Assay Detail
Functional
CHEMBL1785099
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human NK1 receptor expressed in CHO-K1 cells assessed as inhibition of substance P-induced calcium-dependent aequorine luminescence
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design of novel neurokinin 1 receptor antagonists based on conformationally constrained aromatic amino acids and discovery of a potent chimeric opioid agonist-neurokinin 1 receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 4 | 7.48 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1782139 | — | — | 1 | 8.40 |
| CHEMBL1782141 | — | — | 1 | 7.80 |
| CHEMBL1782137 | — | — | 1 | 7.50 |
| CHEMBL1782138 | — | — | 1 | 6.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1782139 | — | Kd | = | 3.981 | nM | 8.40 |
| CHEMBL1782141 | — | Kd | = | 15.85 | nM | 7.80 |
| CHEMBL1782137 | — | Kd | = | 31.62 | nM | 7.50 |
| CHEMBL1782138 | — | Kd | = | 630.96 | nM | 6.20 |