Assay Detail
Binding
CHEMBL4604684
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]epibatidine from human alpha3beta4 nAChR expressed in IMR32 cell membrane by microbeta scintillation counting method
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | IMR-32 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha3/beta4 (CHEMBL1907594) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Discovery and Development of 3-(6-Chloropyridine-3-yloxymethyl)-2-azabicyclo[3.1.0]hexane Hydrochloride (SUVN-911): A Novel, Potent, Selective, and Orally Active Neuronal Nicotinic Acetylcholine α4β2 Receptor Antagonist for the Treatment of Depression.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 6.64 | 8.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4647198 | — | — | 1 | 8.09 |
| CHEMBL4636163 | — | — | 1 | 7.58 |
| CHEMBL1076903 | VARENICLINE | 4.0 | 1 | 7.40 |
| CHEMBL4641432 | — | — | 1 | 7.17 |
| CHEMBL4649507 | — | — | 1 | 6.28 |
| CHEMBL4643543 | — | — | 1 | 6.25 |
| CHEMBL4645367 | — | — | 1 | 5.99 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 5.76 |
| CHEMBL4641810 | — | — | 1 | 5.22 |
| CHEMBL504652 | TC-2216 | 1.0 | 1 | - |
| CHEMBL127071 | POZANICLINE | 2.0 | 1 | - |
| CHEMBL4643942 | — | — | 1 | - |
| CHEMBL4645127 | — | — | 1 | - |
| CHEMBL4642118 | — | — | 1 | - |
| CHEMBL4642865 | — | — | 1 | - |
| CHEMBL4642287 | — | — | 1 | - |
| CHEMBL4638732 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4647198 | — | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL4636163 | — | Ki | = | 26.4 | nM | 7.58 |
| CHEMBL1076903 | VARENICLINE | Ki | = | 39.6 | nM | 7.40 |
| CHEMBL4641432 | — | Ki | = | 68.4 | nM | 7.17 |
| CHEMBL4649507 | — | Ki | = | 525.2 | nM | 6.28 |
| CHEMBL4643543 | — | Ki | = | 558.3 | nM | 6.25 |
| CHEMBL4645367 | — | Ki | = | 1019.0 | nM | 5.99 |
| CHEMBL3 | NICOTINE | Ki | = | 1744.44 | nM | 5.76 |
| CHEMBL4641810 | — | Ki | = | 6014.0 | nM | 5.22 |
| CHEMBL504652 | TC-2216 | Ki | > | 10000.0 | nM | - |
| CHEMBL127071 | POZANICLINE | Ki | > | 10000.0 | nM | - |
| CHEMBL4643942 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4645127 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4642118 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4642865 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4642287 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4638732 | — | Ki | > | 10000.0 | nM | - |