Assay Detail
Functional
CHEMBL2351691
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Deconstruction of sulfonamide inhibitors of the urotensin receptor (UT) and design and synthesis of benzylamine and benzylsulfone antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 6.23 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL522770 | — | — | 1 | 7.85 |
| CHEMBL2348501 | — | — | 1 | 7.37 |
| CHEMBL2348502 | — | — | 1 | 7.22 |
| CHEMBL2348523 | — | — | 1 | 7.00 |
| CHEMBL2348524 | — | — | 1 | 6.92 |
| CHEMBL2348511 | — | — | 1 | 6.72 |
| CHEMBL2348528 | — | — | 1 | 6.46 |
| CHEMBL2348520 | — | — | 1 | 6.26 |
| CHEMBL2348522 | — | — | 1 | 6.22 |
| CHEMBL2348503 | — | — | 1 | 6.13 |
| CHEMBL2348515 | — | — | 1 | 6.12 |
| CHEMBL2348519 | — | — | 1 | 6.02 |
| CHEMBL2348517 | — | — | 1 | 5.95 |
| CHEMBL2348510 | — | — | 1 | 5.89 |
| CHEMBL2348506 | — | — | 1 | 5.88 |
| CHEMBL2348518 | — | — | 1 | 5.85 |
| CHEMBL2348507 | — | — | 1 | 5.84 |
| CHEMBL2348514 | — | — | 1 | 5.73 |
| CHEMBL2348521 | — | — | 1 | 5.70 |
| CHEMBL2348516 | — | — | 1 | 5.51 |
| CHEMBL2348525 | — | — | 1 | 5.26 |
| CHEMBL2348513 | — | — | 1 | 5.22 |
| CHEMBL2348512 | — | — | 1 | - |
| CHEMBL2348509 | — | — | 1 | - |
| CHEMBL2348508 | — | — | 1 | - |
| CHEMBL2348530 | — | — | 1 | - |
| CHEMBL2348505 | — | — | 1 | - |
| CHEMBL2348504 | — | — | 1 | - |
| CHEMBL2348526 | — | — | 1 | - |
| CHEMBL2348527 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL522770 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2348501 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL2348502 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL2348523 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2348524 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2348511 | — | IC50 | = | 191.0 | nM | 6.72 |
| CHEMBL2348528 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL2348520 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL2348522 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL2348503 | — | IC50 | = | 742.0 | nM | 6.13 |
| CHEMBL2348515 | — | IC50 | = | 765.0 | nM | 6.12 |
| CHEMBL2348519 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL2348517 | — | IC50 | = | 1130.0 | nM | 5.95 |
| CHEMBL2348510 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL2348506 | — | IC50 | = | 1328.0 | nM | 5.88 |
| CHEMBL2348518 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL2348507 | — | IC50 | = | 1450.0 | nM | 5.84 |
| CHEMBL2348514 | — | IC50 | = | 1870.0 | nM | 5.73 |
| CHEMBL2348521 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL2348516 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL2348525 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL2348513 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL2348512 | — | IC50 | - | — | - | |
| CHEMBL2348509 | — | IC50 | - | — | - | |
| CHEMBL2348508 | — | IC50 | - | — | - | |
| CHEMBL2348530 | — | IC50 | - | — | - | |
| CHEMBL2348505 | — | IC50 | - | — | - | |
| CHEMBL2348504 | — | IC50 | - | — | - | |
| CHEMBL2348526 | — | IC50 | - | — | - | |
| CHEMBL2348527 | — | IC50 | - | — | - | |
| CHEMBL2348529 | — | IC50 | - | — | - |