Assay Detail
Binding
CHEMBL1021965
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | LMtk- |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of tetrasubstituted imidazolines as potent and selective neuropeptide Y Y5 receptor antagonists: reduced human ether-a-go-go related gene potassium channel binding affinity and potent antiobesity effect.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 8.45 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL521947 | — | — | 1 | 9.10 |
| CHEMBL523134 | — | — | 1 | 9.00 |
| CHEMBL490561 | — | — | 1 | 9.00 |
| CHEMBL506163 | — | — | 1 | 8.96 |
| CHEMBL491288 | — | — | 1 | 8.89 |
| CHEMBL489726 | — | — | 1 | 8.85 |
| CHEMBL490123 | — | — | 1 | 8.80 |
| CHEMBL490903 | — | — | 1 | 8.74 |
| CHEMBL491119 | — | — | 1 | 8.72 |
| CHEMBL523945 | — | — | 1 | 8.70 |
| CHEMBL522456 | — | — | 1 | 8.70 |
| CHEMBL523776 | — | — | 1 | 8.66 |
| CHEMBL491930 | — | — | 1 | 8.62 |
| CHEMBL490902 | — | — | 1 | 8.60 |
| CHEMBL491894 | — | — | 1 | 8.60 |
| CHEMBL522793 | — | — | 1 | 8.59 |
| CHEMBL523305 | — | — | 1 | 8.52 |
| CHEMBL521932 | — | — | 1 | 8.51 |
| CHEMBL491895 | — | — | 1 | 8.49 |
| CHEMBL491567 | — | — | 1 | 8.44 |
| CHEMBL489732 | — | — | 1 | 8.39 |
| CHEMBL490937 | — | — | 1 | 8.37 |
| CHEMBL489725 | — | — | 1 | 8.29 |
| CHEMBL523821 | — | — | 1 | 8.23 |
| CHEMBL490949 | — | — | 1 | 8.07 |
| CHEMBL491762 | — | — | 1 | 7.48 |
| CHEMBL490901 | — | — | 1 | 6.84 |
| CHEMBL491107 | — | — | 1 | 6.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL521947 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL523134 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL490561 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL506163 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL491288 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL489726 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL490123 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL490903 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL491119 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL523945 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL522456 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL523776 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL491930 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL490902 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL491894 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL522793 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL523305 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL521932 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL491895 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL491567 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL489732 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL490937 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL489725 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL523821 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL490949 | — | Ki | = | 8.6 | nM | 8.07 |
| CHEMBL491762 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL490901 | — | Ki | = | 145.0 | nM | 6.84 |
| CHEMBL491107 | — | Ki | = | 300.0 | nM | 6.52 |