Assay Detail
Functional
CHEMBL1048829
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium 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 | RMS13 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Nonpeptide urotensin-II receptor antagonists: a new ligand class based on piperazino-phthalimide and piperazino-isoindolinone subunits.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 6.75 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL567713 | — | — | 1 | 8.10 |
| CHEMBL522770 | — | — | 1 | 8.10 |
| CHEMBL565388 | — | — | 1 | 7.43 |
| CHEMBL567759 | — | — | 1 | 7.33 |
| CHEMBL578207 | — | — | 1 | 7.29 |
| CHEMBL568637 | — | — | 1 | 7.28 |
| CHEMBL568123 | — | — | 1 | 7.23 |
| CHEMBL571625 | — | — | 1 | 7.21 |
| CHEMBL571535 | — | — | 1 | 7.06 |
| CHEMBL565806 | — | — | 1 | 6.89 |
| CHEMBL578205 | — | — | 1 | 6.89 |
| CHEMBL567075 | — | — | 1 | 6.85 |
| CHEMBL567736 | — | — | 1 | 6.82 |
| CHEMBL566433 | — | — | 1 | 6.82 |
| CHEMBL565395 | — | — | 1 | 6.66 |
| CHEMBL567949 | — | — | 1 | 6.66 |
| CHEMBL568165 | — | — | 1 | 6.62 |
| CHEMBL568316 | — | — | 1 | 6.60 |
| CHEMBL565580 | — | — | 1 | 6.58 |
| CHEMBL578206 | — | — | 1 | 6.50 |
| CHEMBL567303 | PALOSURAN | 2.0 | 1 | 6.50 |
| CHEMBL571216 | — | — | 1 | 6.47 |
| CHEMBL565416 | — | — | 1 | 6.39 |
| CHEMBL578203 | — | — | 1 | 6.30 |
| CHEMBL566366 | — | — | 1 | 6.30 |
| CHEMBL566056 | — | — | 1 | 6.30 |
| CHEMBL571537 | — | — | 1 | 6.29 |
| CHEMBL568764 | — | — | 1 | 6.12 |
| CHEMBL569923 | — | — | 1 | 6.09 |
| CHEMBL578204 | — | — | 1 | 5.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL567713 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL522770 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL565388 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL567759 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL578207 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL568637 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL568123 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL571625 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL571535 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL565806 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL578205 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL567075 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL567736 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL566433 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL565395 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL567949 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL568165 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL568316 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL565580 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL578206 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL567303 | PALOSURAN | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL571216 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL565416 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL578203 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL566366 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL566056 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL571537 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL568764 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL569923 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL578204 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL572138 | — | IC50 | = | 1900.0 | nM | 5.72 |