Assay Detail
Binding
CHEMBL2400839
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Displacement of [3H]SP1-7 from substance P receptor (1 to 7 amino acids) binding site in Sprague-Dawley rat spinal cord membranes after 60 mins by liquid scintillation counting analysis
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Constrained H-Phe-Phe-NH2 analogues with high affinity to the substance P 1-7 binding site and with improved metabolic stability and cell permeability.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 7.63 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2396664 | — | — | 1 | 8.66 |
| CHEMBL2397494 | — | — | 1 | 8.48 |
| CHEMBL2397492 | — | — | 1 | 8.21 |
| CHEMBL108438 | — | — | 1 | 8.08 |
| CHEMBL2397484 | — | — | 1 | 8.03 |
| CHEMBL2397493 | — | — | 1 | 7.94 |
| CHEMBL2397490 | — | — | 1 | 7.76 |
| CHEMBL2397485 | — | — | 1 | 7.58 |
| CHEMBL2397487 | — | — | 1 | 7.47 |
| CHEMBL2397488 | — | — | 1 | 7.30 |
| CHEMBL2397491 | — | — | 1 | 7.17 |
| CHEMBL2397483 | — | — | 1 | 7.15 |
| CHEMBL2397489 | — | — | 1 | 7.03 |
| CHEMBL2397486 | — | — | 1 | 6.87 |
| CHEMBL2397482 | — | — | 1 | 6.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2396664 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL2397494 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL2397492 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL108438 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL2397484 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL2397493 | — | Ki | = | 11.5 | nM | 7.94 |
| CHEMBL2397490 | — | Ki | = | 17.5 | nM | 7.76 |
| CHEMBL2397485 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL2397487 | — | Ki | = | 33.9 | nM | 7.47 |
| CHEMBL2397488 | — | Ki | = | 50.5 | nM | 7.30 |
| CHEMBL2397491 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL2397483 | — | Ki | = | 70.4 | nM | 7.15 |
| CHEMBL2397489 | — | Ki | = | 93.1 | nM | 7.03 |
| CHEMBL2397486 | — | Ki | = | 136.0 | nM | 6.87 |
| CHEMBL2397482 | — | Ki | = | 189.0 | nM | 6.72 |