Assay Detail
Binding
CHEMBL747305
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Inhibition of [125I]-substance P binding to human neurokinin-1 (hNK-1) receptor in CHO cells
17
Total Activities
17
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
1,2,4-Triacylpiperidine substance p antagonists: Separation of affinities for the NK-1 receptor and the L-type calcium channel
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 8.11 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL16192 | CP-96345 | — | 1 | 9.30 |
| CHEMBL345520 | — | — | 1 | 9.15 |
| CHEMBL347891 | — | — | 1 | 8.85 |
| CHEMBL153976 | — | — | 1 | 8.74 |
| CHEMBL357757 | — | — | 1 | 8.74 |
| CHEMBL358173 | — | — | 1 | 8.74 |
| CHEMBL345866 | — | — | 1 | 8.46 |
| CHEMBL349113 | — | — | 1 | 8.42 |
| CHEMBL154803 | — | — | 1 | 8.26 |
| CHEMBL346485 | — | — | 1 | 8.10 |
| CHEMBL348594 | — | — | 1 | 7.89 |
| CHEMBL155976 | — | — | 1 | 7.70 |
| CHEMBL156933 | — | — | 1 | 7.48 |
| CHEMBL90416 | — | — | 1 | 7.39 |
| CHEMBL158255 | — | — | 1 | 7.14 |
| CHEMBL63109 | — | — | 1 | 6.89 |
| CHEMBL434272 | — | — | 1 | 6.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL16192 | CP-96345 | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL345520 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL347891 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL153976 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL357757 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL358173 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL345866 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL349113 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL154803 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL346485 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL348594 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL155976 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL156933 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL90416 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL158255 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL63109 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL434272 | — | IC50 | = | 250.0 | nM | 6.60 |