Assay Detail
Functional
CHEMBL4201302
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
6
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of New Allosteric Modulators of the Urotensinergic System through Substitution of the Urotensin II-Related Peptide (URP) Phenylalanine Residue.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 4 | 8.03 | 8.56 |
| pEC50 | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4209654 | — | — | 1 | 8.56 |
| CHEMBL4213538 | — | — | 1 | 7.91 |
| CHEMBL4204786 | — | — | 1 | 7.90 |
| CHEMBL4216988 | — | — | 1 | 7.75 |
| CHEMBL4213101 | — | — | 1 | - |
| CHEMBL4208184 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4209654 | — | EC50 | = | 2.754 | nM | 8.56 |
| CHEMBL4213538 | — | EC50 | = | 12.3 | nM | 7.91 |
| CHEMBL4204786 | — | EC50 | = | 12.59 | nM | 7.90 |
| CHEMBL4216988 | — | EC50 | = | 17.78 | nM | 7.75 |
| CHEMBL4213101 | — | pEC50 | - | — | - | |
| CHEMBL4208184 | — | pEC50 | - | — | - |