Assay Detail
Binding
CHEMBL899345
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Displacement of [125I]SP from human NK1 receptor expressed in CHO cells
25
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Pyrrolidine-carboxamides and oxadiazoles as potent hNK1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 8.98 | 10.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL392466 | — | — | 1 | 10.52 |
| CHEMBL391964 | — | — | 1 | 10.30 |
| CHEMBL391615 | — | — | 1 | 10.30 |
| CHEMBL392463 | — | — | 1 | 10.15 |
| CHEMBL392465 | — | — | 1 | 10.15 |
| CHEMBL235882 | — | — | 1 | 10.05 |
| CHEMBL1471 | APREPITANT | 4.0 | 1 | 10.05 |
| CHEMBL391963 | — | — | 2 | 9.92 |
| CHEMBL392464 | — | — | 1 | 9.77 |
| CHEMBL238220 | — | — | 1 | 9.24 |
| CHEMBL238210 | — | — | 1 | 9.17 |
| CHEMBL393746 | — | — | 1 | 9.13 |
| CHEMBL235219 | — | — | 1 | 9.10 |
| CHEMBL393745 | — | — | 1 | 9.08 |
| CHEMBL237796 | — | — | 1 | 9.01 |
| CHEMBL429798 | — | — | 1 | 8.47 |
| CHEMBL237100 | — | — | 1 | 8.43 |
| CHEMBL235220 | — | — | 1 | 8.39 |
| CHEMBL238209 | — | — | 1 | 7.96 |
| CHEMBL392567 | — | — | 1 | 7.89 |
| CHEMBL236304 | — | — | 1 | 7.62 |
| CHEMBL392566 | — | — | 1 | 7.21 |
| CHEMBL391441 | — | — | 1 | 6.85 |
| CHEMBL237992 | — | — | 1 | 6.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL392466 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL391964 | — | IC50 | = | 0.05 | nM | 10.30 |
| CHEMBL391615 | — | IC50 | = | 0.05 | nM | 10.30 |
| CHEMBL392463 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL392465 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL1471 | APREPITANT | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL235882 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL391963 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL392464 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL391963 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL238220 | — | IC50 | = | 0.58 | nM | 9.24 |
| CHEMBL238210 | — | IC50 | = | 0.68 | nM | 9.17 |
| CHEMBL393746 | — | IC50 | = | 0.74 | nM | 9.13 |
| CHEMBL235219 | — | IC50 | = | 0.79 | nM | 9.10 |
| CHEMBL393745 | — | IC50 | = | 0.84 | nM | 9.08 |
| CHEMBL237796 | — | IC50 | = | 0.97 | nM | 9.01 |
| CHEMBL429798 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL237100 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL235220 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL238209 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL392567 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL236304 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL392566 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL391441 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL237992 | — | IC50 | = | 450.0 | nM | 6.35 |