Assay Detail
Binding
CHEMBL4370028
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Agonist activity at urotensin 2 receptor (unknown origin) 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
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Functional Selectivity Revealed by N-Methylation Scanning of Human Urotensin II and Related Peptides.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 8.16 | 8.73 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL218994 | — | — | 1 | 8.73 |
| CHEMBL3104471 | — | — | 1 | 8.57 |
| CHEMBL4474481 | — | — | 1 | 8.57 |
| CHEMBL593662 | UROTENSIN-II | — | 1 | 8.52 |
| CHEMBL4568153 | — | — | 1 | 8.44 |
| CHEMBL4454498 | — | — | 1 | 8.33 |
| CHEMBL4462940 | — | — | 1 | 8.28 |
| CHEMBL4475783 | — | — | 1 | 8.25 |
| CHEMBL4526244 | — | — | 1 | 7.86 |
| CHEMBL4568539 | — | — | 1 | 7.73 |
| CHEMBL4467241 | — | — | 1 | 7.65 |
| CHEMBL4447811 | — | — | 1 | 6.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL218994 | — | EC50 | = | 1.862 | nM | 8.73 |
| CHEMBL3104471 | — | EC50 | = | 2.692 | nM | 8.57 |
| CHEMBL4474481 | — | EC50 | = | 2.692 | nM | 8.57 |
| CHEMBL593662 | UROTENSIN-II | EC50 | = | 3.02 | nM | 8.52 |
| CHEMBL4568153 | — | EC50 | = | 3.631 | nM | 8.44 |
| CHEMBL4454498 | — | EC50 | = | 4.677 | nM | 8.33 |
| CHEMBL4462940 | — | EC50 | = | 5.248 | nM | 8.28 |
| CHEMBL4475783 | — | EC50 | = | 5.623 | nM | 8.25 |
| CHEMBL4526244 | — | EC50 | = | 13.8 | nM | 7.86 |
| CHEMBL4568539 | — | EC50 | = | 18.62 | nM | 7.73 |
| CHEMBL4467241 | — | EC50 | = | 22.39 | nM | 7.65 |
| CHEMBL4447811 | — | EC50 | = | 104.71 | nM | 6.98 |