Assay Detail
Binding
CHEMBL4370024
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Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
21
Total Activities
21
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
Functional Selectivity Revealed by N-Methylation Scanning of Human Urotensin II and Related Peptides.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 7.40 | 8.76 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4472928 | — | — | 1 | 8.76 |
| CHEMBL4568153 | — | — | 1 | 8.76 |
| CHEMBL4526244 | — | — | 1 | 8.66 |
| CHEMBL4590360 | — | — | 1 | 8.53 |
| CHEMBL4462940 | — | — | 1 | 8.45 |
| CHEMBL4454498 | — | — | 1 | 8.45 |
| CHEMBL218994 | — | — | 1 | 8.34 |
| CHEMBL3104471 | — | — | 1 | 8.20 |
| CHEMBL593662 | UROTENSIN-II | — | 1 | 8.11 |
| CHEMBL4475783 | — | — | 1 | 7.69 |
| CHEMBL4474481 | — | — | 1 | 7.64 |
| CHEMBL4449844 | — | — | 1 | 7.31 |
| CHEMBL4568539 | — | — | 1 | 6.64 |
| CHEMBL4447811 | — | — | 1 | 6.61 |
| CHEMBL4467241 | — | — | 1 | 6.09 |
| CHEMBL4483461 | — | — | 1 | 5.82 |
| CHEMBL4549818 | — | — | 1 | 5.68 |
| CHEMBL4455086 | — | — | 1 | 5.67 |
| CHEMBL4565187 | — | — | 1 | 5.27 |
| CHEMBL4544618 | — | — | 1 | - |
| CHEMBL4540501 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4472928 | — | Ki | = | 1.738 | nM | 8.76 |
| CHEMBL4568153 | — | Ki | = | 1.738 | nM | 8.76 |
| CHEMBL4526244 | — | Ki | = | 2.188 | nM | 8.66 |
| CHEMBL4590360 | — | Ki | = | 2.951 | nM | 8.53 |
| CHEMBL4462940 | — | Ki | = | 3.548 | nM | 8.45 |
| CHEMBL4454498 | — | Ki | = | 3.548 | nM | 8.45 |
| CHEMBL218994 | — | Ki | = | 4.571 | nM | 8.34 |
| CHEMBL3104471 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL593662 | UROTENSIN-II | Ki | = | 7.762 | nM | 8.11 |
| CHEMBL4475783 | — | Ki | = | 20.42 | nM | 7.69 |
| CHEMBL4474481 | — | Ki | = | 22.91 | nM | 7.64 |
| CHEMBL4449844 | — | Ki | = | 48.98 | nM | 7.31 |
| CHEMBL4568539 | — | Ki | = | 229.09 | nM | 6.64 |
| CHEMBL4447811 | — | Ki | = | 245.47 | nM | 6.61 |
| CHEMBL4467241 | — | Ki | = | 812.83 | nM | 6.09 |
| CHEMBL4483461 | — | Ki | = | 1513.56 | nM | 5.82 |
| CHEMBL4549818 | — | Ki | = | 2089.3 | nM | 5.68 |
| CHEMBL4455086 | — | Ki | = | 2137.96 | nM | 5.67 |
| CHEMBL4565187 | — | Ki | = | 5370.32 | nM | 5.27 |
| CHEMBL4544618 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4540501 | — | Ki | > | 10000.0 | nM | - |