Assay Detail
Binding
CHEMBL2412792
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]Epibatidine from rat alpha4beta2 nACHR by liquid scintillation counting analysis
21
Total Activities
21
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; alpha4/beta2 (CHEMBL1907596) ↗| 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 | 21 | 8.48 | 10.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2409631 | — | — | 1 | 10.30 |
| CHEMBL2409635 | — | — | 1 | 10.00 |
| CHEMBL2409636 | — | — | 1 | 9.70 |
| CHEMBL2409634 | — | — | 1 | 9.70 |
| CHEMBL2409627 | — | — | 1 | 9.52 |
| CHEMBL2409621 | — | — | 1 | 9.40 |
| CHEMBL2409625 | — | — | 1 | 9.40 |
| CHEMBL2409622 | — | — | 1 | 9.30 |
| CHEMBL2409637 | — | — | 1 | 9.10 |
| CHEMBL2409620 | — | — | 1 | 8.68 |
| CHEMBL2409633 | — | — | 1 | 8.48 |
| CHEMBL2409619 | — | — | 1 | 8.34 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 8.31 |
| CHEMBL2409618 | — | — | 1 | 7.95 |
| CHEMBL2409630 | — | — | 1 | 7.66 |
| CHEMBL2409629 | — | — | 1 | 7.54 |
| CHEMBL2409626 | — | — | 1 | 7.41 |
| CHEMBL2409628 | — | — | 1 | 7.30 |
| CHEMBL2409623 | — | — | 1 | 7.25 |
| CHEMBL2409632 | — | — | 1 | 7.04 |
| CHEMBL2409624 | — | — | 1 | 5.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2409631 | — | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL2409635 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL2409636 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL2409634 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL2409627 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL2409621 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL2409625 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL2409622 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL2409637 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL2409620 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL2409633 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL2409619 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL3 | NICOTINE | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL2409618 | — | Ki | = | 11.3 | nM | 7.95 |
| CHEMBL2409630 | — | Ki | = | 21.7 | nM | 7.66 |
| CHEMBL2409629 | — | Ki | = | 28.5 | nM | 7.54 |
| CHEMBL2409626 | — | Ki | = | 38.8 | nM | 7.41 |
| CHEMBL2409628 | — | Ki | = | 49.5 | nM | 7.30 |
| CHEMBL2409623 | — | Ki | = | 56.1 | nM | 7.25 |
| CHEMBL2409632 | — | Ki | = | 90.9 | nM | 7.04 |
| CHEMBL2409624 | — | Ki | = | 2176.0 | nM | 5.66 |