Assay Detail
Binding
CHEMBL3877545
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
7
Total Activities
7
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
Synthesis and biological evaluation of novel hybrids of highly potent and selective α4β2-Nicotinic acetylcholine receptor (nAChR) partial agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 6.63 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL389964 | — | — | 1 | 7.82 |
| CHEMBL71085 | — | — | 1 | 7.21 |
| CHEMBL3898434 | — | — | 1 | 6.59 |
| CHEMBL3970672 | — | — | 1 | 6.48 |
| CHEMBL3948977 | — | — | 1 | 6.34 |
| CHEMBL3926480 | — | — | 1 | 5.32 |
| CHEMBL3908556 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL389964 | — | Ki | = | 15.2 | nM | 7.82 |
| CHEMBL71085 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL3898434 | — | Ki | = | 256.0 | nM | 6.59 |
| CHEMBL3970672 | — | Ki | = | 331.0 | nM | 6.48 |
| CHEMBL3948977 | — | Ki | = | 460.0 | nM | 6.34 |
| CHEMBL3926480 | — | Ki | = | 4811.0 | nM | 5.32 |
| CHEMBL3908556 | — | Ki | > | 10000.0 | nM | - |