Assay Detail
Binding
CHEMBL967145
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Displacement of [3H]spiperone from NK1 receptor in human IM9 cells
25
Total Activities
17
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | IM-9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and stereoselective synthesis of the novel isochroman neurokinin-1 receptor antagonist 'CJ-17,493'.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 9.38 | 9.80 |
| Ki | 1 | 9.70 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL468830 | — | — | 3 | 9.80 |
| CHEMBL478392 | — | — | 2 | 9.70 |
| CHEMBL392368 | — | — | 1 | 9.70 |
| CHEMBL477365 | — | — | 4 | 9.68 |
| CHEMBL468350 | — | — | 1 | 9.47 |
| CHEMBL513351 | — | — | 1 | 9.40 |
| CHEMBL319118 | — | — | 1 | 9.40 |
| CHEMBL478620 | — | — | 2 | 9.40 |
| CHEMBL479049 | — | — | 2 | 9.30 |
| CHEMBL468163 | — | — | 1 | 9.15 |
| CHEMBL469176 | — | — | 1 | 9.05 |
| CHEMBL515935 | — | — | 1 | 9.05 |
| CHEMBL476948 | — | — | 1 | - |
| CHEMBL478831 | — | — | 1 | - |
| CHEMBL468162 | — | — | 1 | - |
| CHEMBL513511 | — | — | 1 | - |
| CHEMBL468856 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL468830 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL478392 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL392368 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL477365 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL468350 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL477365 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL319118 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL513351 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL478620 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL479049 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL468163 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL478620 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL469176 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL515935 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL476948 | — | IC50 | < | 0.1 | nM | - |
| CHEMBL468830 | — | IC50 | < | 0.1 | nM | - |
| CHEMBL468830 | — | IC50 | < | 0.1 | nM | - |
| CHEMBL478831 | — | IC50 | < | 0.1 | nM | - |
| CHEMBL477365 | — | IC50 | < | 0.1 | nM | - |
| CHEMBL477365 | — | IC50 | < | 0.1 | nM | - |
| CHEMBL479049 | — | IC50 | < | 0.1 | nM | - |
| CHEMBL468162 | — | IC50 | < | 0.1 | nM | - |
| CHEMBL513511 | — | IC50 | < | 0.1 | nM | - |
| CHEMBL478392 | — | IC50 | < | 0.1 | nM | - |
| CHEMBL468856 | — | IC50 | < | 0.1 | nM | - |