Assay Detail
Binding
CHEMBL867842
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Displacement of [3H]epibatidine from rat forebrain alpha4beta2 nACHR
10
Total Activities
10
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; alpha4/beta2 (CHEMBL1907596) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 6.74 | 10.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | — | 1 | 10.22 |
| CHEMBL497939 | CYTISINICLINE | 3.0 | 1 | 8.72 |
| CHEMBL205644 | — | — | 1 | 8.28 |
| CHEMBL379303 | — | — | 1 | 7.70 |
| CHEMBL208438 | — | — | 1 | 7.42 |
| CHEMBL208066 | — | — | 1 | 5.92 |
| CHEMBL382845 | — | — | 1 | 5.51 |
| CHEMBL378809 | — | — | 1 | 4.68 |
| CHEMBL205379 | — | — | 1 | 4.64 |
| CHEMBL205330 | — | — | 1 | 4.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.06 | nM | 10.22 |
| CHEMBL497939 | CYTISINICLINE | Ki | = | 1.92 | nM | 8.72 |
| CHEMBL205644 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL379303 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL208438 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL208066 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL382845 | — | Ki | = | 3100.0 | nM | 5.51 |
| CHEMBL378809 | — | Ki | = | 21000.0 | nM | 4.68 |
| CHEMBL205379 | — | Ki | = | 23000.0 | nM | 4.64 |
| CHEMBL205330 | — | Ki | = | 48000.0 | nM | 4.32 |