Assay Detail
Binding
CHEMBL2215524
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Displacement of [3H]osanetant from wild type human NK3 receptor expressed in HEK293 cells
11
Total Activities
11
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 | 11 | 8.41 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL346178 | OSANETANT | 2.0 | 1 | 9.22 |
| CHEMBL2203707 | — | — | 1 | 8.92 |
| CHEMBL2203705 | — | — | 1 | 8.82 |
| CHEMBL2203704 | — | — | 1 | 8.77 |
| CHEMBL2203708 | — | — | 1 | 8.62 |
| CHEMBL2203703 | — | — | 1 | 8.54 |
| CHEMBL2203709 | — | — | 1 | 8.46 |
| CHEMBL10188 | TALNETANT | 2.0 | 1 | 8.44 |
| CHEMBL2203706 | — | — | 1 | 7.92 |
| CHEMBL1471 | APREPITANT | 4.0 | 1 | 6.34 |
| CHEMBL16192 | CP-96345 | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL346178 | OSANETANT | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL2203707 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL2203705 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL2203704 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL2203708 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL2203703 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL2203709 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL10188 | TALNETANT | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL2203706 | — | Ki | = | 11.9 | nM | 7.92 |
| CHEMBL1471 | APREPITANT | Ki | = | 454.1 | nM | 6.34 |
| CHEMBL16192 | CP-96345 | Ki | > | 10000.0 | nM | - |