Assay Detail
Binding
CHEMBL965358
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Binding affinity to human urotensin-2 receptor
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Potent and selective small-molecule human urotensin-II antagonists with improved pharmacokinetic profiles.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 7.54 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL453587 | — | — | 1 | 9.52 |
| CHEMBL453067 | — | — | 1 | 8.52 |
| CHEMBL449192 | — | — | 1 | 8.52 |
| CHEMBL507691 | — | — | 1 | 8.40 |
| CHEMBL453329 | — | — | 1 | 8.30 |
| CHEMBL499582 | — | — | 1 | 8.22 |
| CHEMBL402303 | — | — | 1 | 8.22 |
| CHEMBL453074 | — | — | 1 | 7.89 |
| CHEMBL488470 | — | — | 1 | 7.89 |
| CHEMBL527199 | — | — | 1 | 7.82 |
| CHEMBL453075 | — | — | 1 | 7.80 |
| CHEMBL254356 | — | — | 1 | 7.80 |
| CHEMBL488642 | — | — | 1 | 7.70 |
| CHEMBL452298 | — | — | 1 | 6.20 |
| CHEMBL452808 | — | — | 1 | 6.20 |
| CHEMBL254153 | — | — | 1 | 5.80 |
| CHEMBL488635 | — | — | 1 | 5.60 |
| CHEMBL38576 | ICI-199,441 | — | 1 | 5.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL453587 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL453067 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL449192 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL507691 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL453329 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL499582 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL402303 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL453074 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL488470 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL527199 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL453075 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL254356 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL488642 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL452298 | — | Ki | = | 630.0 | nM | 6.20 |
| CHEMBL452808 | — | Ki | = | 630.0 | nM | 6.20 |
| CHEMBL254153 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL488635 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL38576 | ICI-199,441 | Ki | = | 4000.0 | nM | 5.40 |