Assay Detail
Binding
CHEMBL3411101
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Displacement of [3H]SP from human NK1 receptor expressed in CHO cells after 20 mins by liquid scintillation counting analysis
16
Total Activities
16
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 | Autocuration |
Publication
Synthesis and biological evaluation of compact, conformationally constrained bifunctional opioid agonist - neurokinin-1 antagonist peptidomimetics.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 6.64 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1782141 | — | — | 1 | 9.30 |
| CHEMBL3408519 | — | — | 1 | 7.89 |
| CHEMBL1782139 | — | — | 1 | 7.57 |
| CHEMBL3408520 | — | — | 1 | 7.46 |
| CHEMBL3408731 | — | — | 1 | 7.46 |
| CHEMBL3408518 | — | — | 1 | 7.22 |
| CHEMBL3408734 | — | — | 1 | 6.51 |
| CHEMBL3408733 | — | — | 1 | 6.13 |
| CHEMBL3408735 | — | — | 1 | 6.13 |
| CHEMBL3408732 | — | — | 1 | 5.99 |
| CHEMBL3408522 | — | — | 1 | 5.82 |
| CHEMBL3408521 | — | — | 1 | 5.52 |
| CHEMBL3408730 | — | — | 1 | 5.21 |
| CHEMBL3408736 | — | — | 1 | 4.79 |
| CHEMBL1782140 | — | — | 1 | - |
| CHEMBL3408737 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1782141 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3408519 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL1782139 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL3408520 | — | Ki | = | 34.7 | nM | 7.46 |
| CHEMBL3408731 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL3408518 | — | Ki | = | 59.7 | nM | 7.22 |
| CHEMBL3408734 | — | Ki | = | 308.0 | nM | 6.51 |
| CHEMBL3408733 | — | Ki | = | 743.0 | nM | 6.13 |
| CHEMBL3408735 | — | Ki | = | 734.0 | nM | 6.13 |
| CHEMBL3408732 | — | Ki | = | 1020.0 | nM | 5.99 |
| CHEMBL3408522 | — | Ki | = | 1530.0 | nM | 5.82 |
| CHEMBL3408521 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL3408730 | — | Ki | = | 6190.0 | nM | 5.21 |
| CHEMBL3408736 | — | Ki | = | 16050.0 | nM | 4.79 |
| CHEMBL1782140 | — | Ki | - | — | - | |
| CHEMBL3408737 | — | Ki | - | — | - |