Assay Detail
Binding
CHEMBL905184
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]substance P from human NK1 receptor expressed in CHO cells
18
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 8.91 | 9.70 |
| IC50 | 9 | 8.37 | 9.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL229280 | — | — | 2 | 9.70 |
| CHEMBL389652 | — | — | 2 | 9.54 |
| CHEMBL439019 | — | — | 2 | 9.22 |
| CHEMBL387670 | — | — | 2 | 9.15 |
| CHEMBL389651 | — | — | 2 | 9.10 |
| CHEMBL2371977 | — | — | 2 | 9.06 |
| CHEMBL426363 | — | — | 2 | 9.00 |
| CHEMBL2371978 | — | — | 2 | 8.52 |
| CHEMBL22870 | L-732138 | — | 2 | 6.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL229280 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL389652 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL439019 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL387670 | — | Ki | = | 0.71 | nM | 9.15 |
| CHEMBL229280 | — | IC50 | = | 0.7762 | nM | 9.11 |
| CHEMBL389651 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL2371977 | — | Ki | = | 0.88 | nM | 9.06 |
| CHEMBL389652 | — | IC50 | = | 0.955 | nM | 9.02 |
| CHEMBL426363 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL439019 | — | IC50 | = | 2.042 | nM | 8.69 |
| CHEMBL389651 | — | IC50 | = | 2.692 | nM | 8.57 |
| CHEMBL387670 | — | IC50 | = | 2.884 | nM | 8.54 |
| CHEMBL2371977 | — | IC50 | = | 2.951 | nM | 8.53 |
| CHEMBL2371978 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL426363 | — | IC50 | = | 3.388 | nM | 8.47 |
| CHEMBL2371978 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL22870 | L-732138 | Ki | = | 134.0 | nM | 6.87 |
| CHEMBL22870 | L-732138 | IC50 | = | 398.11 | nM | 6.40 |