Assay Detail
Binding
CHEMBL844036
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]PL-17 binding to mu opioid receptor of guinea pig brain homogenate
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Design and synthesis of highly potent and selective cyclic dynorphin A analogs. 2. New analogs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 8.52 | 10.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL265241 | — | — | 1 | 10.04 |
| CHEMBL438274 | — | — | 1 | 9.42 |
| CHEMBL409793 | — | — | 1 | 9.17 |
| CHEMBL438223 | DYNORPHIN A (1-11) | — | 1 | 8.97 |
| CHEMBL414494 | — | — | 1 | 8.90 |
| CHEMBL405618 | ANALOG OF DYNORPHIN A | — | 1 | 8.89 |
| CHEMBL411196 | — | — | 1 | 8.61 |
| CHEMBL444626 | — | — | 1 | 8.37 |
| CHEMBL411557 | DYNORPHIN A (1-17) | — | 1 | 8.30 |
| CHEMBL415406 | — | — | 1 | 8.24 |
| CHEMBL386722 | — | — | 1 | 8.19 |
| CHEMBL384566 | — | — | 1 | 8.01 |
| CHEMBL408497 | — | — | 1 | 7.21 |
| CHEMBL2371443 | — | — | 1 | 6.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL265241 | — | IC50 | = | 0.091 | nM | 10.04 |
| CHEMBL438274 | — | IC50 | = | 0.38 | nM | 9.42 |
| CHEMBL409793 | — | IC50 | = | 0.674 | nM | 9.17 |
| CHEMBL438223 | DYNORPHIN A (1-11) | IC50 | = | 1.08 | nM | 8.97 |
| CHEMBL414494 | — | IC50 | = | 1.26 | nM | 8.90 |
| CHEMBL405618 | ANALOG OF DYNORPHIN A | IC50 | = | 1.29 | nM | 8.89 |
| CHEMBL411196 | — | IC50 | = | 2.48 | nM | 8.61 |
| CHEMBL444626 | — | IC50 | = | 4.26 | nM | 8.37 |
| CHEMBL411557 | DYNORPHIN A (1-17) | IC50 | = | 5.04 | nM | 8.30 |
| CHEMBL415406 | — | IC50 | = | 5.81 | nM | 8.24 |
| CHEMBL386722 | — | IC50 | = | 6.43 | nM | 8.19 |
| CHEMBL384566 | — | IC50 | = | 9.69 | nM | 8.01 |
| CHEMBL408497 | — | IC50 | = | 61.2 | nM | 7.21 |
| CHEMBL2371443 | — | IC50 | = | 106.0 | nM | 6.97 |