Assay Detail
Functional
CHEMBL5055739
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at mouse Neuropeptide S receptor expressed in HEK293 cells assessed as rightward shift in NPS concentration response curve of intracellular calcium mobilization without affecting maximal effect at 100 nM treated for 24 mins prior to NPS addition measured immediately by Fluo-4AM dye based FLIPR assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-Activity Relationship Studies on Oxazolo[3,4-<i>a</i>]pyrazine Derivatives Leading to the Discovery of a Novel Neuropeptide S Receptor Antagonist with Potent <i>In Vivo</i> Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 3 | 7.50 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL469695 | — | — | 1 | 7.82 |
| CHEMBL5077621 | — | — | 1 | 7.59 |
| CHEMBL5091859 | — | — | 1 | 7.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL469695 | — | Kd | = | 15.14 | nM | 7.82 |
| CHEMBL5077621 | — | Kd | = | 25.7 | nM | 7.59 |
| CHEMBL5091859 | — | Kd | = | 79.43 | nM | 7.10 |