Assay Detail
Functional
CHEMBL4201320
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Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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 | 9 | 6.33 | 6.84 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3104471 | — | — | 1 | 6.84 |
| CHEMBL4217514 | — | — | 1 | 6.74 |
| CHEMBL4205274 | — | — | 1 | 6.72 |
| CHEMBL4213538 | — | — | 1 | 6.46 |
| CHEMBL4204786 | — | — | 1 | 6.45 |
| CHEMBL4208184 | — | — | 1 | 6.22 |
| CHEMBL4213101 | — | — | 1 | 6.12 |
| CHEMBL4209654 | — | — | 1 | 5.94 |
| CHEMBL4216988 | — | — | 1 | 5.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3104471 | — | EC50 | = | 144.54 | nM | 6.84 |
| CHEMBL4217514 | — | EC50 | = | 181.97 | nM | 6.74 |
| CHEMBL4205274 | — | EC50 | = | 190.55 | nM | 6.72 |
| CHEMBL4213538 | — | EC50 | = | 346.74 | nM | 6.46 |
| CHEMBL4204786 | — | EC50 | = | 354.81 | nM | 6.45 |
| CHEMBL4208184 | — | EC50 | = | 602.56 | nM | 6.22 |
| CHEMBL4213101 | — | EC50 | = | 758.58 | nM | 6.12 |
| CHEMBL4209654 | — | EC50 | = | 1148.15 | nM | 5.94 |
| CHEMBL4216988 | — | EC50 | = | 3311.31 | nM | 5.48 |