Assay Detail
Binding
CHEMBL872342
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Tested for inhibitory concentration against [3H]DAMGO binding at sites of mu-opioid receptor in guinea pig brain membrane
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 | Expert |
Publication
Isothiocyanate-substituted kappa-selective opioid receptor ligands derived from N-methyl-N-[(1S)-1-phenyl-2-(1-pyrrolidinyl)ethyl] phenylacetamide.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.17 | 7.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL124283 | — | — | 1 | 7.14 |
| CHEMBL38576 | ICI-199,441 | — | 1 | 6.82 |
| CHEMBL95726 | — | — | 1 | 6.14 |
| CHEMBL95001 | — | — | 1 | 5.90 |
| CHEMBL440765 | U-69593 | — | 1 | 5.75 |
| CHEMBL97246 | — | — | 1 | 5.29 |
| CHEMBL95654 | — | — | 1 | - |
| CHEMBL94734 | — | — | 1 | - |
| CHEMBL97392 | — | — | 1 | - |
| CHEMBL31421 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL124283 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL38576 | ICI-199,441 | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL95726 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL95001 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL440765 | U-69593 | IC50 | = | 1760.0 | nM | 5.75 |
| CHEMBL97246 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL95654 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL94734 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL97392 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL31421 | — | IC50 | > | 1000.0 | nM | - |