Assay Detail
Functional
CHEMBL754252
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In vitro inhibition of electrically induced smooth muscle contractions of mouse vas deferens
11
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Tissue | Vas deferens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Design of cyclic deltorphins and dermenkephalins with a disulfide bridge leads to analogues with high selectivity for delta-opioid receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 8.48 | 9.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL289006 | — | — | 1 | 9.64 |
| CHEMBL286629 | — | — | 1 | 9.60 |
| CHEMBL32202 | — | — | 1 | 9.55 |
| CHEMBL317956 | DELTORPHIN C | — | 2 | 9.44 |
| CHEMBL2372208 | — | — | 1 | 8.65 |
| CHEMBL288317 | — | — | 1 | 8.20 |
| CHEMBL2372212 | — | — | 1 | 8.06 |
| CHEMBL2372214 | — | — | 1 | 7.90 |
| CHEMBL2372213 | — | — | 1 | 7.04 |
| CHEMBL284621 | — | — | 1 | 6.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL289006 | — | IC50 | = | 0.23 | nM | 9.64 |
| CHEMBL286629 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL32202 | — | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL317956 | DELTORPHIN C | IC50 | = | 0.36 | nM | 9.44 |
| CHEMBL317956 | DELTORPHIN C | IC50 | = | 0.67 | nM | 9.17 |
| CHEMBL2372208 | — | IC50 | = | 2.24 | nM | 8.65 |
| CHEMBL288317 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL2372212 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL2372214 | — | IC50 | = | 12.7 | nM | 7.90 |
| CHEMBL2372213 | — | IC50 | = | 91.8 | nM | 7.04 |
| CHEMBL284621 | — | IC50 | = | 920.0 | nM | 6.04 |