Assay Detail
Binding
CHEMBL908427
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Displacement of [3H]epibatidine from human recombinant alpha4beta2 nAChR in HEK293 cells by SPA assay
9
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Epibatidine isomers and analogues: structure-activity relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 9.47 | 10.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | — | 1 | 10.25 |
| CHEMBL220476 | — | — | 1 | 10.11 |
| CHEMBL94427 | HOMOEPIBATIDINE | — | 2 | 9.90 |
| CHEMBL363973 | — | — | 2 | 9.74 |
| CHEMBL221066 | — | — | 1 | 9.12 |
| CHEMBL185667 | — | — | 1 | 9.11 |
| CHEMBL497939 | CYTISINICLINE | 3.0 | 1 | 8.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.0558 | nM | 10.25 |
| CHEMBL220476 | — | Ki | = | 0.0785 | nM | 10.11 |
| CHEMBL94427 | HOMOEPIBATIDINE | Ki | = | 0.127 | nM | 9.90 |
| CHEMBL363973 | — | Ki | = | 0.182 | nM | 9.74 |
| CHEMBL94427 | HOMOEPIBATIDINE | Ki | = | 0.343 | nM | 9.46 |
| CHEMBL221066 | — | Ki | = | 0.763 | nM | 9.12 |
| CHEMBL185667 | — | Ki | = | 0.771 | nM | 9.11 |
| CHEMBL363973 | — | Ki | = | 1.23 | nM | 8.91 |
| CHEMBL497939 | CYTISINICLINE | Ki | = | 2.59 | nM | 8.59 |