Assay Detail
Binding
CHEMBL3877549
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Displacement of [3H]epibatidine from rat forebrain alpha4beta2* 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 | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
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 | 7.95 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL389964 | — | — | 1 | 9.10 |
| CHEMBL3948977 | — | — | 1 | 8.57 |
| CHEMBL3898434 | — | — | 1 | 8.57 |
| CHEMBL71085 | — | — | 1 | 8.48 |
| CHEMBL3970672 | — | — | 1 | 8.46 |
| CHEMBL3926480 | — | — | 1 | 7.79 |
| CHEMBL3889475 | — | — | 1 | 7.47 |
| CHEMBL3899499 | — | — | 1 | 6.57 |
| CHEMBL3908556 | — | — | 1 | 6.56 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL389964 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL3948977 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL3898434 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL71085 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL3970672 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL3926480 | — | Ki | = | 16.1 | nM | 7.79 |
| CHEMBL3889475 | — | Ki | = | 33.8 | nM | 7.47 |
| CHEMBL3899499 | — | Ki | = | 269.0 | nM | 6.57 |
| CHEMBL3908556 | — | Ki | = | 274.0 | nM | 6.56 |