Assay Detail
Binding
CHEMBL3863201
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]U69,593 from KOR in guinea pig brain membrane measured after 2 hrs
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
A Cyclic Tetrapeptide ("Cyclodal") and Its Mirror-Image Isomer Are Both High-Affinity μ Opioid Receptor Antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 7.45 | 9.13 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3924888 | — | — | 1 | 9.13 |
| CHEMBL3979449 | — | — | 1 | 9.11 |
| CHEMBL3908315 | — | — | 1 | 8.34 |
| CHEMBL3897031 | — | — | 1 | 8.29 |
| CHEMBL363142 | — | — | 1 | 7.65 |
| CHEMBL3951723 | — | — | 1 | 7.64 |
| CHEMBL3904924 | — | — | 1 | 7.21 |
| CHEMBL3976694 | — | — | 1 | 6.39 |
| CHEMBL3944636 | — | — | 1 | 5.87 |
| CHEMBL507214 | — | — | 1 | 4.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3924888 | — | Ki | = | 0.733 | nM | 9.13 |
| CHEMBL3979449 | — | Ki | = | 0.786 | nM | 9.11 |
| CHEMBL3908315 | — | Ki | = | 4.55 | nM | 8.34 |
| CHEMBL3897031 | — | Ki | = | 5.11 | nM | 8.29 |
| CHEMBL363142 | — | Ki | = | 22.3 | nM | 7.65 |
| CHEMBL3951723 | — | Ki | = | 22.7 | nM | 7.64 |
| CHEMBL3904924 | — | Ki | = | 60.9 | nM | 7.21 |
| CHEMBL3976694 | — | Ki | = | 405.0 | nM | 6.39 |
| CHEMBL3944636 | — | Ki | = | 1340.0 | nM | 5.87 |
| CHEMBL507214 | — | Ki | = | 14900.0 | nM | 4.83 |