Assay Detail
Binding
CHEMBL908428
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]epibatidine from human recombinant alpha-3-beta-4 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; alpha3/beta4 (CHEMBL1907594) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Epibatidine isomers and analogues: structure-activity relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 8.65 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL220476 | — | — | 1 | 9.80 |
| CHEMBL6623 | EPIBATIDINE | — | 1 | 9.72 |
| CHEMBL94427 | HOMOEPIBATIDINE | — | 2 | 9.28 |
| CHEMBL363973 | — | — | 2 | 9.03 |
| CHEMBL185667 | — | — | 1 | 8.63 |
| CHEMBL221066 | — | — | 1 | 8.02 |
| CHEMBL497939 | CYTISINICLINE | 3.0 | 1 | 6.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL220476 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.191 | nM | 9.72 |
| CHEMBL94427 | HOMOEPIBATIDINE | Ki | = | 0.527 | nM | 9.28 |
| CHEMBL363973 | — | Ki | = | 0.944 | nM | 9.03 |
| CHEMBL94427 | HOMOEPIBATIDINE | Ki | = | 0.925 | nM | 9.03 |
| CHEMBL185667 | — | Ki | = | 2.35 | nM | 8.63 |
| CHEMBL363973 | — | Ki | = | 8.73 | nM | 8.06 |
| CHEMBL221066 | — | Ki | = | 9.51 | nM | 8.02 |
| CHEMBL497939 | CYTISINICLINE | Ki | = | 525.0 | nM | 6.28 |