Assay Detail
Binding
CHEMBL885365
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Binding affinity for rat brain Nicotinic acetylcholine receptor alpha4-beta2 using [3H]S-(-)-nicotine
31
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
3-(2-Aminoethyl)pyridine analogs as alpha4beta2 nicotinic cholinergic receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 31 | 7.43 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL58231 | — | — | 1 | 9.30 |
| CHEMBL70050 | — | — | 1 | 9.22 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 8.74 |
| CHEMBL364003 | — | — | 1 | 8.74 |
| CHEMBL294757 | — | — | 1 | 8.74 |
| CHEMBL382287 | — | — | 1 | 8.68 |
| CHEMBL61772 | — | — | 3 | 8.27 |
| CHEMBL190652 | — | — | 1 | 8.00 |
| CHEMBL303530 | — | — | 1 | 7.85 |
| CHEMBL190295 | — | — | 1 | 7.82 |
| CHEMBL191253 | — | — | 1 | 7.75 |
| CHEMBL194593 | — | — | 1 | 7.72 |
| CHEMBL6200 | NORNICOTINE | 1.0 | 1 | 7.52 |
| CHEMBL189470 | — | — | 1 | 7.40 |
| CHEMBL427182 | — | — | 1 | 7.28 |
| CHEMBL196465 | — | — | 1 | 7.16 |
| CHEMBL195950 | — | — | 1 | 7.08 |
| CHEMBL196464 | — | — | 1 | 6.62 |
| CHEMBL195979 | — | — | 1 | 6.51 |
| CHEMBL195929 | — | — | 1 | 6.44 |
| CHEMBL370210 | — | — | 1 | 6.43 |
| CHEMBL372654 | — | — | 1 | 5.75 |
| CHEMBL196501 | — | — | 1 | 5.74 |
| CHEMBL370168 | — | — | 1 | 5.70 |
| CHEMBL193763 | — | — | 1 | 5.50 |
| CHEMBL195928 | — | — | 1 | - |
| CHEMBL190618 | — | — | 1 | - |
| CHEMBL196533 | — | — | 1 | - |
| CHEMBL194263 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL58231 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL70050 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL3 | NICOTINE | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL364003 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL294757 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL382287 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL61772 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL61772 | — | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL190652 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL303530 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL190295 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL191253 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL194593 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL6200 | NORNICOTINE | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL189470 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL427182 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL196465 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL195950 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL196464 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL61772 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL195979 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL195929 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL370210 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL372654 | — | Ki | = | 1780.0 | nM | 5.75 |
| CHEMBL196501 | — | Ki | = | 1840.0 | nM | 5.74 |
| CHEMBL370168 | — | Ki | = | 2015.0 | nM | 5.70 |
| CHEMBL193763 | — | Ki | = | 3150.0 | nM | 5.50 |
| CHEMBL195928 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL190618 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL196533 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL194263 | — | Ki | > | 10000.0 | nM | - |