Assay Detail
Binding
CHEMBL2412795
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]Epibatidine from rat alpha2beta4 nACHR by liquid scintillation counting analysis
15
Total Activities
15
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; alpha2/beta4 (CHEMBL1907590) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Chemistry, pharmacology, and behavioral studies identify chiral cyclopropanes as selective α4β2-nicotinic acetylcholine receptor partial agonists exhibiting an antidepressant profile. Part II.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 6.50 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2409637 | — | — | 1 | 7.70 |
| CHEMBL2409631 | — | — | 1 | 7.29 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 7.16 |
| CHEMBL2409627 | — | — | 1 | 6.89 |
| CHEMBL2409621 | — | — | 1 | 6.69 |
| CHEMBL2409635 | — | — | 1 | 6.67 |
| CHEMBL2409634 | — | — | 1 | 6.63 |
| CHEMBL2409636 | — | — | 1 | 6.50 |
| CHEMBL2409622 | — | — | 1 | 6.34 |
| CHEMBL2409633 | — | — | 1 | 6.26 |
| CHEMBL2409625 | — | — | 1 | 6.21 |
| CHEMBL2409623 | — | — | 1 | 5.11 |
| CHEMBL2409630 | — | — | 1 | 5.00 |
| CHEMBL2409626 | — | — | 1 | - |
| CHEMBL2409619 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2409637 | — | Ki | = | 20.2 | nM | 7.70 |
| CHEMBL2409631 | — | Ki | = | 50.8 | nM | 7.29 |
| CHEMBL3 | NICOTINE | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL2409627 | — | Ki | = | 129.5 | nM | 6.89 |
| CHEMBL2409621 | — | Ki | = | 203.0 | nM | 6.69 |
| CHEMBL2409635 | — | Ki | = | 211.8 | nM | 6.67 |
| CHEMBL2409634 | — | Ki | = | 233.4 | nM | 6.63 |
| CHEMBL2409636 | — | Ki | = | 318.0 | nM | 6.50 |
| CHEMBL2409622 | — | Ki | = | 453.0 | nM | 6.34 |
| CHEMBL2409633 | — | Ki | = | 546.6 | nM | 6.26 |
| CHEMBL2409625 | — | Ki | = | 612.0 | nM | 6.21 |
| CHEMBL2409623 | — | Ki | = | 7850.0 | nM | 5.11 |
| CHEMBL2409630 | — | Ki | = | 9959.0 | nM | 5.00 |
| CHEMBL2409626 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2409619 | — | Ki | > | 10000.0 | nM | - |