Assay Detail
Binding
CHEMBL5730201
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Functional Assay: The functional properties of the ligands were determined by 86Rb+ efflux assays in cells expressing α3β4 and α4β2 nAChR subtypes. The functional activity of each ligand was measured for its agonism, antagonism and desensitization ability. Agonist activity for each of the ligands was tested at eight different concentrations. The responses were compared to that stimulated by 100 μM (−)-nicotine, a near maximally effective concentration. The full concentration-effect curves generated potency (EC50) and efficacy (Emax) of each ligand.
18
Total Activities
6
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
2,5-disubstituted-pyridyl nicotinic ligands, and methods of use thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 6 | 6.63 | 7.62 |
| kon | 6 | - | - |
| k_off | 6 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2024096 | — | — | 3 | 7.62 |
| CHEMBL2323570 | — | — | 3 | 7.20 |
| CHEMBL2323569 | — | — | 3 | 6.80 |
| CHEMBL2323566 | — | — | 3 | 6.51 |
| CHEMBL1076903 | VARENICLINE | 4.0 | 3 | 6.02 |
| CHEMBL3 | NICOTINE | 4.0 | 3 | 5.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2024096 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL2323570 | — | EC50 | = | 63.0 | nM | 7.20 |
| CHEMBL2323569 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL2323566 | — | EC50 | = | 310.0 | nM | 6.51 |
| CHEMBL1076903 | VARENICLINE | EC50 | = | 950.0 | nM | 6.02 |
| CHEMBL3 | NICOTINE | EC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL3 | NICOTINE | kon | = | - | — | - |
| CHEMBL3 | NICOTINE | k_off | = | - | s-1 | - |
| CHEMBL1076903 | VARENICLINE | kon | = | - | — | - |
| CHEMBL1076903 | VARENICLINE | k_off | = | - | s-1 | - |
| CHEMBL2024096 | — | kon | = | - | — | - |
| CHEMBL2024096 | — | k_off | = | - | s-1 | - |
| CHEMBL2323566 | — | kon | = | - | — | - |
| CHEMBL2323566 | — | k_off | = | - | s-1 | - |
| CHEMBL2323569 | — | kon | = | - | — | - |
| CHEMBL2323569 | — | k_off | = | - | s-1 | - |
| CHEMBL2323570 | — | kon | = | - | — | - |
| CHEMBL2323570 | — | k_off | = | - | s-1 | - |