Assay Detail
Binding
CHEMBL1769555
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
12
Total Activities
6
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
Discovery of a potent and efficacious peptide derivative for δ/μ opioid agonist/neurokinin 1 antagonist activity with a 2',6'-dimethyl-L-tyrosine: in vitro, in vivo, and NMR-based structural studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 9.34 | 10.74 |
| Ki | 6 | 9.39 | 10.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1766208 | — | — | 2 | 10.74 |
| CHEMBL1766204 | — | — | 2 | 10.12 |
| CHEMBL1766205 | — | — | 2 | 9.68 |
| CHEMBL22870 | L-732138 | — | 2 | 9.14 |
| CHEMBL1766207 | — | — | 2 | 9.02 |
| CHEMBL1766206 | — | — | 2 | 9.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1766208 | — | IC50 | = | 0.0182 | nM | 10.74 |
| CHEMBL1766204 | — | Ki | = | 0.075 | nM | 10.12 |
| CHEMBL1766204 | — | IC50 | = | 0.166 | nM | 9.78 |
| CHEMBL1766205 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL1766205 | — | IC50 | = | 0.4677 | nM | 9.33 |
| CHEMBL22870 | L-732138 | Ki | = | 0.73 | nM | 9.14 |
| CHEMBL1766207 | — | Ki | = | 0.95 | nM | 9.02 |
| CHEMBL1766206 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL22870 | L-732138 | IC50 | = | 1.479 | nM | 8.83 |
| CHEMBL1766207 | — | IC50 | = | 1.995 | nM | 8.70 |
| CHEMBL1766206 | — | IC50 | = | 2.188 | nM | 8.66 |
| CHEMBL1766208 | — | Ki | = | 0.0079 | nM | - |