Assay Detail
Binding
CHEMBL807968
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-labeled SP from human Tachykinin receptor 1 expressed in CHO cells
15
Total Activities
12
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
2(S)-((3,5-bis(trifluoromethyl)benzyl)-oxy)-3(S)-phenyl-4- ((3-oxo-1,2,4-triazol-5-yl)methyl)morpholine (1): a potent, orally active, morpholine-based human neurokinin-1 receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 8.25 | 10.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL52330 | — | — | 1 | 10.05 |
| CHEMBL406136 | — | — | 1 | 9.89 |
| CHEMBL16192 | CP-96345 | — | 1 | 9.40 |
| CHEMBL441225 | CP-99994 | — | 1 | 9.30 |
| CHEMBL27006 | — | — | 1 | 9.06 |
| CHEMBL48680 | — | — | 1 | 8.96 |
| CHEMBL300856 | — | — | 1 | 8.80 |
| CHEMBL51648 | — | — | 1 | 8.62 |
| CHEMBL300722 | — | — | 2 | 7.72 |
| CHEMBL300303 | — | — | 2 | 7.68 |
| CHEMBL294960 | — | — | 2 | 7.23 |
| CHEMBL51477 | — | — | 1 | 7.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL52330 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL406136 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL16192 | CP-96345 | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL441225 | CP-99994 | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL27006 | — | IC50 | = | 0.87 | nM | 9.06 |
| CHEMBL48680 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL300856 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL51648 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL300722 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL300303 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL294960 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL51477 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL294960 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL300303 | — | IC50 | = | 287.0 | nM | 6.54 |
| CHEMBL300722 | — | IC50 | = | 376.0 | nM | 6.42 |