Assay Detail
Binding
CHEMBL3366482
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Agonist activity at UT receptor in rat aorta assessed as contraction
18
Total Activities
18
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Aorta |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Lead optimization of P5U and urantide: discovery of novel potent ligands at the urotensin-II receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 8.85 | 10.90 |
| pEC50 | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3315148 | — | — | 1 | 10.90 |
| CHEMBL3315144 | — | — | 1 | 10.71 |
| CHEMBL3315139 | — | — | 1 | 9.40 |
| CHEMBL3315152 | — | — | 1 | 9.20 |
| CHEMBL3315140 | — | — | 1 | 9.14 |
| CHEMBL3315146 | — | — | 1 | 9.09 |
| CHEMBL3315150 | — | — | 1 | 8.97 |
| CHEMBL3315147 | — | — | 1 | 8.57 |
| CHEMBL593662 | UROTENSIN-II | — | 1 | 8.50 |
| CHEMBL218994 | — | — | 1 | 8.44 |
| CHEMBL3315141 | — | — | 1 | 8.42 |
| CHEMBL3315142 | — | — | 1 | 8.30 |
| CHEMBL3315149 | — | — | 1 | 7.89 |
| CHEMBL3315143 | — | — | 1 | 7.74 |
| CHEMBL3315145 | — | — | 1 | 7.47 |
| CHEMBL223905 | URANTIDE | — | 1 | - |
| CHEMBL3315151 | — | — | 1 | - |
| CHEMBL3315153 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3315148 | — | EC50 | = | 0.01259 | nM | 10.90 |
| CHEMBL3315144 | — | EC50 | = | 0.0195 | nM | 10.71 |
| CHEMBL3315139 | — | EC50 | = | 0.3981 | nM | 9.40 |
| CHEMBL3315152 | — | EC50 | = | 0.631 | nM | 9.20 |
| CHEMBL3315140 | — | EC50 | = | 0.7244 | nM | 9.14 |
| CHEMBL3315146 | — | EC50 | = | 0.8128 | nM | 9.09 |
| CHEMBL3315150 | — | EC50 | = | 1.072 | nM | 8.97 |
| CHEMBL3315147 | — | EC50 | = | 2.692 | nM | 8.57 |
| CHEMBL593662 | UROTENSIN-II | EC50 | = | 3.162 | nM | 8.50 |
| CHEMBL218994 | — | EC50 | = | 3.631 | nM | 8.44 |
| CHEMBL3315141 | — | EC50 | = | 3.802 | nM | 8.42 |
| CHEMBL3315142 | — | EC50 | = | 5.012 | nM | 8.30 |
| CHEMBL3315149 | — | EC50 | = | 12.88 | nM | 7.89 |
| CHEMBL3315143 | — | EC50 | = | 18.2 | nM | 7.74 |
| CHEMBL3315145 | — | EC50 | = | 33.88 | nM | 7.47 |
| CHEMBL223905 | URANTIDE | pEC50 | - | — | - | |
| CHEMBL3315151 | — | pEC50 | - | — | - | |
| CHEMBL3315153 | — | pEC50 | - | — | - |