Assay Detail
Binding
CHEMBL755330
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Affinity at alpha4-beta2 nACh receptors in rat brain (minus cerebellum) homogenates.
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebellum |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Binding of nicotine and homoazanicotine analogues at neuronal nicotinic acetylcholinergic (nACh) receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 7.29 | 10.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | — | 1 | 10.30 |
| CHEMBL58231 | — | — | 1 | 9.30 |
| CHEMBL70050 | — | — | 1 | 9.22 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 8.89 |
| CHEMBL349623 | — | — | 1 | 8.48 |
| CHEMBL349250 | — | — | 1 | 8.14 |
| CHEMBL313631 | — | — | 1 | 8.11 |
| CHEMBL161944 | — | — | 1 | 7.96 |
| CHEMBL163042 | — | — | 1 | 7.77 |
| CHEMBL292114 | — | — | 1 | 7.66 |
| CHEMBL6200 | NORNICOTINE | 1.0 | 1 | 7.52 |
| CHEMBL163244 | — | — | 1 | 7.42 |
| CHEMBL163748 | — | — | 1 | 7.34 |
| CHEMBL356996 | — | — | 1 | 6.82 |
| CHEMBL329602 | — | — | 1 | 6.69 |
| CHEMBL343169 | — | — | 1 | 6.49 |
| CHEMBL163552 | — | — | 1 | 6.44 |
| CHEMBL141612 | — | — | 1 | 6.07 |
| CHEMBL160034 | — | — | 1 | 5.67 |
| CHEMBL351320 | — | — | 1 | 5.49 |
| CHEMBL423429 | MYOSMINE | — | 1 | 5.48 |
| CHEMBL351446 | — | — | 1 | 5.27 |
| CHEMBL350748 | — | — | 1 | 5.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL58231 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL70050 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL3 | NICOTINE | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL349623 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL349250 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL313631 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL161944 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL163042 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL292114 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL6200 | NORNICOTINE | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL163244 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL163748 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL356996 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL329602 | — | Ki | = | 206.0 | nM | 6.69 |
| CHEMBL343169 | — | Ki | = | 325.0 | nM | 6.49 |
| CHEMBL163552 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL141612 | — | Ki | = | 850.0 | nM | 6.07 |
| CHEMBL160034 | — | Ki | = | 2125.0 | nM | 5.67 |
| CHEMBL351320 | — | Ki | = | 3260.0 | nM | 5.49 |
| CHEMBL423429 | MYOSMINE | Ki | = | 3300.0 | nM | 5.48 |
| CHEMBL351446 | — | Ki | = | 5420.0 | nM | 5.27 |
| CHEMBL350748 | — | Ki | = | 9440.0 | nM | 5.03 |