Assay Detail
Functional
CHEMBL687655
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Concentration of compound to inhibit 50% (IC50) electrically evoked contractions was tested in Guinea pig ileum(GPI) assay.
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
Dermorphin analogues carrying an increased positive net charge in their "message" domain display extremely high mu opioid receptor selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.17 | 8.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL317264 | — | — | 1 | 8.49 |
| CHEMBL2371281 | — | — | 1 | 7.67 |
| CHEMBL38874 | DAMGO | — | 1 | 7.55 |
| CHEMBL2371286 | — | — | 1 | 7.51 |
| CHEMBL2371283 | — | — | 1 | 7.44 |
| CHEMBL2371284 | — | — | 1 | 7.39 |
| CHEMBL2371285 | — | — | 1 | 6.98 |
| CHEMBL2371291 | — | — | 1 | 6.78 |
| CHEMBL8234 | ENKEPHALIN | — | 1 | 6.61 |
| CHEMBL60444 | — | — | 1 | 6.59 |
| CHEMBL436434 | — | — | 1 | 6.59 |
| CHEMBL2371282 | — | — | 1 | 6.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL317264 | — | IC50 | = | 3.23 | nM | 8.49 |
| CHEMBL2371281 | — | IC50 | = | 21.6 | nM | 7.67 |
| CHEMBL38874 | DAMGO | IC50 | = | 28.3 | nM | 7.55 |
| CHEMBL2371286 | — | IC50 | = | 30.6 | nM | 7.51 |
| CHEMBL2371283 | — | IC50 | = | 36.2 | nM | 7.44 |
| CHEMBL2371284 | — | IC50 | = | 40.9 | nM | 7.39 |
| CHEMBL2371285 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL2371291 | — | IC50 | = | 168.0 | nM | 6.78 |
| CHEMBL8234 | ENKEPHALIN | IC50 | = | 246.0 | nM | 6.61 |
| CHEMBL60444 | — | IC50 | = | 254.0 | nM | 6.59 |
| CHEMBL436434 | — | IC50 | = | 257.0 | nM | 6.59 |
| CHEMBL2371282 | — | IC50 | = | 346.0 | nM | 6.46 |