Assay Detail
Binding
CHEMBL921644
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Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
17
Total Activities
17
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
Development of potent and selective small-molecule human Urotensin-II antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 8.36 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL255509 | — | — | 1 | 9.40 |
| CHEMBL257171 | — | — | 1 | 9.40 |
| CHEMBL256989 | — | — | 1 | 9.22 |
| CHEMBL257415 | — | — | 1 | 9.00 |
| CHEMBL255462 | — | — | 1 | 8.92 |
| CHEMBL257767 | — | — | 1 | 8.70 |
| CHEMBL402520 | — | — | 1 | 8.70 |
| CHEMBL256988 | — | — | 1 | 8.52 |
| CHEMBL257150 | — | — | 1 | 8.30 |
| CHEMBL256721 | — | — | 1 | 8.30 |
| CHEMBL255460 | — | — | 1 | 8.22 |
| CHEMBL258251 | — | — | 1 | 8.22 |
| CHEMBL256937 | — | — | 1 | 8.10 |
| CHEMBL254356 | — | — | 1 | 7.80 |
| CHEMBL404289 | — | — | 1 | 7.40 |
| CHEMBL402805 | — | — | 1 | 7.10 |
| CHEMBL402813 | — | — | 1 | 6.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL255509 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL257171 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL256989 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL257415 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL255462 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL257767 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL402520 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL256988 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL257150 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL256721 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL255460 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL258251 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL256937 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL254356 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL404289 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL402805 | — | Ki | = | 79.0 | nM | 7.10 |
| CHEMBL402813 | — | Ki | = | 130.0 | nM | 6.89 |