Assay Detail
Binding
CHEMBL934282
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]substance P from rat NK1 receptor expressed in CHO cells
10
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| 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 | 5 | - | - |
| Ki | 5 | 7.59 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL261390 | — | — | 2 | 8.80 |
| CHEMBL406030 | — | — | 2 | 8.21 |
| CHEMBL438389 | — | — | 2 | 7.48 |
| CHEMBL22870 | L-732138 | — | 2 | 6.89 |
| CHEMBL261608 | — | — | 2 | 6.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL261390 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL406030 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL438389 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL22870 | L-732138 | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL261608 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL261390 | — | logIC50 | = | -8.3 | — | - |
| CHEMBL22870 | L-732138 | logIC50 | = | -6.4 | — | - |
| CHEMBL406030 | — | logIC50 | = | -7.7 | — | - |
| CHEMBL438389 | — | logIC50 | = | -7.0 | — | - |
| CHEMBL261608 | — | logIC50 | = | -6.1 | — | - |