Assay Detail
Functional
CHEMBL745616
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In vitro inhibition of electrically evoked contractions in guinea pig ileum longitudinal muscle myenteric plexus
12
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| 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 | 12 | 5.49 | 8.53 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL289006 | — | — | 1 | 8.53 |
| CHEMBL286629 | — | — | 1 | 5.96 |
| CHEMBL317956 | DELTORPHIN C | — | 2 | 5.50 |
| CHEMBL32202 | — | — | 1 | 5.47 |
| CHEMBL2372209 | — | — | 1 | 5.35 |
| CHEMBL284621 | — | — | 1 | 5.26 |
| CHEMBL2372208 | — | — | 1 | 5.15 |
| CHEMBL2372213 | — | — | 1 | 4.87 |
| CHEMBL2372214 | — | — | 1 | 4.66 |
| CHEMBL288317 | — | — | 1 | 4.17 |
| CHEMBL2372212 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL289006 | — | IC50 | = | 2.98 | nM | 8.53 |
| CHEMBL286629 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL317956 | DELTORPHIN C | IC50 | = | 3180.0 | nM | 5.50 |
| CHEMBL32202 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL2372209 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL284621 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL2372208 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL2372213 | — | IC50 | = | 13500.0 | nM | 4.87 |
| CHEMBL2372214 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL288317 | — | IC50 | = | 68000.0 | nM | 4.17 |
| CHEMBL2372212 | — | IC50 | = | 137000.0 | nM | - |
| CHEMBL317956 | DELTORPHIN C | IC50 | = | 2890.0 | nM | - |