Assay Detail
Binding
CHEMBL753423
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Binding affinity of compound was measured on Opioid receptor mu 1 by competitive inhibition of radioligand [3H]DAMGO using cloned receptors transiently expressed on COS-7 (monkey kidney) cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Cell Type | COS-7 |
| 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 | 4 | 6.56 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2370887 | — | — | 1 | 7.00 |
| CHEMBL2370831 | — | — | 1 | 6.68 |
| CHEMBL2370832 | — | — | 1 | 6.50 |
| CHEMBL2370877 | — | — | 1 | 6.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2370887 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL2370831 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL2370832 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL2370877 | — | Ki | = | 910.0 | nM | 6.04 |