Assay Detail
Functional
CHEMBL687943
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Opioid activity in guinea pig ileum
16
Total Activities
16
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
Synthesis and opioid activity of conformationally constrained dynorphin A analogues. 2. Conformational constraint in the "address" sequence.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.75 | 9.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL405618 | ANALOG OF DYNORPHIN A | — | 1 | 9.72 |
| CHEMBL412413 | — | — | 1 | 8.17 |
| CHEMBL263366 | — | — | 1 | 7.66 |
| CHEMBL408360 | — | — | 1 | 7.54 |
| CHEMBL264481 | — | — | 1 | 7.34 |
| CHEMBL408024 | — | — | 1 | 7.13 |
| CHEMBL2370861 | — | — | 1 | 6.36 |
| CHEMBL414921 | — | — | 1 | 6.28 |
| CHEMBL407076 | — | — | 1 | 6.19 |
| CHEMBL2370831 | — | — | 1 | 6.06 |
| CHEMBL2370877 | — | — | 1 | 6.00 |
| CHEMBL386618 | — | — | 1 | 5.89 |
| CHEMBL406899 | — | — | 1 | 5.85 |
| CHEMBL2370832 | — | — | 1 | 5.57 |
| CHEMBL2370887 | — | — | 1 | 5.55 |
| CHEMBL412364 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL405618 | ANALOG OF DYNORPHIN A | IC50 | = | 0.19 | nM | 9.72 |
| CHEMBL412413 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL263366 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL408360 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL264481 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL408024 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL2370861 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL414921 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL407076 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL2370831 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL2370877 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL386618 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL406899 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL2370832 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL2370887 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL412364 | — | IC50 | > | 5000.0 | nM | - |