Assay Detail
Binding
CHEMBL750484
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Nicotinic acetylcholine receptor binding activity was determined by ability to displace [3H]- (-) cytisine binding from whole rat brain synaptic membranes.
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Structure-activity studies on a novel series of cholinergic channel activators based on a heteroaryl ether framework.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 7.21 | 9.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL328705 | — | — | 1 | 9.89 |
| CHEMBL84149 | — | — | 1 | 9.82 |
| CHEMBL329682 | — | — | 1 | 8.62 |
| CHEMBL329830 | — | — | 1 | 8.57 |
| CHEMBL329004 | — | — | 1 | 8.35 |
| CHEMBL93485 | — | — | 1 | 8.18 |
| CHEMBL329138 | — | — | 1 | 7.93 |
| CHEMBL92037 | — | — | 1 | 7.81 |
| CHEMBL328575 | — | — | 1 | 7.79 |
| CHEMBL94136 | — | — | 1 | 7.55 |
| CHEMBL93026 | — | — | 1 | 7.54 |
| CHEMBL92737 | — | — | 1 | 7.38 |
| CHEMBL328367 | — | — | 1 | 7.33 |
| CHEMBL92702 | — | — | 1 | 7.20 |
| CHEMBL329768 | — | — | 1 | 7.07 |
| CHEMBL92975 | — | — | 1 | 6.80 |
| CHEMBL328429 | — | — | 1 | 6.62 |
| CHEMBL90779 | — | — | 1 | 6.45 |
| CHEMBL93459 | — | — | 1 | 6.39 |
| CHEMBL96797 | — | — | 1 | 6.30 |
| CHEMBL93922 | — | — | 1 | 6.25 |
| CHEMBL93200 | — | — | 1 | 5.91 |
| CHEMBL92085 | — | — | 1 | 5.89 |
| CHEMBL94035 | — | — | 1 | 5.85 |
| CHEMBL93146 | — | — | 1 | 5.10 |
| CHEMBL329338 | — | — | 1 | 4.92 |
| CHEMBL89943 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL328705 | — | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL84149 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL329682 | — | Ki | = | 2.39 | nM | 8.62 |
| CHEMBL329830 | — | Ki | = | 2.67 | nM | 8.57 |
| CHEMBL329004 | — | Ki | = | 4.44 | nM | 8.35 |
| CHEMBL93485 | — | Ki | = | 6.54 | nM | 8.18 |
| CHEMBL329138 | — | Ki | = | 11.7 | nM | 7.93 |
| CHEMBL92037 | — | Ki | = | 15.37 | nM | 7.81 |
| CHEMBL328575 | — | Ki | = | 16.3 | nM | 7.79 |
| CHEMBL94136 | — | Ki | = | 28.17 | nM | 7.55 |
| CHEMBL93026 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL92737 | — | Ki | = | 42.07 | nM | 7.38 |
| CHEMBL328367 | — | Ki | = | 46.4 | nM | 7.33 |
| CHEMBL92702 | — | Ki | = | 63.82 | nM | 7.20 |
| CHEMBL329768 | — | Ki | = | 85.35 | nM | 7.07 |
| CHEMBL92975 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL328429 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL90779 | — | Ki | = | 359.0 | nM | 6.45 |
| CHEMBL93459 | — | Ki | = | 406.0 | nM | 6.39 |
| CHEMBL96797 | — | Ki | = | 495.0 | nM | 6.30 |
| CHEMBL93922 | — | Ki | = | 560.0 | nM | 6.25 |
| CHEMBL93200 | — | Ki | = | 1223.0 | nM | 5.91 |
| CHEMBL92085 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL94035 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL93146 | — | Ki | = | 7914.0 | nM | 5.10 |
| CHEMBL329338 | — | Ki | = | 11900.0 | nM | 4.92 |
| CHEMBL89943 | — | Ki | > | 10000.0 | nM | - |