Assay Detail
Binding
CHEMBL2215060
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of radioligand [3H]osanetant at human NK3 H316W mutant expressed in HEK293 cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK₁/NK₃ antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 6.98 | 8.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL346178 | OSANETANT | 2.0 | 1 | 8.32 |
| CHEMBL10188 | TALNETANT | 2.0 | 1 | 6.91 |
| CHEMBL2203703 | — | — | 1 | 5.70 |
| CHEMBL2203704 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL346178 | OSANETANT | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL10188 | TALNETANT | Ki | = | 122.0 | nM | 6.91 |
| CHEMBL2203703 | — | Ki | = | 2010.0 | nM | 5.70 |
| CHEMBL2203704 | — | Ki | > | 10000.0 | nM | - |