Assay Detail
Binding
CHEMBL1948416
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]epibatidine from human nAChR alpha4beta2 receptor expressed in human HEK293T cells by scintillation counting
26
Total Activities
26
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK-293T |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Structure-based design, synthesis and structure-activity relationships of dibenzosuberyl- and benzoate-substituted tropines as ligands for acetylcholine-binding protein.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 8.10 | 8.30 |
| pKi | 8 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL122270 | LOBELINE | 2.0 | 1 | 8.30 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 7.90 |
| CHEMBL1946185 | — | — | 1 | - |
| CHEMBL1946186 | DEPTROPINE | 2.0 | 1 | - |
| CHEMBL1946187 | — | — | 1 | - |
| CHEMBL1794606 | — | — | 1 | - |
| CHEMBL1946188 | — | — | 1 | - |
| CHEMBL1946189 | — | — | 1 | - |
| CHEMBL1947047 | — | — | 1 | - |
| CHEMBL1947048 | — | — | 1 | - |
| CHEMBL1947049 | — | — | 1 | - |
| CHEMBL1947050 | — | — | 1 | - |
| CHEMBL1947051 | BENZOYL TROPINE | — | 1 | - |
| CHEMBL1947052 | — | — | 1 | - |
| CHEMBL1947053 | — | — | 1 | - |
| CHEMBL1947054 | — | — | 1 | - |
| CHEMBL1947055 | — | — | 1 | - |
| CHEMBL1947056 | — | — | 1 | - |
| CHEMBL1947057 | — | — | 1 | - |
| CHEMBL1947058 | — | — | 1 | - |
| CHEMBL1947059 | — | — | 1 | - |
| CHEMBL1947060 | — | — | 1 | - |
| CHEMBL1947061 | — | — | 1 | - |
| CHEMBL1947062 | — | — | 1 | - |
| CHEMBL1947205 | — | — | 1 | - |
| CHEMBL1947206 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL122270 | LOBELINE | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL3 | NICOTINE | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL1946185 | — | pKi | - | — | - | |
| CHEMBL1946186 | DEPTROPINE | pKi | - | — | - | |
| CHEMBL1946187 | — | Ki | > | 31622.78 | nM | - |
| CHEMBL1794606 | — | pKi | - | — | - | |
| CHEMBL1946188 | — | Ki | > | 31622.78 | nM | - |
| CHEMBL1946189 | — | Ki | > | 31622.78 | nM | - |
| CHEMBL1947047 | — | Ki | > | 31622.78 | nM | - |
| CHEMBL1947048 | — | Ki | > | 31622.78 | nM | - |
| CHEMBL1947049 | — | Ki | > | 31622.78 | nM | - |
| CHEMBL1947050 | — | pKi | - | — | - | |
| CHEMBL1947051 | BENZOYL TROPINE | Ki | > | 31622.78 | nM | - |
| CHEMBL1947052 | — | pKi | - | — | - | |
| CHEMBL1947053 | — | Ki | > | 31622.78 | nM | - |
| CHEMBL1947054 | — | Ki | > | 31622.78 | nM | - |
| CHEMBL1947055 | — | Ki | > | 31622.78 | nM | - |
| CHEMBL1947056 | — | Ki | > | 31622.78 | nM | - |
| CHEMBL1947057 | — | pKi | - | — | - | |
| CHEMBL1947058 | — | pKi | - | — | - | |
| CHEMBL1947059 | — | Ki | > | 31622.78 | nM | - |
| CHEMBL1947060 | — | pKi | - | — | - | |
| CHEMBL1947061 | — | Ki | > | 31622.78 | nM | - |
| CHEMBL1947062 | — | Ki | > | 31622.78 | nM | - |
| CHEMBL1947205 | — | Ki | > | 31622.78 | nM | - |
| CHEMBL1947206 | — | Ki | > | 31622.78 | nM | - |