Assay Detail
Binding
CHEMBL3411023
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Displacement of [3H]DSLET from rat brain DOR after 2 hrs
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| 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 | 8.79 | 9.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3408519 | — | — | 1 | 9.55 |
| CHEMBL3408521 | — | — | 1 | 9.32 |
| CHEMBL3408520 | — | — | 1 | 9.26 |
| CHEMBL1782140 | — | — | 1 | 9.22 |
| CHEMBL3408730 | — | — | 1 | 9.21 |
| CHEMBL3408735 | — | — | 1 | 8.77 |
| CHEMBL3408518 | — | — | 1 | 8.67 |
| CHEMBL3408522 | — | — | 1 | 8.63 |
| CHEMBL3408736 | — | — | 1 | 8.35 |
| CHEMBL1782141 | — | — | 1 | 7.98 |
| CHEMBL3408737 | — | — | 1 | 7.77 |
| CHEMBL1782139 | — | — | 1 | - |
| CHEMBL3408731 | — | — | 1 | - |
| CHEMBL3408732 | — | — | 1 | - |
| CHEMBL3408733 | — | — | 1 | - |
| CHEMBL3408734 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3408519 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL3408521 | — | Ki | = | 0.48 | nM | 9.32 |
| CHEMBL3408520 | — | Ki | = | 0.55 | nM | 9.26 |
| CHEMBL1782140 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL3408730 | — | Ki | = | 0.62 | nM | 9.21 |
| CHEMBL3408735 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL3408518 | — | Ki | = | 2.14 | nM | 8.67 |
| CHEMBL3408522 | — | Ki | = | 2.35 | nM | 8.63 |
| CHEMBL3408736 | — | Ki | = | 4.43 | nM | 8.35 |
| CHEMBL1782141 | — | Ki | = | 10.4 | nM | 7.98 |
| CHEMBL3408737 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL1782139 | — | Ki | - | — | - | |
| CHEMBL3408731 | — | Ki | - | — | - | |
| CHEMBL3408732 | — | Ki | - | — | - | |
| CHEMBL3408733 | — | Ki | - | — | - | |
| CHEMBL3408734 | — | Ki | - | — | - |