Assay Detail
Binding
CHEMBL2215065
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Displacement of radioligand [3H]osanetant at human NK3 Y247F 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 | 8.72 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL346178 | OSANETANT | 2.0 | 1 | 9.30 |
| CHEMBL2203704 | — | — | 1 | 8.74 |
| CHEMBL10188 | TALNETANT | 2.0 | 1 | 8.43 |
| CHEMBL2203703 | — | — | 1 | 8.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL346178 | OSANETANT | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL2203704 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL10188 | TALNETANT | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL2203703 | — | Ki | = | 3.9 | nM | 8.41 |