Assay Detail
Functional
CHEMBL745035
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Neurokinin (NK1) receptor antagonistic activity was evaluated.
15
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Synthesis and NK1 receptor antagonistic activity of (+/-)-1-acyl-3-(3,4- dichlorophenyl)-3-[2-(spiro-substituted piperidin-1'-yl)ethyl]piperidines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 8.01 | 10.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL38763 | — | — | 1 | 10.72 |
| CHEMBL288600 | — | — | 1 | 9.51 |
| CHEMBL288123 | — | — | 2 | 8.72 |
| CHEMBL289727 | — | — | 1 | 8.70 |
| CHEMBL39595 | — | — | 1 | 8.32 |
| CHEMBL38030 | — | — | 1 | 8.20 |
| CHEMBL1201933 | — | — | 1 | 7.80 |
| CHEMBL288840 | — | — | 1 | 7.80 |
| CHEMBL38624 | — | — | 1 | 7.75 |
| CHEMBL38652 | — | — | 1 | 7.51 |
| CHEMBL262540 | — | — | 1 | 7.27 |
| CHEMBL39232 | — | — | 1 | 7.24 |
| CHEMBL1794935 | — | — | 1 | 6.98 |
| CHEMBL39049 | — | — | 1 | 6.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL38763 | — | IC50 | = | 0.019 | nM | 10.72 |
| CHEMBL288600 | — | IC50 | = | 0.31 | nM | 9.51 |
| CHEMBL288123 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL289727 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL39595 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL38030 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL1201933 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL288840 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL38624 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL38652 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL288123 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL262540 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL39232 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL1794935 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL39049 | — | IC50 | = | 710.0 | nM | 6.15 |