Assay Detail
Functional
CHEMBL4201316
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Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation 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 | 7.36 | 8.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3104471 | — | — | 1 | 8.44 |
| CHEMBL4205274 | — | — | 1 | 8.15 |
| CHEMBL4217514 | — | — | 1 | 7.97 |
| CHEMBL4208184 | — | — | 1 | 7.82 |
| CHEMBL4213101 | — | — | 1 | 7.56 |
| CHEMBL4213538 | — | — | 1 | 7.33 |
| CHEMBL4204786 | — | — | 1 | 7.27 |
| CHEMBL4216988 | — | — | 1 | 6.21 |
| CHEMBL4209654 | — | — | 1 | 5.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3104471 | — | EC50 | = | 3.631 | nM | 8.44 |
| CHEMBL4205274 | — | EC50 | = | 7.079 | nM | 8.15 |
| CHEMBL4217514 | — | EC50 | = | 10.72 | nM | 7.97 |
| CHEMBL4208184 | — | EC50 | = | 15.14 | nM | 7.82 |
| CHEMBL4213101 | — | EC50 | = | 27.54 | nM | 7.56 |
| CHEMBL4213538 | — | EC50 | = | 46.77 | nM | 7.33 |
| CHEMBL4204786 | — | EC50 | = | 53.7 | nM | 7.27 |
| CHEMBL4216988 | — | EC50 | = | 616.6 | nM | 6.21 |
| CHEMBL4209654 | — | EC50 | = | 3548.13 | nM | 5.45 |