Assay Detail
Functional
CHEMBL743591
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Concentration of compound to inhibit 50% (IC50) electrically evoked contractions was tested in Mouse vas deferens (MVD) assay.
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| 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 | 6.23 | 7.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL8234 | ENKEPHALIN | — | 1 | 7.94 |
| CHEMBL2371286 | — | — | 1 | 6.82 |
| CHEMBL2371285 | — | — | 1 | 6.57 |
| CHEMBL436434 | — | — | 1 | 6.18 |
| CHEMBL2371284 | — | — | 1 | 6.13 |
| CHEMBL60444 | — | — | 1 | 6.11 |
| CHEMBL317264 | — | — | 1 | 6.10 |
| CHEMBL38874 | DAMGO | — | 1 | 6.02 |
| CHEMBL2371282 | — | — | 1 | 5.96 |
| CHEMBL2371281 | — | — | 1 | 5.89 |
| CHEMBL2371291 | — | — | 1 | 5.64 |
| CHEMBL2371283 | — | — | 1 | 5.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL8234 | ENKEPHALIN | IC50 | = | 11.4 | nM | 7.94 |
| CHEMBL2371286 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL2371285 | — | IC50 | = | 271.0 | nM | 6.57 |
| CHEMBL436434 | — | IC50 | = | 659.0 | nM | 6.18 |
| CHEMBL2371284 | — | IC50 | = | 745.0 | nM | 6.13 |
| CHEMBL60444 | — | IC50 | = | 781.0 | nM | 6.11 |
| CHEMBL317264 | — | IC50 | = | 797.0 | nM | 6.10 |
| CHEMBL38874 | DAMGO | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL2371282 | — | IC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL2371281 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL2371291 | — | IC50 | = | 2290.0 | nM | 5.64 |
| CHEMBL2371283 | — | IC50 | = | 3880.0 | nM | 5.41 |