Assay Detail
Binding
CHEMBL1954993
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Displacement of [125I]BH-SP from tachykinin NK1 receptor in human IM9 cells after 30 mins by scintillation counting
26
Total Activities
25
Compounds Tested
1
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
Novel 3-phenylpiperidine-4-carboxamides as highly potent and orally long-acting neurokinin-1 receptor antagonists with reduced CYP3A induction.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 9.75 | 10.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1951813 | — | — | 1 | 10.77 |
| CHEMBL1951810 | — | — | 2 | 10.70 |
| CHEMBL1951626 | — | — | 1 | 10.49 |
| CHEMBL1951633 | — | — | 1 | 10.46 |
| CHEMBL1951631 | — | — | 1 | 10.37 |
| CHEMBL1951811 | — | — | 1 | 10.34 |
| CHEMBL1951630 | — | — | 1 | 10.33 |
| CHEMBL1951632 | — | — | 1 | 10.32 |
| CHEMBL1951629 | — | — | 1 | 10.28 |
| CHEMBL1951627 | — | — | 1 | 10.19 |
| CHEMBL1951634 | — | — | 1 | 10.14 |
| CHEMBL1951621 | — | — | 1 | 10.01 |
| CHEMBL1951635 | — | — | 1 | 9.96 |
| CHEMBL1951625 | — | — | 1 | 9.85 |
| CHEMBL1951623 | — | — | 1 | 9.77 |
| CHEMBL1951624 | — | — | 1 | 9.74 |
| CHEMBL1951814 | — | — | 1 | 9.70 |
| CHEMBL1951628 | — | — | 1 | 9.68 |
| CHEMBL1951618 | — | — | 1 | 8.59 |
| CHEMBL1951616 | — | — | 1 | 8.59 |
| CHEMBL1951622 | — | — | 1 | 8.57 |
| CHEMBL1951619 | — | — | 1 | 8.49 |
| CHEMBL1951617 | — | — | 1 | 8.25 |
| CHEMBL1951620 | — | — | 1 | 7.92 |
| CHEMBL1951812 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1951813 | — | IC50 | = | 0.017 | nM | 10.77 |
| CHEMBL1951810 | — | IC50 | = | 0.02 | nM | 10.70 |
| CHEMBL1951626 | — | IC50 | = | 0.032 | nM | 10.49 |
| CHEMBL1951633 | — | IC50 | = | 0.035 | nM | 10.46 |
| CHEMBL1951631 | — | IC50 | = | 0.043 | nM | 10.37 |
| CHEMBL1951811 | — | IC50 | = | 0.046 | nM | 10.34 |
| CHEMBL1951630 | — | IC50 | = | 0.047 | nM | 10.33 |
| CHEMBL1951632 | — | IC50 | = | 0.048 | nM | 10.32 |
| CHEMBL1951810 | — | IC50 | = | 0.052 | nM | 10.28 |
| CHEMBL1951629 | — | IC50 | = | 0.052 | nM | 10.28 |
| CHEMBL1951627 | — | IC50 | = | 0.064 | nM | 10.19 |
| CHEMBL1951634 | — | IC50 | = | 0.073 | nM | 10.14 |
| CHEMBL1951621 | — | IC50 | = | 0.098 | nM | 10.01 |
| CHEMBL1951635 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL1951625 | — | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL1951623 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL1951624 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL1951814 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL1951628 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL1951618 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL1951616 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL1951622 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL1951619 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL1951617 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL1951620 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1951812 | — | IC50 | > | 100.0 | nM | - |