Assay Detail
Binding
CHEMBL3411022
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Displacement of [3H]DAMGO from rat brain MOR 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 | 9.67 | 10.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3408518 | — | — | 1 | 10.10 |
| CHEMBL3408519 | — | — | 1 | 10.10 |
| CHEMBL3408522 | — | — | 1 | 10.05 |
| CHEMBL3408736 | — | — | 1 | 10.00 |
| CHEMBL3408730 | — | — | 1 | 9.85 |
| CHEMBL1782140 | — | — | 1 | 9.82 |
| CHEMBL3408521 | — | — | 1 | 9.55 |
| CHEMBL3408520 | — | — | 1 | 9.43 |
| CHEMBL1782141 | — | — | 1 | 9.38 |
| CHEMBL3408735 | — | — | 1 | 9.21 |
| CHEMBL3408737 | — | — | 1 | 8.87 |
| CHEMBL1782139 | — | — | 1 | - |
| CHEMBL3408731 | — | — | 1 | - |
| CHEMBL3408732 | — | — | 1 | - |
| CHEMBL3408733 | — | — | 1 | - |
| CHEMBL3408734 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3408518 | — | Ki | = | 0.08 | nM | 10.10 |
| CHEMBL3408519 | — | Ki | = | 0.08 | nM | 10.10 |
| CHEMBL3408522 | — | Ki | = | 0.09 | nM | 10.05 |
| CHEMBL3408736 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3408730 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL1782140 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL3408521 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL3408520 | — | Ki | = | 0.37 | nM | 9.43 |
| CHEMBL1782141 | — | Ki | = | 0.42 | nM | 9.38 |
| CHEMBL3408735 | — | Ki | = | 0.62 | nM | 9.21 |
| CHEMBL3408737 | — | Ki | = | 1.34 | nM | 8.87 |
| CHEMBL1782139 | — | Ki | - | — | - | |
| CHEMBL3408731 | — | Ki | - | — | - | |
| CHEMBL3408732 | — | Ki | - | — | - | |
| CHEMBL3408733 | — | Ki | - | — | - | |
| CHEMBL3408734 | — | Ki | - | — | - |