Assay Detail
Binding
CHEMBL753467
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro ability to displace [3H](-)-cytisine binding to whole rat brain membranes at Nicotinic acetylcholine receptor alpha4-beta2
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Synthesis and structure-activity relationships of 5-substituted pyridine analogues of 3.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 29 | 9.59 | 10.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL156452 | — | — | 1 | 10.26 |
| CHEMBL160766 | — | — | 1 | 10.19 |
| CHEMBL157188 | — | — | 1 | 10.09 |
| CHEMBL156048 | — | — | 1 | 9.96 |
| CHEMBL348275 | — | — | 1 | 9.96 |
| CHEMBL446684 | — | — | 1 | 9.92 |
| CHEMBL156204 | — | — | 1 | 9.89 |
| CHEMBL159136 | — | — | 1 | 9.82 |
| CHEMBL84149 | — | — | 1 | 9.82 |
| CHEMBL155909 | — | — | 1 | 9.82 |
| CHEMBL346301 | — | — | 1 | 9.80 |
| CHEMBL157250 | — | — | 1 | 9.80 |
| CHEMBL158331 | — | — | 1 | 9.72 |
| CHEMBL156502 | — | — | 1 | 9.66 |
| CHEMBL158162 | — | — | 1 | 9.62 |
| CHEMBL346981 | — | — | 1 | 9.57 |
| CHEMBL349544 | — | — | 1 | 9.51 |
| CHEMBL156049 | — | — | 1 | 9.51 |
| CHEMBL160447 | — | — | 1 | 9.49 |
| CHEMBL347133 | — | — | 1 | 9.49 |
| CHEMBL160624 | — | — | 1 | 9.48 |
| CHEMBL160321 | — | — | 1 | 9.43 |
| CHEMBL157135 | — | — | 1 | 9.41 |
| CHEMBL158529 | — | — | 1 | 9.37 |
| CHEMBL158834 | — | — | 1 | 9.33 |
| CHEMBL158944 | — | — | 1 | 9.25 |
| CHEMBL345206 | — | — | 1 | 8.96 |
| CHEMBL352018 | — | — | 1 | 8.62 |
| CHEMBL160950 | — | — | 1 | 8.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL156452 | — | Ki | = | 0.055 | nM | 10.26 |
| CHEMBL160766 | — | Ki | = | 0.064 | nM | 10.19 |
| CHEMBL157188 | — | Ki | = | 0.082 | nM | 10.09 |
| CHEMBL156048 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL348275 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL446684 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL156204 | — | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL159136 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL84149 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL155909 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL346301 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL157250 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL158331 | — | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL156502 | — | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL158162 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL346981 | — | Ki | = | 0.27 | nM | 9.57 |
| CHEMBL349544 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL156049 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL160447 | — | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL347133 | — | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL160624 | — | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL160321 | — | Ki | = | 0.37 | nM | 9.43 |
| CHEMBL157135 | — | Ki | = | 0.39 | nM | 9.41 |
| CHEMBL158529 | — | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL158834 | — | Ki | = | 0.465 | nM | 9.33 |
| CHEMBL158944 | — | Ki | = | 0.56 | nM | 9.25 |
| CHEMBL345206 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL352018 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL160950 | — | Ki | = | 4.2 | nM | 8.38 |