Assay Detail
Binding
CHEMBL751900
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Inhibition of [125I]-Substance P binding to human NK1 receptors in CHO cells
20
Total Activities
20
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
1,4-Diacylpiperazine-2-(S)-[(N-aminoalkyl)carboxamides] as novel, potent substance P receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.99 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL16192 | CP-96345 | — | 1 | 9.30 |
| CHEMBL93401 | — | — | 1 | 8.05 |
| CHEMBL91438 | — | — | 1 | 8.05 |
| CHEMBL92621 | — | — | 1 | 7.96 |
| CHEMBL431459 | — | — | 1 | 7.77 |
| CHEMBL90416 | — | — | 1 | 7.39 |
| CHEMBL90547 | — | — | 1 | 7.26 |
| CHEMBL314084 | — | — | 1 | 7.24 |
| CHEMBL63109 | — | — | 1 | 6.89 |
| CHEMBL329416 | — | — | 1 | 6.85 |
| CHEMBL93038 | — | — | 1 | 6.70 |
| CHEMBL441458 | — | — | 1 | 6.66 |
| CHEMBL93251 | — | — | 1 | 6.57 |
| CHEMBL299887 | — | — | 1 | 6.55 |
| CHEMBL329168 | — | — | 1 | 6.54 |
| CHEMBL59854 | — | — | 1 | 6.30 |
| CHEMBL90035 | — | — | 1 | 6.22 |
| CHEMBL329840 | — | — | 1 | 6.03 |
| CHEMBL329445 | — | — | 1 | 5.97 |
| CHEMBL59913 | — | — | 1 | 5.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL16192 | CP-96345 | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL93401 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL91438 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL92621 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL431459 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL90416 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL90547 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL314084 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL63109 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL329416 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL93038 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL441458 | — | IC50 | = | 217.0 | nM | 6.66 |
| CHEMBL93251 | — | IC50 | = | 267.0 | nM | 6.57 |
| CHEMBL299887 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL329168 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL59854 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL90035 | — | IC50 | = | 597.0 | nM | 6.22 |
| CHEMBL329840 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL329445 | — | IC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL59913 | — | IC50 | = | 3000.0 | nM | 5.52 |