Assay Detail
Binding
CHEMBL821650
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H](-)-nicotine binding to recombinant rat alpha4-beta2 nAChR was determined; experiment 2
5
Total Activities
5
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
Novel and potent 6-chloro-3-pyridinyl ligands for the alpha4beta2 neuronal nicotinic acetylcholine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.60 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL71583 | — | — | 1 | 7.70 |
| CHEMBL309136 | — | — | 1 | 5.78 |
| CHEMBL539622 | — | — | 1 | 5.62 |
| CHEMBL431760 | — | — | 1 | 4.87 |
| CHEMBL69446 | — | — | 1 | 4.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL71583 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL309136 | — | IC50 | = | 1650.0 | nM | 5.78 |
| CHEMBL539622 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL431760 | — | IC50 | = | 13500.0 | nM | 4.87 |
| CHEMBL69446 | — | IC50 | = | 95300.0 | nM | 4.02 |