Assay Detail
Binding
CHEMBL807955
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-labeled SP from the human Tachykinin receptor 1 expressed in CHO cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 9.82 | 10.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL140745 | — | — | 1 | 10.15 |
| CHEMBL522302 | VOFOPITANT | 2.0 | 1 | 10.10 |
| CHEMBL52330 | — | — | 1 | 10.05 |
| CHEMBL143587 | — | — | 1 | 10.05 |
| CHEMBL1471 | APREPITANT | 4.0 | 1 | 10.05 |
| CHEMBL140626 | — | — | 1 | 10.00 |
| CHEMBL319118 | — | — | 1 | 9.85 |
| CHEMBL358343 | — | — | 1 | 9.57 |
| CHEMBL135022 | — | — | 1 | 9.30 |
| CHEMBL142819 | — | — | 1 | 9.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL140745 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL522302 | VOFOPITANT | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL52330 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL143587 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL1471 | APREPITANT | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL140626 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL319118 | — | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL358343 | — | IC50 | = | 0.27 | nM | 9.57 |
| CHEMBL135022 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL142819 | — | IC50 | = | 0.88 | nM | 9.06 |