Assay Detail
Binding
CHEMBL845233
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mu-selective antagonist binding to opioid receptor of guinea pig ileum
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| 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 | 7.37 | 8.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL405618 | ANALOG OF DYNORPHIN A | — | 1 | 8.94 |
| CHEMBL411557 | DYNORPHIN A (1-17) | — | 1 | 8.60 |
| CHEMBL438223 | DYNORPHIN A (1-11) | — | 1 | 8.42 |
| CHEMBL409793 | — | — | 1 | 8.35 |
| CHEMBL265241 | — | — | 1 | 8.19 |
| CHEMBL438274 | — | — | 1 | 8.13 |
| CHEMBL411196 | — | — | 1 | 7.61 |
| CHEMBL415406 | — | — | 1 | 6.60 |
| CHEMBL444626 | — | — | 1 | 6.54 |
| CHEMBL386722 | — | — | 1 | 6.39 |
| CHEMBL384566 | — | — | 1 | 5.40 |
| CHEMBL2371443 | — | — | 1 | 5.21 |
| CHEMBL408497 | — | — | 1 | - |
| CHEMBL414494 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL405618 | ANALOG OF DYNORPHIN A | IC50 | = | 1.15 | nM | 8.94 |
| CHEMBL411557 | DYNORPHIN A (1-17) | IC50 | = | 2.53 | nM | 8.60 |
| CHEMBL438223 | DYNORPHIN A (1-11) | IC50 | = | 3.81 | nM | 8.42 |
| CHEMBL409793 | — | IC50 | = | 4.46 | nM | 8.35 |
| CHEMBL265241 | — | IC50 | = | 6.51 | nM | 8.19 |
| CHEMBL438274 | — | IC50 | = | 7.33 | nM | 8.13 |
| CHEMBL411196 | — | IC50 | = | 24.6 | nM | 7.61 |
| CHEMBL415406 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL444626 | — | IC50 | = | 286.0 | nM | 6.54 |
| CHEMBL386722 | — | IC50 | = | 411.0 | nM | 6.39 |
| CHEMBL384566 | — | IC50 | = | 3972.0 | nM | 5.40 |
| CHEMBL2371443 | — | IC50 | = | 6180.0 | nM | 5.21 |
| CHEMBL408497 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL414494 | — | IC50 | > | 10000.0 | nM | - |