Assay Detail
Binding
CHEMBL934281
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
14
Total Activities
7
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 | Autocuration |
Publication
A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| logIC50 | 7 | - | - |
| Ki | 7 | 8.74 | 10.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL261390 | — | — | 2 | 10.34 |
| CHEMBL438389 | — | — | 2 | 9.21 |
| CHEMBL22870 | L-732138 | — | 2 | 9.14 |
| CHEMBL406030 | — | — | 2 | 8.85 |
| CHEMBL272665 | — | — | 2 | 8.80 |
| CHEMBL271619 | — | — | 2 | 7.85 |
| CHEMBL261608 | — | — | 2 | 7.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL261390 | — | Ki | = | 0.046 | nM | 10.34 |
| CHEMBL438389 | — | Ki | = | 0.61 | nM | 9.21 |
| CHEMBL22870 | L-732138 | Ki | = | 0.73 | nM | 9.14 |
| CHEMBL406030 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL272665 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL271619 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL261608 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL261390 | — | logIC50 | = | -10.0 | — | - |
| CHEMBL22870 | L-732138 | logIC50 | = | -8.8 | — | - |
| CHEMBL406030 | — | logIC50 | = | -8.5 | — | - |
| CHEMBL438389 | — | logIC50 | = | -8.9 | — | - |
| CHEMBL272665 | — | logIC50 | = | -8.5 | — | - |
| CHEMBL271619 | — | logIC50 | = | -7.5 | — | - |
| CHEMBL261608 | — | logIC50 | = | -6.7 | — | - |