Assay Detail
Binding
CHEMBL873470
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity against human Tachykinin receptor 1 expressed in CHO cells using [3H]-substance P as the radioligand
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Dual NK(1) antagonists--serotonin reuptake inhibitors as potential antidepressants. Part 2: SAR and activity of benzyloxyphenethyl piperazine derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 8.04 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1471 | APREPITANT | 4.0 | 1 | 10.00 |
| CHEMBL108200 | — | — | 1 | 9.00 |
| CHEMBL111176 | — | — | 1 | 8.90 |
| CHEMBL419742 | — | — | 1 | 8.80 |
| CHEMBL108889 | — | — | 1 | 8.80 |
| CHEMBL107875 | — | — | 1 | 8.50 |
| CHEMBL107941 | — | — | 1 | 8.50 |
| CHEMBL108667 | — | — | 1 | 8.50 |
| CHEMBL109937 | — | — | 1 | 8.30 |
| CHEMBL321892 | — | — | 1 | 8.30 |
| CHEMBL109183 | — | — | 1 | 8.30 |
| CHEMBL108422 | — | — | 1 | 8.20 |
| CHEMBL432627 | — | — | 1 | 8.10 |
| CHEMBL320535 | — | — | 1 | 7.90 |
| CHEMBL107829 | — | — | 1 | 7.90 |
| CHEMBL108822 | — | — | 1 | 7.60 |
| CHEMBL107831 | — | — | 1 | 7.60 |
| CHEMBL110086 | — | — | 1 | 7.40 |
| CHEMBL320544 | — | — | 1 | 7.30 |
| CHEMBL109514 | — | — | 1 | 7.00 |
| CHEMBL111304 | — | — | 1 | 7.00 |
| CHEMBL111303 | — | — | 1 | 6.70 |
| CHEMBL111244 | — | — | 1 | 6.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1471 | APREPITANT | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL108200 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL111176 | — | IC50 | = | 1.259 | nM | 8.90 |
| CHEMBL419742 | — | IC50 | = | 1.585 | nM | 8.80 |
| CHEMBL108889 | — | IC50 | = | 1.585 | nM | 8.80 |
| CHEMBL107875 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL107941 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL108667 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL109937 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL321892 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL109183 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL108422 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL432627 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL320535 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL107829 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL108822 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL107831 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL110086 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL320544 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL109514 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL111304 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL111303 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL111244 | — | IC50 | = | 398.11 | nM | 6.40 |