Assay Detail
Binding
CHEMBL3131692
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-epibatidine from alpha4beta2* nAChR in Sprague-Dawley rat cerebral cortex after 4 hrs by liquid scintillation counting analysis
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2'-fluoro-3'-(substituted pyridinyl)-7-deschloroepibatidine analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 9.85 | 10.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | — | 1 | 10.59 |
| CHEMBL3128035 | — | — | 1 | 10.40 |
| CHEMBL3128037 | — | — | 1 | 10.31 |
| CHEMBL3128038 | — | — | 1 | 10.20 |
| CHEMBL3128032 | — | — | 1 | 10.17 |
| CHEMBL3128031 | — | — | 1 | 9.92 |
| CHEMBL1076903 | VARENICLINE | 4.0 | 1 | 9.92 |
| CHEMBL3128028 | — | — | 1 | 9.89 |
| CHEMBL3128034 | — | — | 1 | 9.89 |
| CHEMBL3128039 | — | — | 1 | 9.60 |
| CHEMBL3128036 | — | — | 1 | 9.46 |
| CHEMBL3128033 | — | — | 1 | 8.93 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 8.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.026 | nM | 10.59 |
| CHEMBL3128035 | — | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL3128037 | — | Ki | = | 0.049 | nM | 10.31 |
| CHEMBL3128038 | — | Ki | = | 0.063 | nM | 10.20 |
| CHEMBL3128032 | — | Ki | = | 0.067 | nM | 10.17 |
| CHEMBL3128031 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL1076903 | VARENICLINE | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL3128028 | — | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL3128034 | — | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL3128039 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL3128036 | — | Ki | = | 0.35 | nM | 9.46 |
| CHEMBL3128033 | — | Ki | = | 1.18 | nM | 8.93 |
| CHEMBL3 | NICOTINE | Ki | = | 1.5 | nM | 8.82 |