Assay Detail
Binding
CHEMBL823510
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Inhibition of [3H](-)-nicotine binding to recombinant rat alpha4-beta2 nAChR.
21
Total Activities
21
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
Novel and potent 6-chloro-3-pyridinyl ligands for the alpha4beta2 neuronal nicotinic acetylcholine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.64 | 9.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL72675 | — | — | 1 | 9.04 |
| CHEMBL70050 | — | — | 1 | 8.72 |
| CHEMBL71046 | DESCYANOTHIACLOPRID | — | 1 | 8.64 |
| CHEMBL308637 | — | — | 1 | 8.55 |
| CHEMBL440307 | — | — | 1 | 8.46 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 8.42 |
| CHEMBL309804 | DESNITROIMIDACLOPRID | — | 1 | 8.22 |
| CHEMBL309577 | — | — | 1 | 8.14 |
| CHEMBL431574 | — | — | 1 | 8.06 |
| CHEMBL72334 | — | — | 1 | 7.96 |
| CHEMBL70624 | — | — | 1 | 7.85 |
| CHEMBL307036 | — | — | 1 | 7.85 |
| CHEMBL72201 | — | — | 1 | 7.85 |
| CHEMBL304517 | — | — | 1 | 7.80 |
| CHEMBL73345 | — | — | 1 | 7.64 |
| CHEMBL73887 | — | — | 1 | 7.20 |
| CHEMBL306188 | — | — | 1 | 6.35 |
| CHEMBL71112 | — | — | 1 | 5.50 |
| CHEMBL72542 | — | — | 1 | 5.48 |
| CHEMBL71188 | — | — | 1 | 5.09 |
| CHEMBL306541 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL72675 | — | IC50 | = | 0.91 | nM | 9.04 |
| CHEMBL70050 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL71046 | DESCYANOTHIACLOPRID | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL308637 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL440307 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL3 | NICOTINE | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL309804 | DESNITROIMIDACLOPRID | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL309577 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL431574 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL72334 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL70624 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL307036 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL72201 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL304517 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL73345 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL73887 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL306188 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL71112 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL72542 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL71188 | — | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL306541 | — | IC50 | = | 160000.0 | nM | - |