Assay Detail
Functional
CHEMBL1048827
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
50
Total Activities
50
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Cell Type | CHO-K1 |
| 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 | 49 | 7.44 | 9.00 |
| EC50 | 1 | 9.27 | 9.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL577772 | — | — | 1 | 9.27 |
| CHEMBL567713 | — | — | 1 | 9.00 |
| CHEMBL566056 | — | — | 1 | 9.00 |
| CHEMBL578203 | — | — | 1 | 8.70 |
| CHEMBL568637 | — | — | 1 | 8.52 |
| CHEMBL567736 | — | — | 1 | 8.46 |
| CHEMBL571625 | — | — | 1 | 8.40 |
| CHEMBL571537 | — | — | 1 | 8.40 |
| CHEMBL566433 | — | — | 1 | 8.32 |
| CHEMBL568123 | — | — | 1 | 8.22 |
| CHEMBL578206 | — | — | 1 | 8.22 |
| CHEMBL571535 | — | — | 1 | 8.15 |
| CHEMBL567075 | — | — | 1 | 8.15 |
| CHEMBL565388 | — | — | 1 | 7.96 |
| CHEMBL567759 | — | — | 1 | 7.96 |
| CHEMBL568764 | — | — | 1 | 7.96 |
| CHEMBL578204 | — | — | 1 | 7.89 |
| CHEMBL566894 | — | — | 1 | 7.85 |
| CHEMBL565395 | — | — | 1 | 7.85 |
| CHEMBL571216 | — | — | 1 | 7.80 |
| CHEMBL578205 | — | — | 1 | 7.80 |
| CHEMBL567949 | — | — | 1 | 7.80 |
| CHEMBL565806 | — | — | 1 | 7.70 |
| CHEMBL578207 | — | — | 1 | 7.64 |
| CHEMBL568165 | — | — | 1 | 7.54 |
| CHEMBL522770 | — | — | 1 | 7.47 |
| CHEMBL565416 | — | — | 1 | 7.41 |
| CHEMBL566366 | — | — | 1 | 7.40 |
| CHEMBL566389 | — | — | 1 | 7.16 |
| CHEMBL565580 | — | — | 1 | 7.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL577772 | — | EC50 | = | 0.54 | nM | 9.27 |
| CHEMBL567713 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL566056 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL578203 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL568637 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL567736 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL571625 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL571537 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL566433 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL568123 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL578206 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL571535 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL567075 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL567759 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL565388 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL568764 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL578204 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL566894 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL565395 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL571216 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL578205 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL567949 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL565806 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL578207 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL568165 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL522770 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL565416 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL566366 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL566389 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL565580 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL569238 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL568316 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL572138 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL569689 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL568089 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL566565 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL567866 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL577518 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL569923 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL566187 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL571683 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL565937 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL584545 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL569688 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL566144 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL566145 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL566364 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL568388 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL568358 | — | IC50 | = | 65000.0 | nM | 4.19 |
| CHEMBL567303 | PALOSURAN | IC50 | > | 75000.0 | nM | - |