Assay Detail
Functional
CHEMBL4005265
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of 2-(((1r,4r)-4-(((4-Chlorophenyl)(phenyl)carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetate (Ralinepag): An Orally Active Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 23 | 6.07 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL238804 | SELEXIPAG | 4.0 | 1 | 7.00 |
| CHEMBL494 | ILOPROST | 4.0 | 1 | 6.83 |
| CHEMBL239226 | LASELIPAG | 2.0 | 1 | 6.81 |
| CHEMBL3893346 | — | — | 1 | 6.62 |
| CHEMBL3935924 | — | — | 1 | 6.50 |
| CHEMBL3952237 | — | — | 1 | 6.45 |
| CHEMBL3975122 | — | — | 1 | 6.21 |
| CHEMBL3983767 | — | — | 1 | 6.09 |
| CHEMBL3301604 | RALINEPAG | 3.0 | 1 | 6.07 |
| CHEMBL3952439 | — | — | 1 | 6.07 |
| CHEMBL3919269 | — | — | 1 | 6.01 |
| CHEMBL3932106 | — | — | 1 | 5.99 |
| CHEMBL3914174 | — | — | 1 | 5.94 |
| CHEMBL3900038 | — | — | 1 | 5.77 |
| CHEMBL3928729 | — | — | 1 | 5.76 |
| CHEMBL3926078 | — | — | 1 | 5.69 |
| CHEMBL3933704 | — | — | 1 | 5.56 |
| CHEMBL3922000 | — | — | 1 | 5.41 |
| CHEMBL3981509 | — | — | 1 | 5.30 |
| CHEMBL3966307 | — | — | 1 | 5.29 |
| CHEMBL3930990 | — | — | 1 | - |
| CHEMBL3890685 | — | — | 1 | - |
| CHEMBL3943791 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL238804 | SELEXIPAG | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL494 | ILOPROST | EC50 | = | 147.0 | nM | 6.83 |
| CHEMBL239226 | LASELIPAG | EC50 | = | 154.0 | nM | 6.81 |
| CHEMBL3893346 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL3935924 | — | EC50 | = | 320.0 | nM | 6.50 |
| CHEMBL3952237 | — | EC50 | = | 355.0 | nM | 6.45 |
| CHEMBL3975122 | — | EC50 | = | 620.0 | nM | 6.21 |
| CHEMBL3983767 | — | EC50 | = | 808.0 | nM | 6.09 |
| CHEMBL3301604 | RALINEPAG | EC50 | = | 850.0 | nM | 6.07 |
| CHEMBL3952439 | — | EC50 | = | 860.0 | nM | 6.07 |
| CHEMBL3919269 | — | EC50 | = | 980.0 | nM | 6.01 |
| CHEMBL3932106 | — | EC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL3914174 | — | EC50 | = | 1140.0 | nM | 5.94 |
| CHEMBL3900038 | — | EC50 | = | 1710.0 | nM | 5.77 |
| CHEMBL3928729 | — | EC50 | = | 1720.0 | nM | 5.76 |
| CHEMBL3926078 | — | EC50 | = | 2050.0 | nM | 5.69 |
| CHEMBL3933704 | — | EC50 | = | 2760.0 | nM | 5.56 |
| CHEMBL3922000 | — | EC50 | = | 3870.0 | nM | 5.41 |
| CHEMBL3981509 | — | EC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL3966307 | — | EC50 | = | 5070.0 | nM | 5.29 |
| CHEMBL3930990 | — | EC50 | - | — | - | |
| CHEMBL3890685 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3943791 | — | EC50 | > | 10000.0 | nM | - |