Assay Detail
Binding
CHEMBL753422
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Binding affinity to Opioid receptor mu 1 by competitive inhibition of radioligand [3H]DAMGO using cloned receptors transiently expressed on CHO cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Synthesis and opioid activity of conformationally constrained dynorphin A analogues. 2. Conformational constraint in the "address" sequence.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 8.06 | 9.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL405618 | ANALOG OF DYNORPHIN A | — | 1 | 9.04 |
| CHEMBL408360 | — | — | 1 | 8.92 |
| CHEMBL408024 | — | — | 1 | 8.82 |
| CHEMBL412413 | — | — | 1 | 8.49 |
| CHEMBL264481 | — | — | 1 | 8.36 |
| CHEMBL263366 | — | — | 1 | 8.32 |
| CHEMBL406899 | — | — | 1 | 8.21 |
| CHEMBL407076 | — | — | 1 | 8.08 |
| CHEMBL386618 | — | — | 1 | 7.40 |
| CHEMBL414921 | — | — | 1 | 7.21 |
| CHEMBL412364 | — | — | 1 | 7.12 |
| CHEMBL2370861 | — | — | 1 | 6.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL405618 | ANALOG OF DYNORPHIN A | Ki | = | 0.92 | nM | 9.04 |
| CHEMBL408360 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL408024 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL412413 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL264481 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL263366 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL406899 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL407076 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL386618 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL414921 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL412364 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL2370861 | — | Ki | = | 180.0 | nM | 6.75 |