Assay Detail
Functional
CHEMBL4005262
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at recombinant rat IP 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 | Rattus norvegicus |
| 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 | 6.39 | 9.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL494 | ILOPROST | 4.0 | 1 | 9.16 |
| CHEMBL3893346 | — | — | 1 | 6.78 |
| CHEMBL3935924 | — | — | 1 | 6.76 |
| CHEMBL238804 | SELEXIPAG | 4.0 | 1 | 6.70 |
| CHEMBL3966307 | — | — | 1 | 6.57 |
| CHEMBL3933704 | — | — | 1 | 6.55 |
| CHEMBL3952237 | — | — | 1 | 6.44 |
| CHEMBL3926078 | — | — | 1 | 6.40 |
| CHEMBL3928729 | — | — | 1 | 6.33 |
| CHEMBL3900038 | — | — | 1 | 6.33 |
| CHEMBL3301604 | RALINEPAG | 3.0 | 1 | 6.28 |
| CHEMBL3975122 | — | — | 1 | 6.27 |
| CHEMBL3922000 | — | — | 1 | 6.25 |
| CHEMBL3919269 | — | — | 1 | 6.25 |
| CHEMBL3981509 | — | — | 1 | 6.19 |
| CHEMBL3890685 | — | — | 1 | 5.88 |
| CHEMBL3932106 | — | — | 1 | 5.80 |
| CHEMBL3983767 | — | — | 1 | 5.79 |
| CHEMBL3943791 | — | — | 1 | 5.57 |
| CHEMBL3914174 | — | — | 1 | 5.50 |
| CHEMBL3930990 | — | — | 1 | - |
| CHEMBL3952439 | — | — | 1 | - |
| CHEMBL239226 | LASELIPAG | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL494 | ILOPROST | EC50 | = | 0.69 | nM | 9.16 |
| CHEMBL3893346 | — | EC50 | = | 165.0 | nM | 6.78 |
| CHEMBL3935924 | — | EC50 | = | 174.0 | nM | 6.76 |
| CHEMBL238804 | SELEXIPAG | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3966307 | — | EC50 | = | 272.0 | nM | 6.57 |
| CHEMBL3933704 | — | EC50 | = | 284.0 | nM | 6.55 |
| CHEMBL3952237 | — | EC50 | = | 365.0 | nM | 6.44 |
| CHEMBL3926078 | — | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3928729 | — | EC50 | = | 470.0 | nM | 6.33 |
| CHEMBL3900038 | — | EC50 | = | 472.0 | nM | 6.33 |
| CHEMBL3301604 | RALINEPAG | EC50 | = | 530.0 | nM | 6.28 |
| CHEMBL3975122 | — | EC50 | = | 535.0 | nM | 6.27 |
| CHEMBL3922000 | — | EC50 | = | 561.0 | nM | 6.25 |
| CHEMBL3919269 | — | EC50 | = | 560.0 | nM | 6.25 |
| CHEMBL3981509 | — | EC50 | = | 640.0 | nM | 6.19 |
| CHEMBL3890685 | — | EC50 | = | 1330.0 | nM | 5.88 |
| CHEMBL3932106 | — | EC50 | = | 1570.0 | nM | 5.80 |
| CHEMBL3983767 | — | EC50 | = | 1630.0 | nM | 5.79 |
| CHEMBL3943791 | — | EC50 | = | 2720.0 | nM | 5.57 |
| CHEMBL3914174 | — | EC50 | = | 3190.0 | nM | 5.50 |
| CHEMBL3930990 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3952439 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL239226 | LASELIPAG | EC50 | - | — | - |