Assay Detail
Binding
CHEMBL750057
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Potency to displace [3H]nicotine binding to Nicotinic acetylcholine receptor alpha4-beta2 immuno-isolated from M10 cells
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Gallus gallus |
| Cell Type | M10 |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Structural features of azidopyridinyl neonicotinoid probes conferring high affinity and selectivity for mammalian alpha4beta2 and Drosophila nicotinic receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 7.20 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | — | 1 | 11.00 |
| CHEMBL72675 | — | — | 1 | 9.41 |
| CHEMBL319885 | — | — | 1 | 9.33 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 8.70 |
| CHEMBL309804 | DESNITROIMIDACLOPRID | — | 1 | 8.66 |
| CHEMBL316493 | — | — | 1 | 8.59 |
| CHEMBL317288 | — | — | 1 | 8.08 |
| CHEMBL319510 | — | — | 1 | 7.40 |
| CHEMBL100491 | — | — | 1 | 7.22 |
| CHEMBL330079 | — | — | 1 | 6.96 |
| CHEMBL95352 | THIACLOPRID OLEFIN | — | 1 | 6.92 |
| CHEMBL95904 | — | — | 1 | 6.92 |
| CHEMBL97798 | — | — | 1 | 6.77 |
| CHEMBL98451 | — | — | 1 | 6.77 |
| CHEMBL95531 | — | — | 1 | 6.52 |
| CHEMBL97343 | 5-AZIDOIMIDACLOPRID | — | 1 | 6.47 |
| CHEMBL95367 | DEHYDROIMIDACLOPRID | — | 1 | 6.33 |
| CHEMBL406819 | IMIDACLOPRID | — | 1 | 6.14 |
| CHEMBL96405 | — | — | 1 | 6.09 |
| CHEMBL97016 | — | — | 1 | 5.27 |
| CHEMBL318765 | — | — | 1 | 4.77 |
| CHEMBL327625 | — | — | 1 | 4.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.01 | nM | 11.00 |
| CHEMBL72675 | — | Ki | = | 0.39 | nM | 9.41 |
| CHEMBL319885 | — | Ki | = | 0.47 | nM | 9.33 |
| CHEMBL3 | NICOTINE | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL309804 | DESNITROIMIDACLOPRID | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL316493 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL317288 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL319510 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL100491 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL330079 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL95352 | THIACLOPRID OLEFIN | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL95904 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL97798 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL98451 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL95531 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL97343 | 5-AZIDOIMIDACLOPRID | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL95367 | DEHYDROIMIDACLOPRID | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL406819 | IMIDACLOPRID | Ki | = | 720.0 | nM | 6.14 |
| CHEMBL96405 | — | Ki | = | 820.0 | nM | 6.09 |
| CHEMBL97016 | — | Ki | = | 5400.0 | nM | 5.27 |
| CHEMBL318765 | — | Ki | = | 16900.0 | nM | 4.77 |
| CHEMBL327625 | — | Ki | = | 95800.0 | nM | 4.02 |