Assay Detail
Binding
CHEMBL3610666
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-epibatidine from alpha4beta2 nAChR in rat cerebral cortex homogenates after 4 hrs by liquid scintillation counting
13
Total Activities
13
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, in vitro and in vivo pharmacology properties of 3'-(substituted pyridinyl)-deschloroepibatidine analogs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 9.63 | 10.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL513692 | — | — | 1 | 10.59 |
| CHEMBL3608514 | — | — | 1 | 10.03 |
| CHEMBL3608516 | — | — | 1 | 9.92 |
| CHEMBL1076903 | VARENICLINE | 4.0 | 1 | 9.92 |
| CHEMBL243971 | — | — | 1 | 9.89 |
| CHEMBL3608511 | — | — | 1 | 9.74 |
| CHEMBL3608510 | — | — | 1 | 9.66 |
| CHEMBL3608518 | — | — | 1 | 9.57 |
| CHEMBL3608512 | — | — | 1 | 9.54 |
| CHEMBL3608513 | — | — | 1 | 9.42 |
| CHEMBL3608515 | — | — | 1 | 9.09 |
| CHEMBL3608517 | — | — | 1 | 9.05 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 8.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL513692 | — | Ki | = | 0.026 | nM | 10.59 |
| CHEMBL3608514 | — | Ki | = | 0.094 | nM | 10.03 |
| CHEMBL3608516 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL1076903 | VARENICLINE | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL243971 | — | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL3608511 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL3608510 | — | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL3608518 | — | Ki | = | 0.27 | nM | 9.57 |
| CHEMBL3608512 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL3608513 | — | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL3608515 | — | Ki | = | 0.81 | nM | 9.09 |
| CHEMBL3608517 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL3 | NICOTINE | Ki | = | 1.5 | nM | 8.82 |