — | Ki | = | 107.0 | nM | 6.97 |