Assay Detail
Binding
CHEMBL1028495
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Displacement of [3H]cytisine from alpha4beta2 nicotinic acetylcholine receptor in rat brain cortex membrane homogenates
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Synthesis, binding, and modeling studies of new cytisine derivatives, as ligands for neuronal nicotinic acetylcholine receptor subtypes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 7.18 | 9.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL497939 | CYTISINICLINE | 3.0 | 1 | 9.47 |
| CHEMBL190851 | — | — | 1 | 8.49 |
| CHEMBL502030 | — | — | 1 | 8.14 |
| CHEMBL502295 | — | — | 1 | 7.89 |
| CHEMBL500426 | — | — | 1 | 7.38 |
| CHEMBL519673 | — | — | 1 | 7.36 |
| CHEMBL497946 | — | — | 1 | 7.11 |
| CHEMBL526554 | — | — | 1 | 6.76 |
| CHEMBL524813 | — | — | 1 | 6.74 |
| CHEMBL526340 | — | — | 1 | 6.21 |
| CHEMBL483803 | — | — | 1 | 6.17 |
| CHEMBL508190 | — | — | 1 | 6.00 |
| CHEMBL499636 | — | — | 1 | 5.65 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL497939 | CYTISINICLINE | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL190851 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL502030 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL502295 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL500426 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL519673 | — | Ki | = | 43.5 | nM | 7.36 |
| CHEMBL497946 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL526554 | — | Ki | = | 172.0 | nM | 6.76 |
| CHEMBL524813 | — | Ki | = | 183.0 | nM | 6.74 |
| CHEMBL526340 | — | Ki | = | 611.0 | nM | 6.21 |
| CHEMBL483803 | — | Ki | = | 670.0 | nM | 6.17 |
| CHEMBL508190 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL499636 | — | Ki | = | 2222.0 | nM | 5.65 |