Assay Detail
Binding
CHEMBL841329
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards nAChR (alpha4-beta2) by the displacement of [3H](-)-cytisine in whole rat brain membranes.
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Brain membranes |
| 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 pyridine-modified analogs of 3-[2-((S)-pyrrolidinyl)methoxy]pyridine, A-84543, a potent nicotinic acetylcholine receptor agonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 31 | 8.34 | 9.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL86079 | — | — | 1 | 9.92 |
| CHEMBL84149 | — | — | 1 | 9.82 |
| CHEMBL312964 | — | — | 1 | 9.80 |
| CHEMBL83009 | — | — | 1 | 9.68 |
| CHEMBL82494 | — | — | 1 | 9.57 |
| CHEMBL85998 | — | — | 1 | 9.49 |
| CHEMBL86286 | — | — | 1 | 9.49 |
| CHEMBL83473 | — | — | 1 | 9.32 |
| CHEMBL82322 | — | — | 1 | 9.22 |
| CHEMBL312810 | — | — | 1 | 9.20 |
| CHEMBL84887 | — | — | 1 | 9.19 |
| CHEMBL83133 | — | — | 1 | 9.16 |
| CHEMBL85555 | — | — | 1 | 8.92 |
| CHEMBL86162 | — | — | 1 | 8.90 |
| CHEMBL85755 | — | — | 1 | 8.84 |
| CHEMBL86004 | — | — | 1 | 8.74 |
| CHEMBL84827 | — | — | 1 | 8.72 |
| CHEMBL86212 | — | — | 1 | 8.59 |
| CHEMBL84537 | — | — | 1 | 8.43 |
| CHEMBL315212 | — | — | 1 | 8.38 |
| CHEMBL85778 | — | — | 1 | 8.33 |
| CHEMBL82954 | — | — | 1 | 7.70 |
| CHEMBL84692 | — | — | 1 | 7.64 |
| CHEMBL85956 | — | — | 1 | 7.55 |
| CHEMBL84936 | — | — | 1 | 7.46 |
| CHEMBL412372 | — | — | 1 | 7.01 |
| CHEMBL312962 | — | — | 1 | 6.35 |
| CHEMBL314922 | — | — | 1 | 6.25 |
| CHEMBL86055 | — | — | 1 | 6.22 |
| CHEMBL310893 | — | — | 1 | 5.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL86079 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL84149 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL312964 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL83009 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL82494 | — | Ki | = | 0.27 | nM | 9.57 |
| CHEMBL85998 | — | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL86286 | — | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL83473 | — | Ki | = | 0.48 | nM | 9.32 |
| CHEMBL82322 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL312810 | — | Ki | = | 0.63 | nM | 9.20 |
| CHEMBL84887 | — | Ki | = | 0.64 | nM | 9.19 |
| CHEMBL83133 | — | Ki | = | 0.69 | nM | 9.16 |
| CHEMBL85555 | — | Ki | = | 1.19 | nM | 8.92 |
| CHEMBL86162 | — | Ki | = | 1.26 | nM | 8.90 |
| CHEMBL85755 | — | Ki | = | 1.45 | nM | 8.84 |
| CHEMBL86004 | — | Ki | = | 1.83 | nM | 8.74 |
| CHEMBL84827 | — | Ki | = | 1.91 | nM | 8.72 |
| CHEMBL86212 | — | Ki | = | 2.56 | nM | 8.59 |
| CHEMBL84537 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL315212 | — | Ki | = | 4.12 | nM | 8.38 |
| CHEMBL85778 | — | Ki | = | 4.65 | nM | 8.33 |
| CHEMBL82954 | — | Ki | = | 19.9 | nM | 7.70 |
| CHEMBL84692 | — | Ki | = | 22.9 | nM | 7.64 |
| CHEMBL85956 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL84936 | — | Ki | = | 34.8 | nM | 7.46 |
| CHEMBL412372 | — | Ki | = | 97.35 | nM | 7.01 |
| CHEMBL312962 | — | Ki | = | 451.0 | nM | 6.35 |
| CHEMBL314922 | — | Ki | = | 559.0 | nM | 6.25 |
| CHEMBL86055 | — | Ki | = | 606.0 | nM | 6.22 |
| CHEMBL310893 | — | Ki | = | 2833.0 | nM | 5.55 |
| CHEMBL314597 | — | Ki | = | 9000.0 | nM | 5.05 |