Assay Detail
Binding
CHEMBL3877544
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]epibatidine from rat alpha2beta2 nAChR by liquid scintillation counting
9
Total Activities
9
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/beta2 (CHEMBL1907592) ↗| 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 | 9 | 8.62 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3948977 | — | — | 1 | 9.52 |
| CHEMBL3898434 | — | — | 1 | 9.52 |
| CHEMBL389964 | — | — | 1 | 9.52 |
| CHEMBL3970672 | — | — | 1 | 9.10 |
| CHEMBL71085 | — | — | 1 | 8.96 |
| CHEMBL3926480 | — | — | 1 | 8.51 |
| CHEMBL3889475 | — | — | 1 | 7.74 |
| CHEMBL3899499 | — | — | 1 | 7.37 |
| CHEMBL3908556 | — | — | 1 | 7.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3948977 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3898434 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL389964 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3970672 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL71085 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL3926480 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL3889475 | — | Ki | = | 18.1 | nM | 7.74 |
| CHEMBL3899499 | — | Ki | = | 43.1 | nM | 7.37 |
| CHEMBL3908556 | — | Ki | = | 46.3 | nM | 7.33 |