Assay Detail
Binding
CHEMBL862628
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of endomorphin-2 from mu opioid receptor in guinea pig ileum
14
Total Activities
14
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Potent Dmt-Tic pharmacophoric delta- and mu-opioid receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| pA2 | 8 | - | - |
| Kd | 6 | 7.35 | 8.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL370399 | — | — | 1 | 8.34 |
| CHEMBL261905 | — | — | 1 | 7.71 |
| CHEMBL567175 | NALTRINDOLE | — | 1 | 7.30 |
| CHEMBL370197 | — | — | 1 | 6.99 |
| CHEMBL370398 | — | — | 1 | 6.95 |
| CHEMBL198800 | — | — | 1 | 6.78 |
| CHEMBL200890 | — | — | 1 | - |
| CHEMBL381874 | — | — | 1 | - |
| CHEMBL373668 | — | — | 1 | - |
| CHEMBL198646 | — | — | 1 | - |
| CHEMBL196774 | — | — | 1 | - |
| CHEMBL197185 | — | — | 1 | - |
| CHEMBL373192 | — | — | 1 | - |
| CHEMBL571492 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL370399 | — | Kd | = | 4.571 | nM | 8.34 |
| CHEMBL261905 | — | Kd | = | 19.5 | nM | 7.71 |
| CHEMBL567175 | NALTRINDOLE | Kd | = | 50.12 | nM | 7.30 |
| CHEMBL370197 | — | Kd | = | 102.33 | nM | 6.99 |
| CHEMBL370398 | — | Kd | = | 112.2 | nM | 6.95 |
| CHEMBL198800 | — | Kd | = | 165.96 | nM | 6.78 |
| CHEMBL200890 | — | pA2 | - | — | - | |
| CHEMBL381874 | — | pA2 | - | — | - | |
| CHEMBL373668 | — | pA2 | - | — | - | |
| CHEMBL198646 | — | pA2 | - | — | - | |
| CHEMBL196774 | — | pA2 | - | — | - | |
| CHEMBL197185 | — | pA2 | - | — | - | |
| CHEMBL373192 | — | pA2 | - | — | - | |
| CHEMBL571492 | — | pA2 | - | — | - |