Assay Detail
Binding
CHEMBL5545004
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Positive allosteric modulation of human alpha7 nAChR expressed in xenopus laevis oocytes assessed as increase in acetylcholine induced channel current amplitude at -90 mV holding potential measured after 24 to 72 hrs by two-electrode voltage clamp recording method
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Oocyte |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL2492) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Allosteric Activation of α7 Nicotinic Acetylcholine Receptors by Novel 2-Arylamino-thiazole-5-carboxylic Acid Amide Derivatives for the Improvement of Cognitive Deficits in Mice.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 45 | 5.35 | 5.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5591884 | — | — | 1 | 5.89 |
| CHEMBL5569159 | — | — | 1 | 5.89 |
| CHEMBL5568756 | — | — | 1 | 5.75 |
| CHEMBL5562542 | — | — | 1 | 5.70 |
| CHEMBL5565974 | — | — | 1 | 5.68 |
| CHEMBL5571266 | — | — | 1 | 5.68 |
| CHEMBL257591 | — | — | 1 | 5.60 |
| CHEMBL5563649 | — | — | 1 | 5.60 |
| CHEMBL5575576 | — | — | 1 | 5.52 |
| CHEMBL5573097 | — | — | 1 | 5.42 |
| CHEMBL5568872 | — | — | 1 | 5.40 |
| CHEMBL5591732 | — | — | 1 | 5.39 |
| CHEMBL5583588 | — | — | 1 | 5.39 |
| CHEMBL5571712 | — | — | 1 | 5.35 |
| CHEMBL5574142 | — | — | 1 | 5.32 |
| CHEMBL5573180 | — | — | 1 | 5.27 |
| CHEMBL5575611 | — | — | 1 | 5.19 |
| CHEMBL5571361 | — | — | 1 | 5.17 |
| CHEMBL5567203 | — | — | 1 | 5.16 |
| CHEMBL5572962 | — | — | 1 | 5.08 |
| CHEMBL5568670 | — | — | 1 | 5.04 |
| CHEMBL5565697 | — | — | 1 | 5.01 |
| CHEMBL5571385 | — | — | 1 | 4.99 |
| CHEMBL5573508 | — | — | 1 | 4.81 |
| CHEMBL5570115 | — | — | 1 | 4.33 |
| CHEMBL5564588 | — | — | 1 | - |
| CHEMBL5567447 | — | — | 1 | - |
| CHEMBL5573625 | — | — | 1 | - |
| CHEMBL5575903 | — | — | 1 | - |
| CHEMBL5583868 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5591884 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL5569159 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL5568756 | — | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL5562542 | — | EC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5565974 | — | EC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL5571266 | — | EC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL257591 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL5563649 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL5575576 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL5573097 | — | EC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL5568872 | — | EC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5583588 | — | EC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL5591732 | — | EC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL5571712 | — | EC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL5574142 | — | EC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL5573180 | — | EC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL5575611 | — | EC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL5571361 | — | EC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL5567203 | — | EC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL5572962 | — | EC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL5568670 | — | EC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL5565697 | — | EC50 | = | 9700.0 | nM | 5.01 |
| CHEMBL5571385 | — | EC50 | = | 10300.0 | nM | 4.99 |
| CHEMBL5573508 | — | EC50 | = | 15500.0 | nM | 4.81 |
| CHEMBL5570115 | — | EC50 | = | 47000.0 | nM | 4.33 |
| CHEMBL5575758 | — | EC50 | - | — | - | |
| CHEMBL5579710 | — | EC50 | - | — | - | |
| CHEMBL5583667 | — | EC50 | - | — | - | |
| CHEMBL5567410 | — | EC50 | - | — | - | |
| CHEMBL5571340 | — | EC50 | - | — | - | |
| CHEMBL5567612 | — | EC50 | - | — | - | |
| CHEMBL5574320 | — | EC50 | - | — | - | |
| CHEMBL5564474 | — | EC50 | - | — | - | |
| CHEMBL5569726 | — | EC50 | - | — | - | |
| CHEMBL5563940 | — | EC50 | - | — | - | |
| CHEMBL5594388 | — | EC50 | - | — | - | |
| CHEMBL5575780 | — | EC50 | - | — | - | |
| CHEMBL5574467 | — | EC50 | - | — | - | |
| CHEMBL5569628 | — | EC50 | - | — | - | |
| CHEMBL5584034 | — | EC50 | - | — | - | |
| CHEMBL5583868 | — | EC50 | - | — | - | |
| CHEMBL5575903 | — | EC50 | - | — | - | |
| CHEMBL5573625 | — | EC50 | - | — | - | |
| CHEMBL5567447 | — | EC50 | - | — | - | |
| CHEMBL5564588 | — | EC50 | - | — | - |