Assay Detail
Functional
CHEMBL685649
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of electrically induced smooth muscle contraction in guinea pig ileum.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| Confidence | 1 — Organism |
| Curated By | Expert |
Publication
Design, synthesis, and biological properties of highly potent cyclic dynorphin A analogues. Analogues cyclized between positions 5 and 11.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.32 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL411338 | — | — | 1 | 9.52 |
| CHEMBL216640 | — | — | 1 | 8.97 |
| CHEMBL404929 | — | — | 1 | 7.04 |
| CHEMBL374268 | — | — | 1 | 7.03 |
| CHEMBL2370618 | — | — | 1 | 6.67 |
| CHEMBL2112652 | — | — | 1 | 6.66 |
| CHEMBL2370626 | — | — | 1 | 6.21 |
| CHEMBL2370629 | — | — | 1 | 6.16 |
| CHEMBL2370612 | — | — | 1 | 6.14 |
| CHEMBL2370627 | — | — | 1 | 6.03 |
| CHEMBL2370622 | — | — | 1 | 5.95 |
| CHEMBL414713 | — | — | 1 | 5.84 |
| CHEMBL2370611 | — | — | 1 | 5.78 |
| CHEMBL2370610 | — | — | 1 | 5.46 |
| CHEMBL2370628 | — | — | 1 | 5.44 |
| CHEMBL2369128 | — | — | 1 | 5.21 |
| CHEMBL2370631 | — | — | 1 | 5.00 |
| CHEMBL2111843 | — | — | 1 | 4.72 |
| CHEMBL263509 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL411338 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL216640 | — | IC50 | = | 1.07 | nM | 8.97 |
| CHEMBL404929 | — | IC50 | = | 92.3 | nM | 7.04 |
| CHEMBL374268 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL2370618 | — | IC50 | = | 213.0 | nM | 6.67 |
| CHEMBL2112652 | — | IC50 | = | 219.0 | nM | 6.66 |
| CHEMBL2370626 | — | IC50 | = | 615.0 | nM | 6.21 |
| CHEMBL2370629 | — | IC50 | = | 686.0 | nM | 6.16 |
| CHEMBL2370612 | — | IC50 | = | 716.0 | nM | 6.14 |
| CHEMBL2370627 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL2370622 | — | IC50 | = | 1130.0 | nM | 5.95 |
| CHEMBL414713 | — | IC50 | = | 1460.0 | nM | 5.84 |
| CHEMBL2370611 | — | IC50 | = | 1660.0 | nM | 5.78 |
| CHEMBL2370610 | — | IC50 | = | 3450.0 | nM | 5.46 |
| CHEMBL2370628 | — | IC50 | = | 3640.0 | nM | 5.44 |
| CHEMBL2369128 | — | IC50 | = | 6240.0 | nM | 5.21 |
| CHEMBL2370631 | — | IC50 | = | 10100.0 | nM | 5.00 |
| CHEMBL2111843 | — | IC50 | = | 19100.0 | nM | 4.72 |
| CHEMBL263509 | — | IC50 | > | 30000.0 | nM | - |