Assay Detail
Binding
CHEMBL4201296
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Displacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-counting
9
Total Activities
9
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
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 |
|---|---|---|---|
| IC50 | 9 | 8.04 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4205274 | — | — | 1 | 8.40 |
| CHEMBL4208184 | — | — | 1 | 8.27 |
| CHEMBL4217514 | — | — | 1 | 8.25 |
| CHEMBL3104471 | — | — | 1 | 7.71 |
| CHEMBL4213101 | — | — | 1 | 7.57 |
| CHEMBL4213538 | — | — | 1 | - |
| CHEMBL4216988 | — | — | 1 | - |
| CHEMBL4209654 | — | — | 1 | - |
| CHEMBL4204786 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4205274 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL4208184 | — | IC50 | = | 5.37 | nM | 8.27 |
| CHEMBL4217514 | — | IC50 | = | 5.623 | nM | 8.25 |
| CHEMBL3104471 | — | IC50 | = | 19.5 | nM | 7.71 |
| CHEMBL4213101 | — | IC50 | = | 26.92 | nM | 7.57 |
| CHEMBL4213538 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4216988 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4209654 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4204786 | — | IC50 | > | 1000.0 | nM | - |