Assay Detail
Binding
CHEMBL2020488
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Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and evaluation of spirocyclic derivatives as antagonists of the neuropeptide Y5 receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 7.95 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2016732 | — | — | 1 | 9.15 |
| CHEMBL2016682 | — | — | 1 | 9.10 |
| CHEMBL2016740 | — | — | 1 | 9.05 |
| CHEMBL2016739 | — | — | 1 | 9.00 |
| CHEMBL161724 | — | — | 1 | 8.92 |
| CHEMBL595573 | MK-0557 | 3.0 | 1 | 8.80 |
| CHEMBL2016737 | — | — | 1 | 8.62 |
| CHEMBL2016742 | — | — | 1 | 8.34 |
| CHEMBL2016681 | VELNEPERIT | 2.0 | 1 | 8.30 |
| CHEMBL2016736 | — | — | 1 | 8.10 |
| CHEMBL2016735 | — | — | 1 | 8.00 |
| CHEMBL2016743 | — | — | 1 | 7.96 |
| CHEMBL2016733 | — | — | 1 | 7.66 |
| CHEMBL2016741 | — | — | 1 | 7.09 |
| CHEMBL2016738 | — | — | 1 | 6.73 |
| CHEMBL2016745 | — | — | 1 | 6.52 |
| CHEMBL2016734 | — | — | 1 | 6.07 |
| CHEMBL2016744 | — | — | 1 | 5.63 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2016732 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL2016682 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL2016740 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL2016739 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL161724 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL595573 | MK-0557 | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL2016737 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL2016742 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL2016681 | VELNEPERIT | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL2016736 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL2016735 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL2016743 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL2016733 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL2016741 | — | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL2016738 | — | Ki | = | 188.0 | nM | 6.73 |
| CHEMBL2016745 | — | Ki | = | 301.0 | nM | 6.52 |
| CHEMBL2016734 | — | Ki | = | 849.0 | nM | 6.07 |
| CHEMBL2016744 | — | Ki | = | 2330.0 | nM | 5.63 |