Assay Detail
Binding
CHEMBL2215526
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Displacement of radioligand [3H]SP from wild type human NK1 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 | 8.84 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2203704 | — | — | 1 | 9.52 |
| CHEMBL2203708 | — | — | 1 | 9.40 |
| CHEMBL16192 | CP-96345 | — | 1 | 9.40 |
| CHEMBL2203707 | — | — | 1 | 9.15 |
| CHEMBL2203703 | — | — | 1 | 9.15 |
| CHEMBL2203706 | — | — | 1 | 8.89 |
| CHEMBL2203709 | — | — | 1 | 8.85 |
| CHEMBL2203705 | — | — | 1 | 8.85 |
| CHEMBL1471 | APREPITANT | 4.0 | 1 | 8.52 |
| CHEMBL346178 | OSANETANT | 2.0 | 1 | 6.68 |
| CHEMBL10188 | TALNETANT | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2203704 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL2203708 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL16192 | CP-96345 | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL2203707 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL2203703 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL2203706 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL2203709 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL2203705 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL1471 | APREPITANT | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL346178 | OSANETANT | Ki | = | 209.6 | nM | 6.68 |
| CHEMBL10188 | TALNETANT | Ki | > | 10000.0 | nM | - |